Aug
9
Selective F substitution of H opened up new horizons in biochemistry:
Properties
? Increased metabolic stability
? Increased lipophilicity
? Increased bio-availability
? Modified biological activity
Applications
? Antibacterial
? Ant fungicides
? Antibiotics
? Protease inhibitors
? Anticancer
? Antidepressant
? Fungicides
? Herbicides
? Insecticides
C-F isosteric with C-H cause
Early studies suggested that, due to the ease with which organic F was introduced in the
metabolic pathway undisturbed, C-F was isosteric with C-H.
Recent studies, however, suggest that C-F (van der Waals radius = 1.47 Å) is more nearly
isosteric with C-O (van der Waals radius = 1.52 Å) rather than with the C-H bond (van
der Waals radius = 1.2 Å); but F is still the smallest substituent and can be used as
replacement for the C-H bond.
Fluorine substitution is often used as a strategy to:
1. develop enzyme inhibitors
2. render a compound resistant to chemical degradation
3. enhanced binding (lower Ki)to specific active sites.
Fluoroacetate: a potent TCA cycle inhibitor
1)Fluoroacetate is one of the most deadly simple molecules known. It occurs naturally
in the leaves of a variety of poisonous tropical plants and it is used as rat poison.
2)Fluorocitrate inhibits the TCA transport in the mitochondria and the enzyme cisaconitase.
3) It became immediately obvious that fluorine alters biological activity.
Antidepressants – Serotonin (5-HT) reuptake inhibition
1. In research that led to the development of fluoxetine, a series of N-methyl phenoxyphenylpropylamines was studied. The parent compound effectively blocked 5- HT uptake with an inhibition constant (Ki) of 102 nM but also blocked norepinephrine uptake with a Ki of twice this concentration.
2. The para-trifluoromethyl substituted analogue (fluoxetine) increased potency and
selectivity, having a six-fold increase in potency for inhibition of 5-HT uptake, but a
100-fold decrease in potency for inhibition of norepinephrine uptake
Treatment of Diabetes
Glucagon-Like-Peptide-1 (GLP-1) stimulates insulin release and inhibits glucagons
production.
Glucagons stimulates an increased sugar concentration in the blood.
GLP-1 is inactivated by the serine protease Dipeptidyl peptidase IV (DDP-IV).
THEREFORE finding a DDP-IV inhibitor prolongs the beneficial effects of GLP-1.
MK431 was developed.
Deletion of the –CF3 group reduced bioavailability of MK431 in rats and
led to a 4-fold decrease in enzyme affinity (Ki).
Anti-obesity agents
1. Melanin Stimulating Hormone (MSH) is involved in feeding behaviour:
2 Mice lacking MSH gene have a lean phenotype (“feel full”). Therefore antagonists of
MSH have been developed as anti obesity agents.
3. The fluorinated analogy of the parent compounds showed much lower Ki; this
translates into a lower dosage of the anti obesity agent.
Treatment of cardiovascular diseases
1. An impressive example of drug discovery is found in the development of intestinal
cholesterol uptake by developing acyl-CoA cholesterol acyltransferase (ACAT)
inhibitors.
2. On ACAT parent compound, oxidation at specific sites increased activity and strategic
substitution of fluorine blocked unwanted metabolic oxidation.
Fluorinated Antibacterial agents :
1. Research has assessed that fluorination of the phenyl ring of the quinolone moiety
improved antibacterial activity as compared to the parent compound by binding with
lowered Ki to the P site of the 50S ribosomal subunit impeding transcription and therefore cellular replication and growth.
2. Other improved properties include:
a. better acid stability
b. prolonged serum half-life
c. higher tissue penetration
d. better bioavailability.
Anti-inflammatory agent
1. 3-R,S thalidomide had been developed as a sedative in the 1950s but its teratogenic
effects (cancer causing) led to its withdrawal from the world market in 1962.
2. Recentenly there has been renewed interest in Thalidomide following specific clinical
tests that showed its anti-inflammatory properties.
3. In this example fluorine substitution (FLUOROTHALIDOMIDE, 107) showed
beneficial effects without teratogenic side effects. Fluorine in this case probably acts as
a metabolic cascade modifier.
Anticancer agents: blocking ribosomal unit functionality impedes transcription
1. DNA transcription occurs at the Ribosomal units
2. Tumours are an uncontrolled reproduction of certain undesired cellural strains.
3. Impeding transcription causes cellular death.
This is the basis of Anti-cancer agents.
Note that the 5-Fluorouracyl: the first potent fluorinated chemotherapeutic agent (Heidelberg, 1956).
Alternatives to 5-FU as Thimidylate Inhibitors
1. 5-FU results in being fairly toxic with neurotoxic and cardio toxic side-effects due to:
a. lack of selectivity
b. over production of dUMP to compete with the active site.
c. More tolerable fluorinated 5-FU have therefore been developed.
Alternatives to wide spectrum anti-tumor agents
1. Methotrexate, a thimidilate antagonist, has historically been developed as a wide
spectrum anti-cancer agent.
Its fluorinated analogue, ZD-933 now in phase II/III clinical studies, has been found to
be a specific antagonist to ovarian cancer cell-lines.
2. In this case fluorine changes the specificity of the compound rather than modify its
Action
Pancreatic cancer antagonists
1. Polimerase III antagonists are DNA replication antagonists which have been
discovered to effectively inhibit cell replication.
2. In the case of Gemzar® (hydrogenated) and Gemcitabine (fluorinated) fluorine
substitution increases potency of the drug with respect to its hydrogenated analogue.
Microtubule antagonists
1. Microtubule synthesis inhibition has been found to effectively inhibit cell proliferation.
2. In this case, fluorine substitution prolongues metabolic life of the anticancer agent with
respect to the hydrogenated parent compound..
Estrogen anticancer agents.
1. Mifepristone, the hydrogenated parent compound, has been found to be a good
progesterone receptor antagonist.
2. In this case fluorine substitution generated a new generation of progesterone receptor
antagonists with the highest receptor selectivity.
Protein kinase inhibitors
Most signal transduction pathways are mediated by protein kinases regulating every
aspect of cell function. Since cancer is recognised to be caused by mutation and
aberrant expression of critical genes, protein kinase inhibitors have become the focus
of development of new therapies for cancer.
1. In this example, 61 is 100 times more potent than 57. It therefore shows how, by
increasing the concentration of fluorine in the portion of the substrate which is in
intimate contact with the kinase’s active site increases the effectiveness of the
therapeutic agent.
And therefore, F in medicinal chemistry…...
2. Fluorine will continue to play an important role in the developing areas of medicinal
chemistry due to its attractive properties for inclusion in structure-activity clinical
screens.
Artificial blood: an O2 transport substitute
1. Haemoglobin, one of the main components of blood, is responsible
for O2 transport in tissues and cells.
2. ALKYLFLUORIDES AND PERFLUORINATED ETHERS
HAVE DEMONSTRATED REMAKABLE O2 UPTAKE.
Loss of blood due to injury or major surgery can be a serious
problem in situations where human blood is scarce or absent such
as in emerging countries, during epidemics or in mass-surgeries
(war time).
Per fluorocarbons as artificial blood
1. Per fluorocarbons from 6 –10 carbons in length are used as “artificial blood” for the
treatment of heart attacks and other vascular obstructions as well as adjutants in
coronary angioplasty.
2. The per fluorocarbons are kept in an aqueous solution by means of emulsifiers and
tetra-alkyl ammonium salts; their concentrations range from 0,5 – 2 g/dl
3. The concentration of the per fluorocarbon in the aqueous solution ranges from 5 – 10
g/dl.
Perfluorodecalin: a …bloody special fluorocarbon!
made up of atoms of carbon, fluorine, and/or sulphur.
1. liquids are clear, colourless, odourless, non-conducting, and non-flammable.
2. approximately twice as dense as water, and are capable of dissolving large amounts of
gases mainly oxygen and carbon dioxide.
3. chemically stable compounds that are not metabolized in body tissues.
4. Require a high FIO2 to maintain high oxygen concentrations within the fluid. It is only
the carrier of oxygen and carbon dioxide.
5. Capable of carrying five times more oxygen than haemoglobin.
Perfluoroethers and perfluoropolyethers as artificial blood
1. Due their grater chain mobility and also due to their greater chemical affinity for
perfluoroethers and perfluoropolyethers O2 are more efficient in delivering
“acceptable” (quantities not disclosed) concentrations of O2 both in laboratory
animals and clinical testing on humans.
2. Furthermore, due to their greater solubility in aqueous solutions, perfluoroethers and
perfluoropolyethers don’t require emulsifiers thus simplifying the “artificial blood”
composition.
3. A specific experimental example developed by the ASP school coordinated by Prof.
Walter Navarrini of this Polytechnical Institute is CF3OCF2CF2OCF3 (b.p. = 20°C).
Other fluorine-containing drugs
It has been shown that fluorinated analogues of naturally occurring biologically active compounds
including amino acids, often exhibit unique physiological activity. Fluorination of natural hormones can lead to molecules with new pharmacokinetic and/or pharmacodynamic properties. For example the introduction of fluorine into corticosteroids has a dramatic effect on their metabolism (Bush and Mahesh 1964). Because the metabolism of steroid hormones is very important for their physiological activities, the exchange of a hydrogen atom under fluorine atom can be very meaningful. Also other endogenous compounds markedly exchange their biological properties, if one or more fluorine atoms are installed into their molecule. For example, the potent platelet aggregating agent thromboxane A2 has a half-life in vivo of only 32 seconds.
Incorporation of two fluorine atoms into the oxetane ring of thromboxane A2 reduces the rate of carbonium ion formation and acid hydrolysis, so that 7,7-difluoro-thromboxane A2 has a rate of hydrolysis 108-fold slower than the natural substance (Fried et al. 1984). Likewise prostacyclin, which is an inhibitor of platelet aggregation, has a very short biological half-life. Fluorination improves the stability of the molecule toward acid hydrolysis and the stability in organisms. Thus 10,10-difluoro-13-dehydroprostacyclin exhibits a half-life 150 times, and has equal potency to, the natural compound (Fried et al. 1980). Cerivastatin, a fluorinated drug from the statin class, which had caused deaths and serious adverse health effects was withdrawn from the market in 2001 ( Furberg and Pitt 2001). It had been linked to at least 31 deaths. Cerivastatin also induced muscle destruction (rhabdomyolysis) and displayed compounded toxicity when used with other drugs.
By: kalyan kumar dhar
Properties
? Increased metabolic stability
? Increased lipophilicity
? Increased bio-availability
? Modified biological activity
Applications
? Antibacterial
? Ant fungicides
? Antibiotics
? Protease inhibitors
? Anticancer
? Antidepressant
? Fungicides
? Herbicides
? Insecticides
C-F isosteric with C-H cause
Early studies suggested that, due to the ease with which organic F was introduced in the
metabolic pathway undisturbed, C-F was isosteric with C-H.
Recent studies, however, suggest that C-F (van der Waals radius = 1.47 Å) is more nearly
isosteric with C-O (van der Waals radius = 1.52 Å) rather than with the C-H bond (van
der Waals radius = 1.2 Å); but F is still the smallest substituent and can be used as
replacement for the C-H bond.
Fluorine substitution is often used as a strategy to:
1. develop enzyme inhibitors
2. render a compound resistant to chemical degradation
3. enhanced binding (lower Ki)to specific active sites.
Fluoroacetate: a potent TCA cycle inhibitor
1)Fluoroacetate is one of the most deadly simple molecules known. It occurs naturally
in the leaves of a variety of poisonous tropical plants and it is used as rat poison.
2)Fluorocitrate inhibits the TCA transport in the mitochondria and the enzyme cisaconitase.
3) It became immediately obvious that fluorine alters biological activity.
Antidepressants – Serotonin (5-HT) reuptake inhibition
1. In research that led to the development of fluoxetine, a series of N-methyl phenoxyphenylpropylamines was studied. The parent compound effectively blocked 5- HT uptake with an inhibition constant (Ki) of 102 nM but also blocked norepinephrine uptake with a Ki of twice this concentration.
2. The para-trifluoromethyl substituted analogue (fluoxetine) increased potency and
selectivity, having a six-fold increase in potency for inhibition of 5-HT uptake, but a
100-fold decrease in potency for inhibition of norepinephrine uptake
Treatment of Diabetes
Glucagon-Like-Peptide-1 (GLP-1) stimulates insulin release and inhibits glucagons
production.
Glucagons stimulates an increased sugar concentration in the blood.
GLP-1 is inactivated by the serine protease Dipeptidyl peptidase IV (DDP-IV).
THEREFORE finding a DDP-IV inhibitor prolongs the beneficial effects of GLP-1.
MK431 was developed.
Deletion of the –CF3 group reduced bioavailability of MK431 in rats and
led to a 4-fold decrease in enzyme affinity (Ki).
Anti-obesity agents
1. Melanin Stimulating Hormone (MSH) is involved in feeding behaviour:
2 Mice lacking MSH gene have a lean phenotype (“feel full”). Therefore antagonists of
MSH have been developed as anti obesity agents.
3. The fluorinated analogy of the parent compounds showed much lower Ki; this
translates into a lower dosage of the anti obesity agent.
Treatment of cardiovascular diseases
1. An impressive example of drug discovery is found in the development of intestinal
cholesterol uptake by developing acyl-CoA cholesterol acyltransferase (ACAT)
inhibitors.
2. On ACAT parent compound, oxidation at specific sites increased activity and strategic
substitution of fluorine blocked unwanted metabolic oxidation.
Fluorinated Antibacterial agents :
1. Research has assessed that fluorination of the phenyl ring of the quinolone moiety
improved antibacterial activity as compared to the parent compound by binding with
lowered Ki to the P site of the 50S ribosomal subunit impeding transcription and therefore cellular replication and growth.
2. Other improved properties include:
a. better acid stability
b. prolonged serum half-life
c. higher tissue penetration
d. better bioavailability.
Anti-inflammatory agent
1. 3-R,S thalidomide had been developed as a sedative in the 1950s but its teratogenic
effects (cancer causing) led to its withdrawal from the world market in 1962.
2. Recentenly there has been renewed interest in Thalidomide following specific clinical
tests that showed its anti-inflammatory properties.
3. In this example fluorine substitution (FLUOROTHALIDOMIDE, 107) showed
beneficial effects without teratogenic side effects. Fluorine in this case probably acts as
a metabolic cascade modifier.
Anticancer agents: blocking ribosomal unit functionality impedes transcription
1. DNA transcription occurs at the Ribosomal units
2. Tumours are an uncontrolled reproduction of certain undesired cellural strains.
3. Impeding transcription causes cellular death.
This is the basis of Anti-cancer agents.
Note that the 5-Fluorouracyl: the first potent fluorinated chemotherapeutic agent (Heidelberg, 1956).
Alternatives to 5-FU as Thimidylate Inhibitors
1. 5-FU results in being fairly toxic with neurotoxic and cardio toxic side-effects due to:
a. lack of selectivity
b. over production of dUMP to compete with the active site.
c. More tolerable fluorinated 5-FU have therefore been developed.
Alternatives to wide spectrum anti-tumor agents
1. Methotrexate, a thimidilate antagonist, has historically been developed as a wide
spectrum anti-cancer agent.
Its fluorinated analogue, ZD-933 now in phase II/III clinical studies, has been found to
be a specific antagonist to ovarian cancer cell-lines.
2. In this case fluorine changes the specificity of the compound rather than modify its
Action
Pancreatic cancer antagonists
1. Polimerase III antagonists are DNA replication antagonists which have been
discovered to effectively inhibit cell replication.
2. In the case of Gemzar® (hydrogenated) and Gemcitabine (fluorinated) fluorine
substitution increases potency of the drug with respect to its hydrogenated analogue.
Microtubule antagonists
1. Microtubule synthesis inhibition has been found to effectively inhibit cell proliferation.
2. In this case, fluorine substitution prolongues metabolic life of the anticancer agent with
respect to the hydrogenated parent compound..
Estrogen anticancer agents.
1. Mifepristone, the hydrogenated parent compound, has been found to be a good
progesterone receptor antagonist.
2. In this case fluorine substitution generated a new generation of progesterone receptor
antagonists with the highest receptor selectivity.
Protein kinase inhibitors
Most signal transduction pathways are mediated by protein kinases regulating every
aspect of cell function. Since cancer is recognised to be caused by mutation and
aberrant expression of critical genes, protein kinase inhibitors have become the focus
of development of new therapies for cancer.
1. In this example, 61 is 100 times more potent than 57. It therefore shows how, by
increasing the concentration of fluorine in the portion of the substrate which is in
intimate contact with the kinase’s active site increases the effectiveness of the
therapeutic agent.
And therefore, F in medicinal chemistry…...
2. Fluorine will continue to play an important role in the developing areas of medicinal
chemistry due to its attractive properties for inclusion in structure-activity clinical
screens.
Artificial blood: an O2 transport substitute
1. Haemoglobin, one of the main components of blood, is responsible
for O2 transport in tissues and cells.
2. ALKYLFLUORIDES AND PERFLUORINATED ETHERS
HAVE DEMONSTRATED REMAKABLE O2 UPTAKE.
Loss of blood due to injury or major surgery can be a serious
problem in situations where human blood is scarce or absent such
as in emerging countries, during epidemics or in mass-surgeries
(war time).
Per fluorocarbons as artificial blood
1. Per fluorocarbons from 6 –10 carbons in length are used as “artificial blood” for the
treatment of heart attacks and other vascular obstructions as well as adjutants in
coronary angioplasty.
2. The per fluorocarbons are kept in an aqueous solution by means of emulsifiers and
tetra-alkyl ammonium salts; their concentrations range from 0,5 – 2 g/dl
3. The concentration of the per fluorocarbon in the aqueous solution ranges from 5 – 10
g/dl.
Perfluorodecalin: a …bloody special fluorocarbon!
made up of atoms of carbon, fluorine, and/or sulphur.
1. liquids are clear, colourless, odourless, non-conducting, and non-flammable.
2. approximately twice as dense as water, and are capable of dissolving large amounts of
gases mainly oxygen and carbon dioxide.
3. chemically stable compounds that are not metabolized in body tissues.
4. Require a high FIO2 to maintain high oxygen concentrations within the fluid. It is only
the carrier of oxygen and carbon dioxide.
5. Capable of carrying five times more oxygen than haemoglobin.
Perfluoroethers and perfluoropolyethers as artificial blood
1. Due their grater chain mobility and also due to their greater chemical affinity for
perfluoroethers and perfluoropolyethers O2 are more efficient in delivering
“acceptable” (quantities not disclosed) concentrations of O2 both in laboratory
animals and clinical testing on humans.
2. Furthermore, due to their greater solubility in aqueous solutions, perfluoroethers and
perfluoropolyethers don’t require emulsifiers thus simplifying the “artificial blood”
composition.
3. A specific experimental example developed by the ASP school coordinated by Prof.
Walter Navarrini of this Polytechnical Institute is CF3OCF2CF2OCF3 (b.p. = 20°C).
Other fluorine-containing drugs
It has been shown that fluorinated analogues of naturally occurring biologically active compounds
including amino acids, often exhibit unique physiological activity. Fluorination of natural hormones can lead to molecules with new pharmacokinetic and/or pharmacodynamic properties. For example the introduction of fluorine into corticosteroids has a dramatic effect on their metabolism (Bush and Mahesh 1964). Because the metabolism of steroid hormones is very important for their physiological activities, the exchange of a hydrogen atom under fluorine atom can be very meaningful. Also other endogenous compounds markedly exchange their biological properties, if one or more fluorine atoms are installed into their molecule. For example, the potent platelet aggregating agent thromboxane A2 has a half-life in vivo of only 32 seconds.
Incorporation of two fluorine atoms into the oxetane ring of thromboxane A2 reduces the rate of carbonium ion formation and acid hydrolysis, so that 7,7-difluoro-thromboxane A2 has a rate of hydrolysis 108-fold slower than the natural substance (Fried et al. 1984). Likewise prostacyclin, which is an inhibitor of platelet aggregation, has a very short biological half-life. Fluorination improves the stability of the molecule toward acid hydrolysis and the stability in organisms. Thus 10,10-difluoro-13-dehydroprostacyclin exhibits a half-life 150 times, and has equal potency to, the natural compound (Fried et al. 1980). Cerivastatin, a fluorinated drug from the statin class, which had caused deaths and serious adverse health effects was withdrawn from the market in 2001 ( Furberg and Pitt 2001). It had been linked to at least 31 deaths. Cerivastatin also induced muscle destruction (rhabdomyolysis) and displayed compounded toxicity when used with other drugs.
By: kalyan kumar dhar
Aug
9
Okay ladies, if you have a physical connection with a man, but he just doesn’t get you mentally, what next?
Filed Under Physical Chemistry | 7 Comments
I have a women friend that we have a STRONG physical attraction, chemistry (that’s what you ladies call it) towards each other, but I just can’t get her mentally at all. Each time we talk, the least bit, its painful, she gets upset, I’m pissed cause I’m confused, and it just sucks!!
What do you do next.
By: pluto
Aug
9
Relax With Potassium and Magnesium
Filed Under Biochemistry | Leave a Comment
Potassium and magnesium are the two most common minerals found within the cells of your body. They each have specific individual functions within your body, and together help to maintain the correct balance of electrolytes and the proper functioning of smooth and striated muscles. That includes allowing muscles to relax properly rather than to cramp.
Before discussing this, let’s have a look at the major individual properties of these two metallic minerals with respect to the body’s biochemistry.
Magnesium is needed to ensure the proper functioning of the sodium/potassium pump. This is a complex topic, and we shan’t dwell on it at length here, although the basics are that it is responsible for the movement of ions into and out of cells. Sodium and potassium ions are moved in opposite directions across the cell plasma membrane, three sodium ions being pumped out for every two potassium ions pumped into the cell.
This is of particular importance to nervous cells responsible for transmitting impulses in response to specific stimuli. In the event of a magnesium deficiency, this pumping action is impaired and the sodium/potassium balance within and without the body cells are imbalanced. This in turn impairs the response of nerve cells to stimuli. Both magnesium and potassium can be depleted through the use of diuretics, in which case a magnesium supplement can redress the imbalance.
There are several consequences of such an electrolytic imbalance, some having potentially serious consequences. Many can cause death if left untreated, although the symptoms usually allow appropriate medical treatment prior to the condition becoming fatal, such treatment frequently involving administration of magnesium and potassium. Among these are:
Calcium overload in certain heart cells that reduces the effective use of oxygen and ATP and causes overactive contraction of the heart muscle.
Spasms in coronary blood vessels
Over-activity of the striated muscle fibers, leading to cramps in the calf and thigh muscles, for example.
Cramp and pain in the smooth muscles of hollow organs such as the bladder or uterus that can also cause premature labor.
Several heart problems caused by an increase in energy consumption and a calcium overload and potassium deficiency that leads to cardiac ischemia and arrhythmia that continue to create a serious medical condition and hazard to life. Potassium, that can stop the heart if given in excess, can be just as harmful if present in too small a concentration.
The whole situation creates a self-perpetuating cycle that can be broken by a magnesium and potassium supplement that restores the correct gradient of potassium and magnesium across the cell membrane, improves the function of the sodium/potassium pump and reduces the excess cellular calcium by replacing it with magnesium.
This only works if both potassium and magnesium are taken together: just either alone is no good. It also takes time for the effect to occur, so the supplement is not suitable for emergency use. A regular supply can prevent the condition occurring.
There are many other properties that magnesium and potassium possess with regard to the body’s biochemistry such as the effect of magnesium in activating certain enzymes. However, in discussing relaxation, both of these essential minerals have a significant part to play.
It has been mentioned that a magnesium and calcium deficiency causes spasms and cramps in the smooth and striated muscles, and the corollary is also true. Magnesium and potassium can be used to relieve such cramps, and relax muscle tissue. Hence, because it can relax excited smooth bronchial muscle tissue, magnesium can be used to relieve asthma attacks. The intravenous administration of magnesium is, in fact, an accepted and proven clinical treatment for acute asthma attacks.
In the same way, magnesium has been used to treat muscle spasms and cramps. Again, it is not an immediate treatment for emergency use, but can be used over a period of days to treat athletes with a history of muscle spasms. Such spasm frequently occur after prolonged periods of exercise, when magnesium and potassium, among other electrolytes, can be lost through a combination of sweating and urination.
However, this is not the only means by which magnesium is lost from your body cells, and probably not even the main one. Less obvious, but likely of more importance, is the transfer of magnesium from the plasma into the red blood cells (erythrocytes). The amount by which this occurs is directly proportional to the more anaerobic the exercise, hence the need by athletes and weightlifters for more magnesium. It can be rapidly lost through exercise with insufficient oxygen, and cause their muscles to cramp up.
Magnesium deficiency is common in Americans, although factors such as high calcium intake, alcohol intake, diuretics, and kidney and liver disease are more responsible for this than a dietary deficiency. Potassium is readily available in bananas, brown rice, potatoes, tomatoes and oranges and dietary deficiencies are not common although supplements are readily available.
Magnesium is also known to play an important part in the secretion and use of insulin by the body. Supplementation with magnesium can help diabetics to make best use of insulin, become more tolerant to glucose and improve the fluidity of the membrane of red blood cells. The mineral; also has a small but definite effect in lowering blood pressure. Other uses for magnesium supplements include congenital heart failure, where higher magnesium contents lead to greater life expectancy and chronic fatigue syndrome (CFS) where magnesium supplements can significantly increase energy levels.
Other uses to which your body puts potassium other than to allow proper muscle contraction and relaxation and to maintain the balance of electrolytes in the body, includes the function of brain and nerve neurons. This, however, is academic since should your potassium levels drop by 50%, death would result.
Potassium, Magnesium and Calcium are essential in maintaining the proper workings of your body cells, although the most visible effect of magnesium and potassium is their relaxation properties on the body, put to specific use by sportsmen and women, particularly those involved in the more anaerobic sports.
By: Darrell Miller
Before discussing this, let’s have a look at the major individual properties of these two metallic minerals with respect to the body’s biochemistry.
Magnesium is needed to ensure the proper functioning of the sodium/potassium pump. This is a complex topic, and we shan’t dwell on it at length here, although the basics are that it is responsible for the movement of ions into and out of cells. Sodium and potassium ions are moved in opposite directions across the cell plasma membrane, three sodium ions being pumped out for every two potassium ions pumped into the cell.
This is of particular importance to nervous cells responsible for transmitting impulses in response to specific stimuli. In the event of a magnesium deficiency, this pumping action is impaired and the sodium/potassium balance within and without the body cells are imbalanced. This in turn impairs the response of nerve cells to stimuli. Both magnesium and potassium can be depleted through the use of diuretics, in which case a magnesium supplement can redress the imbalance.
There are several consequences of such an electrolytic imbalance, some having potentially serious consequences. Many can cause death if left untreated, although the symptoms usually allow appropriate medical treatment prior to the condition becoming fatal, such treatment frequently involving administration of magnesium and potassium. Among these are:
Calcium overload in certain heart cells that reduces the effective use of oxygen and ATP and causes overactive contraction of the heart muscle.
Spasms in coronary blood vessels
Over-activity of the striated muscle fibers, leading to cramps in the calf and thigh muscles, for example.
Cramp and pain in the smooth muscles of hollow organs such as the bladder or uterus that can also cause premature labor.
Several heart problems caused by an increase in energy consumption and a calcium overload and potassium deficiency that leads to cardiac ischemia and arrhythmia that continue to create a serious medical condition and hazard to life. Potassium, that can stop the heart if given in excess, can be just as harmful if present in too small a concentration.
The whole situation creates a self-perpetuating cycle that can be broken by a magnesium and potassium supplement that restores the correct gradient of potassium and magnesium across the cell membrane, improves the function of the sodium/potassium pump and reduces the excess cellular calcium by replacing it with magnesium.
This only works if both potassium and magnesium are taken together: just either alone is no good. It also takes time for the effect to occur, so the supplement is not suitable for emergency use. A regular supply can prevent the condition occurring.
There are many other properties that magnesium and potassium possess with regard to the body’s biochemistry such as the effect of magnesium in activating certain enzymes. However, in discussing relaxation, both of these essential minerals have a significant part to play.
It has been mentioned that a magnesium and calcium deficiency causes spasms and cramps in the smooth and striated muscles, and the corollary is also true. Magnesium and potassium can be used to relieve such cramps, and relax muscle tissue. Hence, because it can relax excited smooth bronchial muscle tissue, magnesium can be used to relieve asthma attacks. The intravenous administration of magnesium is, in fact, an accepted and proven clinical treatment for acute asthma attacks.
In the same way, magnesium has been used to treat muscle spasms and cramps. Again, it is not an immediate treatment for emergency use, but can be used over a period of days to treat athletes with a history of muscle spasms. Such spasm frequently occur after prolonged periods of exercise, when magnesium and potassium, among other electrolytes, can be lost through a combination of sweating and urination.
However, this is not the only means by which magnesium is lost from your body cells, and probably not even the main one. Less obvious, but likely of more importance, is the transfer of magnesium from the plasma into the red blood cells (erythrocytes). The amount by which this occurs is directly proportional to the more anaerobic the exercise, hence the need by athletes and weightlifters for more magnesium. It can be rapidly lost through exercise with insufficient oxygen, and cause their muscles to cramp up.
Magnesium deficiency is common in Americans, although factors such as high calcium intake, alcohol intake, diuretics, and kidney and liver disease are more responsible for this than a dietary deficiency. Potassium is readily available in bananas, brown rice, potatoes, tomatoes and oranges and dietary deficiencies are not common although supplements are readily available.
Magnesium is also known to play an important part in the secretion and use of insulin by the body. Supplementation with magnesium can help diabetics to make best use of insulin, become more tolerant to glucose and improve the fluidity of the membrane of red blood cells. The mineral; also has a small but definite effect in lowering blood pressure. Other uses for magnesium supplements include congenital heart failure, where higher magnesium contents lead to greater life expectancy and chronic fatigue syndrome (CFS) where magnesium supplements can significantly increase energy levels.
Other uses to which your body puts potassium other than to allow proper muscle contraction and relaxation and to maintain the balance of electrolytes in the body, includes the function of brain and nerve neurons. This, however, is academic since should your potassium levels drop by 50%, death would result.
Potassium, Magnesium and Calcium are essential in maintaining the proper workings of your body cells, although the most visible effect of magnesium and potassium is their relaxation properties on the body, put to specific use by sportsmen and women, particularly those involved in the more anaerobic sports.
By: Darrell Miller
Aug
8
men-please be serious and answer all questions- my boyfriend told me he cared a lot but not enough chemistry?
Filed Under Physical Chemistry | 2 Comments
most important question- can you care a lot about someone you dont have enough chemisty with?
is chemistry physical attraction and sex? or is chemistry how well too people get along?
can you be physically attracted to a women or man , have awesome sex, but litttle chemistry?
can you have awemome chemistry but little physical attraction?
By: wishing
Aug
7
What are some physical properties of plastic that would be appropriate for making rain boots?
Filed Under Physical Chemistry | 2 Comments
chemistry help! Thanks!
By: Break Dance, Not Hearts!
By: Break Dance, Not Hearts!
Aug
6
Examining The Difference Between Organic Skin Care Formulas
Filed Under Organic Chemistry | Leave a Comment
Organic skin care products from many companies are said to contain all organic materials. What they fail to mention to consumers, however, is that this is not necessarily the case and it shows in the quality and effectiveness of their products. Many of these so-called natural products have lost a large portion of their usefulness before the bottle is ever opened. A new natural skin care line is available that has a longer shelf life and an increased ability to treat various skin afflictions thanks to the development of a new skin care technology known as ‘Ionic Chemistry.’
What Is Wrong With Traditional Organic Skin Care Lines
Almost all organic skin formulas on the market today state that they made from completely natural products, without mentioning the man made materials they add to their products and the consequences of including them to their products. These formulas start to lose their effective properties almost instantly. The look, feel, and smell of these solutions begin to decline along with their effectiveness turning them into nothing more than a perfumed emulsion.
In order to prevent this from happening, skin care manufacturers add chemicals called parabens to their formulas. This does help to maintain their overall makeup, but it is not without a price. These chemically engineered additives attach themselves directly on to the active ingredients found in these solutions, which in turn, reduces the benefits of using the product in the first place. Even worse, chemical additives such as propylparaben, methylparaben, and other chemically engineered additives have been found to have severe consequences on your overall health including diseases such as breast cancer.
The Advantages Of New Organic Skin Care Formulas
There is only one skin care system available today that does not add harmful chemical additives to their formula. It uses the technique known as ‘Ionic Chemistry.’ This method encourages the components of the formula to bond with their ionic mate naturally in order to maximize the effectiveness of their products. The natural bonding process is not only stronger than engineered bonds, but it also encourages each component in the formula to work to its highest potential regardless of the skin type they are used on.
Instead of using substances such as paraben like other organic skin care companies, the new technique of ionic chemistry uses fresh, natural ingredients to the fullest advantage. The distinctive qualities of this new method work perfectly on their own without the addition of harmful chemicals such as binders or thickeners. As an alternative, these new beauty products use phytochemicals, photonutrients, and antioxidants found naturally in the ingredients to promote healthy skin.
This unique method of bonding has made these skin care formulas superior to traditional beauty products. Thanks to the use of ingredients that are both natural and fresh, these products have superior anti-aging and preventative properties. They also balance out the oil levels on the skin while treating skin conditions such as rosacea, acne, and even deforming marks such as scars. To enrich the benefits of these products even further, the formulas can be tailored to meet the needs of any skin type.
Beauty products with the word ‘organic’ on the label have become extremely popular because they are believed to be an easy way to achieve healthy looking skin without the fear of side effects. Unfortunately, this has been completely false until the emergence of the new formula. The ionic chemistry utilized by these products not only extends the life of these formulas, but they have been found to be considerably more effective than typical organic skin care products without the danger of using harsh chemicals.
By: Kent Campbell
What Is Wrong With Traditional Organic Skin Care Lines
Almost all organic skin formulas on the market today state that they made from completely natural products, without mentioning the man made materials they add to their products and the consequences of including them to their products. These formulas start to lose their effective properties almost instantly. The look, feel, and smell of these solutions begin to decline along with their effectiveness turning them into nothing more than a perfumed emulsion.
In order to prevent this from happening, skin care manufacturers add chemicals called parabens to their formulas. This does help to maintain their overall makeup, but it is not without a price. These chemically engineered additives attach themselves directly on to the active ingredients found in these solutions, which in turn, reduces the benefits of using the product in the first place. Even worse, chemical additives such as propylparaben, methylparaben, and other chemically engineered additives have been found to have severe consequences on your overall health including diseases such as breast cancer.
The Advantages Of New Organic Skin Care Formulas
There is only one skin care system available today that does not add harmful chemical additives to their formula. It uses the technique known as ‘Ionic Chemistry.’ This method encourages the components of the formula to bond with their ionic mate naturally in order to maximize the effectiveness of their products. The natural bonding process is not only stronger than engineered bonds, but it also encourages each component in the formula to work to its highest potential regardless of the skin type they are used on.
Instead of using substances such as paraben like other organic skin care companies, the new technique of ionic chemistry uses fresh, natural ingredients to the fullest advantage. The distinctive qualities of this new method work perfectly on their own without the addition of harmful chemicals such as binders or thickeners. As an alternative, these new beauty products use phytochemicals, photonutrients, and antioxidants found naturally in the ingredients to promote healthy skin.
This unique method of bonding has made these skin care formulas superior to traditional beauty products. Thanks to the use of ingredients that are both natural and fresh, these products have superior anti-aging and preventative properties. They also balance out the oil levels on the skin while treating skin conditions such as rosacea, acne, and even deforming marks such as scars. To enrich the benefits of these products even further, the formulas can be tailored to meet the needs of any skin type.
Beauty products with the word ‘organic’ on the label have become extremely popular because they are believed to be an easy way to achieve healthy looking skin without the fear of side effects. Unfortunately, this has been completely false until the emergence of the new formula. The ionic chemistry utilized by these products not only extends the life of these formulas, but they have been found to be considerably more effective than typical organic skin care products without the danger of using harsh chemicals.
By: Kent Campbell
Aug
6
What does natural and organic mean on a cosmetic label?
Filed Under Organic Chemistry | Leave a Comment
What does ‘natural’ and ‘organic’ mean on a cosmetic label?
Nowhere do the terms “natural” or “organic” take a more gratuitous bruising than the cosmetics industry! Here we hope to clarify some basic differences between Miessence and others….
Miessence definition of natural:
“Existing in, or formed by nature; not artificial.”
Commercial definition of natural: “Any ingredient “derived from” a natural substance.”
Explanation: We often see long chemical names followed by the phrase “derived from coconut oil”. For example, to create cocamide DEA from coconut oil requires the use of a carcinogenic synthetic chemical (diethanolamine - DEA). It is therefore no longer natural (or safe). To insinuate that it is a natural substance by adding the phrase “derived from coconut oil” is deceitful. Just because vodka can be made from potatoes, doesn’t mean it’s good for you!
Miessence definition of organic:
“Grown, cultivated and stored without the use of chemicals, herbicides, pesticides, fumigants and other toxins.”
Commercial definition of organic: “Any compound containing carbon.”
Explanation: The organic chemistry definition of organic, is any compound containing carbon. Carbon is found in anything that has ever lived. So, by using this definition of organic we could say that the toxic petrochemical preservative, methyl paraben is “organic” because it was formed by leaves that rotted over thousands of years to become the crude oil used to make this toxic preservative.
By: Sarah Liddle
Nowhere do the terms “natural” or “organic” take a more gratuitous bruising than the cosmetics industry! Here we hope to clarify some basic differences between Miessence and others….
Miessence definition of natural:
“Existing in, or formed by nature; not artificial.”
Commercial definition of natural: “Any ingredient “derived from” a natural substance.”
Explanation: We often see long chemical names followed by the phrase “derived from coconut oil”. For example, to create cocamide DEA from coconut oil requires the use of a carcinogenic synthetic chemical (diethanolamine - DEA). It is therefore no longer natural (or safe). To insinuate that it is a natural substance by adding the phrase “derived from coconut oil” is deceitful. Just because vodka can be made from potatoes, doesn’t mean it’s good for you!
Miessence definition of organic:
“Grown, cultivated and stored without the use of chemicals, herbicides, pesticides, fumigants and other toxins.”
Commercial definition of organic: “Any compound containing carbon.”
Explanation: The organic chemistry definition of organic, is any compound containing carbon. Carbon is found in anything that has ever lived. So, by using this definition of organic we could say that the toxic petrochemical preservative, methyl paraben is “organic” because it was formed by leaves that rotted over thousands of years to become the crude oil used to make this toxic preservative.
By: Sarah Liddle
Aug
3
Feelings of Drug Usages
Filed Under Biochemistry | Leave a Comment
But we can avoid these feelings-at least for the moment–by using drugs. We can do drugs and almost instantly feel “high.” We can forget about life for a while. We can experience pleasure, excitement, power, courage, thrills, joy, enchantment, and a sense of connection with other people and the world around us.Of course, in the long run drugs become less and less effective at bringing these benefits. Over time, the drugs themselves start causing suffering. Soon, we find we’re using drugs to relieve the misery that drugs themselves have caused. This is known as the “vicious cycle of addiction.”
It goes something like this: Life doesn’t feel too good. Bang! Try this drug or that drug, and things feel better. Come down off the drug, and things feel worse, just a little worse than they did before you took the drug in the first place. No matter. Bang! Use the drug and feel good again. Gradually, your biochemistry changes. Your brain learns that it doesn’t have to keep producing the chemicals that make you feel good. These chemicals keep appearing without the brain having to do any work. That’s why each time you try to get off the drugs, you feel a little worse than the time before. It becomes harder and harder for you to get off the drugs because you feel so bad whenever you try to stop.
And it all started with suffering, with your inability to accept suffering as an intimate part of life. You can break a drug habit anywhere along the way, or never start with drugs at all, simply by accepting life’s suffering and facing the suffering head-on. This doesn’t mean that you will live a sad, miserable, and tormented life. There are plenty of ways you can face your suffering and then cope with it. In fact, once you learn these ways and begin using some of them, you’ll feel as if your spirit has been renewed. Of course, it’s your choice. If you choose drugs to cope with life’s suffering, you choose a buy-now-pay-later method. It works in the moment, but it just postpones the suffering. And by postponing it, it builds up, so that when you finally do face it, the suffering is immense. The detoxification from drugs might take a week or two, but the long-term withdrawal, the period of time when your biochemistry (and thus your physical and mental health) returns to normal, can take years. Luckily, during this time, you gradually feel a little bit better, day by day. What can you do to get help? You have many options. First, let’s consider an in-patient rehabilitation facility.
By: Jonas Smith
It goes something like this: Life doesn’t feel too good. Bang! Try this drug or that drug, and things feel better. Come down off the drug, and things feel worse, just a little worse than they did before you took the drug in the first place. No matter. Bang! Use the drug and feel good again. Gradually, your biochemistry changes. Your brain learns that it doesn’t have to keep producing the chemicals that make you feel good. These chemicals keep appearing without the brain having to do any work. That’s why each time you try to get off the drugs, you feel a little worse than the time before. It becomes harder and harder for you to get off the drugs because you feel so bad whenever you try to stop.
And it all started with suffering, with your inability to accept suffering as an intimate part of life. You can break a drug habit anywhere along the way, or never start with drugs at all, simply by accepting life’s suffering and facing the suffering head-on. This doesn’t mean that you will live a sad, miserable, and tormented life. There are plenty of ways you can face your suffering and then cope with it. In fact, once you learn these ways and begin using some of them, you’ll feel as if your spirit has been renewed. Of course, it’s your choice. If you choose drugs to cope with life’s suffering, you choose a buy-now-pay-later method. It works in the moment, but it just postpones the suffering. And by postponing it, it builds up, so that when you finally do face it, the suffering is immense. The detoxification from drugs might take a week or two, but the long-term withdrawal, the period of time when your biochemistry (and thus your physical and mental health) returns to normal, can take years. Luckily, during this time, you gradually feel a little bit better, day by day. What can you do to get help? You have many options. First, let’s consider an in-patient rehabilitation facility.
By: Jonas Smith
Aug
2
Grey’s Anatomy: Episode 4.7 "physical Attraction. Chemical Reaction" Recap
Filed Under Physical Chemistry | Leave a Comment
The last episode of Grey’s Anatomy was all about sex, literally. We saw Izzie complaining about her chemistry with George, or the lack thereof. The same can’t be said about Derek and Meredith, though, as the two were brimming with sexual tension. However, Derek thought that their relationship lacked more of the love. Moreover, Mark teased Derek of being the Chief’s new girlfriend when Derek frequently picked up the Chief’s dry cleaning for him, and subsequently had dinner and a movie with him.
Meredith experienced some sister trouble when she forbid Lexie to sleep with Alex at Meredith’s place. Meredith even told her off, saying that Lexie should start living her own life and get her own friends. Not wanting to get in between them, Alex kept his distance.
Callie, on the other hand, went through a rough time dealing with her administrative responsibilities, and thus asked help from Bailey, who gladly covered for her while she scrubbed in for back-to-back duties.
Featured patients tonight were the marbles-swallowing kid whom George attended, a man who couldn’t move his bowels, who was attended by Alex, and an annoying woman demanding for a facelift, attended by Izzie. The bowel guy and facelift woman annoyed Izzie and Alex so much that they followed Bailey’s advice of placing them in the same room, so that they could annoy each other. However, their plan failed as the two became more than just friends in a matter of hours. The two patients hit it off so well that when Alex and Izzie walked in, they were having sex. This made Izzie realize how much she and George lacked chemistry, and made her resentful about it.
For the night, Cristina attended to a woman who fell down the stairs while carrying her adopted baby. Lexie was in charge of the baby, while Erica took over the mother, who later on died, leaving her husband to take care of the baby he named Keisha.
The end of the episode, Izzie and George finally develop some chemistry, causing them to have the best sex ever.
For more resources about Grey’s Anatomy or for the full story of Grey’s Anatomy: Episode 4.7 “Physical Attraction… Chemical Reaction” Recap please review http://www.buddytv.com
By: Groshan Fabiola
Meredith experienced some sister trouble when she forbid Lexie to sleep with Alex at Meredith’s place. Meredith even told her off, saying that Lexie should start living her own life and get her own friends. Not wanting to get in between them, Alex kept his distance.
Callie, on the other hand, went through a rough time dealing with her administrative responsibilities, and thus asked help from Bailey, who gladly covered for her while she scrubbed in for back-to-back duties.
Featured patients tonight were the marbles-swallowing kid whom George attended, a man who couldn’t move his bowels, who was attended by Alex, and an annoying woman demanding for a facelift, attended by Izzie. The bowel guy and facelift woman annoyed Izzie and Alex so much that they followed Bailey’s advice of placing them in the same room, so that they could annoy each other. However, their plan failed as the two became more than just friends in a matter of hours. The two patients hit it off so well that when Alex and Izzie walked in, they were having sex. This made Izzie realize how much she and George lacked chemistry, and made her resentful about it.
For the night, Cristina attended to a woman who fell down the stairs while carrying her adopted baby. Lexie was in charge of the baby, while Erica took over the mother, who later on died, leaving her husband to take care of the baby he named Keisha.
The end of the episode, Izzie and George finally develop some chemistry, causing them to have the best sex ever.
For more resources about Grey’s Anatomy or for the full story of Grey’s Anatomy: Episode 4.7 “Physical Attraction… Chemical Reaction” Recap please review http://www.buddytv.com
By: Groshan Fabiola
Aug
2
what determines the physical state of a substance at room tempurature?
Filed Under Physical Chemistry | 5 Comments
it is a chemistry hw assignment.
By: lotyr14
By: lotyr14