but What about Today
Established Member
- Reaction score
- 0
Minoxidil sulfate
“An important step in understanding minoxidil’s mechanism of action on hair follicles was to determine the drug’s active form. We used organ-cultured vibrissa follicles to test whether it is minoxidil or its sulfated metabolite, minoxidil sulfate, that stimulates hair growth. Follicles from neonatal mice were cultured with or without drugs and effects were assessed by measuring incorporation of radiolabeled cysteine in hair shafts of the treated follicles. Assays of minoxidil sulfotransferase activity indicated that vibrissae follicles metabolize minoxidil to minoxidil sulfate. Dose-response studies showed that minoxidil sulfate is 14 times more potent than minoxidil in stimulating cysteine incorporation in cultured follicles. Three drugs that block production of intrafollicular minoxidil sulfate were tested for their effects on drug-induced hair growth. Diethylcarbamazine proved to be a noncompetitive inhibitor of sulfotransferase and prevented hair growth stimulation by minoxidil but not by minoxidil sulfate. Inhibiting the formation of intracellular PAPS with chlorate also blocked the action of minoxidil but not of minoxidil sulfate. Acetaminophen, a potent sulfate scavenger blocked cysteine incorporation by minoxidil. It also blocked follicular stimulation by minoxidil sulfate apparently by directly removing the sulfate from the drug. Experiments with U-51,607, a potent minoxidil analog that also forms a sulfated metabolite, showed that its activity was inhibited by both chlorate and diethylcarbamazine. These studies show that sulfation is a critical step for hair-growth effects of minoxidil and that it is the sulfated metabolite that directly affects hair follicles.â€
The authors of the article also mention the possibility that the difference between good responders and poor responders to minoxidil may be due to a difference in their sulfotransferases metabolism in the skin. Since minoxidil sulphate is already sulphated its action does no longer depend on the sulfotransferases, therefore poor minoxidil responders may become good responders with minoxidil sulphate.
The sulfotransferases are also needed to activate physiological growth factors like HGF to their active sulphated form. Cytosolic sulfotransferases (ST) catalyze the sulfation of various phenolic agents, catecholamines, thyroid hormones, steroids, drugs, and procarcinogens, usually resulting in the inactivation and subsequent excretion of the compound. T. P. Dooley did a study Exp Dermatol speculates that sulfotransferases might also be involved in bioinactivation of estrogens and androgens within skin. Therefore it is perhaps not a good idea to distract the sulfotransferases from their normal useful jobs by keeping them busy with the conversion of minoxidil to minoxidil sulphate. Obviously by using directly minoxidil sulphate one can avoid these possible adverse effects.
I wonder how Dr. Lee 15% minoxidil is comparable to minoxidil sulfate, Im going to email him and ask what he thinks. Spectral DNC and Nanominox-MS contain minoxidil sulfate. idk, what you think?
“An important step in understanding minoxidil’s mechanism of action on hair follicles was to determine the drug’s active form. We used organ-cultured vibrissa follicles to test whether it is minoxidil or its sulfated metabolite, minoxidil sulfate, that stimulates hair growth. Follicles from neonatal mice were cultured with or without drugs and effects were assessed by measuring incorporation of radiolabeled cysteine in hair shafts of the treated follicles. Assays of minoxidil sulfotransferase activity indicated that vibrissae follicles metabolize minoxidil to minoxidil sulfate. Dose-response studies showed that minoxidil sulfate is 14 times more potent than minoxidil in stimulating cysteine incorporation in cultured follicles. Three drugs that block production of intrafollicular minoxidil sulfate were tested for their effects on drug-induced hair growth. Diethylcarbamazine proved to be a noncompetitive inhibitor of sulfotransferase and prevented hair growth stimulation by minoxidil but not by minoxidil sulfate. Inhibiting the formation of intracellular PAPS with chlorate also blocked the action of minoxidil but not of minoxidil sulfate. Acetaminophen, a potent sulfate scavenger blocked cysteine incorporation by minoxidil. It also blocked follicular stimulation by minoxidil sulfate apparently by directly removing the sulfate from the drug. Experiments with U-51,607, a potent minoxidil analog that also forms a sulfated metabolite, showed that its activity was inhibited by both chlorate and diethylcarbamazine. These studies show that sulfation is a critical step for hair-growth effects of minoxidil and that it is the sulfated metabolite that directly affects hair follicles.â€
The authors of the article also mention the possibility that the difference between good responders and poor responders to minoxidil may be due to a difference in their sulfotransferases metabolism in the skin. Since minoxidil sulphate is already sulphated its action does no longer depend on the sulfotransferases, therefore poor minoxidil responders may become good responders with minoxidil sulphate.
The sulfotransferases are also needed to activate physiological growth factors like HGF to their active sulphated form. Cytosolic sulfotransferases (ST) catalyze the sulfation of various phenolic agents, catecholamines, thyroid hormones, steroids, drugs, and procarcinogens, usually resulting in the inactivation and subsequent excretion of the compound. T. P. Dooley did a study Exp Dermatol speculates that sulfotransferases might also be involved in bioinactivation of estrogens and androgens within skin. Therefore it is perhaps not a good idea to distract the sulfotransferases from their normal useful jobs by keeping them busy with the conversion of minoxidil to minoxidil sulphate. Obviously by using directly minoxidil sulphate one can avoid these possible adverse effects.
I wonder how Dr. Lee 15% minoxidil is comparable to minoxidil sulfate, Im going to email him and ask what he thinks. Spectral DNC and Nanominox-MS contain minoxidil sulfate. idk, what you think?
