IP Library Granted Patent US 8,410,170
Granted Patent B2
US 8,410,170 · App. 13/231,406 · Granted Apr 2, 2013

Use of isothiocyanates compounds in treating prostatic diseases and skin cancer

Inventors: Jingcai Cheng (Wuxi, CN); Jenwei Chiao (Wuxi, CN); Haiya Jin (Wuxi, CN); Chengjuan Zhong (Wuxi, CN)
Assignee: Wuxi JC Pharmaceutical Technology Co., Ltd.
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Quick Facts
Patent No.
US 8,410,170
App. No.
13/231,406
Granted
Apr 2, 2013
Kind
B2
Abstract

A method for preventing and treating prostatic diseases and skin cancer using naturally or artificially synthesized isothiocyanates compounds or the derivatives or metabolites thereof.

Claims (23)

1. A method for the treatment of prostatitis in a subject, comprising: administrating, to the subject, a composition comprising an effective amount of at least one selected from the group consisting of an isothiocyanate compound, a derivative of an isothiocyanate compound, and a metabolite of an isothiocyanate compound,

wherein the isothiocyanate compound is at least one selected from the group consisting of:

benzyl isothiocyanate (BITC) isothiocyanate (PEITC), allyl isothiocyanate (AITC) and 4-sulfophenylisothiocyanate which have the following formulas (1), (2), (3), and (4), respectively;

and wherein each of said derivative and metabolite is at least one selected from the group consisting of a glutathione-conjugate, a cysteinyl glycine-conjugate, a cysteinyl-conjugate, and an N-acetylcysteine-conjugate.

2. The method of claim 1 , wherein the effective amount is an amount effective for inducing the expression of glutathione S-transferase (GSTP1) gene in prostate cells.

3. The method of claim 1 , wherein the effective amount is an amount effective for inhibiting the expressions of (i) androgen receptor (AR), (ii) transcription factor Sp1, the upstream gene of androgen receptor (AR), and (iii) prostate specific antigen (PSA), the downstream gene of AR.

4. The method of claim 1 , wherein each of the derivative and the metabolite is at least one selected from the group consisting of: N-acetylcysteine conjugate of benzyl isothiocyanate (BITC-NAC), N-acetylcysteine conjugate of phenethyl isothiocyanate (PEITC-NAC), N-acetylcysteine conjugate of allyl isothiocyanate (AITC-NAC), and N-acetylcysteine conjugate of 4-sulfophenylisothiocyanate (SPITC-NAC), which have the following formulas (5), (6), (7), and (8) respectively:

5. The method of claim 1 , wherein the isothiocyanate compound, the derivative, or the metabolite is used alone or used as a formulation with excipients.

6. The method of claim 5 , wherein the formulation is at least one selected from the group consisting of a pharmaceutical product, dietary supplement, food, and cosmetic product.

7. The method of claim 1 , wherein the composition contains the following ingredients:

(a) an active pharmaceutical ingredient(API), wherein said API is at least one selected from the group consisting of an isothiocyanate compound, a derivative of an isothiocyanate compound, and a metabolite of an isothiocyanate compound,

wherein the isothiocyanate compound is at least one selected from the group consisting of: benzyl isothiocyanate (BITC), phenethyl isothiocyanate (PEITC), allyl isothiocyanate (AITC), and 4-sulfophenylisothiocyanate (SPITC), which have the following formulas (1), (2), (3), and (4) respectively;

and wherein said derivative and metabolite is at least one selected from the group consisting of a glutathione-conjugate, a cysteinyl glycine-conjugate, a cysteinyl-conjugate, and an N-acetylcysteine-conjugate, and

(b) a pharmaceutically acceptable carrier for the API, wherein said carrier is at least one selected from the group consisting of a surfactant, a solubilizing agent, an oil ingredient, and an antioxidant;

wherein the surfactant is at least one selected from the group consisting of polyoxyethylene lauryl ether, polyoxyethylene glycol monostearate, vitamin E polyethylene glycol succinate, polyoxyethylene castor oil, polyoxyethylene hydrogenated castor oil, poloxamer, and a polysorbate;

wherein the solubilizing agent is at least one selected from the group consisting of polyvinylpyrrolidone K17, K25, K30, or K90; and polyethylene glycol 400, 4000, or 6000;

wherein the oil ingredient is at least one selected from the group consisting of fatty acids, triglyceride, monoglyceride, diglyceride, soybean oil, corn oil, peanut oil, stearic acid, palmitic acid, palm oil, sunflower oil, olive oil, coconut oil, sesame oil, cottonseed oil, canola oil, oleic acid, linoleic acid, medium-chain triglycerides, glyceryl monooctadecanoate, glyceryl monoacetate, glyceryl diacetate, and glyceryl triacetate; and

wherein the antioxidant is a water-soluble antioxidant or a fat-soluble antioxidant, and is at least one selected from the group consisting of vitamin C, vitamin C palmitate, propyl gallate, tocopherol, tert-butylated-p-hydroxyanisole, and 2,6-di-tert-butyl-p-methylphenol.

8. The method of claim 7 , wherein the composition is at least one selected from the group consisting of a tablet, a capsule, a pill, a powder for injection, an injection, a lyophilized powder, an ointment, a suppository, a cream, a film, an emulsion, a spray, and an implant.

9. The method of claim 7 , wherein the composition is a pharmaceutical product or a dietary supplement.

10. The method of claim 7 , wherein the composition is administered orally, intravenously, muscularly, subcutaneously, intracavitaryly, sublingually, anally, or topically.

11. The method of claim 1 , wherein the composition is administrated alone or in a combined therapy.

12. The method of claim 11 , wherein the combined therapy is at least one therapy selected from the group consisting of surgery, radiation, gene therapy, and biologics.

Priority Claims (2)
CN 2005 1 0095737 · Nov 15, 2005 · national
CN 2006 1 0038112 · Jan 27, 2006 · national
Continuity (2)
Division 12093829
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