生物活性

• 描述Clotrimazole is a broad-spectrum antimycotic drug mainly used for the treatment of Candida albicans and other fungal infections^[3]. In vitro, it is most active against Candida spp., Trichophyton spp., Microsporum spp. and Malazzesia fuffur (Pityrosporon orbiculare). In addition, it has some in vitro activity against certain Gram-positive bacteria, and at very high concentrations has activity against Trichomonas spp^[4]. The antimycotic drug clotrimazole inhibits the function of the gastric H,K-ATPase in a manner similar to that observed for the Na,K-ATPase^[5]. S. officinalis in the form of vaginal tablet, alone and when combined with Clotrimazole, can treat the Vulvovaginal Candidiasis^[6]. Moreover, thirty female Wistar rats with surgically implanted autologous endometrium were treated with CTZ (Clotrimazole) or vehicle (200 mg/kg) via esophageal gavage for 15 consecutive days. CTZ treatment significantly decreased the growth and the size of the implants, and histological examination indicated regression and atrophy, with no toxicity to the animals. CTZ promoted an overall amelioration of endometriosis in a rat model due to the anti-angiogenic properties of the drug^[7].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00835510	Tinea Pedis	Phase 1	Completed	-	United States, California ... more >> Investigator Site Burbank, California, United States Investigator Site San Diego, California, United States United States, Florida Investigator Site Miami, Florida, United States United States, Georgia Investigator Site Martinez, Georgia, United States Investigator Site Stockbridge, Georgia, United States United States, Michigan Investigator Site Clinton Township, Michigan, United States United States, North Carolina Investigator Site Hickory, North Carolina, United States Investigator Site Raleigh, North Carolina, United States Investigator Site Salisbury, North Carolina, United States United States, Ohio Investigator Site Sylvania, Ohio, United States United States, South Carolina Investigator Site Simpsonville, South Carolina, United States United States, Tennessee Investigator Site Bristol, Tennessee, United States Investigator Site Nashville, Tennessee, United States United States, Texas Investigator Site College Station, Texas, United States Investigator Site Houston, Texas, United States Investigator Site San Antonio, Texas, United States Belize Investigator Site Belize City, Belize Collapse <<
  NCT01049633	-	-	-	-	United States, Pennsylvania ... more >> Hospital of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 Collapse <<
  NCT00835510	-	-	Completed	-	-

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• 参考文献

• [1] Eastman RT, Fidock DA. Artemisinin-based combination therapies: a vital tool in efforts to eliminate malaria. Nat Rev Microbiol. 2009 Dec;7(12):864-74.

  [2] Aktas H, Fluckiger R, et al. Depletion of intracellular Ca2+ stores, phosphorylation of eIF2alpha, and sustained inhibition of translation initiation mediate the anticancer effects of clotrimazole. Proc Natl Acad Sci U S A. 1998 Jul 7;95(14):8280-5.

  [3] Crowley PD, Gallagher HC. Clotrimazole as a pharmaceutical: past, present and future. J Appl Microbiol. 2014 Sep;117(3):611-7

  [4] Sawyer PR, Brogden RN, Pinder RM, Speight TM, Avery. Clotrimazole: a review of its antifungal activity and therapeutic efficacy. Drugs. 1975;9(6):424-47

  [5] Witzke A, Lindner K, Munson K, Apell HJ. Inhibition of the gastric H,K-ATPase by clotrimazole. Biochemistry. 2010 Jun 1;49(21):4524-32

  [6] Ahangari F, Farshbaf-Khalili A, Javadzadeh Y, Adibpour M, Sadeghzadeh Oskouei B. Comparing the effectiveness of Salvia officinalis, clotrimazole and their combination on vulvovaginal candidiasis: A randomized, controlled clinical trial. J Obstet Gynaecol Res. 2019 Apr;45(4):897-907

  [7] Machado DE, Perini JA, de Mendonça EM, Branco JR, Rodrigues-Baptista KC, Alessandra-Perini J, Espíndola-Netto JM, Dos Santos TA, Coelho WS, Nasciutti LE, Sola-Penna M, Zancan P. Clotrimazole is effective for the regression of endometriotic implants in a Wistar rat experimental model of endometriosis. Mol Cell Endocrinol. 2018 Nov 15;476:17-26

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