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金钱松主要成分土槿皮酸B的抗真菌活性评价

Antifungal evaluation of pseudolaric acid B, a major constituent of Pseudolarix kaempferi.

作者信息

Li E, Clark A M, Hufford C D

机构信息

Department of Pharmacognosy, School of Pharmacy, University of Mississippi, University 38677.

出版信息

J Nat Prod. 1995 Jan;58(1):57-67. doi: 10.1021/np50115a007.

Abstract

Pseudolaric acid B [1] was isolated and identified as the main antifungal constituent of Pseudolarix kaempferi using bioassay-directed fractionation. Pseudolaric acid B was active against Trichophyton mentagrophytes, Torulopsis petrophilum, Microsporum gypseum, and Candida spp., while its methylated or hydrolyzed derivatives were not active against these same organisms. The minimum inhibitory concentrations and minimum fungicidal concentrations of pseudolaric acid B [1] against Candida and Torulopsis species were comparable with those of amphotericin B. The in vivo activity of pseudolaric acid B was evaluated in a murine model of disseminated candidiasis. Pseudolaric acid B [1] reduced the number of recovered colony-forming units significantly at different dosages. Infected mice treated intravenously with pseudolaric acid B [1] also had a longer survival time than those treated with vehicle alone.

摘要

通过生物活性导向分离法,从金钱松中分离并鉴定出了土槿皮酸B[1],它是金钱松主要的抗真菌成分。土槿皮酸B对须癣毛癣菌、嗜石球拟酵母菌、石膏样小孢子菌和念珠菌属具有活性,而其甲基化或水解衍生物对这些相同的微生物没有活性。土槿皮酸B[1]对念珠菌属和球拟酵母菌属的最低抑菌浓度和最低杀菌浓度与两性霉素B相当。在播散性念珠菌病的小鼠模型中评估了土槿皮酸B的体内活性。不同剂量的土槿皮酸B[1]均能显著减少回收的菌落形成单位数量。静脉注射土槿皮酸B[1]治疗的感染小鼠的存活时间也比仅用赋形剂治疗的小鼠更长。

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