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对抗利什曼原虫药物苦味叶下珠素的脂质体和非离子表面活性剂囊泡形式的体内活性和毒性进行评估。

Evaluation of the in-vivo activity and toxicity of amarogentin, an antileishmanial agent, in both liposomal and niosomal forms.

作者信息

Medda S, Mukhopadhyay S, Basu M K

机构信息

Biomembrane Division, Indian Institute of Chemical Biology, 4, Raja S.C. Mullick Road, Calcutta 700032, India.

出版信息

J Antimicrob Chemother. 1999 Dec;44(6):791-4. doi: 10.1093/jac/44.6.791.

Abstract

The antileishmanial property of amarogentin, a secoiridoid glycoside isolated from the Indian medicinal plant Swertia chirata, was examined in a hamster model of experimental leishmaniasis. The therapeutic efficacy of amarogentin was evaluated in free and two different vesicular forms, liposomes and niosomes. The amarogentin in both liposomal and niosomal forms was found to be a more active leishmanicidal agent than the free amarogentin; and the niosomal form was found to be more efficacious than the liposomal form at the same membrane microviscosity level. Toxicity studies involving blood pathology, histological staining of tissues and specific enzyme levels related to normal liver function showed no toxicity. Hence, amarogentin incorporated in liposomes or niosomes may have clinical application in the treatment of leishmaniasis.

摘要

从印度药用植物獐牙菜中分离得到的裂环烯醚萜苷类化合物苦味叶下珠素的抗利什曼原虫特性,在实验性利什曼病的仓鼠模型中进行了研究。苦味叶下珠素在游离形式以及两种不同的囊泡形式(脂质体和非离子型表面活性剂泡囊)下的治疗效果进行了评估。结果发现,脂质体和非离子型表面活性剂泡囊形式的苦味叶下珠素均比游离苦味叶下珠素具有更强的杀利什曼原虫活性;并且在相同的膜微粘度水平下,非离子型表面活性剂泡囊形式比脂质体形式更有效。涉及血液病理学、组织学染色以及与正常肝功能相关的特定酶水平的毒性研究表明没有毒性。因此,包载于脂质体或非离子型表面活性剂泡囊中的苦味叶下珠素可能在利什曼病的治疗中具有临床应用价值。

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