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(黄水莲)叶提取物和纯化的6,6'-二羟基硫代双去甲乌药碱(DTBN)的抗性质

Anti- Properties of (Yellow Water Lily) Leaf Extracts and Purified 6,6' Dihydroxythiobinupharidine (DTBN).

作者信息

Shmuel Orit, Rasti Aviv, Zaknoun Melodie, Astman Nadav, Golan-Goldhirsh Avi, Sagi Orly, Gopas Jacob

机构信息

Shraga Segal Dept. of Microbiology Immunology and Genetics, Faculty of Health Sciences, Ben Gurion University of the Negev, Beer Sheva 8410501, Israel.

Department of Clinical Biochemistry & Pharmacology, Faculty of Health Sciences, Ben-Gurion University of the Negev, Beer Sheva 8410501, Israel.

出版信息

Pathogens. 2024 May 6;13(5):384. doi: 10.3390/pathogens13050384.

Abstract

Cutaneous leishmaniasis (CL) is a zoonotic disease, manifested as chronic ulcers, potentially leaving unattractive scars. There is no preventive vaccination or optimal medication against leishmaniasis. Chemotherapy generally depends upon a small group of compounds, each with its own efficacy, toxicity, and rate of drug resistance. To date, no standardized, simple, safe, and highly effective regimen for treating CL exists. Therefore, there is an urgent need to develop new optimal medication for this disease. Sesquiterpen thio-alkaloids constitute a group of plant secondary metabolites that bear great potential for medicinal uses. The nupharidines found in belong to this group of compounds. We have previously published that semi-purified extract containing major components of nupharidines has strong anti-leishmanial activity in vitro. Here, we present in vivo data on the therapeutic benefit of the extract against () in infected mice. We also expanded these observations by establishing the therapeutic effect of the extract-purified nupharidine 6,6'-dihydroxythiobinupharidine (DTBN) in vitro against promastigotes and intracellular amastigotes as well as in vivo in -infected mice. The results suggest that this novel anti-parasitic small molecule has the potential to be further developed against

摘要

皮肤利什曼病(CL)是一种人畜共患病,表现为慢性溃疡,可能会留下难看的疤痕。目前尚无针对利什曼病的预防性疫苗或最佳药物。化疗通常依赖于一小类化合物,每种化合物都有其自身的疗效、毒性和耐药率。迄今为止,尚无用于治疗CL的标准化、简单、安全且高效的方案。因此,迫切需要为这种疾病开发新的最佳药物。倍半萜硫代生物碱是一类具有巨大药用潜力的植物次生代谢产物。在[具体植物]中发现的睡莲碱属于这类化合物。我们之前发表过含有睡莲碱主要成分的半纯化提取物在体外具有很强的抗利什曼原虫活性。在此,我们展示了该提取物对感染小鼠体内[具体病原体]的治疗益处的体内数据。我们还通过确定提取物纯化的睡莲碱6,6'-二羟基硫代双睡莲碱(DTBN)在体外对前鞭毛体和细胞内无鞭毛体以及在体内对[具体病原体]感染小鼠的治疗效果来扩展这些观察结果。结果表明,这种新型抗寄生虫小分子有进一步开发用于[治疗对象]的潜力

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4e58/11124111/7a0bfed2b024/pathogens-13-00384-g001.jpg

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