• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

荷蘭地麻素和其他化合物及其在抗非洲锥虫病、利什曼病和疟疾病因物中的活性。

The activities of suaveolol and other compounds from Hyptis suaveolens and Momordica charantia against the aetiological agents of African trypanosomiasis, leishmaniasis and malaria.

机构信息

Department of Biotechnology, Nigerian Defence Academy, PMB 2109, Kaduna, Kaduna State, Nigeria.

Department of Biological Sciences, Nigerian Defence Academy, PMB 2109, Kaduna, Kaduna State, Nigeria.

出版信息

Exp Parasitol. 2024 Aug-Sep;263-264:108807. doi: 10.1016/j.exppara.2024.108807. Epub 2024 Jul 21.

DOI:10.1016/j.exppara.2024.108807
PMID:39043327
Abstract

African trypanosomiasis and malaria are among the most severe health challenges to humans and livestock in Africa and new drugs are needed. Leaves of Hyptis suaveolens Kuntze (Lamiaceae) and Momordica charantia L. (Cucurbitaceae) were extracted with hexane, ethyl acetate, and then methanol, and subjected to silica gel column chromatography. Structures of six isolated compounds were elucidated through NMR and HR-EIMS spectrometry. Callistrisic acid, dehydroabietinol, suaveolic acid, suaveolol, and a mixture of suaveolol and suaveolic acid (SSA) were obtained from H. suaveolens, while karavilagenin D and momordicin I acetate were obtained from M. charantia. The isolated biomolecules were tested against trypomastigotes of Trypanosoma brucei brucei and T. congolense, and against Plasmodium falciparum. The most promising EC values were obtained for the purified suaveolol fraction, at 2.71 ± 0.36 μg/mL, and SSA, exhibiting an EC of 1.56 ± 0.17 μg/mL against T. b. brucei trypomastigotes. Suaveolic acid had low activity against T. b. brucei but displayed moderate activity against T. congolense trypomastigotes at 11.1 ± 0.5 μg/mL. Suaveolol and SSA were also tested against T. evansi, T. equiperdum, Leishmania major and L. mexicana but the antileishmanial activity was low. Neither of the active compounds, nor the mixture of the two, displayed any cytotoxic effect on human foreskin fibroblast (HFF) cells at even the highest concentration tested, being 200 μg/mL. We conclude that suaveolol and its mixture possessed significant and selective trypanocidal activity.

摘要

非洲锥虫病和疟疾是非洲人类和牲畜面临的最严重的健康挑战之一,需要新的药物。从 Hyptis suaveolens Kuntze(唇形科)和 Momordica charantia L.(葫芦科)的叶子中用己烷、乙酸乙酯和甲醇提取,并进行硅胶柱层析。通过 NMR 和 HR-EIMS 光谱学阐明了六种分离化合物的结构。从 H. suaveolens 中得到了 Callistrisic 酸、脱氢枞醇、suaveolic 酸、suaveolol 以及 suaveolol 和 suaveolic 酸的混合物(SSA),而从 M. charantia 中得到了 karavilagenin D 和 momordicin I 乙酸酯。分离的生物分子针对 Trypanosoma brucei brucei 和 T. congolense 的锥虫和 Plasmodium falciparum 进行了测试。从纯化的 suaveolol 部分获得了最有希望的 EC 值,为 2.71 ± 0.36 μg/mL,而 SSA 对 T. b. brucei 锥虫的 EC 值为 1.56 ± 0.17 μg/mL。suaveolic 酸对 T. b. brucei 的活性较低,但对 T. congolense 锥虫的活性适中,为 11.1 ± 0.5 μg/mL。Suaveolol 和 SSA 也针对 T. evansi、T. equiperdum、Leishmania major 和 L. mexicana 进行了测试,但抗利什曼原虫活性较低。即使在测试的最高浓度 200 μg/mL 下,也没有任何一种活性化合物或两者的混合物对人包皮成纤维细胞(HFF)细胞显示出任何细胞毒性作用。我们得出结论,suaveolol 及其混合物具有显著的选择性杀锥虫活性。

相似文献

1
The activities of suaveolol and other compounds from Hyptis suaveolens and Momordica charantia against the aetiological agents of African trypanosomiasis, leishmaniasis and malaria.荷蘭地麻素和其他化合物及其在抗非洲锥虫病、利什曼病和疟疾病因物中的活性。
Exp Parasitol. 2024 Aug-Sep;263-264:108807. doi: 10.1016/j.exppara.2024.108807. Epub 2024 Jul 21.
2
In vitro antiprotozoal activity and cytotoxicity of extracts and isolated constituents from Greenwayodendron suaveolens.光滑绿径树提取物及分离成分的体外抗寄生虫活性和细胞毒性
J Ethnopharmacol. 2016 Dec 4;193:510-516. doi: 10.1016/j.jep.2016.09.051. Epub 2016 Sep 29.
3
Bioassay-guided isolation of active principles from Nigerian medicinal plants identifies new trypanocides with low toxicity and no cross-resistance to diamidines and arsenicals.基于生物测定的尼日利亚药用植物活性成分分离鉴定出具有低毒性和无交叉耐药性的新型抗锥虫药物,与双脒类和砷剂无交叉耐药性。
J Ethnopharmacol. 2017 Apr 18;202:256-264. doi: 10.1016/j.jep.2017.03.028. Epub 2017 Mar 20.
4
Antiparasitic activities of two sesquiterpenic lactones isolated from Acanthospermum hispidum D.C.从糙叶斑种草中分离得到的两种倍半萜内酯的抗寄生虫活性
J Ethnopharmacol. 2012 May 7;141(1):411-7. doi: 10.1016/j.jep.2012.03.002. Epub 2012 Mar 13.
5
Discovery of 2-(1H-imidazo-2-yl)piperazines as a new class of potent and non-cytotoxic inhibitors of Trypanosoma brucei growth in vitro.发现2-(1H-咪唑-2-基)哌嗪类化合物作为一类新型的体外抑制布氏锥虫生长的强效且无细胞毒性的抑制剂。
Bioorg Med Chem Lett. 2018 Dec 15;28(23-24):3689-3692. doi: 10.1016/j.bmcl.2018.10.028. Epub 2018 Oct 22.
6
Oral administration of azithromycin ameliorates trypanosomosis in Trypanosoma congolense-infected mice.口服阿奇霉素可改善感染刚果锥虫的小鼠的锥虫病。
Parasitol Res. 2017 Sep;116(9):2407-2415. doi: 10.1007/s00436-017-5542-7. Epub 2017 Jul 4.
7
3-(Oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei, the causative agent for human African trypanosomiasis.3-(恶唑并[4,5-b]吡啶-2-基)苯胺类作为新型有效的克氏锥虫抑制剂,克氏锥虫是引起人类非洲锥虫病的病原体。
Eur J Med Chem. 2013 Aug;66:450-65. doi: 10.1016/j.ejmech.2013.05.007. Epub 2013 May 16.
8
In vitro trypanocidal activity of the anti-helminthic drug niclosamide.抗蠕虫药氯硝柳胺的体外杀锥虫活性。
Exp Parasitol. 2008 Apr;118(4):637-40. doi: 10.1016/j.exppara.2007.12.001. Epub 2007 Dec 15.
9
Inhibition of trypanosome alternative oxidase without its N-terminal mitochondrial targeting signal (ΔMTS-TAO) by cationic and non-cationic 4-hydroxybenzoate and 4-alkoxybenzaldehyde derivatives active against T. brucei and T. congolense.对布氏锥虫和刚果锥虫具有活性的阳离子和非阳离子4-羟基苯甲酸酯及4-烷氧基苯甲醛衍生物对没有N端线粒体靶向信号的锥虫交替氧化酶(ΔMTS-TAO)的抑制作用
Eur J Med Chem. 2018 Apr 25;150:385-402. doi: 10.1016/j.ejmech.2018.02.075. Epub 2018 Feb 26.
10
Cucurbitane-type triterpenoids from the stems and leaves of Momordica charantia.苦瓜茎和叶中的葫芦烷型三萜。
Fitoterapia. 2014 Jun;95:75-82. doi: 10.1016/j.fitote.2014.03.005. Epub 2014 Mar 14.