In vivo anti-malarial activity and toxicity studies of triterpenic esters isolated form Keetia leucantha and crude extracts.
In vivo anti-malarial activity and toxicity studies of triterpenic esters isolated form Keetia leucantha and crude extracts.
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DOI：
10.1186/s12936-017-2054-y
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发表时间：
2017-10-10
期刊：
影响因子：
3
通讯作者：
Bero J
中科院分区：
文献类型：
--
作者：
Beaufay C;Hérent MF;Quetin-Leclercq J;Bero J
为开发新的抗疟药物，对传统上用于治疗疟疾的离体抗疟植物白花Keetia leucantha（茜草科）进行了深入研究。本文旨在评价克雷伯氏菌的体内抗疟作用。白花三萜酯先前被鉴定为抗恶性疟原虫的最具体外活性的组分，以及它们的潜在毒性以及抗疟疾提取物的毒性。这八个三萜酯和主要的抗疟原虫三萜酸，熊果酸和油酸，量化的树枝二氯甲烷提取物通过验证的HPLC-UV方法。它们占该提取物的约19%（酸为16.9%，酯为1.8%）。HPLC-HRA还在树枝水煎液中鉴定出微量这些化合物。结果还表明，浸提液和酯类不会产生任何溶血，并且在总累积剂量分别为800和150 mg/kg时没有任何急性毒性。此外，与溶剂处理的小鼠相比，以50 mg/kg/天腹腔内给予伯氏疟原虫感染的小鼠的酯在感染后第4天显示出非常显著（p < 0.01）的寄生虫血症抑制（27.8 ± 5.4%）。这些结果为K. leucantha的使用和从其二氯甲烷提取物中鉴定抗疟疾化合物。其活性可以通过三萜酸和酯的存在来解释，其体内活性和安全性首次得到证实。
Considering the need for new anti-malarial drugs, further investigations on Keetia leucantha (Rubiaceae), an in vitro antiplasmodial plant traditionally used to treat malaria, were carried out. This paper aimed to assess the in vivo anti-malarial efficacy of K. leucantha triterpenic esters previously identified as the most in vitro active components against Plasmodium falciparum and their potential toxicity as well as those of anti-malarial extracts. These eight triterpenic esters and the major antiplasmodial triterpenic acids, ursolic and oleanolic acids, were quantified in the twigs dichloromethane extract by validated HPLC–UV methods. They account for about 19% of this extract (16.9% for acids and 1.8% for esters). These compounds were also identified in trace in the twigs decoction by HPLC-HRMS. Results also showed that extracts and esters did not produce any haemolysis, and were devoid of any acute toxicity at a total cumulative dose of 800 and 150 mg/kg respectively. Moreover, esters given intraperitoneally at 50 mg/kg/day to Plasmodium berghei-infected mice showed a very significant (p < 0.01) parasitaemia inhibition (27.8 ± 5.4%) on day 4 post-infection compared to vehicle-treated mice. These results bring out new information on the safety of K. leucantha use and on the identification of anti-malarial compounds from its dichloromethane extract. Its activity can be explained by the presence of triterpenic acids and esters which in vivo activity and safety were demonstrated for the first time.
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β酸和ursolic酸类似物的合成和抗血流活性。
DOI：
10.3390/molecules171012003
发表时间：
2012-10-12
期刊：
Molecules (Basel, Switzerland)
影响因子：
--
作者：
Innocente AM;Silva GN;Cruz LN;Moraes MS;Nakabashi M;Sonnet P;Gosmann G;Garcia CR;Gnoatto SC
通讯作者：
Gnoatto SC
影响因子：
3.4
作者：
Broniatowski, Marcin;Flasinski, Michal;Miskowiec, Pawel
通讯作者：
Miskowiec, Pawel
影响因子：
2.7
作者：
Drag-Zalesinska, Malgorzata;Kulbacka, Julita;Drag, Marcin
通讯作者：
Drag, Marcin
影响因子：
6
作者：
Chinaeke, E. E.;Chime, S. A.;Okore, V. C.
通讯作者：
Okore, V. C.
影响因子：
3
作者：
Deharo E;Ginsburg H
通讯作者：
Ginsburg H