Three cassane type diterpenoid lactone compounds with activity against plasmodium falciparum
A technology of Plasmodium falciparum and diterpene lactones, applied in the fields of organic active ingredients, organic chemistry, resistance to vector-borne diseases, etc., can solve problems such as undiscovered
Inactive Publication Date: 2010-08-25
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI +1
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Compounds 5α, 14β-dihydroxy-1α, 6α, 7β-triacetyl-13(15), 11(12)-diene-16, 12-lactone (I) and 12α-methoxy 5α, 14β-dihydroxy-1α, 6α, 7β-triacetyl-13(15)-ene-16,12-lactone (Ⅱ) are two new compounds, and their antimalarial biological activity is discovered for the first time. The antimalarial biological activity of the compound neocaesalpin L(Ⅲ) was also discovered for the first time. So far, no patents or literature reports have been found for the above research results
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Abstract
The invention relates to a type of cassane type diterpenoid lactone compounds with activity against plasmodium falciparum, which are prepared by taking seeds of a leguminous medicinal plant of caesalpinia minax hance as raw materials, using a specific solvent for extraction, carrying out a variety of chromatography and finally obtaining three cassane type diterpenoid lactone monomeric compounds, which are 5 alpha, 14 beta-dihydroxy-1 alpha, 6 alpha, 7 beta-triacetyl-13(15), 11(12)-diene-16, 12-lactone (I), 12 alpha-methoxy, 5 alpha, 14 beta-dihydroxy-1 alpha, 6 alpha, 7 beta-triacetyl-13(15)-ene-16, 12-lactone (II) and neocaesalpin L (III) respectively, wherein the compound I and the compound II are new compounds. The first research test of in vitro anti-malarial pharmacodynamics of the three compounds shows that the three compounds have obvious effect of suppressing the plasmodium falciparum and can be used for preparing drugs for treating and / or preventing malaria.
Description
technical field The invention relates to three kinds of kazane-type diterpene lactone monomer compounds separated from the seeds of the medicinal plant Caesalpinia minax Hance by means of phytochemical extraction and separation, wherein there are two compounds for new compounds. The preparation method of the three compounds, the structure of the two new compounds and the application of the three compounds in the preparation of medicines for treating and / or preventing malaria are applied for patent protection. Background technique There are more than 100 species of plants in the genus Caesalpinia Linn of the Leguminosoe family, mainly distributed in subtropical and tropical regions. About 17 species are produced in my country, especially Caesalpinia japonica Sieb. The production of Yunshi (Caesalpinia minax Hance.) is relatively large, mainly in five provinces of Hainan, Guangdong, Guangxi, Yunnan and Guizhou in the south and southwest, and there are 14 kinds of medicines (se...
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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/77A61K31/365A61P33/06
CPCY02A50/30
Inventor 许旭东马丽焱缪剑华程燕袁经权许娜
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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