Conversion method of caperia diterpene alcohol derivatives and its use in the preparation of antitumor drugs

A technology of capers and diterpene alcohols, applied in the field of biopharmaceuticals, can solve the problems of difficult-to-transform products and microbial transformation studies of caperia diterpenoids that have not yet been seen
CN107164422BActive Publication Date: 2021-01-22FUDAN UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
FUDAN UNIV
Publication Date
2021-01-22

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Abstract

The invention belongs to the technical field of the biological medicine, and relates to a microbial conversion method for a euphorbia lathyris diterpene compound. The method comprises the following steps: performing the microbial conversion to euphorbia lathyris phorbol and 7-hydroxy euphorbia lathyris phorbol by using Nocard's bacillus (i) Nocardia sp. ( / i) NRRL 5646, and preparing 3-carbonyl euphorbia lathyris phorbol and 7-acetoxyl euphorbia lathyris phorbol derivatives. Proved by the experiment, the polarity of the 3-carbonyl euphorbia lathyris phorbol in the derivative is reduced. Compared with a substrate, the derivative has the better cytotoxic activity. The derivative is an antitumor lead compound with development value.
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Description

technical field

[0001] The invention belongs to the field of biopharmaceuticals, and relates to a method for transforming caperia diterpenoid compounds, in particular to using known microorganisms to perform microbial transformation of caperia diterpene alcohols and derivatives thereof to prepare caperia caperis with anticancer activity Diterpenoid derivatives. Background technique

[0002] It is disclosed in the prior art that the diterpene-type compound of Caperia spp. belongs to the natural product of the diterpene skeleton, and has obvious anti-tumor activity and anti-tumor multidrug resistance (MDR). The study of structure-activity relationship shows that the difference of substituents on the core can obviously change the antitumor activity and MDR activity of this kind of compound.

[0003] Some studies have disclosed that the diterpenoid compounds of Caperia chinensis are from Euphorbiaceae Euphorbia lathyris was first isolated from L. (Tetrahedron Letters, 1971,...

Claims

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