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Artemisinin a-s and artemisinin a-g and their pharmaceutical compositions and applications

A composition and drug technology, applied in the direction of drug combination, preparation of organic compounds, active ingredients of heterocyclic compounds, etc., can solve the problems of no report of pharmaceutical composition, no report of liver cancer drug application of pharmaceutical composition, etc.

Active Publication Date: 2022-05-17
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there are no reports of artemyrianolides A-S (artemyrianolides A-S, 1-19) and artemyrianins A-G (artemyrianins A-G, 20-26) in the prior art, and there is no report of their pharmaceutical compositions as active ingredients. report, and there is no report on the application of its pharmaceutical composition in the preparation or treatment of liver cancer drugs

Method used

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  • Artemisinin a-s and artemisinin a-g and their pharmaceutical compositions and applications
  • Artemisinin a-s and artemisinin a-g and their pharmaceutical compositions and applications
  • Artemisinin a-s and artemisinin a-g and their pharmaceutical compositions and applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Preparation of compound 1-26:

[0024] The dried aerial parts of Artemisia multiflora were crushed, extracted by cold soaking with 90% ethanol twice, each time for 4 days, the ethanol extracts were combined and concentrated under reduced pressure until there was no alcohol smell, and the ethanol extract was obtained. The extract was suspended in water and extracted three times with ethyl acetate to obtain an ethyl acetate extract (1.2 kg). The fraction extracted from ethyl acetate was chromatographed on a silica gel column with gradient elution of acetone-petroleum ether (5:95, 10:90, 20:80, 30:70, 40:60, 50:50) to obtain 6 fractions Fr .A~Fr.F. Fr.C (150g) was subjected to medium pressure MCI CHP20P column chromatography, and gradient elution with water-methanol (50:50, 30:70, 20:80, 0:100) to obtain 4 components Fr.C1~Fr. C4; Fr.D (230g) was subjected to medium-pressure MCI CHP 20P column chromatography, and gradient elution with water-methanol (50:50, 30:70, 10:90)...

Embodiment 2

[0316] Cytotoxic activity of compounds 1-26 against liver cancer cell lines.

[0317] 1. Materials and Methods

[0318] 1.1 Materials

[0319]Liver cancer cell lines (HepG2, Huh7 and SMMC-7721) were purchased from Shanghai Ji Ning Biotechnology Co., Ltd.; medium (Dulbecco's Modified Eagle Medium, DMEM) was purchased from Thermo Fisher Scientific (Suzhou, China); serum (fetal bovine serum, FBS ) was purchased from Life Technologies (NY, USA); RPMI-1640 was purchased from ThermoFisher Biochemical Products (Beijing, China).

[0320] 1.2 Instruments

[0321] Flex Station 3 desktop multifunctional microplate reader (Bio-RAD 680, the United States); analytical balance (AG135, Metler Toledo, China); incubator (DHP-9082, Shanghai).

[0322] 1.3 Experimental process

[0323] 1). Take the logarithmic growth of liver cancer cells, discard the old medium, wash with PBS twice, and discard the PBS;

[0324] 2). Digest the cells with 0.25% trypsin, and quickly absorb the trypsin when it...

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Abstract

The present invention provides 26 novel compounds shown in structural formula (I), artemyrianins A-S (artemyrianolides A-S, 1-19) and artemyrianins A-G (artemyrianins A-G, 20-26) , and a preparation method and application thereof, a pharmaceutical composition and application thereof, and relate to the technical field of medicines. The compound has significant cytotoxic activity on human liver cancer cell lines HepG2, Huh7 and SMMC-7721, can form a pharmaceutical composition with a pharmaceutically acceptable carrier or excipient, and can be used to prepare anti-liver cancer drugs.

Description

Technical field: [0001] The invention belongs to the technical field of medicines. Specifically, it relates to artemyrianolides A-S (artemyrianolides A-S, 1-19) and artemyrianins A-G (artemyrianins A-G, 20-26), their preparation methods and applications, pharmaceutical compositions and applications thereof. Background technique: [0002] Primary liver cancer is one of the most common and most malignant tumors in the world, of which 90% to 95% are hepatocellular carcinoma (HCC), and the rest are intrahepatic cholangiocarcinoma (ICC) and mixed liver cancer. According to the latest global cancer statistics, the global incidence of liver cancer is increasing year by year. Every year, the number of new cases of liver cancer worldwide is about 800,000, and the number of deaths exceeds 780,000. About half of the new cases and deaths occur in my country. . As a systemic disease, HCC cannot be solved by surgical resection or local treatment alone. Moreover, most HCC patients have b...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/93C07D493/08C07D493/10C07D493/04C07D493/18C07D307/92C07D317/54C07D407/14C07C49/757C07C45/78C07C45/79C07C69/732C07C67/48C07C67/56A61K31/365A61K31/36A61K31/35A61K31/122A61K31/215A61P35/00A61P1/16
CPCC07D307/93C07D493/08C07D493/10C07D493/04C07D493/18C07D307/92C07D317/54C07D407/14C07C49/757C07C45/78C07C45/79C07C69/732C07C67/48C07C67/56A61P35/00A61P1/16C07C2603/78C07C2602/30C07C2602/28C07B2200/07Y02A50/30
Inventor 陈纪军唐爽耿长安张心湉马云保黄晓燕李天泽张雪梅
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI