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Triterpenes in leaves of Phyllanthus acidus as well as pharmaceutical composition and application of triterpenes

A technology of triterpene compounds and compositions, applied in the field of triterpene compounds

Active Publication Date: 2021-02-26
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

However, so far, there are no reports of dichapetalin-type triterpenoids pacidusin A (1), pacidusin B (2), pacidusin C (3) and pacidusin D (4) derived from this plant in the prior art, and there are no reports of these 4 A report of a compound and its pharmaceutical composition as an anti-acute leukemia, lung cancer, liver cancer, breast cancer and colon cancer and other common human cancer drugs

Method used

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  • Triterpenes in leaves of Phyllanthus acidus as well as pharmaceutical composition and application of triterpenes
  • Triterpenes in leaves of Phyllanthus acidus as well as pharmaceutical composition and application of triterpenes
  • Triterpenes in leaves of Phyllanthus acidus as well as pharmaceutical composition and application of triterpenes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Preparation and evaluation of anticancer activity of compounds pacidusin A(1) and pacidusin C(3).

[0030] The preparation of compound pacidusin A (1) and pacidusin C (3): the air-dried leaves (30kg) of Indian gooseberry were pulverized, soaked in 95% ethanol water (100L), and refluxed and extracted 3 times (2h / time) at 60°C ). After filtration, the filtrate was concentrated under reduced pressure to remove the organic solvent to obtain 4.5 kg of crude extract. The crude extract was extracted with water and ethyl acetate, and the ethyl acetate part (2.0kg) was subjected to silica gel column chromatography, using petroleum ether: ethyl acetate (20:1,10:1,8:1,2:1,1 :1 and 0:1) solution for gradient elution to obtain 6 main parts (A-F), part B was subjected to MCI column chromatography, eluted with 90% methanol water to obtain 72g yellow gum, this part was continued to use silica gel Column chromatography, carry out gradient elution with petroleum ether: acetone (9:1-1:2...

Embodiment 2

[0037] Preparation and evaluation of anticancer activity of compounds pacidusin B(2) and pacidusin D(4).

[0038] Preparation of compounds pacidusinB(2) and pacidusinD(4): Air-dried leaves of Indian gooseberry (30kg) were pulverized, soaked in 95% ethanol water (100L), and refluxed at 60°C for 3 times (2h / time). After filtration, the filtrate was concentrated under reduced pressure to remove the organic solvent to obtain 4.5 kg of crude extract. The crude extract was extracted with water and ethyl acetate, and the ethyl acetate part (2.0kg) was subjected to silica gel column chromatography, using petroleum ether: ethyl acetate (20:1,10:1,8:1,2:1,1 :1 and 0:1) solution for gradient elution to obtain 6 main parts (A-F), part B was subjected to MCI column chromatography, eluted with 90% methanol water to obtain 72g yellow gum, this part was continued to use silica gel Column chromatography, carry out gradient elution with petroleum ether: acetone (9:1-1:2) solution, obtain 6 fra...

preparation Embodiment 1

[0056] According to the method of Examples 1 and 2, the air-dried leaves (30 kg) of Indian gooseberry were crushed, soaked in 95% ethanol water (100 L), and refluxed at 60° C. for 3 times (2 h / time). After filtration, the filtrate was concentrated under reduced pressure to remove the organic solvent to obtain 4.5 kg of crude extract. The crude extract was extracted with water and ethyl acetate, and the ethyl acetate part (2.0kg) was subjected to silica gel column chromatography, using petroleum ether: ethyl acetate (20:1,10:1,8:1,2:1,1 :1 and 0:1) solution for gradient elution to obtain 6 main parts (A-F), part B was subjected to MCI column chromatography, eluted with 90% methanol water to obtain 72g yellow gum, this part was continued to use silica gel Column chromatography, carry out gradient elution with petroleum ether: acetone (9:1-1:2) solution, obtain 6 fractions (B 1 -B 6 ). B 2 Compound 1-4 was partially obtained by using preparative liquid phase (85% methanol-wat...

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Abstract

The invention provides triterpenes in leaves of Phyllanthus acidus as well as a pharmaceutical composition and application of the triterpenes, provides four new dichapetalin type triterpenes compounds1-4 as shown in a structural formula (I) in the description as well as a pharmaceutical composition and application thereof, and belongs to the technical field of medicines, wherein the English namesof the new dichapetalin type triterpenes compounds 1-4 are pacidusin A-D. The compound 1-4 disclosed by the invention has remarkable cytotoxic activity on human acute leukemia cells HL-60, lung cancer cells A-549, liver cancer cells SMMC-7721, breast cancer cells MCF-7 and colon cancer cells SW--480, can form a pharmaceutical composition together with a medicinal carrier or excipient, and is usedfor preparing related anti-cancer drugs.

Description

technical field [0001] The invention belongs to the technical field of medicines. Specifically, it relates to triterpenoid pacidusin A-D, its preparation method and application, pharmaceutical composition and application thereof. Background technique [0002] At present, the number of deaths caused by cancer is second only to cardiovascular diseases, and tends to exceed the mortality rate of heart disease, which brings heavy economic and spiritual burdens to society and families. In my country, the incidence of cancer is higher than that of lung cancer, stomach cancer, liver cancer, and colon cancer. In recent years, great achievements have been made in the research and development of new anticancer drugs. The application of anticancer drugs represented by cisplatin and paclitaxel can effectively increase the survival rate of cancer patients within a certain period of time and prolong the survival time of cancer patients. However, the application of chemotherapy drugs sti...

Claims

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Application Information

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IPC IPC(8): C07J71/00A61K31/58A61P35/02A61P35/00
CPCC07J71/0005A61P35/02A61P35/00
Inventor 朱宏涛张颖君耿慧春王东杨为农杨崇仁
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI
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