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Application of jolkinolide B and analogues thereof to preparation of medicines for resisting tuberculosis

A technology of eupholide and eupholide, which is applied in the field of application of eupholide B and its analogues in the preparation of anti-tuberculosis drugs, can solve the problems of no anti-tuberculosis effect, achieve small side effects, Good effect

Active Publication Date: 2020-05-12
DALIAN MEDICAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there have been reports about the anti-tumor activity of rock euphoride B and its analogs, but so far there is no relevant report about the anti-tuberculosis effect of rock euphoride B and its analogs

Method used

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  • Application of jolkinolide B and analogues thereof to preparation of medicines for resisting tuberculosis
  • Application of jolkinolide B and analogues thereof to preparation of medicines for resisting tuberculosis
  • Application of jolkinolide B and analogues thereof to preparation of medicines for resisting tuberculosis

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Embodiment Construction

[0027] 1. The chemical structure spectrum data of petroglide B and 17-hydroxy euphoride B used in the experiment

[0028] Self-made rock euphoralide B (white powder), the H-NMR spectrum and the C-NMR spectrum are as follows Figure 7 , Figure 8 shown. UV (CH 3 OH) λ max 239.3 nm, suggesting a p-π conjugated structure. exist 1 H-NMR (600 MHz, CDCl 3 ) spectrum, δ The four methyl proton signals of 2.09 (3H, s), 0.94 (3H, s), 0.85 (3H, s), and 0.82 (3H, s) are 17, 18, 19, and 20 methyl proton signals; δ 4.04 (1H, s) is the hydrogen proton signal on the 11-position oxygen carbon; δ 3.68 (1H, s) is the hydrogen proton signal on the 14-position oxygen carbon; δ 2.29 (1H, s) is the 9-position hydrogen proton signal (Table 1). exist 13 C-NMR (150 MHz, CDCl 3 ) spectrum, a total of 20 carbon signals are given, among which δ 169.6 is the carbonyl carbon signal, δ 148.6, 130.3 are two double bond carbon signals, δ 66.1, 61.0, 85.2, and 55.3 are four oxycarbon sign...

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Abstract

The invention discloses an application of jolkinolide B and analogues thereof to preparation of medicines for resisting tuberculosis, and relates to the technical field of new purposes of the jolkinolide B and analogues thereof. The inventor of the invention finds that the jolkinolide B and the analogues thereof can notably restrain mycobacterium tuberculosis H37Ra and various clinical multidrug resistance type mycobacterium tuberculosis, further the application of the jolkinolide B and the analogues thereof to the medicines for resisting tuberculosis is invented, new anti-tuberculosis medicines which are small in action effects and small in side effects are provided and can be in united application with clinical frontline anti-tuberculosis medicines (rifampicin, isoniazide, ethambutol andthe like), and synergistic interaction effects can be achieved.

Description

technical field [0001] The present invention relates to the new application of petogenolide B and its analogues, especially the application of petroglypholide B and its analogues in the preparation of anti-tuberculosis drugs. Background technique [0002] According to the 2018 WHO Global Tuberculosis Report, tuberculosis is one of the top ten causes of death. In 2017, an estimated 10 million people were newly infected with TB, and about 1.6 million people died from TB. China had an estimated 889,000 new TB infections, second only to India. About 1.7 billion people (23% of the global population) are estimated to have latent TB infection and are at risk of developing active TB. Drug-resistant tuberculosis remains a public health crisis. It is estimated that 558,000 people worldwide had rifampicin-resistant tuberculosis (RR-TB) in 2017, and 82% of these people had multi-drug-resistant tuberculosis (MDR-TB). MDR / RR-TB cases account for about 13% of the world, ranking second. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61P31/06
CPCA61K31/58A61P31/06
Inventor 王超马骁驰马郁芳鄢秋龙冯磊宁静霍晓奎
Owner DALIAN MEDICAL UNIVERSITY