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Sesquiterpenoids, composition thereof, method for extracting the same from plants and application

A technology of sesquiterpenoids and compounds, which is applied to the extracts of Chrysanthemum orchidaceae plants, and the application field of preparing antifungal drugs, which can solve the problems of high toxicity and narrow therapeutic range

Inactive Publication Date: 2010-07-14
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Although there are many drugs for fungal infection, some of these drugs are relatively toxic, and some of them have a narrow therapeutic range, and more and more fungi are resistant to the commonly used antifungal infection drugs in clinical practice. Therefore, it is necessary to Pharmacists continue to develop new drugs or prodrugs with good antifungal activity

Method used

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  • Sesquiterpenoids, composition thereof, method for extracting the same from plants and application
  • Sesquiterpenoids, composition thereof, method for extracting the same from plants and application
  • Sesquiterpenoids, composition thereof, method for extracting the same from plants and application

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preparation example Construction

[0055] The preparation method of sesquiterpene compound of the present invention

[0056]As mentioned above, the compounds of the present invention are natural products. Natural products such as compounds of formula Ia, Ib or Ic can be extracted from plant extracts of the family Chrysanthaceae. The genus belonging to the Chloranthus family is selected from Sarcandra, Chloranthus or Hedyosmum. The species of the genus Chloranthus is preferably selected from the group consisting of C. angustifoliu, C. oldhami, C. spicatus, C. holostegius, C. anhuiensis, C. tianmushanensis, C. henryi, C. sessilifolius, C. fortunei, C. elatior, C. japonicas , C. serratus and C. multistachys. In a preferred embodiment, the Chloranthus species is Chloranthus spicatus. These natural products can be obtained from active site extracts. Using the method according to the invention an active fraction extract can be produced.

[0057] Therefore, the present invention provides a method for extracting s...

Embodiment 1

[0076] Total extracts of Chrysanthemum officinalis with antifungal activity

[0077] The dried whole plant of Chloranthus spicatus (10kg) was pulverized into powder, soaked and extracted with ethanol at room temperature for 3 times, each time for 3 days, filtered and evaporated to dryness of the ethanol solution to obtain the total ethanol extract (475g).

Embodiment 2

[0079] Extracts from active parts of Chrysanthaceae plants with antifungal activity

[0080] The total extract in Example 1 was dissolved in 20L distilled water to make a suspension, which was extracted with ethyl acetate and n-butanol successively to obtain 300g of ethyl acetate extract; 300g of ethyl acetate extract was subjected to silica gel column layer Analysis, gradient elution with petroleum ether-acetone by volume ratio 100:0, 20:1, 10:1, 5:1, 3:1 and 1:1, received a total of six fractions, each fraction received 1500ml; the organic solution of fractions eluted at a volume ratio of 5:1 was evaporated to dryness to obtain the active site extract (16.9g).

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Abstract

The invention pertains to the pharmaceutical chemistry field, disclosing sesquiterpenoids extracted from chloranthus family, combination, extraction method and application to preparation of antifungal drugs thereof. The invention also discloses an extractive of chloranthus family that has antifungal activity. The structure formula of sesquiterpenoids disclosed in the invention shows as formula I.The sesquiterpenoids, the combinations thereof and the extractive of the chloranthus family of the invention have antifungal activity.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and more specifically, relates to sesquiterpenoids extracted from Chrysanthemum orchidaceae and its composition, extraction method and application in the preparation of antifungal drugs. The present invention also relates to Extract of the Chrysanthemum orchidaceae plant. Background technique [0002] In recent years, with the increasing number of cancer and AIDS patients, the widespread development of organ transplantation, catheter intubation and endoscopic techniques, the wide application of high-efficiency broad-spectrum antibiotics, immunosuppressants and corticosteroids, the rate of fungal infections has continued to increase, especially Is a sharp increase in the rate of deep fungal infection. Moreover, with the extensive application of antifungal drugs, fungal drug resistance continues to emerge, making the treatment of fungal infections more and more difficult. Therefore, it is of gr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C13/48C07C47/56C07C39/17C07C63/36C07C65/32A61K31/015A61K31/05A61K31/11A61K31/192A61K36/898A61P31/10
Inventor 叶阳徐勇将张继宝沈金贵李希强唐春萍柯昌强
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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