Indole-4-formaldehyde compound with bacteriostatic activity in taxillus chinensis, and preparation method and application of indole-4-formaldehyde compound

A technology for bacteriostatic activity and mulberry parasite, applied in the field of phytochemistry, can solve problems such as unpublished antibacterial activity, and achieve the effects of widening application routes, wide distribution and simple preparation method

Active Publication Date: 2021-02-05
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

CN111187220A (trifluoromethylpyrimidine derivatives containing Schiff base structural unit and its preparation method and application) announced the in vitro anti-tumor activity of trifluoromethylpyrimidine derivatives but did not disclose antibacterial activity, and did not mention it in the patent Indole-4-carbaldehyde

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  • Indole-4-formaldehyde compound with bacteriostatic activity in taxillus chinensis, and preparation method and application of indole-4-formaldehyde compound
  • Indole-4-formaldehyde compound with bacteriostatic activity in taxillus chinensis, and preparation method and application of indole-4-formaldehyde compound
  • Indole-4-formaldehyde compound with bacteriostatic activity in taxillus chinensis, and preparation method and application of indole-4-formaldehyde compound

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Embodiment 1

[0032] Embodiment 1: the preparation of the indole-4-carboxaldehyde compound that has antibacterial activity in the mulberry

[0033] Sangjishen was dried and crushed to 60 mesh, and 3 kg of the sample was extracted 3 times with ethanol aqueous solution (solid-liquid ratio 1:10) with a mass fraction of 95%, each time for 8 hours; the 3 extractions were combined, filtered, and Concentrate under pressure to a relative density of 1.10 to obtain 160 g of extract. The extract was dissolved in water at 50°C, extracted with n-butanol and dichloromethane in turn, and the dichloromethane extract was concentrated under reduced pressure to a relative density of 1.10 to obtain the extract of dichloromethane extract. Take 20 g of dichloromethane extract and dissolve it with 1 part by weight of the extract in methanol, then mix the sample with 1 part by weight of the extract of 250-mesh silica gel and perform silica gel column chromatography. Normal-phase silica gel column chromatography (...

Embodiment 2

[0034] Embodiment 2: Determination of antibacterial ability of compounds with antibacterial activity in Sangji

[0035] 1. Experimental materials and methods

[0036] 1.1 Strains and reagents: Methicillin-resistant Staphylococcus aureus ATCC43300 (Guangdong Provincial Culture Conservation Center); BHI agar medium (Guangdong Huankai Microbial Technology Co., Ltd.); MH broth medium (Guangdong Huankai Microbial Technology Co., Ltd. ); sterile TTC solution (Guangdong Huankai Microbial Technology Co., Ltd.).

[0037] 1.2 Activation of strains: resuscitate methicillin-resistant Staphylococcus aureus ATCC43300 freeze-dried bacterial powder, inoculate it into BHI medium, and culture it in a constant temperature incubator at 37°C for 12 hours. The methicillin-resistant Staphylococcus aureus was subcultured and purified by the same inoculation method for later use.

[0038] 1.3 Drug preparation: Accurately weigh 4.096g of indole-4-carboxaldehyde, dissolve it in 10mL of dimethyl sulfox...

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Abstract

The invention discloses a compound with antibacterial activity in taxillus chinensis, a preparation method and application of the compound in preparation of antibacterial drugs, and belongs to the field of phytochemistry. The preparation method comprises the following steps of: drying taxillus chinensis as a raw material in the sun, crushing the taxillus chinensis, soaking and extracting with an organic solvent, merging extracting solutions, filtering and concentrating to obtain taxillus chinensis extract extractum; then extracting with n-butyl alcohol and dichloromethane, and carrying out vacuum concentration on the dichloromethane extract to obtain dichloromethane extract extractum; and dissolving the dichloromethane extract extractum, stirring, carrying out silica gel column chromatography, concentrating the eluent, carrying out normal phase silica gel chromatographic column (200-300 meshes) separation and purification, and carrying out gel column chromatography separation and purification to obtain a target, namely pure indole-4-formaldehyde. The indole-4-formaldehyde compound has a relatively strong bacteriostatic effect, and the minimal inhibitory concentration MIC value of the indole-4-formaldehyde compound on methicillin-resistant staphylococcus aureus is 128[mu]g / mL, so that the bacteriostatic effect of the indole-4-formaldehyde compound is far superior to that of clindamycin hydrochloride (MIC is equal to 1024[mu]g / mL).

Description

technical field [0001] The invention belongs to the field of phytochemistry, and in particular relates to a compound having antibacterial activity in mulberry plants, a preparation method and an application in preparing antibacterial drugs. Background technique [0002] Sangji (Taxillμs chinensis (DC.) Danser), formerly known as Sangshangji, also known as Guangji, is a plant of the genus Amblysia in the family Morushiaceae of the order Sandalwood, mostly parasitic on mulberry trees, pear trees, plum trees, camellia oleifera, pachyderm Incense, walnut and other plants. In 2015, Sangjisi included in the Pharmacopoeia of the People's Republic of China is a dry plant with leafy stems and branches belonging to the family Morushiaceae. [0003] The main active ingredients of Sangjishen include small molecular compounds such as flavonoids, terpenes, polypeptides, lectins, organic acids, and macromolecular compounds such as alkaloids and polysaccharides. Therefore, from ancient ti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/08A61K31/404A61P31/04
CPCC07D209/08A61P31/04
Inventor 高波黄思璐乔子安刘长旻闫敏
Owner JILIN UNIV
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