A kind of indole-4-carbaldehyde compound with antibacterial activity in mulberry parasite, preparation method and application thereof

A technology of antibacterial activity and mulberry parasitism, applied in the field of phytochemistry, can solve the problems of unpublished antibacterial activity, etc., and achieve the effect of broadening application channels, increasing medicinal value, and wide distribution

Active Publication Date: 2022-02-08
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

Method used

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  • A kind of indole-4-carbaldehyde compound with antibacterial activity in mulberry parasite, preparation method and application thereof
  • A kind of indole-4-carbaldehyde compound with antibacterial activity in mulberry parasite, preparation method and application thereof
  • A kind of indole-4-carbaldehyde compound with antibacterial activity in mulberry parasite, preparation method and application thereof

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Experimental program
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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 mulberry plants, a preparation method and its application in the preparation of antibacterial drugs, belonging to the field of phytochemistry. The present invention uses mulberry as raw material, dried and pulverized, soaked and extracted with an organic solvent, and then the extracts are combined, filtered and concentrated to obtain a mulberry extract; then extracted with n-butanol and methylene chloride, the The dichloromethane extract is concentrated under reduced pressure to obtain the dichloromethane extract extract; the dichloromethane extract extract is dissolved, mixed and then subjected to silica gel column chromatography, and the eluent is concentrated and then normal phase silica gel chromatography column (200 ~300 mesh) separation and purification, and gel column chromatography separation and purification to obtain the pure product of the target indole-4-formaldehyde. The product of the present invention has stronger antibacterial effect, and the minimum inhibitory concentration MIC value of described indole-4-formaldehyde compound to methicillin-resistant Staphylococcus aureus is 128 μ g / mL, and its antibacterial effect is far better than clindamylate hydrochloride Mycin (MIC=1024 μg / 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 Patents(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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