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A method for screening inos inhibitors in Radix Ophiopogon japonicus and screening obtained inos inhibitors

An inhibitor, the technology of Ophiopogon japonicus, applied in the field of medicine, can solve problems such as adverse reactions

Active Publication Date: 2020-08-28
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Current research shows that iNOS inhibitors are mostly synthetic drugs, and synthetic drugs can cause adverse reactions. Therefore, finding natural iNOS inhibitors has certain guiding significance for the development of new drugs

Method used

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  • A method for screening inos inhibitors in Radix Ophiopogon japonicus and screening obtained inos inhibitors
  • A method for screening inos inhibitors in Radix Ophiopogon japonicus and screening obtained inos inhibitors
  • A method for screening inos inhibitors in Radix Ophiopogon japonicus and screening obtained inos inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: A method for screening iNOS inhibitors in Ophiopogon japonicus

[0030] 1. Experimental equipment and reagents

[0031] High-performance liquid chromatography-fluorescence detection instrument (Shimadzu Corporation of Japan); high-performance liquid chromatography-Q-TOF-mass spectrometry instrument (Agilent Corporation of the United States); low-temperature high-speed centrifuge (Thermo Fisher Scientific Corporation of the United States) ; Ultrapure water treatment system (Millipore, USA); ultrasonic cleaner (Kunshan Ultrasonic Instrument Co., Ltd.); rotary evaporator (Shanghai Yarong Biochemical Instrument Factory); vacuum drying oven (Shanghai Heheng Instrument Equipment Co., Ltd.).

[0032] Ultrafiltration centrifuge tube (Pall, USA); Supelclean TM ENVI TM -18SPE solid-phase extraction column (3mL) (Sigma, USA); Ophiopogon japonicus medicinal material was purchased from Cixi, Zhejiang (identified by Professor Qi Jin from the School of Chinese Materia Me...

Embodiment 2

[0073] Example 2: A method for targeted enrichment of iNOS inhibitors in Ophiopogon japonicus

[0074] Including the following steps:

[0075] Step 1, preparation of Ophiopogon japonicus extract

[0076] Ophiopogon japonicus medicinal material, pulverized, passed through a 60-mesh sieve, accurately weighed 2.0g of the powder, ultrasonically extracted with 50mL methanol solution (25°C, 30min), filtered with suction, the filtrate was evaporated to dryness under reduced pressure, the extract was dissolved in 5mL of water, and used SPE solid phase extraction column chromatography separation, followed by elution with 5mL water, 5mL 20% methanol-water solution, 5mL methanol, collected methanol eluate 45 ℃ vacuum drying, finally added DMSO reconstitution to obtain Ophiopogon japonicus sample liquid, stored for later use.

[0077] Step 2. Using iNOS to target and enrich the active ingredients in Ophiopogon japonicus that have affinity adsorption with iNOS, namely: Pennogenin-3-O-α-L-...

Embodiment 3

[0083] Example 3: Pennogenin-3-O-α-L-rhamnopyranosyl-(1→2)-β-D-xylopyranosyl-(1→4)-β-D-glucopyranoside, Ophiopogon flavanone A, methyl wheat Use of asparagus flavanone A, ophiopogon flavanone B, ophiopogonin D and ophiopogonin D' as iNOS inhibitors

[0084] The present invention finds that Pennogenin-3-O-α-L-rhamnopyranosyl-(1→2)-β-D-xylopyranosyl-(1→4)-β-D-glucopyranoside, Ophiopogon flavanone A, methyl wheat Asparagus flavanone A, methyl ophiopogon flavanone B, ophiopogon saponin D, and ophiopogon saponin D' are effective iNOS inhibitors, and the IC50 values ​​of each compound have been recorded in Example 1. Those skilled in the art know that iNOS inhibitors can be used to treat diseases caused by excessive NO, such as hypertension, neurodegeneration, rheumatoid arthritis, colitis, cancer (reference: Inducible nitric oxide synthase inhibition Research progress of pharmaceutical agents, Chinese Journal of Medicinal Chemistry, Volume 27, Issue 6, December 2017), so, Pennogen...

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Abstract

The invention discloses a method for screening an iNOS inhibitor in ophiopogon japonicus and the screened iNOS inhibitor. Verified by molecular docking and iNOS inhibition experiment of chemical pureproducts, firstly, the screening method can effectively and reliably screen to obtain compounds with iNOS inhibiting activity from the ophiopogon japonicus, including Pennogenin-3-O-alpha-L-rhamnopyranosyl-(1 to 2)-beta-D-xylopyranosyl-(1 to 4)-beta-D-glucopyranoside, ophiopogon japonicus flavanone A, methyl ophiopogon japonicus flavanone A, methyl radix ophiopogonis flavanone B, ophiopogon japonicus saponin D and radix ophiopogonis D'; secondly, the method can be used for targeting the iNOS inhibitor enriched in the radix ophiopogonis; thirdly, the iNOS inhibiting activity of chemical components in the ophiopogon japonicus is found for the first time, so that the radix ophiopogonis can be prepared into the iNOS inhibitor to treat diseases caused by excessive NO, such as hypertension, neurodegeneration, rheumatoid arthritis, colitis and cancers.

Description

technical field [0001] The invention belongs to the field of medicine and relates to the screening and discovery of active ingredients of traditional Chinese medicines, in particular to a method for screening iNOS inhibitors in Radix Ophiopogon japonicus and the iNOS inhibitors obtained through screening. Background technique [0002] Nitric oxide (NO) is an important biological signal molecule in the body, which participates in the regulation of various physiological and pathological processes, such as nerve conduction, blood pressure regulation and immune response. The main source of endogenous NO is nitric oxide synthase. The main function of nitric oxide synthase (NOS) is to catalyze the production of NO and L-citrulline from L-arginine. According to the different parts of its distribution, it is divided into three types: neural type (nNOS), endothelial type (eNOS) and inducible type (iNOS). Both nNOS and eNOS are constitutive, they have Ca 2+ dependency. iNOS, on th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): G01N30/02G01N30/08
CPCG01N30/02G01N30/08
Inventor 余伯阳戚进郭瑜婕
Owner CHINA PHARM UNIV
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