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Application of carex rigescens for preparing anti-HIV drug

A technology of Carex sylvestris and medicine, applied in the field of application of Carex syringae in preparation of anti-HIV drugs

Inactive Publication Date: 2009-09-09
JINAN JINNIU BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although 27 anti-HIV drugs have been developed and put into clinical practice, including ① protease inhibitors, such as atazanavir, exert potent anti-HIV activity by blocking the viral precursor protein encoded by the gag and gag-pol genes of the virus, ② Reverse transcriptase inhibitors, such as nucleoside reverse transcriptase inhibitors (NRTIs) ganciclovir, non-nucleoside reverse transcriptase inhibitors (NNRTIs) efavirenz, etc., ③ invasion inhibitors (such as T20), ④ integration Enzyme inhibitors (such as elvitegravir), etc. have developed helicase inhibitors in recent years. However, these drugs still have not broken through the problems of toxic and side effects and are deeply trapped in the dilemma of drug resistance.

Method used

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  • Application of carex rigescens for preparing anti-HIV drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: prepare a kind of anti-HIV medicine, the steps are as follows:

[0026] (1) Extraction with organic solvent: crush 100Kg of dry Carex alba, put it into 200L of 30% acetone aqueous solution, soak at room temperature for 12 hours, repeat the extraction twice, combine the extracts, and distill off the organic solvent under reduced pressure to obtain an aqueous suspension.

[0027] (2) Adjust the pH value of the above water suspension to 4 with acetic acid, let stand at room temperature for 30 minutes, and then centrifuge to obtain a precipitate.

[0028] (3) Normal-phase chromatographic column separation: the above-mentioned precipitate is chromatographed on a silica gel column, eluted with a chloroform-methanol gradient, and the eluent whose volume ratio of chloroform and methanol is 50:50 to 10:90 is collected, and distilled under reduced pressure , Concentrate, get the normal phase chromatographic column separation product.

[0029] (4) Reversed-phase chr...

Embodiment 2

[0032] Embodiment 2: prepare a kind of anti-HIV medicine, the steps are as follows:

[0033] (1) Organic solvent extraction: crush 200 g of dried Carex alba, put it into 400 mL of 70% ethanol aqueous solution, ultrasonically extract for 3 hours, repeat the extraction twice, combine the extracts, and distill off the organic solvent under reduced pressure to obtain an aqueous suspension.

[0034] (2) Adjust the pH value of the above water suspension to 4 with acetic acid, let stand at room temperature for 30 minutes, and then centrifuge to obtain a precipitate.

[0035] (3) Normal-phase chromatographic column separation: the above-mentioned precipitate is chromatographed on a silica gel column, eluted with a chloroform-methanol gradient, and the eluent whose volume ratio of chloroform and methanol is 50:50 to 10:90 is collected, and distilled under reduced pressure , Concentrate, get the normal phase chromatographic column separation product.

[0036] (4) Reversed-phase chromat...

Embodiment 3

[0038] Embodiment 3: prepare a kind of anti-HIV medicine, the steps are as follows:

[0039] (1) Extraction with organic solvent: crush 200 g of dried Carex alba, put it into 400 mL of 60% acetone aqueous solution, soak at room temperature for 14 hours, repeat the extraction twice, combine the extracts, and distill off the organic solvent under reduced pressure to obtain an aqueous suspension.

[0040] (2) Adjust the pH value of the above water suspension to 4 with acetic acid, let stand at room temperature for 30 minutes, and then centrifuge to obtain a precipitate.

[0041] (3) Normal-phase chromatographic column separation: the above-mentioned precipitate is chromatographed on a silica gel column, eluted with a chloroform-methanol gradient, and the eluent whose volume ratio of chloroform and methanol is 50:50 to 10:90 is collected, and distilled under reduced pressure , Concentrate, get the normal phase chromatographic column separation product.

[0042] (4) Reversed-phase...

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Abstract

The invention discloses a novel use of carex rigescens in pharmacy, more particularly relates to the application of the carex rigescens for preparing anti-HIV drug. The application comprises the following steps: firstly, the carex rigescens is pretreated to obtain extractive; and then, the extractive and medically receivable auxiliary materials are jointly made into anti-HIV drug, and the dosage forms of the drug is any one of injection, capsule, troche, granular formulation, pill, mixture, tincture and oral liquid. By adopting the extractive of the carex rigescens to do an HIV PR inhibition experiment and make comparison with positive control drug Indinavir, the result shows that the carex rigescens has remarkable HIV prolease (HIV PR) inhibition activity and has certain guidance significance for developing the anti-HIV drug, thereby having important reference value.

Description

technical field [0001] The present invention relates to the new application of Carex alba in pharmacy, in particular to the application of Carex alba in preparing anti-Human Immunodeficiency Virus (Human Immunodeficiency Virus, HIV) medicine. Background technique [0002] White Carex, Carex Rigescens (Franch.) V.Krecz. (C.stenophylla Wahlb.var.rigescens Franch.), perennial herb. "Chinese Materia Medica" records that it belongs to the triple burner, spleen, stomach, and kidney meridians, and has the effect of clearing away heat, diuresis and treating stranguria. The whole herb is used as medicine to treat chyluria. Mainly distributed in Northeast China and Hebei, Shaanxi, Shandong, Jiangsu, Anhui, Henan, Hubei, Sichuan and other places. At present, there are very few studies on this medicinal material at home and abroad, only: a report on tablet preparation technology data in the 1980s [Ni Peizhong, Wang Li, Gao Yuanqing, et al. Development of Carex bacilli tablets (granules...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/89A61P31/18
Inventor 高川
Owner JINAN JINNIU BIOTECH CO LTD
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