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Antituberculosis compositions of byttneria species

The technology of a kind of Echinopsis genus, composition, is applied in the field of the composition comprising the extract of Echinopsis genus species

Inactive Publication Date: 2014-05-21
COUNCIL OF SCI & IND RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Furthermore, this can be a strategy to overcome multidrug resistant bacilli that gradually render conventional treatment regimens ineffective

Method used

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  • Antituberculosis compositions of byttneria species
  • Antituberculosis compositions of byttneria species
  • Antituberculosis compositions of byttneria species

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1: Protocol for the identification of MtbGS inhibitors:

[0045] The test mixture contained 50 mM HEPES (4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid), pH 6.8 buffer, 220 mM L-glutamic acid (pH adjusted to 6.8), 7.5 mM chloride Ammonium, 32.5 mM magnesium chloride and 62.5 μg / ml enzyme (Mycobacterium tuberculosis glutamine synthetase). To 85 μl reaction mixture was added 5 μl of the sample (Pipa japonica extract). 5 μl DMSO (dimethyl sulfoxide) was added to the control and 5 μl 420 mM EDTA (ethylenediaminetetraacetic acid) was added to the blank. Reactions were initiated by adding 7.6 mM ATP (pH adjusted to ~6.8) to the reaction mixture and incubated at 25°C for 2 hours. The reaction was terminated by adding a stopping reagent followed by citrate to block further hydrolysis of ATP. The whole mixture was left at room temperature for an additional 30 minutes to read the color by a SpectraMax plate reader at 655 nm. Methanol extracts of Echinopsis sp. wer...

Embodiment 2

[0047] Example 2: Column Chromatography of the Methanol Extract of Example 1:

[0048] Chromatography was performed on a sample of 19 gms through 200 gms of silica gel (100-200 mesh) using a gradient mobile phase according to Table-1. 25 fractions were collected at this stage. Use 5:95MeOH:CHCl 3 Developed phase TLC of all these collected fractions was performed on alumina-coated silica gel TLC plates to check purity. Fractions showing similar TLC (Panel-I) patterns were pooled and placed in 15 ml glass test tubes to obtain 11 fractions (A, B, C, D, E, F, G, H, I , J, K). After removal of the solvent, the bioactivity of these fractions was evaluated using the protocol mentioned in Example 1. Fractions D (fraction 4) and K (fraction 11) were found to exhibit activity against MtbGS.

[0049] Table I

[0050]

Embodiment 3

[0051] Example 3: Purification of Fraction D (Fraction 4):

[0052] Re-chromatography was performed on 100 mg of Fraction D using 36 gms of silica gel (100-200 mesh) and mobile phase as described in Table II. Perform TLC of all collected fractions (Figure-2). After analysis of the TLC plate, the fractions were pooled into 10 final fractions D1-D10. An assay as in Example 1 was carried out to identify the active fraction. Fraction D4 was found to be active.

[0053] Table-II

[0054]

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PUM

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Abstract

Active fractions exhibiting anti-tuberculous activity from the plant Byttneria herbecea (family—Sterculiaceae) are described. Methanol extracts of the aerial part of Byttneria herbecea exhibited activity against MtbGS in primary screening of biosynthetic assay. Subsequent fractionation was carried out in organic solvents. Out of all these, two fractions (fraction D and K) are exhibiting inhibitory activity against M. tuberculosis glutamine synthetase activity. These fractions D and K are inhibiting 74% and 44% respectively at 7.5 mg / ml concentrations. The determined IC50 value of the fraction K is found to be 4.5 mg / ml from the dose response curve against the purified Mycobacterium tuberculosis Glutamine Synthetase. The IC50 value for M. bovis BCG is 1.56 μg / ml. It was observed that there was no significant effect on proliferation of HL-60 cell line at 10×MIC levels of the hits. This data indicated that these compounds could be initially considered to be safe.

Description

technical field [0001] The present invention relates to a composition comprising an extract of the genus Echinopsis for the inhibition of Mycobacterium tuberculosis glutamine synthetase of Mycobacterium tuberculosis which causes tuberculosis. More particularly, the present invention relates to the anti-tuberculosis activity of Echinopsis species by inhibiting the MtbGS enzyme (Mycobacterium tuberculosis glutamine synthetase). Background technique [0002] WHO estimates that there were 9.27 million new cases of TB in 2007, compared to 9.24 million new cases in 2006. Of these 9.27 million new cases, an estimated 44% or 4.1 million (61 cases per 100,000 population) were new smear-positive cases. India sees more new TB cases each year than any other country. The greatest incidence of the disease is known to occur in the Indian population, of which up to 1.8 million are infected. An estimated 1.37 million HIV-positive TB cases occurred in 2007 (14.8% of all cases) and 456,000 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K36/185A61P31/06
CPCA61K36/185A61P31/06
Inventor D·萨卡尔S·P·乔希U·辛格K·D·舒巴利R·R·库尔卡尼
Owner COUNCIL OF SCI & IND RES
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