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Compositions for prostaglandin transporter inhibition and related therapeutic applications

A prostaglandin and transporter technology, applied in the field of compositions for inhibiting prostaglandin transporters, can solve the problems of no reported inhibition or blocking

Pending Publication Date: 2022-03-01
SAMI SABINSA GRP LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, no plant-based compositions have been reported for inhibiting or blocking PGT

Method used

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  • Compositions for prostaglandin transporter inhibition and related therapeutic applications
  • Compositions for prostaglandin transporter inhibition and related therapeutic applications
  • Compositions for prostaglandin transporter inhibition and related therapeutic applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Details of the composition

[0039] The present invention discloses a composition comprising 30-60% w / w garlic extract, 10-30% w / w beet extract, 5-15% w / w nigella extract and 10- 30% w / w Terminalia arjuna extract for inhibition of PGT. The above extracts have been reported to elicit cardioprotective and antihypertensive effects individually. Some of the medicinal properties of the above extracts are mentioned below:

[0040] Garlic is a well known plant which is used in the traditional Ayurveda system. It has been reported to elicit many therapeutic effects against different diseases, including cardiovascular diseases, regulate blood pressure, and lower blood sugar and cholesterol levels. It is also effective against bacterial, viral, fungal, and parasitic infections and reportedly boosts the immune system. The plant also has antitumor properties (Ayaz and Alpsoy, Garlic (Allium sativum) and traditional medicine, Turkiye Parazitol Derg. 2007; 31(2):145-9)...

Embodiment 2

[0047] Example 2: Inhibition of Prostaglandin Transporter

[0048]The formulation was evaluated for its ability to inhibit the prostaglandin transporter (PGT). The kidney cell line MDCK was seeded on six-well plates at 30% confluency. Three days later, they were treated with 10 [mu]M bradykinin (to increase endogenous PGE2 synthesis, available at Sigma-Aldrich) at 37[deg.] C. for different durations in the presence of vehicle (DMSO). The formulations were added simultaneously to the cell culture in graded concentrations and incubated for a further 24 hours. Culture medium was collected for measurement of extracellular PGE2 concentration. Cells were washed twice with phosphate-buffered saline, lysed with 250 μl of phosphate-buffered saline containing 0.1 M HCl and 0.1% Triton X-100 for 15 min at room temperature, and then scraped off the plate. Pipette the cell suspension up and down several times to ensure complete lysis. Cell lysates were collected and centrifuged at 10,0...

Embodiment 3

[0053] Embodiment 3: the antihypertensive effect of preparation

[0054] method

[0055] Normotensive Wistar rats were used for the experiments. By administering DOCA (deoxycorticosterone acetate), a synthetic mineralocorticoid derivative, 25 mg / kg s.c, twice a week and 1% w / v NaCl in drinking water, for a period of 30 days (model: DOCA in rats Salt-induced hypertension) spontaneously induces hypertension in rats. Rats were divided into the following groups, each containing 6 rats:

[0056] Table 2: Grouping

[0057] Group describe I normal control II salt loaded III 50 mg / kg body weight formulation IV 100 mg / kg body weight formulation V 200 mg / kg body weight formulation VI 400mg / kg body weight formulation

[0058] The following parameters were estimated to evaluate the antihypertensive effect of the formulation

[0059] · PGT expression

[0060] · Nitric Oxide Estimation

[0061] ·blood pressure

[0062] · Heart ...

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Abstract

The invention discloses a composition. The present invention relates to a composition comprising a garlic extract standardized to contain not less than 0.3% w / w S-allylcysteine, a beet extract standardized to contain not less than 2% w / w nitrate, a nigella margarita extract standardized to contain 0.1% w / w to 5% w / w thymoquinone, 0.01% to 10% w / w thymoquinone, about 20% to 95% w / w fatty acid, about 0.001% to 3% w / w alpha-hedeine or hederagenin, and a Terminalia arjuna extract standardized to contain 3% w / w Terminalia arjuna glucoside for use as a prostaglandin transporter inhibitor. The invention also discloses application of the composition in treatment and management of hypertension and cardiovascular complications.

Description

technical field [0001] The present invention generally relates to compositions comprising plant extracts. More specifically, the present invention relates to compositions for inhibiting the prostaglandin transporter (PGT) and related therapeutic applications. Background technique [0002] Prostaglandins (PGs) are naturally occurring unsaturated fatty acids that are involved in mediating various pathophysiological processes and homeostatic functions in different organs. They are derived from arachidonic acid through the action of the cyclooxygenase isoenzyme. There are four main commonly produced bioactive PGs: prostaglandin E2 (PGE2), prostacyclin (PGI2), prostaglandin D2 (PGD2), and prostaglandin F2α (PGF2α), which function as autocrine and paracrine mediators to Maintain homeostatic function (Ricciotti et al., Prostaglandins and Inflammation, Arteriosclerosis, Thrombosis, and Vascular Biology. 2011; 31:986–1000). PG plays a major role in regulating many disease states i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A23L33/105A23G3/48A23G3/36A61K36/8962A61P9/12
CPCA23L2/39A23L2/52A23L33/105A23L33/175A61K36/185A61K36/8962A61K36/71A61P9/00Y02A50/30A61K2300/00
Inventor 穆罕迈德.玛杰德K.纳加布沙南S.巴尼A.潘迪
Owner SAMI SABINSA GRP LTD
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