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      Antihypertensive activity, toxicity and molecular docking study of newly synthesized xanthon derivatives (xanthonoxypropanolamine)

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      PLoS ONE
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          Abstract

          Context

          Xanthone derivatives have been reported to possess a wide range of biological properties. In effort to search new effective antihypertensive compounds, we have synthesizednovel xanthone derivatives (xanthonoxypropanolamines) and got patent for these compounds (The Patent Office, Government of India, S. No.: 011–016308, Patent No.: 250538).

          Objective

          In the present work, we attempted to establish the antihypertensive activity, toxicity and molecular docking study forthese newly synthesized compounds (1a, 1b and 2).

          Materials and method

          The preliminary antihypertensive screening was performed by administering synthesized compounds and standard drugs intraperitonially and orally into wistar rats. The change in systolic, diastolic and the mean blood pressure before and after the treatment of the drugs was measured on a Digital LE-S100 Blood Pressure Meter by Tail-cuff method non-invasively. Toxicity studies were carried out after oral administration of synthesized compounds to rats at doses of 25, 50, and 100mg/kg. The serum samples were tested for different toxicity parameters such as liver function test, kidney function test etc. The docking simulations of all the compounds were performed using Maestro, version 9.4 implemented from Schrodinger software suite.

          Results and discussion

          The result showed that the compound 1a, 1b and 2 have greater antihypertensive activity with almost equal or less toxicity profile in comparison to standard drug Propranolol and Atenolol. The docking score for the compound 1b was found -9.1 while for compound 1a and 2 were found -8.7 and -8.6 respectively.

          Conclusion

          These novel compounds i.e. 1a, 1b, and 2 have greater antihypertensive activity in comparison to standard drugs Propranolol and Atenolol. All these compounds do not have any toxicity.

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          Most cited references24

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          Biological Activities and Bioavailability of Mangosteen Xanthones: A Critical Review of the Current Evidence

          Mangosteen (Garcinia mangostana L.) is a tropical tree native to Southeast Asia that produces a fruit whose pericarp contains a family of tricyclic isoprenylated polyphenols referred to as xanthones. Numerous in vitro studies have shown that these xanthones possess anti-oxidant, anti-proliferative, pro-apoptotic, anti-inflammatory and anti-carcinogenic activities. Aggressive marketing of such health promoting benefits has resulted in mangosteen’s classification as a “superfruit”. This has led to sales of mangosteen containing beverages in USA alone exceeding $200 million in 2008 despite very limited animal and human studies. This review will (a) critically address recent reports of in vivo studies on the bioavailability and metabolism of mangosteen xanthones, (b) update the in vitro and in vivo data on anti-cancer and anti-inflammatory activities of mangosteen xanthones, and (c) suggest needed areas of inquiry regarding the absorption, metabolism and efficacy of mangosteen xanthones.
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            Rusting of the lock and key model for protein-ligand binding.

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              Comparison of improved precipitation methods for quantification of high-density lipoprotein cholesterol.

              We compared the standard Lipid Research Clinics heparin-Mn2+ (46 mmol/L) method and five improved precipitation methods for quantification of high-density lipoprotein (HDL) cholesterol. Three of these methods--a dextran sulfate-Mg2+ procedure, reported as a Selected Method, a modified heparin-Mn2+ (92 mmol/L) method, and a modified phosphotungstate-Mg2+ procedure--all gave similar results. Three other methods--the standard heparin-Mn2+ (46 mmol/L) method and two polyethylene glycol methods (75 g/L or pH 10 reagent at 100 g/L final concentrations)--gave slightly higher values for HDL cholesterol. Addition of NaCl or glucose to specimens did not significantly change protein precipitation. In terms of sedimentation effectiveness with hypertriglyceridemic specimens, the methods were ranked in the following order: polyethylene glycol (pH 10, 100 g/L) greater than dextran sulfate-Mg2+ greater than heparin-Mn2+ (92 mmol/L) = polyethylene glycol (75 g/L) greater than phosphotungstate-Mg2+ greater than heparin-Mn2+ (46 mmol/L).
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                Author and article information

                Contributors
                Role: Writing – original draft
                Role: Supervision
                Role: Editor
                Journal
                PLoS One
                PLoS ONE
                plos
                plosone
                PLoS ONE
                Public Library of Science (San Francisco, CA USA )
                1932-6203
                15 August 2019
                2019
                : 14
                : 8
                : e0220920
                Affiliations
                [001]Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard University, New Delhi,India
                Aligarh Muslim University, INDIA
                Author notes

                Competing Interests: The authors have declared that no competing interests exist.

                Author information
                http://orcid.org/0000-0002-9298-0696
                http://orcid.org/0000-0002-6834-9781
                Article
                PONE-D-19-14313
                10.1371/journal.pone.0220920
                6695135
                31415607
                dbb6758f-7500-4e9b-92a9-5982c53592fb
                © 2019 Goshain, Ahmed

                This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

                History
                : 1 June 2019
                : 25 July 2019
                Page count
                Figures: 8, Tables: 4, Pages: 13
                Funding
                Funded by: UGC, New Delhi
                Award ID: Grant no: F.40-276/2011 (SR)
                Award Recipient :
                This research work was funded by University Grants Commission, Bhadurshah Zafar Marg, New Delhi, India, Grant no: F.40-276/2011 (SR).
                Categories
                Research Article
                Medicine and Health Sciences
                Vascular Medicine
                Blood Pressure
                Medicine and Health Sciences
                Pharmacology
                Drugs
                Antihypertensives
                Biology and Life Sciences
                Toxicology
                Toxicity
                Medicine and Health Sciences
                Pathology and Laboratory Medicine
                Toxicology
                Toxicity
                Medicine and Health Sciences
                Pharmaceutics
                Drug Therapy
                Drug Administration
                Medicine and Health Sciences
                Pharmacology
                Drugs
                Antihypertensive Drugs
                Medicine and Health Sciences
                Pharmacology
                Drug Screening
                Physical Sciences
                Chemistry
                Computational Chemistry
                Molecular Docking
                Physical Sciences
                Chemistry
                Chemical Compounds
                Organic Compounds
                Alcohols
                Ethanol
                Physical Sciences
                Chemistry
                Organic Chemistry
                Organic Compounds
                Alcohols
                Ethanol
                Custom metadata
                All relevant data are within the manuscript.

                Uncategorized
                Uncategorized

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