Topic
Xanthone
About: Xanthone is a research topic. Over the lifetime, 1639 publications have been published within this topic receiving 25870 citations. The topic is also known as: 9-oxo-xanthene & Diphenyline ketone oxide.
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TL;DR: A review of the contributions of the corresponding author (M.M.P.) and her research group to Medicinal Chemistry concerning the isolation from plant and marine sources of xanthone derivatives as well as their synthesis, biological/pharmacological activities, formulation and analytical applications is presented in this paper.
Abstract: This work reviews the contributions of the corresponding author (M.M.M.P.) and her research group to Medicinal Chemistry concerning the isolation from plant and marine sources of xanthone derivatives as well as their synthesis, biological/pharmacological activities, formulation and analytical applications. Although her group activity has been spread over several chemical families with relevance in Medicinal Chemistry, the main focus of the investigation and research has been in the xanthone family. Xanthone derivatives have a variety of activities with great potential for therapeutic applications due to their versatile framework. The group has contributed with several libraries of xanthones derivatives, with a variety of activities such as antitumor, anticoagulant, antiplatelet, anti-inflammatory, antimalarial, antimicrobial, hepatoprotective, antioxidant, and multidrug resistance reversal effects. Besides therapeutic applications, our group has also developed xanthone derivatives with analytical applications as chiral selectors for liquid chromatography and for maritime application as antifouling agents for marine paints. Chemically, it has been challenging to afford green chemistry methods and achieve enantiomeric purity of chiral derivatives. In this review, the structures of the most significant compounds will be presented.
42 citations
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TL;DR: A series of xanthone derivatives was synthesized and tested in‐vitro for their ability to inhibit aggregation of rabbit washed platelets and human platelet‐rich plasma induced by various inducers.
Abstract: A series of xanthone derivatives was synthesized and tested in-vitro for their ability to inhibit aggregation of rabbit washed platelets and human platelet-rich plasma (PRP) induced by various inducers.
2-Prenyloxyxanthone showed the most potent inhibition of rabbit washed platelet aggregation induced by arachidonic acid (IC50 = 10.2 μM). Of the compounds tested in human PRP, 2-[3 (propylamino)-2-hydroxypropoxy]xanthone (4) hydrochloride salt exhibited the most potent inhibition of platelet aggregation induced by adrenaline (IC50 = 4.4 μM), whereas in evaluation of mouse antithrombotic activity, compound 4 exhibited the most potent protection of mice from thrombotic challenge. Compound 4, 2-[3-(isopropylamino)-2-hydroxypropoxylxanthone hydrochloride salt and 2,5 dihydroxyxanthone suppressed the secondary aggregation induced by adrenaline in human PRP.
We conclude that the antiplatelet effects of these compounds are mainly due to an inhibitory effect on thromboxane formation.
42 citations
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TL;DR: Of the isolated metabolites, 2 exhibited significant anti-mycobacterial activity against Mycobacterium tuberculosis.
42 citations
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TL;DR: A thorough structure-activity relationship (SAR) analysis of a series of nonpeptidic amphiphilic xanthone derivatives in an attempt to identify more potent compounds with lower hemolytic activity and greater membrane selectivity identified 3a with potent MICs and could be used as a lead compound for further structural optimization for the treatment of MRSA infection.
Abstract: We recently reported the bioinspired synthesis of a highly potent nonpeptidic xanthone, 2c (AM-0016), with potent antibacterial activity against MRSA. Herein, we report a thorough structure–activity relationship (SAR) analysis of a series of nonpeptidic amphiphilic xanthone derivatives in an attempt to identify more potent compounds with lower hemolytic activity and greater membrane selectivity. Forty-six amphiphilic xanthone derivatives were analyzed in this study and structurally classified into four groups based on spacer length, cationic moieties, lipophilic chains, and triarm functionalization. We evaluated and explored the effects of the structures on their membrane-targeting properties. The SAR analysis successfully identified 3a with potent MICs (1.56–3.125 μ/mL) and lower hemolytic activity (80.2 μg/mL for 3a versus 19.7 μg/mL for 2c). Compound 3a displayed a membrane selectivity of 25.7–50.4. Thus, 3a with improved HC50 value and promising selectivity could be used as a lead compound for further...
41 citations
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TL;DR: This review focuses on mangosteen pericarp extracts, xanthones and derivatives for the future laboratory experiment and development in pharmacological aspects and concludes that xanthone compounds may play a major role in therapeutic treatment of the diseases.
Abstract: Objective This review focuses on mangosteen pericarp extracts, xanthones and derivatives for the future laboratory experiment and development in pharmacological aspects. Material and method All relevant literature databases were searched up to 2 March 2014. The search terms included mangosteen, xanthone, mangostin, and gatanin in all of the human, animal, in vitro and in vivo studies. Anti-intflammation, antioxidant, antibacterial, anticancer and antiulcer properties of each substance were the key parameters. Results Xanthones are a group of oxygen-containing heterocyclic compounds including alpha-mangostin, gamma-mangostin, mangosteen extract, xanthone derivatives and synthetic xanthones, which provide remarkable and diverse pharmacological effects such as anticancer, antioxidant, anti-inflammatory and antimicrobial activities. Conclusion These xanthone compounds may play a major role in therapeutic treatment ofthe diseases but precise mechanisms ofaction are still unclear and needfurther investigation.
41 citations