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      Chemistry, Biosynthesis, Physicochemical and Biological Properties of Rubiadin: A Promising Natural Anthraquinone for New Drug Discovery and Development


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          Anthraquinones (AQs) are found in a variety of consumer products, including foods, nutritional supplements, drugs, and traditional medicines, and have a wide range of pharmacological actions. Rubiadin, a 1,3-dihydroxy-2-methyl anthraquinone, primarily originates from Rubia cordifolia Linn (Rubiaceae). It was first discovered in 1981 and has been reported for many biological activities. However, no review has been reported so far to create awareness about this molecule and its role in future drug discovery. Therefore, the present review aimed to provide comprehensive evidence of Rubiadin’s phytochemistry, biosynthesis, physicochemical properties, biological properties and therapeutic potential. Relevant literature was gathered from numerous scientific databases including PubMed, ScienceDirect, Scopus and Google Scholar between 1981 and up-to-date. The distribution of Rubiadin in numerous medicinal plants, as well as its method of isolation, synthesis, characterisation, physiochemical properties and possible biosynthesis pathways, was extensively covered in this review. Following a rigorous screening and tabulating, a thorough description of Rubiadin’s biological properties was gathered, which were based on scientific evidences. Rubiadin fits all five of Lipinski’s rule for drug-likeness properties. Then, the in depth physiochemical characteristics of Rubiadin were investigated. The simple technique for Rubiadin’s isolation from R. cordifolia and the procedure of synthesis was described. Rubiadin is also biosynthesized via the polyketide and chorismate/o-succinylbenzoic acid pathways. Rubiadin is a powerful molecule with anticancer, antiosteoporotic, hepatoprotective, neuroprotective, anti-inflammatory, antidiabetic, antioxidant, antibacterial, antimalarial, antifungal, and antiviral properties. The mechanism of action for the majority of the pharmacological actions reported, however, is unknown. In addition to this review, an in silico molecular docking study was performed against proteins with PDB IDs: 3AOX, 6OLX, 6OSP, and 6SDC to support the anticancer properties of Rubiadin. The toxicity profile, pharmacokinetics and possible structural modifications were also described. Rubiadin was also proven to have the highest binding affinity to the targeted proteins in an in silico study; thus, we believe it may be a potential anticancer molecule. In order to present Rubiadin as a novel candidate for future therapeutic development, advanced studies on preclinical, clinical trials, bioavailability, permeability and administration of safe doses are necessary.

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          Most cited references111

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          Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings

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            The Lancet, 367(9527), 2010-2018
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              CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant.

              Anaplastic lymphoma kinase (ALK) is a tyrosine kinase that is constitutively activated in certain cancers, following gene alterations such as chromosomal translocation, amplification, or point mutation. Here, we identified CH5424802, a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing preferential antitumor activity against cancers with gene alterations of ALK, such as nonsmall cell lung cancer (NSCLC) cells expressing EML4-ALK fusion and anaplastic large-cell lymphoma (ALCL) cells expressing NPM-ALK fusion in vitro and in vivo. CH5424802 inhibited ALK L1196M, which corresponds to the gatekeeper mutation conferring common resistance to kinase inhibitors, and blocked EML4-ALK L1196M-driven cell growth. Our results support the potential for clinical evaluation of CH5424802 for the treatment of patients with ALK-driven tumors. Copyright © 2011 Elsevier Inc. All rights reserved.

                Author and article information

                Drug Des Devel Ther
                Drug Des Devel Ther
                Drug Design, Development and Therapy
                03 November 2021
                : 15
                : 4527-4549
                [1 ]Department of Pharmaceutical Chemistry, Faculty of Pharmacy and Health Sciences, Universiti Kuala Lumpur Royal College of Medicine Perak , Ipoh, Perak, 30450, Malaysia
                [2 ]Faculty of Pharmacy & Centre of Excellence for Biomaterials Engineering, AIMST University , Kedah, 08100, Malaysia
                [3 ]School of Pharmacy, Monash University Malaysia , Bandar Sunway, Selangor Darul Ehsan, 47500, Malaysia
                [4 ]Department of Pharmacology, Sri Ramachandra Faculty of Pharmacy, Sri Ramachandra Institute of Higher Education and Research (DU) , Chennai, Tamil Nadu, 600116, India
                [5 ]Centre for Virus and Vaccine Research, School of Medical and Life Sciences, Sunway University , Selangor, 47500, Malaysia
                [6 ]Department of Biological Sciences, School of Medical and Life Sciences, Sunway University , Selangor, 47500, Malaysia
                [7 ]Faculty of Medicine, Bioscience and Nursing, MAHSA University , Selangor, 42610, Malaysia
                [8 ]Faculty of Applied Science & Centre of Excellence for Biomaterials Engineering, AIMST University , Kedah, 08100, Malaysia
                [9 ]Department of Chemistry, Karpagam Academy of Higher Education , Coimbatore, Tamil Nadu, 640 021, India
                [10 ]Faculty of Pharmacy and Health Sciences, Universiti Kuala Lumpur Royal College of Medicine Perak , Ipoh, Perak, 30450, Malaysia
                [11 ]Department of Pharmaceutical Chemistry, School of Life Sciences, JSS Academy of Higher Education and Research Mauritius , Vacoas, Mauritius
                [12 ]College of Pharmacy, National University of Science and Technology , Muscat, 130, Oman
                [13 ]Department of Pharmaceutical Chemistry, Sri Adichunchanagiri College of Pharmacy, Adichunchanagiri University , Mandya, Karnataka, 571418, India
                Author notes
                Correspondence: Neeraj Kumar Fuloria; Shivkanya Fuloria Faculty of Pharmacy & Centre of Excellence for Biomaterials Engineering, AIMST University , Kedah, 08100, Malaysia Tel +60 16 4037685; +60 14 3034057 Email neerajkumar@aimst.edu.my; shivkanya_fuloria@aimst.edu.my
                Author information
                © 2021 Watroly et al.

                This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution – Non Commercial (unported, v3.0) License ( http://creativecommons.org/licenses/by-nc/3.0/). By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms ( https://www.dovepress.com/terms.php).

                : 09 September 2021
                : 13 October 2021
                Page count
                Figures: 10, Tables: 3, References: 114, Pages: 23
                Funded by: no funding;
                There is no funding to report.

                Pharmacology & Pharmaceutical medicine
                rubiadin,rubia cordifolia,biosynthesis,physicochemical properties,anticancer,pharmacology


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