Chemistry, biosynthesis, physicochemical and biological properties of rubiadin: A promising natural anthraquinone for new drug discovery and development

Mohd Nasarudin Watroly, Mahendran Sekar, Shivkanya Fuloria, Siew Hua Gan, Srikanth Jeyabalan, Yuan Seng Wu, Vetriselvan Subramaniyan, Kathiresan V Sathasivam, Subban Ravi, Nur Najihah Izzati Mat Rani, Pei Teng Lum, Jaishree Vaijanathappa, Dhanalekshmi Unnikrishnan Meenakshi, Shankar Mani, Neeraj Kumar Fuloria

Research output: Contribution to journalReview ArticleResearchpeer-review

31 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)4527-4549
Number of pages23
JournalDrug Design, Development and Therapy
Publication statusPublished - 2021


  • Anticancer
  • Biosynthesis
  • Pharmacology
  • Physicochemical properties
  • Rubia cordifolia
  • Rubiadin

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