AUTHOR=Alafnan Ahmed , Sridharagatta Swathi , Saleem Hammad , Khurshid Umair , Alamri Abdulwahab , Ansari Shabana Yasmeen , Zainal Abidin Syafiq Asnawi , Ansari Siddique Akber , Alamri Abdulhakeem S. , Ahemad Nafees , Anwar Sirajudheen 

TITLE=Evaluation of the Phytochemical, Antioxidant, Enzyme Inhibition, and Wound Healing Potential of Calotropis gigantea (L.) Dryand: A Source of a Bioactive Medicinal Product

JOURNAL=Frontiers in Pharmacology

VOLUME=12

YEAR=2021

URL=https://www.frontiersin.org/journals/pharmacology/articles/10.3389/fphar.2021.701369

DOI=10.3389/fphar.2021.701369

ISSN=1663-9812

ABSTRACT=<p>Traditionally, plants of the genus <italic>Calotropis</italic> have been used to cure various common diseases. The present research work explores the chemical and biological characterization of one of the most common species of this genus, i.e., <italic>Calotropis gigantea</italic> (L.) Dryand (syn. <italic>Calotropis gigantea</italic> (L.) Dryand.), having multiple folklore applications. The ethanolic extract of leaves of <italic>Calotropis gigantea</italic> (L.) Dryand was analyzed for the phytochemical composition by determining the total bioactive (total phenolic and total flavonoid) contents and UHPLC-MS secondary metabolites analysis. For phytopharmacological evaluation, <italic>in vitro</italic> antioxidant (including DPPH, ABTS, FRAP, CUPRAC, phosphomolybdenum, and metal chelation antioxidant assays) activities, enzyme inhibition potential (against AChE, BChE, α-amylase, and tyrosinase enzymes), and <italic>in vivo</italic> wound healing potential were determined. The tested extract has been shown to contain considerable flavonoid (46.75 mg RE/g extract) and phenolic (33.71 mg GAE/g extract) contents. The plant extract presented considerable antioxidant potential, being the most active for CUPRAC assays. Secondary metabolite UHPLC-MS characterization, in both the positive and negative ionization modes, indicated the tentative presence of 17 different phytocompounds, mostly derivatives of sesquiterpene, alkaloids, and flavonoids. Similarly, the tested extract exhibited considerable inhibitory effects on tyrosinase (81.72 mg KAE/g extract), whereas it showed weak inhibition ability against other tested enzymes. Moreover, in the case of <italic>in vivo</italic> wound healing assays, significant improvement in wound healing was observed in both the tested models at the doses of 0.5 percent w/w (<italic>p &lt; 0.001</italic>) and 2.0 percent w/w (<italic>p &lt; 0.01</italic>) on the 16<sup>th</sup> day. The outcomes of the present research work suggested that <italic>C. gigantea</italic> (L.) Dryand plant extract could be appraised as a potential origin of bioactive molecules having multifunctional medicinal uses.</p>