In Vitro and In Silico Antidiabetic and Antimicrobial Evaluation of Constituents from Kickxia ramosissima (Nanorrhinum ramosissimum)

Abstract

Background and Aims: Kickxia ramosissima (Wall.) Janch (or Nanorrhinum ramosissimum (Wall.) Betsche is a well-known medicinal plant in Pakistan that is traditionally used in diabetic and inflammatory conditions. Because little information is available on its phytochemical composition, a range of constituents were isolated and evaluated in vitro in assays related to the traditional use.Methods: Dried whole plant material was extracted and chromatographically fractionated. Isolated constituents were evaluated in silico and in vitro in assays related to the traditional use against diabetes (inhibition of α-glucosidase activity; inhibition of advanced glycation endproducts) and in inflammatory conditions (inhibition of AAPH induced linoleic acid peroxidation, inhibition of 15-LOX, antimicrobial activity).Results: Phytochemical analysis of the extracts and fractions led to isolation of 7 compounds, including the iridoids kickxiasine (being a new compound), mussaenosidic acid, mussaenoside and linarioside; the flavonoids pectolinarigenin and pectolinarin; and 4-hydroxy-benzoic acid methyl ester. The iridoids showed weak antiglycation activity. The flavonoids, however, showed interesting results as pectolinarigenin was highly active compared to pectolinarin. In the α-glucosidase inhibition assay, only weak activity was observed for the iridoids. However, the flavonoid pectolinarigenin showed good activity, followed by pectolinarin. In the 15-LOX experiment, moderate inhibition was recorded for most compounds, the iridoids mussaenosidic acid and mussaenoside being the most active. In the AAPH assay, weak or no inhibition was recorded for all compounds. The in silico assays for the α-glucosidase and 15-LOX assays confirmed the results of respective in vitro assays. Pectolinarigenin showed moderate antimicrobial activity Kickxia Ramosissimaagainst Staphylococcus aureus, Plasmodium falciparum K1, and Trypanosoma cruzi, but it was not cytotoxic on a human MRC-5 cell line.Conclusion: Our findings may in part contribute to explain the traditional use of K. ramosissima.

Flavonoids isolated from the South African weed Chromolaena odorata (Asteraceae) have pharmacological activity against uropathogens

“…Plumeria ambigens S. F and Plumeria floribunda L. (Apocynaceae) [61], Clerodendrum phlomidis L.f. (Verbenaceae) [55], Kickxia ramosissima (Wall.) (Plantaginaceae) [62], and Lippia species (Verbenaceae) [63]. The compound has also been obtained through hydrolysis of the rutinose unit of pectolinarin isolated from Linaria reflexa L. (Plantaginaceae) [64].…”

Iridoids of Chemotaxonomy Relevance, a New Antirrhinoside Ester and Other Constituents from Kickxia spuria subsp. integrifolia (Brot.) R.Fern.

“…of Bignoniaceae, and Viburnum mullaha Buch .‐ Ham . ex D. Don of Adoxaceae . For what concerns the bioactivity context, this compound exerts good analgesic, anti‐inflammatory, hepato‐protective, and cytotoxic effects …”

“…FRITSCH [11] Linarioside (9) exhibits strong antidiabetic properties. [27] Mussaenosidic acid (10) is not a new phytochemical for the nominal species [11] as well as for the genus, having been previously identified also in K. abahica D.A. SUTTON and K. ramosissima (WALL).…”

An in silico approach for evaluating the antitumor and epigenetic modulating potential of phenolic compounds occurring in edible and medicinal mushrooms

“…The increasing number of in silico papers on antitumor and other biological activities appearing in the literature indicates that the transition is starting to happen. [50][51][52] Conclusion ''Let food be your epigenetic medicine'' could represent a novel interpretation of what Hippocrates said already 25 centuries ago. 34 As such, it will be a challenge for future preventive cancer research to identify novel epigenetic targets which allow selective modulation of cancer signaling.…”