Heliotropium is one of the most important plant genera to have conventional folklore importance, and hence is a potential source of bioactive compounds. Thus, the present study was designed to explore the therapeutic potential of Heliotropium crispum Desf., a relatively under-explored medicinal plant species. Methanolic extracts prepared from a whole plant of H. crispum were studied for phytochemical composition and possible in vitro and in silico biological properties. Antioxidant potential was assessed via six different assays, and enzyme inhibition potential against key clinical enzymes involved in neurodegenerative diseases (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)), diabetes (α-amylase and α-glucosidase), and skin problems (tyrosinase) was assayed. Phytochemical composition was established via determination of the total bioactive contents and reverse phase ultra-high performance liquid chromatography mass spectrometry (RP-UHPLC-MS) analysis. Chemical profiling revealed the tentative presence of 50 secondary metabolites. The plant extract exhibited significant inhibition against AChE and BChE enzymes, with values of 3.80 and 3.44 mg GALAE/g extract, respectively. Further, the extract displayed considerable free radical scavenging activity against DPPH and ABTS radicals, with potential values of 43.19 and 41.80 mg TE/g extract, respectively. In addition, the selected compounds were then docked against the tested enzymes, which have shown high inhibition affinity. To conclude, H. crispum was found to harbor bioactive compounds and showed potent biological activities which could be further explored for potential uses in nutraceutical and pharmaceutical industries, particularly as a neuroprotective agent.

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Purpose: To determine the urease-inhibitory activity and chemical constituents of fractions of Calligonum polygonoides and Crateva adansonii separated by physical properties. Methods: The anti-urease activities of different fractions of the plants (methanol, n-hexane, CHCl3, nbutanol) were evaluated using a standard procedure. The chemical constituents of the extracts with the highest urease-inhibitory activity were determined by gas chromatography-mass spectrometry. Results: The n-hexane fractions of both plants had higher urease-inhibitory activity and a lower halfmaximal inhibitory concentration (IC50) than the other extracts. GC-MS evaluation revealed that nhexane fraction of C. polygonoides was rich in fatty acids (39.36 %), sterols (22.29 %), long chain alkanes (98.5 %), and a few volatiles (5.26 %), while the n-hexane fraction of C. adansonii had high levels of alkanes (35.03 %), sterols (10.46 %), fatty acid esters (46.82 %), and triterpenes (23.76 %). Conclusion: The n-hexane fractions of the plants demonstrate high urease-inhibitory activity. Thus, these plant-based anti-urease fractions can potentially serve as a starting point for the development of novel antibacterial agents with enhanced efficacy and reduced antibiotic resistance in the treatment of pathological conditions and infections associated with urease.

In this study, flavonoid-rich chloroform fraction (FRCF) of nine different citrus species was isolated by solvent fractionation technique and its effect on αglucosidase, α-amylase, glucose uptake by yeast cells and glycosylation of haemoglobin was studied. FRCF of Citrus maxima was found to show higher activity in the in vitro assays and thus it was characterized by Electrospray Ionization Mass Spectrometry (ESI-MS) analysis. This led to the identification of icariin, hesperidin and diosmetin-6,8-di-C-glucoside. Their binding efficacy with targeted proteins such as glucokinase (GK), glycogen synthase kinases 3β (GSK 3β) and peroxisome proliferator-activated receptor-γ (PPAR-γ ) was studied by in silico analysis using Schrödinger Maestro software. Icariin exhibited maximum docking energy with GSK 3β, relatively less for GK and null for PPAR-γ. Hesperidin and diosmetin-6, 8-di-C-glucoside showed good binding affinity with PPAR-γ compared to GSK 3β.