Roots of Rondeletia odorata are a rich source of phytochemicals with high antioxidant potential and thus may possess health benefits. This study used the LC-MS technique to identify phytoconstituents in R. odorata roots extract/fractions. Results revealed that n-butanol fraction and ethanolic extract contained total phenolic and flavonoid contents with values of 155.64 ± 0.66 mgGAE/g DE and 194.94 ± 0.98 mgQE/g DE, respectively. Significant potential of antioxidants was observed by DPPH, CUPRAC and FRAP methods while the ABTS method showed moderate antioxidant potential. Maximum % inhibition for urease, tyrosinase and carbonic anhydrase was shown by ethanolic extract (73.39 ± 1.11%), n-butanol soluble fraction (80.26 ± 1.59%) and ethyl acetate soluble fraction (76.50 ± 0.67%) which were comparable with thiourea (standard) (98.07 ± 0.74%), kojic acid (standard) (98.59 ± 0.92%) and acetazolamide (standard) (95.51 ± 1.29%), respectively, while all other extract/fractions showed moderate inhibition activity against these three enzymes. Hemolytic activity was also observed to range from 18.80 ± 0.42 to 3.48 ± 0.69% using the standard (triton X-100) method. In total, 28 and 20 compounds were identified tentatively by LC-MS analysis of ethanolic extract and n-butanol soluble fraction, respectively. Furthermore, molecular docking was undertaken for major compounds identified by LC-MS for determining binding affinity between enzymes (urease, tyrosinase and carbonic anhydrase) and ligands. It was concluded that active phytochemicals were present in roots of R. odorata with potential for multiple pharmacological applications and as a latent source of pharmaceutically important compounds. This should be further explored to isolate important constituents that could be used in treating different diseases.
Zaleya pentandra L. jaffery is the only species of the genus Zaleya that grows in the Cholistan desert, Pakistan. It is a Xero-halophyte plant with high phenolic and flavonoid content. The present research was designed to investigate the phytochemical composition, biological activities, and in silico molecular docking of the ethanolic extract of Z. pentandra. The phytochemical evaluation was done through preliminary phytochemical testing, estimation of total bioactive content, and gas chromatography–mass spectrometry (GC–MS) analysis for the identification of volatile compounds. For the evaluation of biological activities, antioxidants, and enzyme inhibition (α-glucosidase, cholinesterase, and tyrosinase), antibacterial and antiviral assays were performed. GC–MS analysis revealed the presence of 29 tentative volatile compounds. The ethanolic extract of Z. pentandra contains high phenolic content (119.6 ± 0.12 mg GAE/g extract) and flavonoid content (45.5 ± 0.19 mg QE/g extract), which correlates with the strong DPPH, FRAP, and enzyme inhibition results. The ethanolic extract of Z. pentandra also showed dose-dependent antibacterial activity. Micrococcus luteus and Pseudomonas aeruginosa were found to be most susceptible, with 16 mm and 17 mm zone of inhibitions at a maximum dose of 20 mg/mL. Antiviral results showed that the ethanol extract has excellent activity against H9, IBV, and NDV viral strains. Additionally, in silico molecular docking was performed in order to determine the interaction and binding affinity between the enzymes and compounds identified by GC–MS. α-glucosidase, cholinesterase, and tyrosinase showed the highest binding affinity toward 1,2-benzenedicarboxylic acid, 2-hydroxy-n-(2-phenylethyl) benzamide, γ-sitosterol, and lactose. These findings can serve as a benchmark for anti-diabetic-, neuro-, and skin-protective uses of this plant and can be used for the isolation of pure bioactive compounds in the future.
Poor solubility is a global issue of copious pharmaceutical industries as large number of drugs in development stage as well as already marketed products are poorly soluble which results in low dissolution and ultimately dosage increase. Current study is aimed at developing a polyvinylpyrrolidone- (PVP-K30-) based nanogel delivery system for solubility enhancement of poorly soluble drug olanzapine (OLP), as solubilization enhancement is the most noteworthy application of nanosystems. Crosslinking polymerization with subsequent condensation technique was used for the synthesis of nanogels, a highly responsive polymeric networks in drug’s solubility. Developed nanogels were characterized by percent entrapment efficiency, sol-gel, percent swelling, percent drug loaded content (%DLC), percent porosity, stability, solubility, in vitro dissolution studies, FTIR, XRD, and SEM analysis. Furthermore, cytotoxicity study was conducted on rabbits to check the biocompatibility of the system. Particle size of nanogels was found with , and in vitro dissolution study exhibited that drug release properties were considerably enhanced as compared to the marketed formulation OLANZIA. The solubility studies indicated that solubility of OLP was noticeably improved up to 36.7-fold in phosphate buffer of pH 6.8. In vivo cytotoxicity study indicated that prepared PVP-K30-based formulation was biocompatible. On the basis of results obtained, the developed PVP-K30-co-poly (AMPS) nanogel delivery system is expected to be safe, effective, and cost-effective for solubility improvement of poorly soluble drugs.