<p>The leaves of <i>Macrosphyra longistyla</i> (DC.) Hiern., Rubiaceae, are eaten as vegetables, in addition to the plant’s medicinal properties. Presently, the anti-inflammatory activity of the ethanol extract of <i>M. longistyla</i> leaves and its fractions was evaluated. The crude extract and fractions obtained via vacuum liquid chromatography technique were investigated for anti-inflammatory activity using inducible nitric oxide synthase and carrageenan- and xylene-induced edema assays. The plant components were screened using UHPLC-UV-HRMS analysis, and the total flavonoid, phenols, and steroids contents were determined quantitatively. The crude extract showed potent inhibitory activity towards NO production with an IC<sub>50</sub> value of 31&#xa0;µg/ml. The 5% <sup>v</sup>/<sub>v</sub> DCM:MeOH fraction showed the highest inhibition (IC<sub>50</sub> 19&#xa0;µg/ml). The crude extract (100, 200, and 400&#xa0;mg/kg, <i>p.o</i>.) elicited significant (<i>p</i> &lt; 0.05) time- and dose-dependent inhibition of edema development in the carrageenan test, with a peak effect comparable to the effect of indomethacin. Similarly, the fractions at 400&#xa0;mg/kg exhibited significant (<i>p</i> &lt; 0.05) time-dependent inhibition of edema development in the carrageenan test. The UHPLC-UV-HRMS screening revealed the presence of mainly polyphenolic metabolites with 38 flavonoids or flavonoid glycosides characterized. Among all crude extract and fractions of the plant, total flavonoid content values were highest (158.11 ± 0.61&#xa0;mg QE/g extract) followed by total steroid content (111.96 ± 0.2&#xa0;mg CE/g extract) while total phenol content (104.78 ± 0.42&#xa0;mg GAE/g extract) was the least. These results indicated that <i>M. longistyla</i> leaf extract predominantly contains flavonoid metabolites with anti-inflammatory potential that can be isolated and characterized for drug discovery.</p> Graphical Abstract <p></p>

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Phytoconstituents of Extract and Fractions of Macrosphyra longistyla Leaves Inhibit Nitric Oxide and Prostaglandins Inflammatory Mediators: In Vitro, In vivo, and Chemical Profiling

  • Mutiat B. Ibrahim,
  • Oluwaseun T. Ajayi,
  • Yan-Hong Wang,
  • Hari B. Kothapalli,
  • Ikhlas A. Khan,
  • Zulfiqar Ali

摘要

The leaves of Macrosphyra longistyla (DC.) Hiern., Rubiaceae, are eaten as vegetables, in addition to the plant’s medicinal properties. Presently, the anti-inflammatory activity of the ethanol extract of M. longistyla leaves and its fractions was evaluated. The crude extract and fractions obtained via vacuum liquid chromatography technique were investigated for anti-inflammatory activity using inducible nitric oxide synthase and carrageenan- and xylene-induced edema assays. The plant components were screened using UHPLC-UV-HRMS analysis, and the total flavonoid, phenols, and steroids contents were determined quantitatively. The crude extract showed potent inhibitory activity towards NO production with an IC50 value of 31 µg/ml. The 5% v/v DCM:MeOH fraction showed the highest inhibition (IC50 19 µg/ml). The crude extract (100, 200, and 400 mg/kg, p.o.) elicited significant (p < 0.05) time- and dose-dependent inhibition of edema development in the carrageenan test, with a peak effect comparable to the effect of indomethacin. Similarly, the fractions at 400 mg/kg exhibited significant (p < 0.05) time-dependent inhibition of edema development in the carrageenan test. The UHPLC-UV-HRMS screening revealed the presence of mainly polyphenolic metabolites with 38 flavonoids or flavonoid glycosides characterized. Among all crude extract and fractions of the plant, total flavonoid content values were highest (158.11 ± 0.61 mg QE/g extract) followed by total steroid content (111.96 ± 0.2 mg CE/g extract) while total phenol content (104.78 ± 0.42 mg GAE/g extract) was the least. These results indicated that M. longistyla leaf extract predominantly contains flavonoid metabolites with anti-inflammatory potential that can be isolated and characterized for drug discovery.

Graphical Abstract