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Urena lobata is an herbal remedy traditionally used to cure certain ailments. Its flavonoid and phenol-rich content has been shown to have free radical scavenging activity. Nitric oxide (NO) is an active gaseous substance that is released by cells and plays a role in inflammation. This study examined the ability of U. lobata leaf extract to induce NO production and suppress inducible NO synthase (iNOS). The leaves of U. lobata were extracted with ethanol. The phytoconstituents of the extract were identified, their physicochemical and pharmacokinetic properties were predicted, and their anti-inflammatory activity was evaluated. The structures of the phytoconstituents were determined using the molecular docking approach. Griess technique was used to evaluate NO generation in IL-1β-treated hepatocyte culture media containing the extract. An in silico approach was employed to investigate the suppression of iNOS by phytoconstituents from U. lobata. The results showed that stigmasterol and gossypetin were identified in the extract and had a strong inhibitory effect on iNOS based on the inhibition constant. However, it has lower potency than β-sitosterol. The ethanol extract of U. lobata (IC50 = 163.03 µg/mL) had a lower potency than gossypin (IC50 = 100.31 µg/mL) but was comparable to gossypetin (IC50 = 164.18 µg/mL) for inhibiting NO generation. The ethanol extract of U. lobata demonstrated anti-inflammatory action by lowering NO level, but at a lower concentration than gossypin and gossypetin. The study revealed that U. lobata ethanol extract inhibited NO production through active substances, like gossypetin, mangiferin, β-sitosterol, and stigmasterol, thereby suppressing iNOS activity. [ABSTRACT FROM AUTHOR]

Pulutan (Urena lobata L.) is a medicinal plant that has been traditionally used to treat fever, infection, and inflammation. However, preclinical studies on its activity as an analgesic and anti-inflammatory agent are still limited. The present study was aimed at investigating the analgesic and anti-inflammatory activities of U. lobata leaf extracts, as well as predicting the biological properties of the active components. Eight (two control and six test) groups of male Wistar rats were used in this study. Water and ethanol were used to extract the leaves of U. lobata, and each prepared in doses of 125, 250, and 500 mg/kg body weight (BW) for the treatments. The antiinflammatory and analgesic activities of the extracts were evaluated. Following active compound identification using UHPLC-MS/MS, several compounds were analyzed for drug-likeness and ADME-T properties. The results revealed that both aqueous and ethanolic extracts of U. lobata at 125 and 250 mg/kg BW significantly (p < 0.05) inhibited paw edema with an area under curve (AUC) volume of 10 and 5%, respectively, compared to the control group. For analgesic activity, the aqueous extract of U. lobata was able to significantly (p<0.05) increase the AUC for pain threshold by 30-100 % compared to the control group. However, the activity of the ethanolic extract was lower than the aqueous extract. The drug-likeness analysis indicated that all the phytoconstituents were within the range established by Lipinski's rule of five. Stigmasterol, ß-sitosterol, and mangiferin were predicted to have better ADME-T properties than that of the other compounds. [ABSTRACT FROM AUTHOR]