As expected, all tested ligands were capable of forming hydrogen interactions with residues at their respective binding sites, but the DHVA ligand was capable of creating slightly more hydrogen bonds when docked to either 4COX or 5KIR than the other tested ligands, thus demonstrating the participation of this compound in the anti-inflammatory and antialgic responses observed in the in vivo assays as a COX-2 inhibitor. Therefore, the results obtained support the traditional use of OPe for inflammatory and gastric problems.

No abstract

The results suggest that relaxant effect of AMEO might be due to blockade of calcium influx in guinea-pig trachea smooth muscle. It is possible that estragole and d-limonene could contribute majority in the relaxant effect of AMEO.

Results: Crude extracts of T. sylvatica fruits, separated from seed and pericarp, showed sedative effect in mice. The aqueous (ED 50 ¼ 4.9 AE 0.8 mg/kg) seed extracts is the most active among them. This extract also decrease locomotor activity and disrupt motor coordination of mice. This extract was also the most toxic extract (LD 50 ¼ 5.0 AE 1.4 mg/kg; i.p.). The triterpene glycoside 28-O-[b-L-6-rhamnopyranosyl]-R 1 -barrigenol was identified in this extract as one of the active sedative compounds (ED 50 ¼ 0.12 AE 0.01 mg/kg) also with toxic effect (LD 50 ¼ 1.11 AE 0.23 mg/kg). Conclusion:The results suggest that T. sylvatica fruits has toxic activity rather than CNS depressant activity in mice and that this effect might be related to the presence of 28-O-[b-L-6-rhamnopyranosyl]-R 1 -barrigenol, one of the active principles of T. sylvatica fruits with sedative and toxic effect.

(Z,Z')-Diligustilide (DLG) or levistolide A is a dimeric phthalide isolated from Ligusticum porteri (Osha), the roots of which are used in the traditional treatment of many diseases including gastric aches. However, its action has not been completely elucidated. We analyzed the contributions of hydrogen sulfide and S-nitrosothiols to the action of DLG. Animals were pretreated with freshly formed in vitro nitrosothiol using NaS and sodium nitroprusside to elucidate participation in the action of DLG. We also evaluated the production of HS in vivo and in real time on the stomach via a specific electrode introduced into the stomachs of anaesthetized animals pretreated with DLG. Treatment with 10 mg/kg DLG increases gastric HS production in vivo from 7.8 ± 0.81 ppm to 13.1 ± 3.01 ppm and prevents the decrease in gastric injury caused by absolute ethanol. In addition, it maintains endogenous concentrations of GSH and NO. Exogenous S-nitrosothiols protect the gastric mucosa from damage, suggesting that the action of DLG might be associated with S-nitrosothiol and HS formation.

No abstract

The study of pharmacological interactions between herbal remedies and conventional drugs is important because consuming traditional herbal remedies as supplements or alternative medicine is fairly common and their concomitant administration with prescribed drugs could either have a favorable or unfavorable effect. Therefore, this work aims to determine the pharmacological interactions of a turmeric acetone extract (TAE) and its main metabolite (curcumin) with common anti-ulcer drugs (ranitidine and bismuth subsalicylate), using an ethanol-induced ulcer model in Wistar rats. The analysis of the interactions was carried out via the Combination Index-Isobologram Equation method. The combination index (CI) calculated at 0.5 of the affected fraction (fa) indicated that the TAE or curcumin in combination with ranitidine had a subadditive interaction. The results suggest that this antagonistic mechanism is associated to the mucoadhesion of curcumin and the TAE, determined by rheological measurements. Contrastingly, both the TAE and curcumin combined with bismuth subsalicylate had an additive relationship, which means that there is no pharmacological interaction. This agrees with the normalized isobolograms obtained for each combination. The results of this study suggest that mucoadhesion of curcumin and the TAE could interfere in the effectiveness of ranitidine, and even other drugs.

α-Sanshool is an alkamide isolated from the stem bark of Zanthoxylum liebmannianum, a Mexican medicinal plant known as Colopahtle. Our research group has reported that the intraperitoneal administration of α-sanshool induces tonic-clonic seizures in mice. In the present study, we investigated the convulsive effect of this alkamide and elucidated its mechanism of action by comparing with well-known convulsive and anticonvulsive drugs in an in vivo approach. α-Sanshool showed a potent (ED50 [CL 95%]=3.06 [2.92–3.22] mg/kg) and immediate (2±2 s) seizure effect after the intraperitoneal administration in mice. The convulsive effect of this alkamide was only observed for intraperitoneal administration; the oral route did not show any effect. α-Sanshool was less potent than strychnine (ED50 [CL 95%]=1.53 [1.44–1.62] mg/kg), but more effective than bicuculline, 4-aminopyridine, affinin, and pentylenetetrazol, in that order. The seizures induced by α-sanshool were reduced by capsazepine and diazoxide, suggesting the involvement of TRPV1 and potassium channels in the mechanism of action of this compound.