Efficacy and safety of Syferol-IHP for the treatment of peptic ulcer disease: a pilot, double-blind randomized trial.

BACKGROUND: To our knowledge, there is no prior randomized study on the utility of Syferol-IHP (blend of virgin coconut oil and Ocimum sanctum oil) when coadministered with a triple therapy schedule. AIM: This study determined the efficacy and safety of Syferol-IHP as adjunct to conventional triple therapy for the treatment of peptic ulcer disease (PUD). METHODS: A pilot double-blind randomized trial was conducted in patients with confirmed diagnosis (endoscopy-guided biopsy) of PUD. Eligible patients were randomized to Pylorest (a three-in-one tablet containing rabeprazole 20 mg, amoxicillin 1 g, and clarithromycin 500 mg) and Syferol-IHP for 2 weeks, followed by rabeprazole and Syferol-IHP for 2 weeks or Pylorest and placebo for 2 weeks, followed by rabeprazole and placebo for 2 weeks. Repeat endoscopy-guided biopsy and histology were done 4 weeks posttherapy. Primary outcome measures were the healing of ulcer and eradication of Helicobacter pylori. Secondary outcome measures were the disappearance of epigastric pain, gastritis, and duodenitis. Analysis was by intention-to-treat. RESULTS: Of the 63 patients enrolled, 60 patients had complete evaluation, with 37 patients receiving Pylorest and Syferol-IHP and 23 patients receiving Pylorest and Placebo. Healing of the PUD in favor of Pylorest and Syferol-IHP was significantly higher for gastric ulcer (RR=0.000, 95% CI=undefined, P=0.048) but not for duodenal ulcer (RR=0.400, 95% CI=0.07-2.37, P=0.241). H. pylori eradication was 100% with Syferol-IHP vs 50% with placebo (P=0.066). Epigastric pain (reduction to 16.2% vs 43.5%; P=0.021), gastritis (reduction to 13.5% vs 39.1%; P = 0.024), and duodenitis (reduction to 0% vs 8.7%; P=0.327) were observed in the Syferol-IHP and Pylorest vs placebo and Pylorest groups, respectively. Adverse events (RR=0.971, 95% CI=0.46-2.04, P=0.937) and laboratory parameters were not significantly different pre- and posttherapies (P>0.05, for both groups). CONCLUSION: Although both treatment arms were equally safe, co-administration of Syferol-IHP and triple therapy is more efficacious than triple therapy alone for treating PUD. Pan African Clinical trial registry identifier number is PACTR201606001665364.

beta-Amyrin and alpha-amyrin acetate isolated from the stem bark of Alstonia boonei display profound anti-inflammatory activity.

CONTEXT: Alstonia boonei De Wild (Apocyanaceae) is used in ethnomedicine for the management of malaria, ulcer, rhematic pain, toothache, and inflammatory disorders. OBJECTIVE: To investigate the anti-inflammatory potential of ß-amyrin and α-amyrin acetate isolated from the stem bark of Alstonia boonei using animal models. MATERIALS AND METHODS: Chromatographic purification of the crude methanol extract led to the isolation and structure elucidation of ß-amyrin and α-amyrin acetate. Their anti-inflammatory activities were evaluated in rodents using egg albumen-induced paw edema and xylene-induced ear edema models. The gastric ulcerogenic, in vivo leucocyte migration, and RBC membrane stabilization tests were also investigated. RESULTS: α-Amyrin acetate at 100 mg/kg showed significant (p < 0.05) inhibition of egg albumen-induced paw edema with % inhibition of 40 at the 5th hour. Oral administration up to 100 mg/kg did not produce significant (p > 0.01) irritation of the gastric mucosa while significant (p < 0.01) ulceration was recorded for indomethacin at 40 mg/kg compared with the negative control. At 100 µg/mL, both ß-amyrin and α-amyrin acetate inhibited heat-induced hemolysis to as much 47.2 and 61.5%, respectively, while diclofenac sodium (100 µg/mL) evoked only 40.5% inhibition. Both compounds at 100 µg/ear produced significant (p < 0.01) inhibition of ear edema in mice by 39.4 and 55.5%, respectively. Also at 100 mg/kg (p.o.) α-amyrin acetate evoked 60.3% reduction in total leucocyte count and significant (p < 0.05) suppression (47.9%) of neutrophil infiltration. DISCUSSION AND CONCLUSION: This study generally provided evidence of profound anti-inflammatory activity of ß-amyrin and α-amyrin acetate isolated from the Alstonia boonei stem bark.

Two trypanocidal dipeptides from the roots of Zapoteca portoricensis (Fabaceae).

Zapoteca portoricensis (Jacq) HM Hernández is used with remarkable efficacy in ethnomedicinal management of tonsillitis in the Eastern part of Nigeria. Previous pharmacological studies have validated the antiinflammatory and antimicrobial activities of the crude extract. In this study, two dipeptides, saropeptate (aurantiamide acetate) and anabellamide, were isolated from the methanol root extract of Zapoteca portoricensis and their chemical structures deduced by one dimensional and two dimensional NMR and mass spectrometry. These compounds were isolated for the first time from this plant, and no report has been found on their previous isolation from the genus Zapoteca. Evaluation of their trypanocidal activity showed that compound 1 exhibited potent activity against Trypanosoma brucei rhodesiense with an IC50 value of 3.63 µM and selectivity index of 25.3.

Inhibition of inflammatory mediators and reactive oxygen and nitrogen species by some depsidones and diaryl ether derivatives isolated from Corynespora cassiicola, an endophytic fungus of Gongronema latifolium leaves.

In this study, some depsidones and diaryl ether derivatives isolated from Corynespora cassicola, a fungi endophyte of Gongronema latifolium, were assessed for their anti-inflammatory potentials. The isolated metabolites corynesidone A (1), corynesidone C (2), corynesidone D (3) and corynether A (4) were screened for their effects on tumour necrosis factor-α (TNF-α), inducible nitric oxide (iNO), and reactive oxygen species (ROS) and reactive nitrogen species (RNS) production by stimulated RAW264.7 macrophages. Concentration of 1, 2, 3 and 4 up to 100 µM did not remarkably affect the viability of treated macrophages. The compounds were found to cause a concentration-dependent decrease in lipopolysaccharide-induced TNF-α and iNO in RAW264.7 cells. Pre-treatment with 100 µM of 1, 2, 3 and 4 suppressed iNO by as much as 96.28%, 95.71%, 78.14% and 73.28%; with IC(50) of 8.16, 9.49, 15.29 and 26.52 µM, respectively. Similarly, pre-treatment with 100 µM of 1, 2, 3 and 4 caused an inhibition of 99.17%, 99.59%, 95.02% and 74.07% in the formation of iNO production, respectively, with IC(50) of 1.88, 3.99, 7.48 and 37.22 µM. Treatment of with compounds 1-4 (10, 30 and 100 µM) followed by stimulation with phorbol 12-myristate 13-acetate (1 µM) caused significant (p < 0.05) suppression of ROS/RNS-evoked chemiluminescence of luminol by as much as 100.96 ± 1.88%, 98.59 ± 1.38%, 87.35 ± 1.41% and 79.22 ± 0.30%, respectively at 100 µM. The depsidone derivatives (1-4) showed more potent inhibition of TNF-α and NO production and better scavenging ROS/RNS than the diaryl ether derivative (4). These chemical scaffolds can serve as suitable lead molecules for further development into novel anti-inflammatory and/or anti-cancer agents.