Oxidative stress plays a significant role in the pathogenesis of metabolic syndrome including diabetes mellitus (DM). The inhibition of alpha-amylase is an important therapeutic target in the regulation of postprandial increase of blood glucose in diabetic patients. The present study investigated the alpha-amylase inhibitory and antioxidant potential of selected herbal drugs used in the treatment of DM by the traditional healers in Isiala Mbano and Ikwuano regions of southeastern Nigeria. Antioxidant activity was evaluated in terms of free radical scavenging, reducing power, and total phenolic (TPC) and flavonoid content (TFC) in consonance with the TLC profiling. The results showed that methanol crude extracts from Anacardium occidentale (AO) and Ceiba pentandra (CP) recorded higher TPC and TFC, potent free radical scavenging, and efficient reducing power (RP) as compared with other plant samples. All the plant extracts exhibited a relative alpha-amylase inhibition apart from Strophanthus hispidus (SH) extract with a negative effect. We discovered a mild to weak correlation between alpha-amylase inhibition or antioxidative capacity and the total phenol or flavonoid content. At least in part, the results obtained in this work support the traditional use of certain plant species in the treatment of patients with DM.

Ethnopharmacological importance: Capsicum and ginger are used widely in human diets and in folklore medicines. Chemically, gingerol is a relative of capsaicin and both classes of compounds are notable for their spiciness and characteristic pungent aroma. Previous studies have demonstrated that these compounds contain antimicrobial compounds with robust pharmacological importance. Aim: The present study evaluated the in vitro antibacterial activities of capsaicinoids and gingerols against a panel of clinical MRSA strains and their inhibitory effect on the conjugal transfer of R-plasmids harboured in E. coli. Materials and methods: Crude methanol extract of C. annum was fractionated using solid phase extraction (SPE) and screened for R-plasmid transfer inhibition: TP114, PUB 307, PKM 101, R6K and R7K. The bio-guided assay led to the isolation of bioactive compounds with strong R-plasmid transfer inhibition. The compounds were identified using Nuclear Magnetic resonance (NMR) and Mass spectroscopy (MS). Capsaicin analogues nonivamide, 6-gingerol, 6-shogaol, capsaicin and dihydrocapsaicin were screened for antimicrobial activity against a panel of methicillin-resistant Staphylococcus aureus (MRSA) and Gramnegative bacteria strains using microdilution method while the plasmid transfer inhibition assay of the compounds was determined by broth mating method. Results: The bioactive fraction Ca-11 showed good inhibition rates (8.57-25.52%) against three R-plasmids PUB307, PKM 101, TP114 followed by the crude extract of C. annum (8.59%) respectively leading to the bioassay-guided isolation of capsaicin and dihydrocapsaicin as the bioactive principles. The antiplasmid effect of pure capsaicin and dihydrocapsaicin were broad and within active ranges (5.03-31.76%) against the various antibiotic resistance-conferring plasmids including R6K, R7K.

Curtisia dentata (CD) is a vulnerable medicinal plant used for the treatment of stomach ailments in South Africa. However, there is a lack of sufficient data on its phytochemical components and medicinal properties. The phytochemical analysis of the extract was estimated using standard assay methods while its antibacterial activity was determined by the agar dilution method against selected bacteria. The antioxidant activity of the extract was done using ferric reducing power, 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2′-azino-bis-3-ethylbenzothiazoline-6-sulfonic-acid (ABTS), nitric oxide (NO), hydrogen peroxide (H2O2) and lipid peroxidation (LPO). The cytotoxicity assay of the extract was assessed using the brine shrimp lethality test with LC50 value of 0.302 mg/mL. The antibacterial activity of the extract demonstrated an appreciable broad spectrum activity against the tested bacteria with minimum inhibitory concentration (MIC) ranges between 5000 and 0.5 mg/L. Both phenol and flavonoid concentrations were 14.86 mg tannic acid equivalent/g and 13.64 mg quercetin equivalent/g, respectively. The percentage composition of saponins (13.26) was highest, followed by steroids (1.42), while alkaloids and tannins had the same value of 0.51. Similarly, IC50 values of the extract against DPPH, ABTS, H2O2, LPO and NO were 0.017, 0.018, 0.159, 0.06 and 0.052 mg/mL, respectively. The reducing power of the extract was found to be concentration dependent. Our data suggest that the 70% ethanol extract from the CD extract has antibacterial and antioxidant properties due to the presence of bio-active compounds and thus support its folkloric use in the treatment of diseases.

No abstract

Rosa canina (RC, the Dog Rose) is used in European folk medicine for the treatment of various human ailments. The crude methanol extract of this botanical was tested against multidrug-resistant (MDR) bacterial strains including methicillin-resistant Staphylococcus aureus SA1199B, EMRSA-16 and XU212 harbouring NorA, PBP2a and TetK resistance mechanisms, respectively, as well as S. aureus ATCC25923, a standard antimicrobialsusceptible laboratory strain. Inhibition of the conjugal transfer of plasmids PKM101 and TP114 by the RC extract was also evaluated. The RC extract demonstrated a mild to poor antibacterial activity against the panel of bacteria having MIC values ranging from 256 to >512 mg/L, but strongly potentiated tetracycline activity (64-fold) against XU212, a tetracycline-effluxing and resistant strain. Furthermore, the extract showed moderate capacity to inhibit the conjugal transfer of TP114 and PKM101; transfer frequencies were between 40% and 45%. Cytotoxicity analysis of the RC extract against HepG2 cells line showed the IC50 >500µg/mL and thus was considered non-toxic toward human cells. Phytochemical characterisation of the extracts was performed by the assessment of total phenolic content (RC: 60.86 mg TAE/g) and by HPLC fingerprint determination. The results from this study provide new mechanistic evidence justifying, at least in part, the traditional use of this extract. However, the inhibition of bacterial plasmid conjugation opens the possibility of combination therapies to overcome antibiotic-resistance.