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The treatment of Salmonella infections is threatened by multidrug resistance necessitating the search for alternative treatments, such as from medicinal plants. There are several reports on the antibacterial activity of Annona muricata. This study assessed the activity against multidrug-resistant (MDR) Salmonella and also the toxicity of the leaves of this plant. The hexane and methanol extracts of the leaves were screened against characterized MDR isolates by disc diffusion and microdilution methods. A cytotoxicity test was performed on monkey kidney epithelial cells; an acute toxicity test was conducted in BALB/c mice and the liver and kidney functions were assessed at the end of the test. Both extracts recorded weak activity in the disc test. Conversely, the extracts showed a wide range of activity against specific Salmonella isolates in the microdilution assay, and the lowest minimum inhibitory concentration value recorded was 0.0625 mg/mL. The hexane extract (ANOHEX) was not cytotoxic (CC50 = 57.7 µg/mL) and was also not toxic to the mice at 2000 mg/Kg bodyweight, while the methanol extract (ANOMET) was cytotoxic (CC50 = 18.44 µg/mL), and mortality was recorded at 2000 mg/Kg but not at 300 mg/Kg. There were no significant changes in biomarkers of the liver (alanine aminotransferase and aspartate aminotransferase) and kidney (creatinine and urea) functions P > 0.05 , except for ANOHEX which significantly decreased creatinine P = 0.01 , in the test mice which was not considered a toxic effect. In conclusion, this study has demonstrated high bacteriostatic activity against MDR Salmonella and a low risk of toxicity of A. muricata leaves. Hence, the leaves are a potential alternative treatment for resistant Salmonella infection. The natural products should be further investigated in vitro and in vivo. [ABSTRACT FROM AUTHOR]

Background. The threat to human health posed by multidrug-resistant strains of Salmonella typhi (S. typhi) and Salmonella paratyphi (S. paratyphi) is of growing concern. Generally, there has been increasing resistance and even multidrug resistance to almost all classes of antibiotics. This has rendered treatment with antibiotics difficult and costly. The present study investigated the bioactivity of pectin and pectin hydrolysates derived from a local fruit, Spondias dulcis, against four strains of Salmonellae. Methods. Pectin was extracted from alcohol extractives-free peel by acidic hydrolysis at a temperature of 80°C for one hour at pH 2 and 4. The pectin was precipitated with 95% alcohol at an extract to alcohol ratio of 1:10 v/v. Antimicrobial activity was determined using agar well diffusion technique. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values were determined using the broth dilution technique. An in vivo study was then carried out with the bioactive extracts against the most resistant bacteria strain, to fully establish the therapeutic effect of these extracts. Balb/C mice were used, and ciprofloxacin was the positive control antibiotic. The extracts were administered to mice at two doses, 5mg/Kg and 10mg/Kg. The efficacy of extracts in the treatment of typhoid was evaluated based on survival rate, change in body weight, and change in bacteria load. Results. Only one of the extracts (crude pectin pH 2.5) was active against all the Salmonellae by well diffusion, and the growth inhibition varied from 12mm to 15mm at100 μg/ml. Three of the extracts (crude pectin pH 2.5, pH 4, 12h hydrolysate, and pH 4, 1h hydrolysate) had MIC and MBC against all four Salmonellae strains with MIC ranging from 5.68 to 44.45 μg/ml and MBC from 11.36 to 44.45 μg/mL. Three treatments, namely, the pH4-12 hr, hydrolysate at 10mg/Kg and 5mg/Kg, and the pH4-1hr, hydrolysate at 10mg/Kg, had therapeutic effects against Salmonella infection in mice. Conclusion. The present study highlights the potential of pectin oligosaccharides as new source of anti-Salmonella drugs. Further investigations including exploration of mechanism of action of the most active pectin extracts/hydrolysates are envisaged. [ABSTRACT FROM AUTHOR]

Background: Malaria is an old life-threatening parasitic disease that is still affecting many people, mainly children living in sub-Saharan Africa. Availability of effective antimalarial drugs played a significant role in the treatment and control of malaria. However, recent information on the emergence of P. falciparum parasites resistant to one of the artemisinin-based combination therapies suggests the need for discovery of new drug molecules. Therefore, this study aimed to evaluate the antiplasmodial activity of extracts, fractions and isolated compound from medicinal plants traditionally used in the treatment of malaria in Tanzania. Methods: Dry powdered plant materials were extracted by cold macerations using different solvents. Norcaesalpin D was isolated by column chromatography from dichloromethane root extract of Caesalpinia bonducella and its structure was assigned based on the spectral data. Crude extracts, fractions and isolated compound were evaluated for antiplasmodial activity against chloroquine-sensitive P. falciparum (3D7), chloroquine-resistant P. falciparum (Dd2, K1) and artemisinin-resistant P. falciparum (IPC 5202 Battambang, IPC 4912 Mondolkiri) strains using the parasite lactate dehydrogenase assay. Results: The results indicated that extracts of Erythrina schliebenii, Holarrhena pubescens, Dissotis melleri and C. bonducella exhibited antiplasmodial activity against Dd2 parasites. Ethanolic root extract of E. schliebenii had an IC50 of 1.87 µg/mL while methanolic and ethanolic root extracts of H. pubescens exhibited an IC50 = 2.05 µg/mL and IC50 = 2.43 µg/mL, respectively. Fractions from H. pubescens and C. bonducella roots were found to be highly active against K1, Dd2 and artemisinin-resistant parasites. Norcaesalpin D from C. bonducella root extract was active with IC50 of 0.98, 1.85 and 2.13 µg/mL against 3D7, Dd2 and IPC 4912-Mondolkiri parasites, respectively. Conclusions: Antiplasmodial activity of norcaesalpin D and extracts of E. schliebenii, H. pubescens, D. melleri and C. bonducella reported in this study requires further attention for the discovery of antimalarial lead compounds for future drug development. [ABSTRACT FROM AUTHOR]

Background: Diabetes mellitus (DM) is a metabolic disease characterized by chronic hyperglycaemia generally associated with oxidative stress. The present study aims at evaluating the antioxidant and antidiabetic potential of methanol and hydroethanol extracts of the stem bark and leaves of Pricralima nitida and the Sonchus oleraceus whole plant respectively. Methods: The in vitro antioxidant activity was assessed using 1,1-Diphenyl-2-picrilhydrazyl (DPPH) for free radical-scavenging properties of the extracts, and the Folin-Ciocalteu method in determining their phenol contents. The antidiabetic activity was tested in mice following streptozotocin diabetes induction, and selected oxidative stress markers (Malondialdehyde, Hydrogen peroxides and Catalase) were measured in order to evaluate the level of oxidative stress in treated animals. Results: The in vitro antioxidant activity using DPPH showed IC50 ranging from 0.19 ± 0.08 to 1.00 ± 0.06 mg/mL. The highest activity was obtained with the hydroethanol extracts of S. oleraceus (0.19 mg/mL and P. nitida (0.24 mg/mL). Polyphenol contents ranged from 182.25 ± 16.76 to 684.62 ± 46.66 μg Eq Cat/g. The methanol extract of P. nitida showed the highest activity, followed by the hydroethanol extract of S. oleraceus (616.89 ± 19.20 μEq Cat/g). The hydroethanol extract of whole plants (150 mg/Kg) and methanol leave extract of P. nitida (300 mg/Kg) exhibited significant antidiabetic activities with 39.40% and 38.48% glycaemia reduction, respectively. The measurement of stress markers in plasma, liver and kidney after administration of both extracts showed significant reduction in MDA and hydrogen peroxide levels, coupled with a substantial increase in catalase activity. Conclusions: These findings suggest that S. oleraceus whole plant and P. nitida leaves possess both antidiabetic and antioxidant properties, and therefore could be used as starting point for the development of herbal medicines and/or source of new drug molecules against diabetes. [ABSTRACT FROM AUTHOR]

Background: Traditional medicinal plants are one of the potential sources of anti-malarial drugs and there is an increasing interest in the use and development of traditional herbal remedies for the treatment of malaria and other ailments. This study was carried out with the aim to investigate the phytochemical screening, cytotoxic effect and antiplasmodial activities of Dichrostachys cinerea and Commiphora africana. Both plants are used by the Maasai in Tanzania in suspected malaria and other diseases. No previous work appears to have investigated the potential anti-malarial activity of the two plants. Methods: This study aimed to investigate the in vitro anti-malarial activity of methanol and dichloromethane extracts of the two plants against chloroquine sensitive (D6) and chloroquine resistant (Dd2) strains of Plasmodium falciparum. The anti-malarial property was assessed by the lactate dehydrogenase method (pLDH). The in vivo anti-malarial study was carried out using the Peters' 4-day suppressive test in Plasmodium berghei in Balb/c mice. Cytotoxic tests were carried out using monkey kidney epithelial cell line in [3(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] (MTT) assay. Qualitative phytochemical screening was carried out using standard methods of analysis. Results: The phytochemical screening of plant extracts revealed the presence of alkaloids, flavonoids, tannins, steroids, triterpenoids, glycosides and saponins. However, alkaloids were absent in most plant extracts. The dichloromethane extracts of C. africana (stem bark); D. cinerea (stem bark) and methanol extracts of D. cinerea (whole stem) all showed promising in vitro anti-malarial activities. All other extracts did not show any significant anti-malarial activity. The two most promising extracts based on in vitro studies, DCM extracts of C. africana (stem bark) and D. cinerea (stems bark), equally exhibited very significant anti-malarial activities in the mouse model. They exhibited parasite suppression rates of 64.24 and 53.12%, respectively, and considerable improvement in weight and survival rate. Most plant extracts were not cytotoxic except for DCM extract of D. cinerea (whole stem) CC50 (29.44 µg/mL). Conclusion: The findings of this study provide scientific evidence supporting the traditional use of the plants in the treatment of malaria by the Maasai in Arusha region, Tanzania. Consequently, further work including bioassay-guided fractionation and advanced toxicity testing may yield new anti-malarial drug candidates from the two plants. [ABSTRACT FROM AUTHOR]

The aims of the present study were to identify the compounds responsible for the anti-malarial activity of Dacryoedes edulis (Burseraceae) and to investigate their suitability as leads for the treatment of drug resistant malaria. Five compounds were isolated from ethyl acetate and hexane extracts of D. edulis stem bark and tested against 3D7 (chloroquine-susceptible) and Dd2 (multidrug-resistant) strains of Plasmodium falciparum, using the parasite lactate dehydrogenase method. Cytotoxicity studies were carried out on LLC-MK2 monkey kidney epithelial cell-line. In silico analysis was conducted by calculating molecular descriptors using the MOE software running on a Linux workstation. The “drug-likeness” of the isolated compounds was assessed using Lipinski criteria, from computed molecular properties of the geometry optimized structures. Computed descriptors often used to predict absorption, distribution, metabolism, elimination and toxicity (ADMET) were used to assess the pharmacokinetic profiles of the isolated compounds. Antiplasmodial activity was demonstrated for the first time in five major natural products previously identified in D. edulis, but not tested against malaria parasites. The most active compound identified was termed DES4. It had IC50 values of 0.37 and 0.55 µg/mL, against 3D7 and Dd2 respectively. In addition, this compound was shown to act in synergy with quinine, satisfied all criteria of “Drug-likeness” and showed considerable probability of providing an antimalarial lead. The remaining four compounds also showed antiplasmodial activity, but were less effective than DES4. None of the tested compounds was cytotoxicity against LLC-MK2 cells, suggesting their selective activities on malaria parasites. Based on the high in vitro activity, low toxicity and predicted “Drug-likeness” DES4 merits further investigation as a possible drug lead for the treatment of malaria. [ABSTRACT FROM AUTHOR]