Role of Chitosan-Loaded Solanine Glycoalkaloid from Solanum scabrum Mill. Leaf Extract as Anti-Inflammatory and In Vitro Anticancer Agents.

Objectives: Solanum scabrum Mill. commonly "African nightshade" or "huckleberry" is a plant, whose leaves are used by tribes in Nigeria and Cameroon for making the popular "Kombi" and "Njama Njama" soups, respectively. This study aimed to evaluate the anti-inflammatory and anticancer activities of the leaf crude methanol extract from S. scabrum. Materials and Methods: Fractions of the plant were tested for anti-inflammatory potential and in vitro anticancer activity on MCF-7 and HMVII cell lines by carrageenan-induced oedema in mice, and cytotoxicity assays such as 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide, transwell migration and invasion assays, and apoptosis study by flow cytometry, respectively. Results: Bioguided isolation yielded a white crystalline compound 3-nitro dibenzofuran (C12H7NO3, m/z; 213.19 g/mol, m.p.; 181.49 °C). 1H-NMR showed seven signals at δ (ppm) 2.8-4.3 consisting of two doublets and five singlets, while 13C-NMR revealed twelve carbons, which are majorly methyl carbons at δ (ppm) between 120 and 195. All tested samples demonstrated dose-dependent anti-inflammatory activity in carrageenan-induced mice. The isolated compound, i.e. solanine, and chitosan-loaded drugs showed significant inhibitory activity on the cell lines with inhibitory concentration 50 (IC50) values of 8.52, 0.82, and 22.1 µg/mL, respectively on MCF-7 cell line and 4.54, 0.08, and 12.1 µg/mL, respectively, on HMVII cell line, while doxorubicin (adriamycin) positive control, had IC50 values of 0.02 and 0.06 µg/mL, respectively, on MCF-7 and HMVII cancer cells. Selectivity index of solanine was the lowest in the study, hence, it lacks the ability to differentiate between cancerous and normal cell Vero E6 cell lines. Chitosan-loaded drugs quicken early apoptosis and sustained late apoptosis in cells with much improved selective indices. Conclusion: The results obtained from this study further affirmed the use of chitosan nanoparticles as carriers for anticancer drugs.

Pharmacognostic profiles, evaluation of analgesic, anti-inflammatory and anticonvulsant activities of Newbouldia laevis (P. Beauv.) Seem. ex Bureau leaf and root extracts in Wistar rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Newbouldia laevis is a popular medicinal plant whose leaves and roots are used in Nigeria as ethnomedicinal prescriptions for pain, inflammation, convulsion, and epilepsy. These claims have not been scientifically verified prior to this study. AIM OF THE STUDY: To determine pharmacognostic profiles of the leaves and roots and evaluate the analgesic, anti-inflammatory, and anticonvulsant activities of methanol leaf and root extracts in Wistar rats. MATERIAL AND METHODS: The pharmacognostic profiles of the leaves and roots were determined using standard procedures to serve as fingerprints for the plant. The methanol leaf and root extracts of Newbouldia laevis were tested for acute toxicity using the OECD's up and down method at the maximum dose of 2000 mg/kg (orally) in Wistar rats. Analgesic studies were carried out in acetic acid-induced writhing in rats and tail immersion. The anti-inflammatory activity of the extracts was evaluated using carrageenan-induced rat paw-oedema and formalin-induced inflammation in rats' mode. The anticonvulsant activity was determined using strychnine-induced, pentylenetetrazol-induced, and maximal electroshock-induced rat convulsion models. For each of these studies, the extracts doses of 100, 200 and 400 mg/kg were administered to the rats following the oral route. RESULTS: The pharmacognostic profiles showed that the leaves possessed deep-sunken paracytic stomata (5-8-16 mm2; adaxial, 8-11-24 mm2; abaxial epidermis), vein islets (2-4-10 mm2; adaxial), vein terminations (10-14-18 mm2; adaxial), palisade ratio (8.3-12.5-16.4 mm2; adaxial, 2.5-6.8-12.2 mm2; adaxial), covering unicellular trichome (8-14; adaxial), spheroidal calcium oxalate crystals (3-5 µm), and oval-shaped striated starch grain with no hilum (0.5-4.3 µm). The transverse section of the leaf showed the presence of spongy and palisade parenchyma as well as a closed vascular bundle. The root powder showed the presence of brachy sclereid, fibers without lumen, and lignin. All physicochemical parameters fall within the acceptable limits, phytochemical contents showed mainly glycosides, alkaloids, and steroids while acute oral toxicity (LD50) of the parts for 14 days did not produce any toxicity signs or mortality in the rats. The extracts produced dose-dependent (100-400 mg/kg) analgesic involving opioid receptors, anti-inflammatory, and anticonvulsant activities in the rats which were significant (p ≤ 0.05) when compared to the standard drugs. The leaf extract possessed the most potent analgesic and anti-inflammatory effects in the rats, while the most anticonvulsant effects were observed in rats treated with the leaf extract. Both extracts showed elevated levels of protection against strychnine-induced, pentylenetetrazol-induced, and maximal electroshock-induced seizure in rats. CONCLUSION: Our study revealed some pharmacognostic profiles of Newbouldia laevis leaves and roots that are vital for its identification from closely related species often used for adulteration in traditional medicine. The study further showed that the leaf and root extracts of the plant possessed dose-dependent analgesics, anti-inflammatory and anti-convulsant activities in rats, thus, justifying its use for the treatment of these diseases in Nigerian traditional medicine. There is a need to further study its mechanisms of action towards drug discovery.

Silymarin abrogates acrylamide-induced oxidative stress-mediated testicular toxicity via modulation of antioxidant mechanism, DNA damage, endocrine deficit and sperm quality in rats.

Acrylamide (ACR) is a toxic chemical formed in foods processed at high temperature; it is a food-borne toxicant with increasing public health attention due to its carcinogenic, neurotoxic and reproductive toxicities. However, till date, it is unknown whether silymarin (SIL) could attenuate ACR testicular toxicity. Therefore, the present study investigated the effect of SIL on ACR testiculotoxicity in rats. Rats were randomly divided and administered respective agents in Control group, ACR group, SIL group and ACR + SIL group for consecutive 14 days. Rat exposure to ACR resulted in significant reduction in the level of serum testosterone, whereas FSH and LH levels prominently increased compared to control. Acrylamide induced marked decreases in sperm count and sperm motility followed by a considerable increase in sperm abnormality percentage in the ACR-exposed rats in comparison to control. The testicular activities of glutathione peroxidase (GPx), catalase (CAT), and superoxide dismutase (SOD) were significantly diminished, whereas malondialdehyde (MDA) level considerably increased. Additionally, ACR induced marked DNA fragmentation and histopathological lesions compared to control. Interestingly, the co-treatment of SIL with ACR attenuated the altered reproductive indices and restored antioxidant balance and DNA integrity. Overall, SIL prevents ACR-induced testicular reproductive deficits via modulation of antioxidant mechanism in rats.

Elemental Composition and Associated Health Risk of Honey Obtained from Apiary Farms in Southeast Nigeria.

ABSTRACT: This study investigated the levels of lead, selenium, arsenic, iron, manganese, copper, zinc, chromium, cadmium, and nickel in honey and their potential health risks to consumers, using standard protocols. The honey samples were obtained from apiary farms at nine different locations in southeast Nigeria. They were digested at optimal conditions and analyzed using a flame atomic absorption spectrophotometer. Levels of the studied elements in the honey were found to vary relative to the sample source; however, all were below European Commission maximum permissible limits, with the exception of lead, whose level in some samples exceeded the recommended set limit. Estimated daily intakes of the elements via ingestion of the honey were all below the maximum permissible limit set by the European Food Safety Authority, with the exception of arsenic, whose values in some samples slightly exceeded the set limit. For all samples, estimated health risk values for the elements quantified were higher in children than in adults. The hazard quotient for arsenic, hence, the hazard index for the elements, indicated a significant risk (>1) for children for some of the honey samples studied. Arsenic was the major contributor to incremental lifetime cancer risk; its estimated value for children in all the honey samples exceeded the U.S. Environmental Protection Agency (EPA) threshold limit (>1.0 × 10-4); hence, the total cancer risk values for the carcinogenic elements indicated an absolute unacceptable risk level for children based on EPA threshold limit.

Polyphenols isolated from virgin coconut oil attenuate cadmium-induced dyslipidemia and oxidative stress due to their antioxidant properties and potential benefits on cardiovascular risk ratios in rats.

OBJECTIVE: Literature has confirmed the pathogenic role of cadmium (Cd) and its exposure in the induction of dyslipidemia implicated in the development and increasing incidence of cardiovascular diseases. The current study explored whether polyphenolics isolated from virgin coconut oil (VCO) prevent Cd-induced dyslipidemia and investigate the underlying mechanism of action, in rats. MATERIALS AND METHODS: Rats were pretreated with VCO polyphenols (10, 20 and 50 mg/kg body weight; orally) 2 weeks prior to concurrent Cd administration (5 mg/kg) for 5 weeks. Subsequently, serum concentrations of lipid and lipoprotein cholesterol and cardiovascular risk ratios were determined. Hepatic activities of superoxide dismutase (SOD) and catalase (CAT) as well as reduced glutathione (GSH) and malondialdehyde (MDA) contents were analyzed. RESULTS: Sub-chronic Cd administration significantly increased the serum levels of total cholesterol, triglycerides, low density lipoprotein cholesterol and very low density lipoprotein cholesterol while markedly reduced high density lipoprotein cholesterol. Hepatic activities of SOD and CAT as well as GSH content were suppressed by Cd, whereas MDA level was obviously increased. The co-administration of VCO polyphenol with Cd remarkably restored lipid profile and cardiovascular risk ratios and stabilized antioxidant defense systems comparable to control group. CONCLUSION: This is the first study presenting that polyphenols isolated from VCO prevent Cd-induced lipid abnormalities and cardiovascular risk ratios by improving antioxidant defense systems.

Assessment of nephrotoxicity and histopathological lesions of albino rats exposure to DD-force and baygon insecticides / Evaluación de la nefrotoxicidad y lesiones histopatológicas tras la exposición de ratas Albino a los insecticidas DD-Force y Baygon

Although studies suggest adverse effects of pesticides, human exposure to insecticides in homes is increasing and reports on their health effects are limited. The study investigated nephrotoxic effects of organo phosphate and carbamate insecticides, DD-Force and Baygon, in albino rats. Forty-five albino rats divided into groups were exposed to DD-Force (dichlorvos) or Baygon (propoxur) indoor insecticidein wooden boxes in separate exposure duration of 1, 2, 3 and 4 hours/day for 14 consecutive days. Serum and kidney tissue obtained after sacrifice were used to determine markers of renal damage and histopathological analysis, respectively. Exposure of rats to the insecticides showed duration-dependent significant increases (p<0.05) in serum levels of urea, uric acid and creatinine compared to control. However, rats exposed to DD-Force insecticide induced significantly higher levels of urea, uric acid and creatinine compared to Baygon (p<0.05). Histopathological lesions were observed in rats exposed to the insecticides, particularly in the exposure duration of 3 or 4 hours/day. These findings suggest that acute exposure to DD-Force and Baygonis nephrotoxic and may induce renal damage in rats.

Aunque los estudios sugieren efectos adversos de los pesticidas, la exposición humana a los insecticidas en los hogares está aumentando y los informes sobre sus efectos sobre la salud son limitados. Este estudio investigó los efectos nefrotóxicos de los insecticidas órgano fosfato y carbamato, DD-Force y Baygon, en ratas albinas. Cuarenta y cinco ratas albinas divididas en grupos fueron expuestas a DD-Force (diclorvos) o Baygon (propoxur) insecticidas de interior en cajas de madera en una duración de exposición separada de 1, 2, 3 y 4 horas / día durante 14 días consecutivos. Muestras séricas y de tejido renal obtenidas después del sacrificio se utilizaron para determinar los marcadores de daño renal y el análisis histopatológico, respectivamente. La exposición de las ratas a los insecticidas mostró aumentos significativos dependientes de la duración (p<0.05) en los niveles séricos de urea, ácido úrico y creatinina en comparación con el control. Sin embargo, las ratas expuestas al insecticida DD-Force indujeron niveles significativamente más altos de urea, ácido úrico y creatinina en comparación con Baygon (p<0.05). Se observaron lesiones histopatológicas en ratas expuestas a los insecticidas, particularmente en la duración de exposición de 3 o 4 horas/día. Estos hallazgos sugieren que la exposición aguda a DD-Force y Baygonis nephrotóxico y puede inducir daño renal en ratas.