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The cytotoxic effects of Cymbopogon schoenanthus L. aerial part ethanol extract were examined against some cancer cell lines, and HUVEC normal cell lines using MTT assay. The ethanolic extract was prepared by ultrasonic-assisted extraction and analyzed by GC-MS and HPLC. The extract was found to be rich in terpene compounds. The extract proved to be highly selective and effective against breast and prostate cancer cell lines (MDA-MB-435, MCF-7, and DU 145) with IC50 as low as 0.7913 ± 0.14, 12.841 ± 0.21, and 30.51 ± 0.18 µg/ml, respectively. In silico modeling was performed to investigate the binding orientation and affinity of the major identified compounds against Polo-like kinase (PLK1 protein) a cancer molecular target using molecular docking and molecular dynamic whereas eudesm-5-en-11-ol, piperitone, and 2,3-dihydrobenzofuran displayed better binding affinity and stability against PLK1 compared to the reference drug. These findings encourage further in vivo studies to assess the anti-cancer effects of C. schoenanthus extract and its components.

International audience; A total synthesis in four steps of racemic paecilocin A, a natural marine phthalide is reported. The synthetic pathway includes an iodine-magnesium exchange followed by a condensation on an aldehyde and represents a sufficiently flexible approach to allow the synthesis of twelve analogs. The synthesized compounds were investigated for their antibacterial activity against methicillin-sensitive Staphylococcus aureus (MSSA) and methicillin-resistant strain (MRSA). Three analogs were found to have similar or better antibacterial activity than the natural compound on MRSA. (C) 2021 Elsevier Ltd. All rights reserved.

Background/Objectives: Hibiscus sabdariffa L. (H. sabdariffa (HS)) extract has a vascular relaxant effect on isolated rat thoracic aorta, but data on small resistance arteries, which play an important role on the development of hypertension, are still missing. The purposes of this study were (1) to assess the effect on isolated mesenteric arteries (MA) from normotensive (Wistar and Wistar-Kyoto (WKY)) and spontaneous hypertensive rats (SHR), (2) to elucidate the mechanism(s) of action underling the relaxant effect in light of bioactive components. Methods: Vascular effects of HS aqueous fraction (AF) on isolated MA rings, as well as its mechanisms of action, were assessed using the contractility and intracellular microelectrode technique. The patch clamp technique was used to evaluate the effect of HS AF on the L-type calcium current. Extraction and enrichment of AF were carried out using liquid&ndash, liquid extraction, and the yield was analyzed using HPLC. Results: The HS AF induced a concentration-dependent relaxant effect on MA rings of SHR (EC50 = 0.83 &plusmn, 0.08 mg/mL), WKY (EC50 = 0.46 &plusmn, 0.04 mg/mL), and Wistar rats (EC50 = 0.44 &plusmn, 0.08 mg/mL) pre-contracted with phenylephrine (10 &micro, M). In Wistar rats, the HS AF maximum relaxant effect was not modified after endothelium removal or when a guanylate cyclase inhibitor (ODQ, 10 &micro, M) and a selective &beta, 2-adrenergic receptor antagonist (ICI-118551, 1 &micro, M) were incubated with the preparation. Otherwise, it was reduced by 34.57 &plusmn, 10.66% when vascular rings were pre-contracted with an 80 mM [K+] solution (p &lt, 0.001), which suggests an effect on ionic channels. HS AF 2 mg/mL significantly decreased the peak of the L-type calcium current observed in cardiac myocytes by 24.4%. Moreover, though the vasorelaxant effect of HS, AF was reduced by 27% when the nonselective potassium channels blocker (tetraethylammonium (TEA) 20 mM) was added to the bath (p &lt, 0.01). The extract did not induce a membrane hyperpolarization of smooth muscle cells, which might suggest an absence of a direct effect on background potassium current. Conclusion: These results highlight that the antihypertensive effect of HS probably involves a vasorelaxant effect on small resistance arteries, which is endothelium independent. L-type calcium current reduction contributes to this effect. The results could also provide a link between the vasorelaxant effect and the bioactive compounds, especially anthocyanins.

International audience; Aristolochic acids are biologically active and highly toxic secondary metabolites that recently became an important pharmacological tool for in vivo models of acute kidney disorders. Only aristolochic acid I and a mixture of aristolochic acids I and II are currently commercially available. A method based on the strong-ion exchange displacement mode in centrifugal partition chromatography was developed to extract and purify arictolochic acids, naturally present in Aristolochia bracteolata Lam. (Aristolochiaceae). The extraction and purification of aristolochic acids were performed at a flow rate of 2 mL min−1 in the descending mode by using the biphasic solvent system methyl-ter-butylether, acetone, methanol and water (3:1:1:3, v/v/v/v). Trioctylmethylammonium chloride (Aliquat 336®) was used as the anion exchanger in the organic stationary phase and sodium iodide as the displacer in the aqueous mobile phase. From 5 g of crude extract of A. bracteolata, 45.5 mg, 77.2 mg and 35.1 mg of aristolochic acids I, II and IIIa were obtained respectively with purities greater than 95%.

Medicinal plants contain physiologically active principles that over the years had been exploited in traditional medicine for the treatment of various ailments. The present study was undertaken to investigate the effects of ethanolic extract of Hibiscus sabdariffa calyx on rat reproductive hormones. The effects on the basal levels of estradiol, testosterone, prolactin and follicle stimulating hormone were conducted in experimental animals. H. sabdariffa calyx extract at a dose of 250 mg/kg produced minor effects on rat reproductive hormones, namely testosterone and estradiol while no change was observed on both prolactin and follicle stimulating hormone levels. Moreover, no histological changes were detected on both testes and ovaries of the experimental animals after 28 days of administration. It can be concluded that H. sabdariffa calyx extract at a dose of 250 mg/kg caused mild effects on rat reproductive hormones. Key words: Estrogenic effect, reproductive hormones, Hibiscus sabdariffa extract.

Background: Medicinal plants contain physiologically active principles that over the years have been exploited in traditional medicine for the treatment of various ailments. Objectives and Methods: This study aimed to investigate the effects of the methanolic extract of Pausinystalia yohimbe bark (5 mg/ml) on isolated rabbit aortic strip and rat uterus. Results: methanolic extract of P. yohimbe bark (5 mg/ml) produced relaxation of the phenylephrine precontracted-rabbit aortic strip. This relaxation may be resulted through nitric oxide (NO), since the pretreatment of the isolated rabbit aortic strip with methylene blue inhibited the NO-mediated relaxation. Moreover, the extract exhibited relaxation of rat uterine muscles, which appeared to be not mediated by activation of β2-adrenoceptors and/or H2 receptors, since the relaxant effect continued even after the pretreatment of the tissue with propranolol and ranitidine respectively. Conclusion: The obtained results revealed that methanolic extract of P. yohimbe bark caused relaxation of both isolated rat uterus and rabbit aortic strip through facilitating the role of endogenous compounds such as NO.

Background: Pausinystalia yohimbe (L.) is a member of the family Rubiaceae. It is a valuable medicinal tree, distributed in evergreen closed-canopy forests in West Africa. It is traditionally used for treatment of erectile dysfunction and diabetes. Objective: This was an attempt to evaluate the effects of methanolic extract of P. yohimbe bark on blood glucose level in normal fasting rats. Methods: Different doses of methanolic extract of P. yohimbe bark (5, 10, 20, 40 and 80 mg/kg/mL) were orally administered to normal fasting rats to assess their effects on blood glucose levels. Results: The methanolic extract of P. yohimbe bark in different concentrations (5, 10, 20, 40 and 80 mg/kg/mL) when administered to normal fasting rats, only a considerable reduction (26.57 mg/dL) was produced by the dose of 20 mg/kg/mL. Conclusion and Recommendation: Although P. yohimbe has long been reported to regulate blood glucose levels; such effect is unclear and remains requiring further studies.

Background Aristolochic Acids (AAs) are major components of plants in Aristolochia and have been found to be nephrotoxic, carcinogenic and mutagenic. Herein reported are the isolation, identification and quantity determination methods of Aristolochic Acid-I (AA-I) and Aristolochic Acid-II (AA-II) toxic compounds of Aristolochia bracteolata indigenous to Central Sudan and medicinally used in diverse biological functions including analgesic and diuretic effects, treatment of tumors, malaria and/or fevers. Methods and results AAs mixture was extracted with methanol from the defatted material of Aristolochia bracteolata whole plant at room temperature and was isolated from the aqueous methanol extract by chloroform. Moreover, Silica-gel column chromatography and Preparative Thin Layer Chromatography (PTLC) using chloroform/methanol gradient mixtures were used to isolate AAs mixtures as a yellow crystalline solid. A preliminary detection of AAs was made by Thin Layer Chromatography (silica-gel, chloroform: methanol (6:1)). The Rf value of the acids mixture was 0.43-0.46. The presence of AAs in plant sample was confirmed by High Performance Liquid Chromatography/Ultraviolet (HPLC/UV) analysis using 1% acetic acid and methanol (40:60) as mobile phase and maximum absorption wave length of 250 nm. Quantitative determination of AA-II (49.03 g/kg) and AA-I (12.98 g/kg) was also achieved by HPLC/UV. Recommendation It is recommended that the use of Aristolochia bracteolata as a medicinal plant should be extremely limited or strictly prohibited. The chromatograms obtained in this study can serve as fingerprints to identify AAs in plant samples.

Background Diabetes mellitus is a heterogeneous group of disorders characterized by abnormalities of carbohydrate, protein and lipid metabolism. Type 1 diabetes mellitus is an autoimmune disease caused by destruction of pancreatic beta cells and characterized by defect in insulin secretion while type 2 diabetes mellitus results from abnormalities in insulin secretion and/or insulin action or both. Objectives The present study was conducted to investigate the clinical hypoglycemic effects of Allium cepa in type 1 and type 2 diabetic patients. Results In assessment of hypoglycaemic activity of Allium cepa in type 1 and type 2 diabetic patients, ingestion of crude Allium cepa (100 g) caused a considerable reduction in fasting blood glucose levels by about 89 mg/dl in relation to insulin (145 mg/dl) in type 1 diabetic patients and it reduced fasting blood glucose levels by 40 mg/dl, compared to glibenclamide (81 mg/dl) in type 2 diabetic patients, 4 hours later. The same dose of crude Allium cepa produced a significant reduction in the induced hyperglycemia (GTT) by about 120 mg/dl compared to water (77 mg/dl) and insulin (153 mg/dl) in type 1 diabetic patients and considerably reduced GTT by 159 mg/dl in relation to water (55 mg/dl) and glibenclamide (114 mg/dl) in type 2 diabetic patients, after 4 hours. Conclusion It was evident that, crude Allium cepa produced hypoglycemic effects, thus it could be used as a dietary supplement in management of type 1 and/or type 2 diabetes mellitus.

Ten plants indigenous to Sudan and of common use in Sudanese folk-medicine, were examined in vitro for antimalarial activity against schizonts maturation of Plasmodium falciparum, the major human malaria parasite. All plant samples displayed various antiplasmodial activity. Three plant extracts caused 100% inhibition of the parasite growth at concentrations of plant material ≤ 500 ug/ml. The two most active extracts that produced 100% inhibition of the parasite growth at concentration of plant material ≥ 50 μg/ml were obtained from the seeds of Nigella sativa and the whole plant of Aristolochia bracteolata. The ten plants were phytochemically screened for their active constituents. The two most active plants showed the presence of sterols, alkaloids and tannins.

Eumycetoma is a debilitating chronic inflammatory fungal infection that exists worldwide but it is endemic in many tropical and subtropical regions. The major causative organism is the fungus Madurella mycetomatis. The current treatment of eumycetoma is suboptimal and characterized by low cure rate and high recurrence rates. Hence, an alternative therapy is needed to address this. Here we determined the antifungal activity of seven Sudanese medicinal plant species against Madurella mycetomatis. Of these, only three species; Boswellia papyrifera, Acacia nubica and Nigella sativa, showed some antifungal activity against M. mycetomatis and were further studied. Crude methanol, hexane and defatted methanol extracts of these species were tested for their antifungal activity. B. papyrifera had the highest antifungal activity (MIC50 of 1 ug/ml) and it was further fractionated. The crude methanol and the soluble ethyl acetate fractions of B. papyrifera showed some antifungal activity. The Gas-Liquid-Chromatography hybrid Mass-Spectrophotometer analysis of these two fractions showed the existence of beta-amyrin, beta-amyrone, beta-Sitosterol and stigmatriene. Stigmatriene had the best antifungal activity, compared to other three phytoconstituents, with an MIC-50 of 32 μg/ml. Although the antifungal activity of the identified phytoconstituents was only limited, the antifungal activity of the complete extracts is more promising, indicating synergism. Furthermore these plant extracts are also known to have anti-inflammatory activity and can stimulate wound-healing; characteristics which might also be of great value in the development of novel therapeutic drugs for this chronic inflammatory disease. Therefore further exploration of these plant species in the treatment of mycetoma is encouraging., Author Summary This study was an attempt to discover new safe therapeutic modalities of natural origin for the treatment eumycetoma. The methanolic extracts of seven selected local plants were screened for their antifungal activity. All seven plant extracts were able to inhibit Madurella mycetomatis growth at a concentration of 50 μg/ml or less. Three plant species out of the seven managed to inhibit the growth of Madurella mycetomatis at a concentration as low as 781 μg/ml; these were: Boswellia papyrifera, Acacia nubica and Nigella sativa. Further analysis of B. Papyrifera, using Gas-Liquid-Chromatography hybrid Mass-Spectrophotometer (GC-MS); showed the occurrence of four phytoconstituents, triterpenoid in nature and these were Beta-amyrin, Beta-amyrone, Beta-Sitosterol and Stigmatriene. Stigmatriene was the best to show anti-mycetoma activity at an MIC equal to 32 μg/ml. This MIC is much higher than the MIC of the whole extract (8 μg/ml), indicating that other compounds or a combination of compounds has a better ability to inhibit M. mycetomatis growth. These results are promising and further detailed studies are highly recommended.