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An extensive phytochemical investigation of the EtOH/H 2 O (7:3) extracts of Sida rhombifolia L. and Sida acuta Burm. f., yielded a previously undescribed ceramide named rhombifoliamide ( 1 ) and a xylitol dimer ( 2 ), naturally isolated here for the first time, as well as the thirteen known compounds viz , oleanolic acid ( 3 ), β -amyrin glucoside ( 4 ), ursolic acid ( 5 ), β -sitosterol glucoside ( 6 ), tiliroside ( 7 ), 1,6-dihydroxyxanthone ( 8 ), a mixture of stigmasterol ( 9 ) and β -sitosterol ( 10 ), cryptolepine ( 11 ), 20-Hydroxyecdysone ( 12 ), ( E )-suberenol ( 13 ), thamnosmonin (1 4 ) and xanthyletin (1 5 ). Their structures were elucidated by the analyses of their spectroscopic and spectrometric data (1 D and 2 D NMR, and HRESI-MS) and by comparison with the previously reported data. The crude extracts, fractions, and some isolated compounds were tested against chloroquine-sensitive (3D7) and chloroquine-resistant (Dd2) Plasmodium falciparum strains. All the tested samples demonstrated moderate and/or significant activities against 3D7 (IC 50 values: 0.18-20.11 µg/mL) and Dd2 (IC 50 values: 0.74-63.09 µg/mL).[Formula: see text].

Ethnopharmacological Relevance: Xylopia staudtii is a medicinal plant which fruits are traditionally used in western Cameroon as a spice in the preparation of soups known for their abdominal cramp relieving properties. Often identified as Xylopia africana, its bark is used in the treatment of dysentery in Mont Cameroun localities. This plant could therefore contain active ingredients against intestinal pathogens, including Shigella spp, which are responsible of the deathly dysenteric diarrhoea., Aim of the Study: This study aims to assess the efficacy of the hydroethanolic extract from Xylopia staudtii bark in immunodepressed mice infected with Shigella flexneri., Materials and Methods: Qualitative detection of compounds in the crude extract was done using UPLC-DAD-(HR) ESI-MS analysis in an attempt to link the activity to the chemical composition. The MIC and the MBC of the extract was determined using broth dilution method. Shigellosis was induced by intraperitoneal administration of Shigella flexneri to immunodepressed mice pretreated with streptomycin. These infected mice were then treated with the extract (100, 200 and 400 mg/kg), and reference substances (ciprofloxacin and saline). During the 9 days of treatment, animal morphology, fecal pathology and deaths were recorded. At the end of the treatment period, blood and organs were collected from any surviving animals for hematological, biochemical and histopathological analyses., Results: The extract was found to be significantly active, with a bactericidal effect against Shigella and a bacteriostatic effect against Escherichia coli. It was able to reduce and stop the faecal pathology caused by the infection in mice, as well as the rate of deaths which was brought to zero (0) in animal treated at 400 mg/kg. The bacteria load in faeces was reduced by 100% in animal treated at 400 mg/kg. Xylopia staudtii extract elicited anti-inflammatory properties by reducing MPO activity and Lcn2 intestinal level. It also prevents damages in the intestinal tissue and the shortening of colon which characterise Shigella infection. The serum level of ASAT, ALAT, bilirubin, urea and creatinine in animals treated with the extract was similar to those of normal animal used in the study. These activities of the plant may be due at least in part to the presence of ent-kauran type diterpens such as kaurenoic acid identified in the extract., Conclusion: These findings support the usage of Xylopia staudtii as an antimicrobial against bacillary dysentery, making this plant a potential candidate for the formulation of an improved standardized traditional medicine., (Copyright © 2021 Elsevier B.V. All rights reserved.)

Background: Plants represent an intricate and innovative source for the discovery of novel therapeutic remedies for the management of infectious diseases. The current study aimed at discovering new inhibitors of Leishmania spp., using anti-leishmanial activity-guided investigation approach of extracts from Diospyros gracilescens Gürke (1911) (Ebenaceae), targeting the extracellular (promastigotes) and intracellular (amastigotes) forms of Leishmania donovani., Methods: The plant extracts were prepared by maceration using H 2 0: EtOH (30:70, v/v) and further fractionated using a bio-guided approach. Different concentrations of D. gracilescens extracts, fractions and isolated compounds were tested in triplicate against L. donovani promastigotes and amastigotes in vitro. The antileishmanial potency and cytotoxicity on RAW 264.7 cells were determined using the resazurin colorimetric assay. The time kill kinetic profile of the most active sample was also investigated. The structures of all compounds were elucidated on the basis of extensive spectroscopic analyses, including 1D and 2D NMR, and HR-ESI-MS and by comparison of their data with those reported in the literature., Results: The hydroethanolic crude extract of D. gracilescens trunk showed the most potent antileishmanial activity (IC 50  = 5.84 μg/mL). Further fractionation of this extract led to four (4) fractions of which, the hexane fraction showed the most potent activity (IC 50  = 0.79 μg/mL), and seven (07) compounds that exhibited moderate potency (IC 50  = 13.69-241.71 μM) against L. donovani. Compound 1-deoxyinositol (7) inhibited the promastigote and amastigote forms of L. donovani with IC 50 values of 241.71 μM and 120 μM respectively and also showed the highest selectivity against L. donovani promastigotes (SI > 5.04). To the best of our knowledge, the antileishmanial activity of this compound is being reported here for the first time. The promising hexane fraction showed significant inhibition of parasites growth at different concentrations, but with no evidence of cidal effect over an exposure period of 120 h., Conclusions: The results obtained indicated that the hydroethanolic extract from the D. gracilescens trunk and the derived hexane fraction have very potent inhibitory effect on cultivated promastigotes and amastigotes of L. donovani parasite. The isolated compounds showed a lesser extent of potency and selectivity. However, further structure-activity-relationship studies of 1-deoxyinositol could lead to more potent and selective hit derivatives of interest for detailed drug discovery program against visceral leishmaniasis.

Phytochemical investigation of the twigs of Garcinia nobilis led to the isolation of a new xanthone, named l-hydroxy-2,5-dimethoxyxanthone (1), together with 15 known compounds (2-16). The structures of the new and known compounds were established by means of spectroscopic methods and by comparison with previously reported data. The structure of compound 1 was confirmed by X-ray diffraction data. Compounds 1-16 were tested for their cytotoxic activity against human cervix carcinoma cell line KB-3-1. Compounds 5 and 11 showed moderate activity while others showed weak biological activity in these cytotoxicity assays. Compounds 4 and 9 were found to be inactive.

Phytochemical investigation of the seeds of Salacia longipes var. camerunensis led to the isolation of four sesquiterpenoid derivatives, salaterpene A (1) (1α,2β,8β-triacetoxy-6β,9β-dibenzoyloxy-4β-hydroxy-dihydro-β-agarofuran), salaterpene B (2) (1α,2β,8β-triacetoxy-9β-benzoyloxy-6β-cinnamoyloxy-4β-hydroxy-dihydro-β-agarofuran), salaterpene C (3) (1α,2β-diacetoxy-6β,9β-dibenzoyloxy-4β-hydroxy-dihydro-β-agarofuran) and salaterpene D (4) (2β-acetoxy-1α,6β-dibenzoyloxy-4β-hydroxy-9β-nicotinoyloxy-dihydro-β-agarofuran) together with two known compounds (5 and 6). The structures of the compounds were established by means of NMR spectroscopy. Compounds 1-4 and 6 were tested in vitro for their antiplasmodial activity against Plasmodium falciparum chloroquine-resistant strain W2. All the tested compounds exhibited a moderate potency with IC50 below 2.7 μM., (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Ethnopharmacological Relevance: Vitex cienkowskii Kotschy & Peyritsch is a deciduous tree, prescribed by Cameroonian traditional healers as one of the most popular plant widely used in many disorders including cardiovascular diseases. The preliminary pharmacological studies carried out on Vitex cienkowskii showed its vasorelaxant activities on guinea-pig aortic rings., Aim of the Study: The present work evaluated the vasorelaxant activity of extract and isolated compounds from Vitex cienkowskii., Materials and Methods: Rat aortic rings were used to evaluate the in vitro vascular effect of the extract. The antioxidant activity was determined by measuring the reduction of the free radical 1,1-diphenyl-1-picryl-hydrazyl (DPPH)., Results: Vitex cienkowskii induced significant relaxation in a concentration- and endothelium-dependent manner (EC(50)=12.12 μg/ml, CH(2)Cl(2)-MeOH, 1:1) and did not produce a vasorelaxant effect on contraction evoked by KCl (60 mM). In order to determine its mode of action, Vitex cienkowskii-induced relaxant effect was evaluated in the presence of indomethacin (10 μM), L-NAME (100 μM), ODQ (1 μM) and SQ22356 (100 μM). Relaxation was significantly blocked by L-NAME and ODQ. These results indicate that Vitex cienkowskii-mediated relaxation is endothelium dependent, probably due to NO release, and the consequent activation of vascular smooth muscle soluble guanylate cyclase (sGC), a signal transduction enzyme that forms the second messenger cGMP. Bio-guided study of Vitex cienkowskii allowed the isolation of the known pentacyclic triterpenoids and a ceramide. It is the first report of salvin A, maslinic acid and a ceramide from Vitex cienkowskii. The activity induced by these compounds indicated that they may be partly responsible for the vasorelaxant effect of the plant extract. A dose of 40 mg/kg of CH(2)Cl(2)-MeOH (1:1) extract administered intravenously induced a decrease of mean arterial pressure but did not affect the heart rate. Moreover the plant extracts were found to be highly active in the DPPH radical scavenging assay., Conclusion: Vitex cienkowskii extract possesses antioxidant property, vasorelaxing, and hypotensive effect linked to the endothelium related factors, where nitric oxide is involved., (Copyright © 2010 Elsevier Ireland Ltd. All rights reserved.)

Phytochemical investigation of the stem bark of Beilschmiedia zenkeri led to the isolation of four new methoxylated flavonoid derivatives, (2S,4R)-5,6,7-trimethoxyflavan-4-ol (1), (2S,4R)-4,5,6,7-tetramethoxyflavan (2), beilschmieflavonoid A (3), and beilschmieflavonoid B (4), together with seven known compounds. The structures of 1-4 were established by spectroscopic methods, and their relative configurations confirmed by X-ray crystallographic and CD analysis. The isolated compounds were evaluated in vitro for their antibacterial activity against three strains of bacteria, Pseudomonas agarici, Bacillus subtilis, and Streptococcus minor, and for their antiplasmodial activity against Plasmodium falciparum, chloroquine-resistant strain W2.

Two pentacyclic triterpenes, 1alpha,3beta-dihydroxybauer-7-en-28-oic acid (1) and 3beta-hydroxybauer-7-en-28-oic acid (2), together with sitosterol-3-beta-O-d-glucopyranoside and stigmasterol have been isolated from the bark of the plant Maesopsis eminii. Their structures have been elucidated by spectroscopic methods. One of the triterpenes (1) is new, and its structure was confirmed by X-ray crystallographic analysis. This new triterpene displayed moderate antibacterial activity against Bacillus subtilis ATCC 6633.