Antileishmanial anthraquinones from the rhyzomes of Rumex abyssinicus Jacq (Polygonaceae).

Phytochemical investigation of the rhyzomes of Rumex abyssinicus (Polygonaceae) afforded six anthraquinones viz chrysophanol (1), physcion (2), emodin (3), mixture of physcion-8-O-ß,D-glucopyranoside (4) and chrypsophanol-8-O-ß,D-glucopyranoside (5), and emodin-8-O-ß,D-glucopyranoside (6). All the compounds were characterised and identified by comparison of their MS and NMR data with available literature data. The isolated compounds were evaluated for their antileishmanial activity. Emodin (3) was the most active compounds with IC50 13.82 and 0.26 µg/mL against Leishmania donovani amastigotes and promastigotes, respectively. Emodin-8-O-ß,D-glucopyranoside (6) also showed a moderate activity with IC50 27.53 and 37.08 µg/mL. This is the first report of antileishmanial compounds from R. abyssinicus and the antileishmanial activities of compounds 2, 4, 5 and 6 are here reported for the first time.

In Vitro Cercaricidal and Schistosomicidal Activities of the Raffia Wine and Hydroethanolic Extracts of Pedilanthus tithymaloides Linn (Poit). Stem Barks.

Schistosomiasis control remains a public health concern, and there is a need to evaluate new strategies for targeting larval and adult stages of the parasite. As Pedilanthus tithymaloides is empirically used to treat schistosomiasis, it becomes essential to know its effective action scientifically. This study assessed the cercaricidal and schistosomicidal activity of P. tithymaloides stem barks raffia wine extract (RwPt) and hydroethanolic extract (HePt). Different concentrations of these extracts were tested against cercariae (31.25-1000 µg/mL) and adult worms (62.5-2000 µg/mL) of Schistosoma mansoni. Niclosamide-olamine 5% (1 µg/mL) and praziquantel (10 µg/mL) were used as pharmacological controls. Cercariae viability was determined every 30 min for 180 min, and adult worms' motor activity and viability after 24 and 48 h incubation. In addition, cytotoxicity and phytochemical analysis were performed. HePt was lethal to cercariae and adult worms with LC50 of 73.91 µg/mL after 60 min of incubation and 731.17 µg/mL after 48 h of incubation, respectively. Furthermore, a significant reduction of 94.44% in motor activity was observed in surviving worms at the concentration of 2000 µg/mL. RwPt was less effective on S. mansoni cercariae with an LC50 of 617.86 µg/mL after 180 min and on adult worms with a mortality rate of 9.83% at 2000 µg/mL for 48 h incubation. Both extracts showed a weak cytotoxicity profile with an IC50 of 983.50 µg/mL for HePt and more than 1000 µg/mL for RwPt. The LC-MS analysis of HePt allowed the detection of two annotated diterpenoids. Based on the selectivity index, the hydroethanolic extract of P. tithymaloides stem barks disclosed an intense cercaricidal activity and a moderate schistosomicidal effect with low cytotoxicity. These findings may support the potential use of Pedilanthus tithymaloides as a natural product or a source of natural-derived compounds for interrupting schistosomiasis transmission.

A new isoquinoline and ceramide from the stem barks of Discoglypremna caloneura (Pax) Prain (Euphorbiaceae) with antiproteinase and cytotoxic activities.

Two new compounds, an isoquinoline (1) and caloneuramide (2), a ceramide were isolated from the stem bark of Discoglypremna caloneura together with seven known compounds namely aurantiamide acetate (3), acetylaleuritolic acid (4), 3α-hydroxylaleuritolic acid 2α-p-hydroxybenzoate (5), mixture of stigmasterol (6) and ß-sitosterol (7), mixture of 7-oxo-stigmasterol (8) and 7-oxo-ß-sitosterol (9). Their structures were determined based on data from literature and spectroscopic methods. Derivatization reactions on the isoquinoline led to two new compounds, the methylated (10) and acetylated (11) derivatives. Some compounds and extracts were evaluated for their cytotoxic and antiproteinase activity. Antiproteinase effect of compounds 1, 10 and 11 exhibited IC50 values of 10.77, 1.19 and 3.61 µg/mL respectively; significantly low compared to the standard drug, acetyl salicylic acid (IC50 = 20.28 µg/mL). Ethyl acetate and methanol extract exhibited moderate cytotoxicity activity on Chang liver cells with CC50 values of 167.90 ± 2.20 and 106.30 ± 2.03 µg/mL compared to the reference drug cucurmin (CC50 = 11.05 ± 1.04 µg/mL).

Antileishmanial activity of long chain alkyl benzene and other constituents from seeds of Sesamum indicum. L (Pedaliaceae).

The methanolic extract of the waste seeds of Sesamum indicum L. (Pedaliaceae) was subjected to chromatographic fractionation; it led to the isolation of an alkyl benzene identified as 1,3-bis (pentadecyl)benzene (1) along with three known fatty acids: oleic acid (2), linoleic acid (3), and palmitic acid (4); one monosaturated cardanol, 3-pentadecylphenol (5) and two phytosteroids identified as sitostanol (6) and campestanol (7). The structures of these compounds were elucidated by chemical and spectroscopic analyses. Compounds 1, 5 and 6 were evaluated against protozoan parasites. Compound 1 moderately inhibited the promastigote form of Leishmania donovani LG13 with IC50 equal to 16.9 µM.

Pharmacological evidence of Vitex thyrsiflora, Entandrophragma cylindricum, and Anonidium mannii used for the management of inflammation in Cameroon.

Background Inflammation is the most common health problem faced in life relating to a vast number of diseases. The present study evaluated the pharmacological effect of three plants (Vitex thyrsiflora, Entandrophragma cylindricum, and Anonidium mannii) commonly used in the Cameroon pharmacopeia for the management of inflammatory response. Methods The pharmacological effect was characterized by the antioxidant capacity, anti-inflammatory, analgesic, and antipyretic properties of the ethanol extracts of the three plants. Antioxidant capacity was determined using total phenolic content, total flavonoid content, hydrogen peroxide, ferric reducing antioxidant power (FRAP), 2,2-diphenyl-1-picrylhydrazyl (DPPH), and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonate) (ABTS) radical scavenging assays. Anti-inflammatory activity was evaluated in vitro by protein denaturation and hypotonic-induced hemolysis methods and in vivo by carrageenan paw edema method. Analgesic and antipyretic activities were studied in vivo using acetic acid-induced writhing and brewer's yeast-induced hyperpyrexia models. Results All selected extracts showed high phenolic (15.93-64.45 mgCAE/g) and flavonoid (336.03-1053.48 mgCAE/g) contents and high ferric reducing power (288.75-364.91 mgCAE/g). These extracts exhibited good DPPH (IC50 = 0.30-1.65 µg/mL), ABTS (IC50 = 0.52-1.90 µg/mL), and H2O2 (IC50 = 1.40-3.55 µg/mL) radical scavenging activities. All extracts inhibited protein denaturation (6.79-82.27%) and protected the erythrocyte membrane from lysis induced by hypotonic solution (18.90-88.00%). The extracts significantly reduced dose-dependent paw edema (p < 0.05), fever, and abdominal writhing (p < 0.001) especially at 400 mg/kg. Conclusions All extracts exhibited interesting antioxidant properties, as well as significant anti-inflammatory, analgesic, and antipyretic effects.