A lupeol derivative and other isolates with antiplasmodial activity from the stem root of Rauvolfia mannii Stapf. (Apocynaceae).

Rauvolfia mannii is a plant from western and eastern areas of African continent and is widely used in folk medicine for the treatment of various diseases including malaria. Herein, one previously undescribed acylated triterpene (1), together with five already published natural products (2-6) were removed from its roots. The chemical structures of these compounds were determined by spectroscopic and spectrometric means (NMR, HRESIMS, IR and UV). In addition to the isolated triterpenoids, components 5 and 6 are also newly reported from the genus Rauvolfia. Moreover, some constituents were further tested against the chloroquine-sensitive strain of P. falciparum (3D7). It has been found that 3 and 4 showed a moderate antiplasmodial activity with IC50 values of 46.25 and 39.79 µM respectively.

Antidiabetic and Antiradical Effects of Garcinia kola Seeds in Dexamethasone-Induced Hyperglycemic Rats.

Background: In traditional medicine, the maceration of seeds of Garcinia kola (GK) is used to treat various diseases including diabetes. In traditional pharmacopoeia, GK seeds are used to strengthen the immune system and as a stimulant and aphrodisiac. Aims: This study aimed to evaluate the antidiabetic free radical scavenging effects of the hydroalcoholic extract of GK seeds (HAEGS) in a dexamethasone-induced hyperglycemic (DexIH) rat model. Settings and Design: This study was an interventional study. Subjects and Methods: Here using in vivo model, we assessed some pharmacological properties of HAEGS in DexIH rat. Hypoglycemia, antihyperglycemia, spasmolytic and laxative activities were also evaluated in DexIH. In vitro study assessed antiradical activity. The HAEGS was obtained by decoction introducing 250 g with water-ethanol mixture (30:70). The plant extract was administered to the animals at doses of 50 (GK50) and 100 (GK100) mg/kg body weight. All animal experiments were in accordance with ARRIVE guidelines and were performed in accordance with the scientific procedures of UK Animals. Antiradical activity of GK was assessed in vitro by inhibition of the activity of 2,2-diphenyl-1-picrylhydrazyl. Statistical Analysis Used: Statistical analysis was performed using GraphPad Prism 5.03 software, and P values less than 0.05 were considered statistically significant. Results: At doses 50 and 100 mg/kg, GK significantly (P < 0.001) regulated DexIH after two weeks of treatment compared to the normoglycemic control and hyperglycemic rats. The extract at both doses significantly (P < 0.001) inhibited the spasmolytic activity in both normoglycemic and hyperglycemic rats compared to Imodium®. In rats DexIH rats, only dose 100 mg/kg significantly (P < 0.05) increased laxative effects when compared to the negative control. In vitro antiradical activity of GK revealed vitamin C-like antiradical activity. Conclusions: This study justifies the traditional use of GK seeds as an antidiabetic.

Glycosides of polygalacic acid from the stem barks of Piper guineense Schum and Thonn.

In a continuation of our study on constituents of P. guineense now focusing on the search for saponins, phytochemical investigation of the n-BuOH fraction of P. guineense stem bark led to the isolation of three previously undescribed triterpenoid saponins, named guineenosides A─C (1─3). Their structures were established on the basis of extensive analysis of 1D and 2D NMR (1H, 13C NMR, DEPT, COSY, TOCSY, NOESY, HSQC, HSQC-TOCSY and HMBC) and HRESIMS experiments, and by chemical evidence as 3-O-{α-l-rhamnopyranosyl-(1 â†’ 3)-ß-d-xylopyranosyl-(1 â†’ 2)-α-l-arabinopyranosyl-(1 â†’ 4)-α-l-rhamnopyranosyl-(1 â†’ 3)-[α-l-arabinofuranosyl-(1 â†’ 4)]-α-l-rhamnopyranosyl-(1 â†’ 3)-ß-d-fucopyranosyl} polygalacic acid 28-O-α-l-rhamnopyranosyl-(1 â†’ 4)-α-l-rhamnopyranosyl-(1 â†’ 3)-ß-d-xylopyranosyl ester (1), 3-O-{α-l-rhamnopyranosyl-(1 â†’ 3)-ß-d-xylopyranosyl-(1 â†’ 2)-α-l-arabinopyranosyl-(1 â†’ 4)-α-l-rhamnopyranosyl-(1 â†’ 3)-[α-l-arabinofuranosyl-(1 â†’ 4)]-α-l-rhamnopyranosyl-(1 â†’ 3)-ß-d-fucopyranosyl} polygalacic acid 28-O-ß-d-glucopyranosyl-(1 â†’ 3)-α-l-rhamnopyranosyl-(1 â†’ 4)-α-l-rhamnopyranosyl-(1 â†’ 3)-ß-d-xylopyranosyl ester (2), and 3-O-{α-l-rhamnopyranosyl-(1 â†’ 2)-ß-d-xylopyranosyl-(1 â†’ 3)-ß-d-fucopyranosyl} polygalacic acid 28-O-[α-l-rhamnopyranosyl-(1 â†’ 4)-α-l-rhamnopyranosyl-(1 â†’ 3)-ß-d-xylopyranosyl ester (3). This is the first report of triterpenoid saponins from P. guineense.

Chemical constituents of the leaves of Anthonotha macrophylla (Leguminosae).

The present study deals with the isolation and the characterization of the chemical constituents from the leaves of Anthonotha macrophylla (Leguminosae). Using various chromatographic techniques (TLC, CC, HPLC), the methanolic extract of the leaves of Anthonotha macrophylla yielded one new alkaloid (1) as well as six known compounds amongst which an alkane (2), isolated for the first time from a natural product, an ester of fatty acid (3), two isocoumarines (4-5), a sterol (6) and a disaccharide (7). Their structures were elucidated using spectroscopic technics including extensive 1-D and 2-D NMR, HR-SM experiments.

A new flavanolignan and a new alkane from the Stem bark of Newtonia griffoniana.

Two new compounds a flavanolignan (1), and an alkane (2) along with four known compounds including two fatty acid esters (3-4) and two isocoumarins (5-6) were isolated from the methanolic extract of the stem bark of Newtonia griffoniana. Their structures were elucidated using spectroscopic methods including extensive 1-D and 2-D NMR experiments.

Newtonoate as an active principle of Newtonia griffoniana for anxiolytic activity in Swiss mice.

BACKGROUND: Newtonia griffoniana (Mimosaceae) is a Central African rain forest tree, whose bark extracts are used in Cameroonian folk medicine for the treatment of anxiety and sleep disorders. METHODS: We evaluated the anxiolytic effects of N. griffoniana stem bark methanol extract and its major isolated constituent 2,3,4-trihydroxybutylpentatriacontanoate (newtonoate) on the elevated plus maze. RESULTS: Significant increases in the percentage of entries into open arms were induced by both N. griffoniana extract (100 and 150 mg/kg BW; p<0.01) and newtonoate (doses of 3 and 15 mg/kg BW; p<0.05). Conversely, decreases in the percentage of entries into closed arms were observed at the same doses. In addition, N. griffoniana methanol extract (100 mg/kg) and the isolated newtonoate (30 mg/kg) induced significant (p<0.01 and p<0.05, respectively) increases in the time spent in the open arms, while inducing a decrease in the time spent in the closed arms. Newtonoate treatment also decreased head dipping number at doses of 3 and 15 mg/kg, while N. griffoniana methanol extract induced the same effect at 200 mg/kg. CONCLUSIONS: These results suggest that N. griffoniana bark extract has anxiolytic properties, which justify its use in folk medicine. Such effects are at least partly mediated by newtonoate.