Diterpenoids with thioredoxin reductase inhibitory activities from Jatropha multifida.

Chemical investigation of the Jatropha multifida has led to the isolation of nine diterpenoids (1-9), including a new jatromulone A, four podocarpane diterpenoids (2-5), two lathyrane-type diterpenoids (6 and 7) and two dinorditerpenoids (8 and 9). Their structures were elucidated by spectroscopic analysis, and the absolute configurations of 1 were determined by CD analysis. All of the diterpenoids were screened for inhibitory activity against thioredoxin reductase (TrxR), which is a potential target for cancer chemotherapy with redox balance and antioxidant functions. Compounds 6 and 7 exhibited stronger activity (IC50: 23.4 and 10.6 μM, respectively) than the positive control, curcumin (IC50 = 25.0 μM). Compounds 2-9 were isolated from J. multifida for the first time

Antiparasitic Constituents of Beilschmiedia louisii and Beilschmiedia obscura and Some Semisynthetic Derivatives (Lauraceae)

Waleguele CC, Mba’ning BM, Awantu AF, et al. Antiparasitic Constituents of Beilschmiedia louisii and Beilschmiedia obscura and Some Semisynthetic Derivatives (Lauraceae). Molecules. 2020;25(12): 2862.The MeOH/CH2Cl2 (1:1) extracts of the roots and leaves of Beilschmiedia louisii and B. obscura showed potent antitrypanosomal activity during preliminary screening on Trypanosoma brucei brucei. Phytochemical investigation of these extracts led to the isolation of a mixture of two new endiandric acid derivatives beilschmiedol B (1) and beilschmiedol C (2), and one new phenylalkene obscurene A (3) together with twelve known compounds (4–15). In addition, four new derivatives (11a–11d) were synthesized from compound 11. Their structures were elucidated based on their NMR and MS data. Compounds 5, 6, and 7 were isolated for the first time from the Beilschmiedia genus. Additionally, the NMR data of compound 4 are given here for the first time. The isolates were evaluated for their antitrypanosomal and antimalarial activities against Tb brucei and the Plasmodium falciparum chloroquine-resistant strain Pf3D7 in vitro, respectively. From the tested compounds, the mixture of new compounds 1 and 2 exhibited the most potent antitrypanosomal activity in vitro with IC50 value of 4.91 μM

Antiplasmodial and cytotoxic activities of flavonoids and arylbenzofuran derivatives from Morus mesozygia

Morus mesozygia Stapf (Moraceae) is a plant found in many regions and used in treating many diseases including malaria and fever. Fractionation of the methanolic extract of its stem bark, using various chromatographic methods has led to the isolation and identification of 3 flavonoids: artocarpesin, artochamin C and kushenol E. And 4 arylbenzofuran derivatives: moracin M, moracin C, moracin L and mulberofuran F. The methanolic extract and the seven isolated compounds were tested for antiplasmodial activity against the chloroquine-resistant FcB1 Plasmodium falciparum strain and cytotoxicity on MCF-7 human breast cancer cells. Relating to the antiplasmodial activity, it was found that all compounds were active against the FcB1 strain of Plasmodium with artocarpesin, koushenol E and mulberrofuran F showing particular potency (with the median inhibitory concentrations IC50 = 2.5-2.6 μg/ml). Cytotoxicity tests performed on MCF-7 cells revealed all the IC50 varying from <1.0 to 5.0 ± 0.6 μg/mL. A structure – activity relationship is discussed

Cytotoxic and Antiplasmodial Xanthones from Pentadesma butyracea

Four new xanthones, butyraxanthones A-D (1-4), were isolated from the stem bark of Pentadesma butyracea, together with six known xanthones (5-10) and a triterpenoid (lupeol). The structures of 1-4 were established by spectroscopic methods. Compounds 1-10 were tested in vitro for antiplasmodial activity against a Plasmodium falciparum chloroquine-resistant strain and for cytotoxicity against a human breast cancer cell line (MCF-7). Nearly all of these xanthones exhibited good antiplasmodial activity, and some of them also demonstrated potent cytotoxicity

Effects of the aqueous and hexane extracts of Mondia whitei on the sexual behaviour and some fertility parameters of sexually inexperienced male rats

The effects of Mondia whitei Hook (Skeels) were studied on the sexual behaviour and some fertility parameters of sexually inexperienced male rats. Animals were orally administered 100 mg/kg and 500 mg/kg of body weight (b.w) of either the aqueous or the hexane extracts of Mondia whitei whilst the control group received 10 mL/kg b.w of 0.3% Tween 80 once/day for 14 days. Their sexual behaviour was monitored on days 0, 1, 7 and 14 days of treatment and 14 days post-treatment. Some fertility parameters (index libido, quantal pregnancy, fertility index) of the treated rat were evaluated on day 13 of treatment by pairing it overnight with two proestrus females. Results showed that Mondia whitei extracts significantly (p0.05) on intromission, ejaculation and erection. The fertility of the animals remained unaffected. It's concluded that Mondia whitei had sexual enhancement of the sexually inexperienced male rats. Keywords: Mondia whitei; sexual behaviour; inexperienced male rats The African Journal of Traditional, Complementary and Alternative Medicines Vol. 4 (1) 2007: pp. 37-4

Procerenone: a Fatty Acid Triterpenoid from the Fruit Pericarp of Omphalocarpum procerum (Sapotaceae)

Phytochemical investigation of a dichloromethane-methanol (1:1) extract of the fruit pericarp of Omphalocarpum procerum which exhibited antiplasmodial activity during preliminary screening led to the isolation of the new fatty ester triterpenoid 3β-hexadecanoyloxy-28-hydroxyolean-12-en-11-one (1), together with five known compounds 2-6. The structure of the new compound as well as those of the known compounds was established by means of spectroscopic methods and by comparison with previously reported data. Compounds 1- 4 were evaluated in-vitro for their cytotoxicity against L6 cell lines and antiprotozoal activities against Plasmodium falciparum, Leishmania donovani, Trypanosoma brucei rhodesiense and Trypanosoma cruzi (species responsible for human malaria, visceral leishmaniasis, African trypanosomiasis and Chagas disease, respectively). The tested compounds showed weak to moderate antiprotozoal activity and, no significant effect was detected regarding their cytotoxic potency

Synthesis, Urease Inhibition and Molecular Modelling Studies of Novel Derivatives of the Naturally Occurring β-Amyrenone

Abstract Urease enzyme (UE) has been reported to be a potent virulence factor for Helicobacter pylori (HP) bacteria indicated to be responsible for various gastrointestinal diseases. Therefore, the spread of HP, currently regarded by the World Health Organization as a class 1 carcinogen, could be better controlled by targeting UE. It is in this line that we have synthesized three new derivatives (2–4) of the naturally occurring olean-12-en-3-one (1), which was previously isolated from the figs of Ficus vallis-choudae Delile (Moraceae). Among the synthesized compounds, 3 and 4 contain an indole moiety. Their structures were unambiguously assigned by spectroscopic and spectrometric techniques (1D-NMR, 2D-NMR and MS). The starting material and the synthesized compounds were screened for UE inhibition activity, and showed significant activities with IC50 values ranging from 14.5 to 24.6 μM, with compound (1) being the most potent as compared to the positive control thiourea (IC50 = 21.6 μM). Amongst the synthetic derivatives, compound 4 was the most potent (IC50 = 17.9 μM), while the others showed activities close to that of the control. In addition, molecular docking study of target compounds 2–4 was performed in an attempt to explore their binding mode for the design of more potent UE inhibitors. Graphical Abstrac