Bioactive abietenolide diterpenes from Suregada procera.

The phytochemical investigation of the leaves and the roots of Suregada procera afforded the new ent-abietane diterpenoid sureproceriolide A (1) along with the known secondary metabolites 8,14β:11,12α-diepoxy-13(15)-abietane-16,12-olid (2), jolkinolide A (3), jolkinolide E (4), ent-pimara-8(14),15-dien-19-oic acid (5), sitosterol (6), oleana-9(11):12-dien-3β-ol (7), and oleic acid (8). Their structures were elucidated by NMR spectroscopic and mass spectrometric analyses, and the structure of jolkinolide A (3) was confirmed by single-crystal X-ray diffraction analysis. Sureproceriolide A (1) showed modest activity against the Gram-positive bacterium Staphylococcus lugdunensis (MIC = 31.

Antiplasmodial and antimicrobial activities of e-abietane diterpenoids from the roots of .

The root extract of Baill. afforded six previously described -abietane diterpenoids, namely 7-oxo--abieta-5(6),8(14),13(15)-trien-16,12-olide (), mangiolide (), 8,14:11,12-diepoxy-13(15)-abietane-16,12-olide (), 7,11,12-trihydroxy--abieta-8(14),13(15)-diene-16,12-olide (), 8α,14-dihydro-7-oxo-jolkinolide E (), jolkinolide A (), together with 3-sitosterol (), scopoletin () and vanillin (). Their structures were deduced through 1D and 2D NMR spectroscopic techniques, and HRESIMS, as well as by comparison of the NMR data with those reported in the literature.

Strategies for improving hydrolytic efficiency of crude multienzyme extracts in mushroom processing.

The current study investigated and optimized key process parameters affecting mushroom hydrolysis with crude enzymatic extract. The crude enzyme was prepared by solid-state fermentation of pineapple peels using . The reaction parameters viz.

A new gnidiflavanone-flavonol dimer and other constituents from .

A new 3,8''-flavanone-flavonol dimer gnidiflavanone-flavonol () and 10 known compounds (-), including four rare primula-type flavones -, were isolated from the roots of . Compounds - and were reported for the first time from the plant family Thymelaeceae. Structures of the isolated compounds were established by spectroscopic data, including 1D and 2D NMR (COSY, HMBC, HSQC and ROESY) and mass spectrometry, as well as by the comparison with literature data.

Selective Interactions of -Methylated Flavonoid Natural Products with Human Monoamine Oxidase-A and -B.

A set of structurally related -methylated flavonoid natural products isolated from (), ( and ), (), (), and () plant species were characterized for their interaction with human monoamine oxidases (MAO-A and -B) in vitro. Compounds , , and showed selective inhibition of MAO-A, while and showed selective inhibition of MAO-B. Compound showed ~2-fold selectivity towards inhibition of MAO-A.

Synthesis of a pyrrolidine derivative of a carvotacetone and monoterpenes for anti-methicillin-resistant and anti-cryptococcal properties.

Monoterpene derivatives are of great biological relevance in the pharmaceutical industry. In the present study, pyrrolidine derivative of a carvotacetone, 3-benzylcarvotacetone (), and selected monoterpenes (3-hydroxy-2-isopropyl-5-methyl--benzoquinone () and piperitol ()) were prepared to provide ()-1-(4-(benzyloxy)-5-isopropyl-2-methylcyclohexa-1,3-dien-1-yl)-pyrrolidine (), 2-isopropyl-5-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl acetate (), 3-hydroxypiperitone () and carvacrol (). Structure of was determined based on NMR and HRMS spectral data.

Synthesis, structural assignments and antiinfective activities of 3--benzyl-carvotacetone and 3-hydroxy-2-isopropyl-5-methyl--benzoquinone.

In an attempt to synthesize carvotacetone analogues, new 3--benzyl-carvotacetone ( and previously reported 3-hydroxy-2-isopropyl-5-methyl--benzoquinone () were synthesized from piperitone (). In this work, we describe the synthesis of and other analogues from . Luche reduction of to -piperitol (, followed by benzylation yielded 3--benzyl-piperitol ().

Cytotoxicity of fagaramide derivative and canthin-6-one from (Rutaceae) species against multidrug resistant leukemia cells.

In our continuous search for cytotoxic compounds from the genus chromatographic separation of the MeOH/CHCl (1:1) extract of yielded one new alkamide; 4-(isoprenyloxy)-3-methoxy-3,4-deoxymethylenedioxyfagaramide () and a known one; fagaramide (). Similarly, from the MeOH/CHCl (1:1) extract of the stem bark of four known compounds; canthin-6-one (), dihydrochelerythrine (), lupeol () and sesamin () were isolated. Characterization of the structures of these compounds was achieved using spectroscopic techniques (NMR and MS).

Cytotoxicity of naturally occurring phenolics and terpenoids from Kenyan flora towards human carcinoma cells.

Background: Cancer constitutes a major hurdle worldwide and its treatment mainly relies on chemotherapy.

Objectives: The present study was designed to evaluate the cytotoxicity of eleven naturally occurring compounds including six phenolics amongst them were 4 chalcones and 2 flavanones as well as 5 terpenoids (3 clerodane and 2 trachylobane diterpenoids) against 6 human carcinoma cell lines and normal CRL2120 fibroblasts.

Materials And Methods: The neutral red uptake (NR) assay was used to evaluate the cytotoxicity of the compounds, whilst caspase-Glo assay was used to detect caspase activation.

Biopiracy versus One-World Medicine-From colonial relicts to global collaborative concepts.

Background: Practices of biopiracy to use genetic resources and indigenous knowledge by Western companies without benefit-sharing of those, who generated the traditional knowledge, can be understood as form of neocolonialism.

Hypothesis: The One-World Medicine concept attempts to merge the best of traditional medicine from developing countries and conventional Western medicine for the sake of patients around the globe.

Study Design: Based on literature searches in several databases, a concept paper has been written.

Antimycoplasmal Activities of Compounds from and against Strains from the Cluster.

Infections caused by species belonging to the cluster' negatively affect the agricultural sector through losses in livestock productivity. These strains are resistant to many conventional antibiotics due to the total lack of cell wall. Therefore, there is an urgent need to develop new antimicrobial agents from alternative sources such as medicinal plants to curb the resistance threat.

Study of Anti-Tuberculosis Activity Behaviour of Natural Kaurane and Trachylobane Diterpenes Compared with Structural Properties Obtained by Theoretical Calculations.

A set of seven diterpenes, three kauranes and four trachylobanes, isolated from the African plant Psiadia punctulata were assayed against Mycobacterium tuberculosis and reached activity comparable with cycloserine, a second line drug used to treat tuberculosis (TB). Several structural properties of those diterpenes, such as lipophilicity, HOMO and LUMO energies, charge density, and intramolecular hydrogen bond (IHB) formation, were obtained by theoretical calculations and compared with their activities. Peculiar correlations were observed, especially between activity, lipophilicity and IHB formation.

Methyl and p-Bromobenzyl Esters of Hydrogenated Kaurenoic Acid for Controlling Anthracnose in Common Bean Plants.

Kaurenoic acid derivatives were prepared and submitted to in vitro assays with the fungus Colletotrichum lindemuthianum, which causes anthracnose disease in the common bean. The most active substances were found to be methyl and p-bromobenzylesters, 7 and 9, respectively, of the hydrogenated kaurenoic acid, which presented a minimum inhibitory concentration (MIC) of 0.097 and 0.

Cytotoxicity of Plumbagin, Rapanone and 12 other naturally occurring Quinones from Kenyan Flora towards human carcinoma cells.

Background: Cancer is a major public health concern globally and chemotherapy remains the principal mode of the treatment of various malignant diseases.

Methods: This study was designed to investigate the cytotoxicity of 14 naturally occurring quinones including; 3 anthraquinones, 1 naphthoquinone and 10 benzoquinones against 6 human carcinoma cell lines and normal CRL2120 fibroblasts. The neutral red uptake (NR) assay was used to evaluate the cytotoxicity of the compounds, whilst caspase-Glo assay was used to detect caspases activation.

Compounds from Terminalli brownii Extracts with Toxicity against the Fish Pathogenic Bacterium Flavobacterium columnare.

The pond-raised channel catfish (Ictaluruspunctatus) industry in the United States of America can incur losses of over a $100 million annually due to bacterial diseases including columnaris disease caused by Flavobacterium columnare. One management approach available to catfish producers is the use of medicated- feed containing antibiotics. However, the negative attributes of antibiotic use in agriculture include public concerns and the potential development of antibiotic-resistant bacteria.

Selected ethno-medicinal plants from Kenya with in vitro activity against major African livestock pathogens belonging to the "Mycoplasma mycoides cluster".

Ethnopharmocological Relevance: Members of 'Mycoplasma mycoides cluster' are important ruminant pathogens in Africa. Diseases caused by these Mycoplasma negatively affect the agricultural sector especially in developing countries through losses in livestock productivity, mortality and international trade restrictions. There is therefore urgent need to develop antimicrobials from alternative sources such as medicinal plants to curb these diseases.

Antibacterial activities and structure-activity relationships of a panel of 48 compounds from Kenyan plants against multidrug resistant phenotypes.

In the current study forty eight compounds belonging to anthraquinones, naphthoquinones, benzoquinones, flavonoids (chalcones and polymethoxylated flavones) and diterpenoids (clerodanes and kauranes) were explored for their antimicrobial potential against a panel of sensitive and multi-drug resistant Gram-negative and Gram-positive bacteria. The minimal inhibitory concentration (MIC) determinations on the tested bacteria were conducted using modified rapid INT colorimetric assay. To evaluate the role of efflux pumps in the susceptibility of Gram-negative bacteria to the most active compounds, they were tested in the presence of phenylalanine arginine β-naphthylamide (PAβN) (at 30 µg/mL) against selected multidrug resistance (MDR) bacteria.

Isolation of a new β-carboline alkaloid from aerial parts of Triclisia sacleuxii and its antibacterial and cytotoxicity effects.

A new β-carboline alkaloid named sacleuximine A (1) together with known compounds palmatine (2), isotetrandrine (3), trans-N-feruloyltyramine (4), trans-N-caffeoyltyramine (5), yangambin (6), syringaresinol (7), sesamin (8), (+) epi-quercitol (9), 4-hydroxybenzaldehyde (10), β-sitosterol (11), quercetin 3-O-rutinoside (12) and myricetin 3-O-β-glucose (1→6) α-rhamnoside (13) have been isolated from methanol extract of Triclisia sacleuxii aerial parts. Compounds 1-10 were evaluated for their cytotoxicity against human adenocarcinoma (HeLa), human hepatocarcinoma (Hep3B) and human breast carcinoma (MCF-7) cells lines and also for antibacterial activities against both Gram-positive and Gram-negative bacteria. The cytotoxicity (IC) values ranged between 0.

New ent-Clerodane and Abietane Diterpenoids from the Roots of Kenyan Croton megalocarpoides Friis & M. G. Gilbert.

The roots of the endangered medicinal plant Croton megalocarpoides collected in Kenya were investigated and twenty-two compounds isolated. Among them were twelve new ent-clerodane (1-12) and a new abietane (13) diterpenoids, alongside the known crotocorylifuran (4 a), two known abietane and four known ent-trachylobane diterpenoids, and the triterpenoids, lupeol and acetyl aleurotolic acid. The structures of the compounds were determined using NMR, HRMS and ECD.

Biopiracy of natural products and good bioprospecting practice.

Background: Biopiracy mainly focuses on the use of biological resources and/or knowledge of indigenous tribes or communities without allowing them to share the revenues generated out of economic exploitation or other non-monetary incentives associated with the resource/knowledge.

Methods: Based on collaborations of scientists from five continents, we have created a communication platform to discuss not only scientific topics, but also more general issues with social relevance. This platform was termed 'PhytCancer -Phytotherapy to Fight Cancer' (www.

Cytotoxicity of 91 Kenyan indigenous medicinal plants towards human CCRF-CEM leukemia cells.

Ethnopharmacological Relevance: Plants from Kenyan flora are traditionally used against many ailments, including cancer and related diseases. Cancer is characterized as a condition with complex signs and symptoms. Recently there are recommendations that ethnopharmacological usages such as immune and skin disorders, inflammatory, infectious, parasitic and viral diseases should be taken into account when selecting plants that treat cancer.

Isolation and characterization of an antifungal compound 5-hydroxy-7,4'-dimethoxyflavone from Combretum zeyheri.

Background: Combretum zeyheri, belongs to the family Combretaceae and is one of the most popular herbal plants in tropical and subtropical countries. The leaves of Combretum zeyheri have been used as herbal medicine and have been reported to have pharmacological activity which includes anti-bacterial, anti-fungal, anticancer and antioxidant properties. The goal of this study was to isolate, identify and characterize compounds from C.

Antiplasmodial and cytotoxic activities of the constituents of Turraea robusta and Turraea nilotica.

Ethnopharmacological Relevance: Turraea robusta and Turraea nilotica are African medicinal plants used for the treatment of a wide variety of diseases, including malaria. The genus Turraea is rich in limonoids and other triterpenoids known to possess various biological activities.

Materials And Methods: From the stem bark of T.

Anti-vancomycin-resistant Enterococcus faecium and E. faecalis activities of (-)-gossypol and derivatives from Thespesia garckeana.

The root extract of Thespesia garckeana yielded three known oxidatively coupled sesquiterpenoids, namely (-)-gossypol (1) and two of its derivatives (-)-6-methoxygossypol (2) and (+)-6,6'-dimethoxygossypol (3), and the stem bark afforded (E)-docosyl-3-(3,4-dihydroxyphenyl) acrylate (4), stigmasterol (5) and betulinic acid (6). The structures of the isolated compounds were determined on the basis of full spectral data (1D and 2D NMR and HRMS) and comparison with literature values. Compound 1 showed potent antibacterial activity against vancomycin-resistant Enterococcus faecium (VRE) with IC50/MIC/MBC values of 1.