Many secondary metabolites derived from Rumex extracts exhibited potent activities against a panel of phytopathogens including those of Phytophthora spp. Phytochemical investigation of Rumex abyssinicus has led to the isolation of nine compounds, including one phenolic acid (1), five anthraquinones (2–6) and three flavanols (7–9). Compounds 1, 4, 6–9 are reported here from R. abyssinicus for the first time. The isolated compounds were evaluated for their inhibitory activity against zoospores of the oomycete phytopathogen Phytophthora capsici. Physcion (3) displayed strongest motility inhibitory activity with a MIC value of 15μgmL−1, and showed lytic activities against zoospores at 500μgmL−1.

Malignancies constitute a global health concern and chemotherapy remains the main mode of treatment. The present study was designed to evaluate the cytotoxicity of 8 compounds from Desbordesia glaucescens namely lanosta-7,24-dien-3-one (1), friedelanone (2), friedelanol (3), 3,3′-di-O-methylellagic acid (4), 3,3′,4′-tri-O-methylellagic acid (5), ellagic acid (6), 3′,4′-di-O-methylellagic acid 4-O-β-d-glucopyranoside (7) and 3,3′-di-O-methylellagic acid 4′-O-β-d-xylopyranoside (8) against 4 human carcinoma cell lines and normal CRL2120 fibroblasts. The neutral red uptake (NRU) assay was used for cytotoxicity testing. Caspase-Glo assay, cell cycle analysis, measurements of mitochondrial membrane potential (MMP) and levels of reactive oxygen species (ROS) were used to evaluate apoptosis induction. Compounds 4 and 6 as well as doxorubicin had IC50 values below 45μM in the four tested cancer cell lines meanwhile other compounds displayed selective activity. The IC50 values ranged from 11.23μM (towards breast adenocarcinoma MCF-7 cells) to 44.65μM (colon carcinoma Caco-2 cells) for 4, from 14.07μM (towards MCF-7 cells) to 77.73μM (Caco-2 cells) for 6 and from 0.07μM (towards SPC212 cells) to 1.01μM (A549 cells) for doxorubicin. Compound 4 induced apoptosis in MCF-7 cells mediated by MMP loss. The constituents of Desbordesia glaucescens and especially ellagic acid (6) and its derivative 4 are potential cytotoxic compounds that deserve more investigations towards developing novel antiproliferative drugs against human carcinoma.

Background: We decided to investigate the antimicrobial and the antioxidant activities of extracts and compounds isolated from Dissotis perkinsiae, Adenocatpus mannii and Barteria fistulosa, three Cameroonian medicinal plants used for the treatment of skin diseases, wounds, fever, rheumatism, malaria and/or infectious diseases.Methods: Standard chromatographic and spectroscopic methods were used to isolate and identify ten compounds from the three plant species [1-5 (from D. perkinsiae), 2, 6-8 (from A. mannii) and 2, 4, 9, and 10 (from B. fistulosa)]. A two-fold serial microdilution method was used to determine the minimum inhibitory concentration (MIC) against a panel of fungal and bacterial species. The radical scavenging capacity using 2,2-diphenyl-1-picryhydrazyl (DPPH) was determined to evaluate the antioxidant activity of the samples.Results: The compounds isolated were: ursolic acid (1), oleanolic acid (2), quercetin 3-O-(6 ''-O-galloyl)-beta-galactopyranoside (3), 3-O-beta-D-glucopyranoside of sitosterol (4), ellagic acid (5), isoprunetin (6), chrysin 7-O-beta-D-glucopyranoside (7), isovitexin (8), hederagenin (9) and shanzhiside methyl ester (10). The ethanol extract of D. perkinsiae had good antibacterial activity against Enterococcus faecalis (MICs 0.04 and 0.08 mg/ml), Escherichia coli (MIC 0.08 mg/ml) and Staphylococcus aureus (MIC 0.08 mg/ml). The extract of B. fistulosa had significant antifungal activity against Ciyptococcus neoformans with an MIC of 0.08 mg/ml. Other extracts had moderate to poor antimicrobial activities with the MIC ranging from 0.16 to 2.50 mg/ml. The isolated compounds were generally more active against bacteria (MIC ranging from 16 to 250 mu g/ml) than fungi (MIC between 31 and 250 mu g/ml). Moderate antibacterial activity was obtained with compound 3 against E. faecalis and E. coli (MIC of 16 mu g/ml in both cases), compounds 6 and 10 against E. faecalis (MIC of 16 mu g/ml), and compound 9 against E. faecalis (MIC 31 mu g/ml) and S. aureus (MIC 31 mu g/ml). The B. fistulosa extract had the greatest radical scavenging activity (IC50 100.16 mu g/ml) followed by extracts of D. perkinsiae (IC50 130.66 mu g/ml), and A. mannii (IC50 361.30 mu g/ml). Compounds 3 and 5 had significant antioxidant activities with the IC50 of 9.84 and 9.99 mu g/ml as compared to that of ascorbic acid (IC50 2.41 mu g/ml).Conclusion: The results obtained support the traditional use of the three plant species (D. perkinsiae, A. mannii and B. fistulosa) in traditional medicine for the treatment of infections. Some extracts and isolated compounds could be useful in development of antimicrobial agents. We are currently investigating the toxicity and other pharmacological activities with the potential use as topical antimicrobial agents. (C) 2013 SAAB. Published by Elsevier B.V. All rights reserved.

The present study evaluates the anti-nociceptive and anti-inflammatory properties of the aqueous and methylene chloride/methanol (CH2Cl2 / CH3OH) extracts of the stem bark of Croton macrostachyus. The extracts administered orally at the doses of 150, 300 and 600 mg/kg were examined against pain induced by acetic acid, formalin and pressure and against inflammation induced by carragenan, histamine and formalin. Both extracts induced a significant dosedependent (P < 0.001) reduction in the number of abdominal constrictions induced by acetic acid. The three doses of the two extracts also significantly reduced (P < 0.001) the two phases of pain induced by formalin. At the dose of 600 mg/kg, the aqueous and the CH2Cl2 / CH3OH extracts exhibited a significant analgesic activity against pressure-induced pain. The two extracts also exhibited anti-inflammatory activity, the CH2Cl2 / CH3OH extract being the most active, inhibited acute inflammation induced by carrageenan, histamine and formalin. Both extracts also significantly reduced the chronic inflammation induced by formalin. These results show that the aqueous and CH2Cl2 / CH3OH extracts of the stem bark of Croton macrostachyus possess analgesic and anti-inflammatory properties. These findings are in accordance with the traditional use of the plant and indicate that Croton macrostachyus is a potent source of analgesic and antiinflammatory principles.

Aim: This study describes the activity-guided isolation of antimicrobial and antioxidant agents from Trilepisium madagascariense stem bark.Methods: The methanol crude extract of T. madagascariense was partitioned sequentially into n-hexane, ethyl acetate, n-butanol and the residual aqueous fractions. The ethyl acetate fraction was subjected to column chromatography and the structures of isolated compounds were elucidated using GC MS and/or NMR data by comparing with those reported in the literature. Antimicrobial activity was assayed by agar well diffusion and broth microdilution techniques on 8 bacteria and 10 yeasts. The antioxidant activity was determined by DPPH radical scavenging method.Results: The bioassay-guided fractionation of the crude methanol extract of T. madagascariense afforded two known compounds [vanillic acid (1) and isoliquiritigenin (2)] and two mixtures of fatty acids (n-hexane fraction and first column fraction of ethyl acetate fraction, F1). The fractionation of the crude methanol extract enhanced the antimicrobial activity. Compound 2 was generally more active than compound 1. For all the tested samples, the most sensitive microbes were Enterococcus faecalis ATCC 10541 (MIC range of 60-780 mu g/ml) for bacteria and Candida guillermondi (MIC range of 0.01-190 mu g/ml) for yeasts. The DPPH radical scavenging activity (RSa) of compound 2 (RSa(50)=28.73 mu g/ml) was comparable to that of the crude methanol extract (RSa(50)=29.92 mu g/ml).Conclusion: The antimicrobial activities and the antioxidant properties of the methanol crude extract, fractions and compounds 1 and 2 from the stem bark of T. madagascariense are being reported for the first time. These results may justify the traditional use of this plant for the treatment of gastrointestinal disorders. (C) 2010 SAAB. Published by Elsevier B.V. All rights reserved.

Background: Arthritis in familial Mediterranean fever (FMF) is typically monoarticular, of sudden onset, self-limiting, rarely destructive, and a frequent manifestation of FMF. The mechanisms governing the initiation and resolution of this highly inflammatory disease entity are not fully understood. Therefore, to decipher the complexity of articular autoinflammation, we defined inflammatory cells and some mediators of inflammation and apoptosis in the synovial membrane of a patient with FMF. Methods: A synovial tissue sample obtained from an inflamed hip joint of a boy homozygous for mutation M694I in pyrin/marenostrin was studied by immunohistochemistry using commercially available antibodies specific for tryptase, CD68, CD3, CD20 and CD138. With the same technique, we also analyzed the expression and distribution of myeloperoxidase, lysozyme, galectin-1, galectin-3, p65 (RelA)/NF-κB, iNOS, COX-2 and activated caspase-3. Results: Abundant neutrophils, macrophages and mast cells, but also B cells were observed, which were more numerous than T lymphocytes or plasma cells. Neutrophils had no granules containing myeloperoxidase or lysozyme in their cytoplasm. Galectin-1 was found in many mononuclear cells sparse throughout the synovial tissue, whereas the expression of galectin-3 was less prominent and scattered. Neither of the galectins was detected in neutrophils. p65 (RelA)/NF-κB and iNOS were both up-regulated in most of the inflammatory cells, whereas COX-2 expression was low, and cleaved caspase-3, used as proxy to demonstrate intrinsic apoptosis, was undetectable. Conclusions: The exquisitely inflammatory, yet non-destructive character of FMF arthritis may correlate with the presence of non-pathogenic neutrophils lacking effector molecules and the preferential expression of iNOS and anti-inflammatory galectin-1 in regulatory cells of the innate immune system, most likely in macrophages. Intrinsic apoptosis seemed irrelevant for controlling synovial autoinflammation, but regulation through pyroptosis, mast cells and the adaptive immune system are possible alternatives.

La reaction dans le toluene du zinc formate dihydrate, Zn(HCOO) 2 .2H 2 O avec le 2-isopropylimidazole a temperature ambiante a conduit a l’obtention du nouveau complexe  bisformatobis(2-isopropylimidazole)zinc(II) de formule  [Zn(N 2 H 10 C 6 ) 2 (OOCH) 2 ]. Ce materiau a ete caracterise par diverses techniques (analyse elementaire, spectroscopies IR et RMN) et l’analyse thermogravimetrique (ATG). Les analyses spectroscopiques (IR, 1 H-RMN, 13 C- RMN) ont montre que ce materiau aurait une structure exhibant le site actif observe dans certaines metalloproteines telles que les carboxypeptidase A ou B. L’analyse thermogravimetrique montre que ce materiau est stable jusqu’a 100°C. The reaction of zinc formate with 2-isopropylimidazole at room temperature using toluene as solvent has produced the new complex  bisformatobis(2-isopropylimidazole)zinc(II) or [Zn(N 2 H 10 C 6 ) 2 (OOCH) 2 ]. This compound has been characterized using different analytical techniques (elemental analysis, IR and NMR spectroscopies). The spectroscopic analysis (IR, 1 H-NMR, 13 C-NMR) showed that this material would have a structure exhibiting the active site observed in certain metalloproteins such as carboxypeptidase A or B. The thermal analysis (TGA) showed that this material is stable up to 100°.

An ethnobotanical survey was made on plants used in the treatment of infectious diseases in Mbouda subdivision, Cameroon. According to our survey, one of the most important medicinal plants in that area is Bryophyllum pinnatum (Lank.) Oken (Crassulaceae), a succulent plant native to Africa. B. pinnatum (leaves or whole plant) was found to be well known and was used against blennorrhoea, syphilis, jaundice, candidiasis and for the treatment of others ailments such as dysmenorrhoea, external ulcers, burns, convulsions and as analgesic. In order to identify the biologically active compounds of the plant and to confirm or infirm its ethnopharmacological claims, phytochemical study of ethyl acetate extract of the whole plant was carried out. As a result of this kaempferol rhamnosides, kaempferol 3,7-O-bis-α-L-rhamnopyranoside (kaempferitrin) [1], kaempferol 3-O-α-L-(3-acetyl)rhamnoside-7-O-α-L-rhamnopyranoside [2], kaempferol 3-O-α-L-rhamnoside (afzelin) [1] and kaempferol 7-O-α-L-rhamnoside (α-rhamnoisorobin) [1] were isolated and identified by extensive NMR and MS studies. All compounds were described for the first time in this species. These isolates are reported in other plant species to possess antioxidant, antinociceptive and anti-inflammatory activities [3, 4], therefore the kaempferol rhamnosides of B. pinnatum may account for the medicinal use of the plant against pain and inflammatory disorders.

BACKGROUND:Typhoid fevers and urogenital infections continue to be serious health problems in developing countries. In our search for therapeutic agents from natural sources with potential for the treatment of typhoid fevers and urogenital infections, extract and compounds were obtained from Crinum purpurascens and tested.METHODS:Two alkaloids (4,5-ethano-9,10-methylenedioxy-7-phenanthridone or hippadine (1) and 4,5-ethano-9-hydroxy-10-methoxy-7-phenanthridone or pratorimine (2)) and one steroid (â-D-glucopyranoside of sitosterol (3)) were isolated from the CH(2)Cl(2)/MeOH (1:1) leaf extract of Crinum purpurascens and screened for antibacterial activity using both agar diffusion and broth dilution techniques.RESULTS:For the CH(2)Cl(2)/MeOH extract, the MIC values obtained were 3 mg/ml (against P. aeruginosa), 4 mg/ml (against E. coli, K. pneumoniae and S. aureus) and 6 mg/ml (against S. typhi and S. paratyphi B), whereas the MBC values varied between 7 and 12 mg/ml. For compound 1, the MIC values varied between 200 and 250 µg/ml, whereas the MBC value was 300 µg/ml against all the bacteria strains used. Compound 2 did not show any antimicrobial activity against these bacteria strains. For compound 3, the MIC values varied between 250 and 300 µg/ml, whereas the MBC values were 300 µg/ml (against S. typhi and S. paratyphi B) and > 300 µg/ml (against the other bacteria strains).CONCLUSION:These data suggest that C. purpurascens leaf extract contains antibacterial agents which could be used in the treatment of typhoid fevers and urogenital infections.

Objective: To identify the antimicrobial components present in Microglossa angolensis following fractionation of the methylene chloride extract of the aerial part of this plant. Materials and Methods: The plant was dried and extracted by percolation with methylene chloride. The dry extract was fractionated and purified by silica gel column chromatography. The isolated compounds were identified by comparison of their Nuclear Magnetic Resonance (NMR) spectral data with those reported in the literature. Antimicrobial activity was assayed by broth macro dilution method. Results: The crude extract of M. angolensis displayed significant antifungal and antibacterial activities (MIC = 312.50-1250g/ml). 6-(2-methylbut-2(Z)-enoyl)-3,4,15,16-bis-epoxy-8,10H-ent-cleroda-13(16),14-dien-20,12-olide and spinasterol were the most active compounds (MIC = 1.56-100g/ml) and the most sensitive microorganisms were Enterococcus faecalis and Candida tropicalis for bacteria and yeasts respectively. Conclusion: The isolation of these active antibacterial and antifungal principles supports the use of M. angolensis in traditional medicine for the treatment of gastro-intestinal disorders.

Antimicrobial-guided fractionation of the EtOAc extract of the stem bark of Croton macrostachys afforded five known compounds including two lupane triterpenoids, lupeol (1) and betulin (2), and three clerodane diterpenoids, floridolide A (3), hardwickic acid (4) and 12-oxo-hardwickic acid (5). Their structures were elucidated on the basis of spectral studies and comparison with published data. The EtOAc extract and compounds 1, 2, 4 and 5 were evaluated for their antibacterial and antifungal activities by macro-dilutionmethod. The extract displayed significant antibacterial and antifungal activities (MIC = 31.25-1000 μg/ml). Betulin (2) and 12-oxo-hardwickic acid (5) were the most active compounds (MIC = 7.81-500 μg/ml). Themost sensitive microorganisms were Staphylococcus aureus ATCC 25922 for bacteria and two Candida species, Candida albicans ATCC 24433 and Candida krusei ATCC 6258, for fungi. The isolation of these active antibacterial and antifungal principles supports the use of C. macrostachys in traditional medicine for the treatment of microbial infections.Keywords: Croton macrostachys; Euphorbiaceae; triterpenes; diterpenes; antibacterial; antifungal.

A new glyceryl derivative (Glyceryl-1-hexacosanoate) and a flavone derivative (methyletherapigenin) were isolated from the stem bark extract of Piptadenia africana, a western Cameroonian plant species. Common terpenes like sitosterol, beta-amyrin and eicosane were also isolated. These compounds were identified using physical and spectroscopic methods including mp, IR, (1)H and (13)C-NMR, DEPT, COSY, HMQC, HMBC, EI MS, HREI MS as well as some chemical transformations. The antibacterial activity of the extract, the fractions and the pure compounds is also discussed.

Background: Cystic fibrosis (CF) results from mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene, which encodes a chloride channel localized at the plasma membrane of diverse epithelia. The most common mutation leading to CF, F508, occurs in the first nucleotide-binding domain (NBD1) of CFTR. The F508 mutation disrupts protein processing, leading to a decreased level of mutant channels at the plasma membrane and reduced transepithelial chloride permeability. Partial correction of the F508 molecular defect in vitro is achieved by incubation of cells with several classes of chemical chaperones, indicating that further investigation of novel small molecules is warranted as a means for producing new therapies for CF. Materials and Methods: The yeast two-hybrid assay was used to study the effect of CF-causing mutations on the ability of NBD1 to self-associate and form dimers. A yeast strain demonstrating defective growth as a result of impaired NBD1 dimerization due to F508 was used as a drug discovery bioassay for the identification of plant natural product compounds restoring mutant NBD1 interaction. Active compounds were purified and the chemical structures determined. The purified compounds were tested in epithelial cells expressing CFTR F508 Address correspondence and reprint requests to: John Teem, Department of Biological Science, Biounit-238, Florida State University, Tallahassee, Florida 32306, USA. Phone: (850) 644-5121; fax: (850) 644-0481; e-mail: teem@bio.fsu.edu and the resulting effect on transepithelial chloride permeability was assessed using short-circuit chloride current measurements. Results: Wild-type NBD1 of CFTR forms homodimers in a yeast two-hybrid assay. CF-causing mutations within NBD1 that result in defective processing of CFTR ( F508, I507, and S549R) disrupted NBD1 interaction in yeast. In contrast, a CF-causing mutation that does not impair CFTR processing (G551D) had no effect on NBD1 dimerization. Using the yeast-based assay, we identified a novel limonoid compound (TS3) that corrected the F508 NBD1 dimerization defect in yeast and also increased the chloride permeability of Fisher Rat Thyroid (FRT) cells stably expressing CFTR F508. Conclusion: The establishment of a phenotype for the F508 mutation in the yeast two-hybrid system yielded a simple assay for the identification of small molecules that interact with the mutant NBD1 and restore dimerization. The natural product compound identified using the system (TS3) was found to increase chloride conductance in epithelial cells to an extent comparable to genistein, a known CFTR activator. The yeast system will thus be useful for further identification of compounds with potential for CF drug therapy.

A new guanidine alkaloid, millaurine A (1), was isolated from the methanol extract of the seeds of Millettia laurentii. The structure of the new compound was elucidated on the basis of spectral analysis.

The genus Drimiopsis Lindl. (Hyacinthaceae) is endemic to sub-Saharan Africa, where it is represented by approximately 20 species [1]. Drimiopsis barterii Bak is the only specie of the genus which occurs in Cameroon. The plant is used by the Bamileke people of the Western province of Cameroon to treat fever. In a continuation of our search for bioactive compounds from natural source [2], a methylene chloride-methanol (1:1) extract of Drimiopsis barterii (whole plant) was investigated. Two new alkaloids (Drimiopsine A (1) and B(2)) and nine homoisoflavonids with two new structures (3, 4) were isolated.The structure of the compounds were established by MS, 1D and 2D spectroscopy including DEPT, COSY, HMQC and HMBC experiments.

A new binaphthoquinone bearing two 4-hydroxy-5-methyleoumarin-3-yl units has been isolated from the stem bark of Diospyros canaliculata De Wildeman in addition to five known compounds: lupenone, betulinic acid, gerberinol, plumbagin and canaliculatin. Their structures were established on the basis of 1D (H-1, C-13 and DEPT) and 2D (H-1-H-1 COSY, HMQC and HMBC) NMR experiments. Some of the above compounds showed a significant antimicrobial activity against bacteria and yeasts.

Three new isoflavonoids, griffonianone F, G and H were isolated from the seeds of Millettia griffoniana, along with the known prebarbigerone, pseudobaptigenin, pseudobaptigenin methyl ether, tephrosin, dipterixine, odorantine, 7,4',5'-tetramethoxyisoflavone and isojamaicin. Their structures were assigned on the basis of spectroscopic data and chemical transformations.