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The root extract of Suregada zanzibariensis Baill. afforded six previously described ent -abietane diterpenoids, namely 7-oxo- ent -abieta-5(6),8(14),13(15)-trien-16,12-olide ( 1 ), mangiolide ( 2 ), 8,14 β :11,12 α -diepoxy-13(15)-abietane-16,12-olide ( 3 ), 7 β ,11 β ,12 β -trihydroxy- ent -abieta-8(14),13(15)-diene-16,12-olide ( 4 ), 8α,14-dihydro-7-oxo-jolkinolide E ( 5 ), jolkinolide A ( 6 ), together with 3 β -sitosterol ( 7 ), scopoletin ( 8 ) and vanillin ( 9 ). 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. The crude extract and compounds 1 - 9 were evaluated for their antiplasmodial, antifungal and antibacterial activities. Mangiolide ( 2 ) showed strong in vitro antiplasmodial activity against chloroquine sensitive (D6) and resistant (W2) strains of Plasmodium falciparum with IC 50 values of 0.79 and 0.87 µg/mL, respectively, while 3 (IC 50 1.24 and 1.17 µg/mL) was less active than 2 . Compound 2 also displayed antimicrobial activity against Cryptococcus neoformans , methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecium (VRE) with IC 50 values of 1.20, 3.90 and 7.20 µg/mL, respectively.

A new 3,8''-flavanone-flavonol dimer gnidiflavanone-flavonol ( 1 ) and 10 known compounds ( 2 - 11 ), including four rare primula-type flavones 2 - 5 , were isolated from the roots of Gnidia apiculata . Compounds 2 - 5 and 7 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. The crude roots extract and isolated compounds were evaluated for antimicrobial and antiplasmodial activities. Among isolated compounds, 6-hydroxyflavone ( 4 ) and 6- O -acetylflavone ( 4a ) showed antiplasmodial activity against chloroquine-sensitive (D6) and chloroquine-resistant (W2) strains of Plasmodium falciparum .

Monoterpene derivatives are of great biological relevance in the pharmaceutical industry. In the present study, pyrrolidine derivative of a carvotacetone, 3- O- benzylcarvotacetone ( 1 ), and selected monoterpenes (3-hydroxy-2-isopropyl-5-methyl- p -benzoquinone ( 3 ) and cis- piperitol ( 5 )) were prepared to provide ( R )-1-(4-(benzyloxy)-5-isopropyl-2-methylcyclohexa-1,3-dien-1-yl)-pyrrolidine ( 2 ), 2-isopropyl-5-methyl-3,6-dioxocyclohexa-1,4-dien-1-yl acetate ( 4 ), cis- 3-hydroxypiperitone ( 6 ) and carvacrol ( 7 ). Structure of 2 was determined based on NMR and HRMS spectral data. Compound 4 exhibited activity against fungi Cryptococcus neoformans with an IC 50 value of < 0.8   µg/mL. In addition, this compound 4 had an IC 50 value of 14.97   µg/mL against methicillin resistant Staphylococcus aureus bacteria. Previous to the current study, both compound 6 and 7 had been reported to have anti-microbial and anti-fungal activities.

In an attempt to synthesize carvotacetone analogues, new 3- O -benzyl-carvotacetone ( 10) and previously reported 3-hydroxy-2-isopropyl-5-methyl- p -benzoquinone ( 11 ) were synthesized from piperitone ( 7 ). In this work, we describe the synthesis of 10 and other analogues from 7 . Luche reduction of 7 to cis -piperitol ( 8) , followed by benzylation yielded 3- O -benzyl-piperitol ( 9 ). Riley oxidation of 9 afforded corresponding ketone 10 , 11 and 3-benzyloxy-4-isopropylcyclohex-1-enecarbaldehyde ( 12) . Structures of these compounds were determined based on NMR, IR and LC-MS spectral data. Compound 11 , exhibited antiplasmodial activities against chloroquine-sensitive (D6) and resistant (W2) strains of Plasmodium falciparum with IC 50 value s of 0.697 and 0.653   µg/mL, respectively. In addition, compound 11 was active against Cryptococcus neoformans with an IC 50 value of 3.11   µg/mL, compared to reference standard fluconazole (IC 50 value of 1.87   µg/mL), while 10 and 12 were inactive against both organisms. This is the first report of the antiplasmodial and anticryptococcal activity of compound 11 .

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., Aim: The present study was aimed at investigating the cytotoxicity of a plethora of 145 plant parts from 91 medicinal plants, most of which are used in the management of cancer and related diseases by different communities in Kenya, against CCRF-CEM leukemia cell line., Materials and Methods: Extracts from different plant parts (leaves, stems, stem bark, roots, root barks, aerial parts and whole herb) were obtained by cold percolation using different solvent systems, such as (1:1v/v) dichloromethane (CH2Cl2) and n-hexane (1), methanol (MeOH) and CH2Cl2 (2); neat MeOH (3), 5% H2O in MeOH (4) and with ethanol (EtOH, 5); their cytotoxicities were determined using the resazurin reduction assay against CCRF-CEM cells., Results: At a single concentration of 10μg/mL, 12 out of 145 extracts exhibited more than 50% cell inhibition. These include samples from the root bark of Erythrina sacleuxii (extracted with 50% n-hexane-CH2Cl2), the leaves of Albizia gummifera, and Strychnos usambarensis, the stem bark of Zanthoxylum gilletii, Bridelia micrantha, Croton sylvaticus, and Albizia schimperiana; the root bark of Erythrina burttii and E. sacleuxii (extracted with 50% CH2Cl2-MeOH), the stem bark of B. micrantha and Z. gilletii (extracted using 5% MeOH-H2O) and from the berries of Solanum aculeastrum (extracted with neat EtOH). The EtOH extract of the berries of S. aculeastrum and A. schimperiana stem bark extract displayed the highest cytotoxicity towards leukemia CCRF-CEM cells, with IC50 values of 1.36 and 2.97µg/mL, respectively. Other extracts having good activities included the extracts of the stem barks of Z. gilletii and B. micrantha and leaves of S. usambarensis with IC50 values of 9.04, 9.43 and 11.09µg/mL, respectively., Conclusions: The results of this study provided information related to the possible use of some Kenyam medicinal plants, and mostly S. aculeastrum, A. schimperiana, C. sylvaticus, Z. gilletii, B. micrantha and S. usambarensis in the treatment of leukemia. The reported data helped to authenticate the claimed traditional use of these plants. However, most plants are used in combination as traditional herbal concoctions. Hence, the cytotoxicity of corresponding plant combinations should be tested in vitro to authenticate the traditional medical practitioners actual practices., (Copyright © 2015 Elsevier Ireland Ltd. All rights reserved.)

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 1.71/4.82/19.31 µM, respectively, whereas the reference standard vancomycin was found to be inactive. The mono- and di-methoxylated derivatives of this compound, (-)-6-methoxygossypol (2) and (+)-6,6'-dimethoxygossypol (3), were less active with respective IC50/MIC/MBC values of 2.73/4.70/9.40 µM and 6.14/18.32/18.32 µM against this microbe. Compound 2 was more potent than 1 against the low level VRE strain with I50/MIC/MBC values of 4.34/9.40/9.40 µM (vs 5.23/19.31/19.3 µM for 1). This compound also showed interesting activities against Candida glabrata with an I50 value of 2.97 µM, but was less active against methicillin-resistant S. aureus (MRSA) exhibiting an IC50 value of 17.33 µM. Compound 1 demonstrated modest activity against the