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1.
Yumin Dai Liva Harinantenaina Peggy J. Brodie Chris Birkinshaw Richard Randrianaivo Wendy Applequist Michel Ratsimbason Vincent E. Rasamison Yongchun Shen Karen TenDyke David G. I. Kingston 《化学与生物多样性》2013,10(2):233-240
Investigation of the endemic Madagascan plant Nematostylis anthophylla (Rubiaceae) for antiproliferative activity against the A2780 ovarian cancer cell line led to the isolation of the known triterpene saponin randianin ( 1 ), and the two new bioactive triterpene saponins 2″‐O‐acetylrandianin ( 2 ) and 6″‐O‐acetylrandianin ( 3 ). The structures of the two new compounds were elucidated based on analysis of their 1D‐ and 2D‐NMR spectra, and mass spectrometric data. The three isolated triterpene saponins displayed moderate but selective antiproliferative activities, with IC50 values of 1.2, 1.7, and 2.2 μM , respectively, against the A2780 ovarian cancer, but only weak inhibitions of the proliferation of A2058 melanoma and the H522 lung cancer cell lines. 相似文献
2.
Yixi Liu Liva Harinantenaina Peggy J. Brodie Jessica D. Bowman Maria B. Cassera Carla Slebodnick Martin W. Callmander Richard Randrianaivo Etienne Rakotobe Vincent E. Rasamison Wendy Applequist Chris Birkinshaw Gwilym P. Lewis David G.I. Kingston 《Bioorganic & medicinal chemistry》2013,21(24):7591-7594
Bioassay-directed fractionation of the leaf and root extracts of the antiproliferative Madagascar plant Stuhlmannia moavi afforded 6-acetyl-5,8-dihydroxy-2-methoxy-7-methyl-1,4-naphthoquinone (stuhlmoavin, 1) as the most active compound, with an IC50 value of 8.1 μM against the A2780 human ovarian cancer cell line, as well as the known homoisoflavonoid bonducellin (2) and the stilbenoids 3,4,5′-trihydroxy-3′-methoxy-trans-stilbene (3), piceatannol (4), resveratrol (5), rhapontigenin (6), and isorhapontigenin (7). The structure elucidation of all compounds was based on NMR and mass spectroscopic data, and the structure of 1 was confirmed by a single crystal X-ray analysis. Compounds 2?5 showed weak A2780 activities, with IC50 values of 10.6, 54.0, 41.0, and 74.0 μM, respectively. Compounds 1?3 also showed weak antimalarial activity against Plasmodium falciparum with IC50 values of 23, 26, and 27 μM, respectively. 相似文献
3.
Castelhano AL Dong H Fyfe MC Gardner LS Kamikozawa Y Kurabayashi S Nawano M Ohashi R Procter MJ Qiu L Rasamison CM Schofield KL Shah VK Ueta K Williams GM Witter D Yasuda K 《Bioorganic & medicinal chemistry letters》2005,15(5):1501-1504
The synthesis, SAR and biological evaluation of a series of ureas that activate glucokinase, a target for diabetes therapy as a result of its critical role in the regulation of whole-body glucose homeostasis, are described. Some of the urea-containing glucokinase activators lowered blood glucose levels in vivo following oral dosing to C57BL/6J mice. 相似文献
4.
Isolation of the New Antiplasmodial Butanolide,Malleastrumolide A,from Malleastrum sp. (Meliaceae) from Madagascar
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Yongle Du Alexander K. Abedi Ana Lisa Valenciano Maria L. Fernández‐Murga Maria B. Cassera Vincent E. Rasamison Wendy L. Applequist James S. Miller David G. I. Kingston 《化学与生物多样性》2017,14(12)
An extract of Malleastrum sp. (Meliaceae) collected in Madagascar by the Madagascar International Cooperative Biodiversity Group was found to have antimalarial activity, with an IC 50 value between 2.5 and 5 μg ml?1. After purification by liquid‐liquid partition, chromatography on a Diaion open column, C 18 SPE and C 18 reversed phase HPLC , the new butanolide, malleastrumolide A, was isolated. The structure of malleastrumolide A was determined by mass spectrometry, NMR , and ECD . The double bond position was determined by cross‐metathesis and mass spectrometry. The compound has antiproliferative activity against the A2780 ovarian cancer cell line with an IC 50 value of 17.4 μm and antiplasmodial activity against the drug‐resistant Dd2 strain of Plasmodium falciparum with an IC 50 value of 2.74 μm . 相似文献
5.
Wendy L. Applequist Michel Ratsimbason Alyse Kuhlman Stephan Rakotonandrasana Vincent Rasamison David G. I. Kingston 《Economic botany》2017,71(1):75-82
Bioassay screening of plant extracts can identify unique lead compounds for drug development, but the “hit rate” from random screening is very low. Targeted screening of medicinal plants has been repeatedly reported to increase the percentage of samples displaying bioactivity. Contrarily, Maranz (2012) suggested that African antimalarial plants were unsuitable sources of antimalarial drugs because high prevalence of malaria would result in rapid evolution of resistance to active compounds that directly targeted the parasite. As malaria is highly prevalent in much of Madagascar, it was of interest to determine whether Malagasy antimalarial plants would outperform randomly selected plants in conventional antimalarial assays being conducted as part of a discovery program. Of 1294 plant samples screened for antimalarial activity, 39.6% had an IC50 <50 μg/ml and 21.1% had an IC50 <20 μg/ml (the minimum to qualify as a first-pass “hit”). Ethnobotanical uses were coded at both the generic and the species level, as neither samples nor use reports in literature were always identifiable to species level. The 526 samples belonging to genera having reported uses for malaria were slightly more likely than average to display activity (44.3% with IC50 <50 μg/ml, p < .01; 23.2% with IC50 <20 μg/ml). Of these, 67 samples from individual species with documented use were still more likely to be modestly active (49.3% with IC50 <50 μg/ml), yet less likely to be highly active (17.9% with IC50 <20 μg/ml). Thus, in this specific context, ethnobotanically directed screening would not have substantially improved screening efficiency and would have missed most of the potential hits. 相似文献
6.
Pan E Harinantenaina L Brodie PJ Callmander M Rakotonandrasana S Rakotobe E Rasamison VE Tendyke K Shen Y Suh EM Kingston DG 《Bioorganic & medicinal chemistry》2011,19(1):422-428
Investigation of the endemic Madagascar plant Leptadenia madagascariensis Decne. (Apocynaceae) for antiproliferative activity against the A2780 ovarian cancer cell line led to the isolation of the four new cardenolides 1-4. The structure elucidations of these compounds were based on analyzes of their 1D and 2D NMR spectra and mass spectrometric data. The cardenolides were strongly antiproliferative to the A2780 ovarian cancer cell line, with IC50 values of 0.18, 0.21, 0.17, and 0.29 ??M line, and to the H460 human lung cancer cell line, with IC50 values of 0.16, 0.68, 0.37, and 0.48 ??M, respectively. 相似文献
7.
Cao S Hou Y Brodie P Miller JS Randrianaivo R Rakotobe E Rasamison VE Kingston DG 《化学与生物多样性》2011,8(4):643-650
Bioassay‐guided fractionation of the EtOH extracts obtained from a plant identified as Cyphostemma greveana Desc . (Vitaceae) led to the identification of one macrolide, lasiodiplodin ( 1 ), three sesquiterpenoids, 12‐hydroxy‐15‐oxoselina‐4,11‐diene ( 2 ), 1β,6α‐dihydroxyeudesm‐4(15)‐ene ( 3 ), and (7R*)‐opposit‐4(15)‐ene‐1β,7‐diol ( 5 ), and a new diterpenoid, 16,18‐dihydroxykolavenic acid lactone ( 4 ). All the isolates were tested against the A2780 human ovarian cancer cell line, and compound 4 and a fraction containing 5 as the major constituent showed antiproliferative activities with IC50 values of 0.44 μM (0.14 μg/ml) and 0.045 μg/ml, respectively. A partial synthesis of compound 5 was carried out, but the pure synthetic compound was inactive, indicating that the activity of the fraction containing it must be due to a very minor and as yet unidentified substance. 相似文献
8.
Hanrahan P Bell J Bottomley G Bradley S Clarke P Curtis E Davis S Dawson G Horswill J Keily J Moore G Rasamison C Bloxham J 《Bioorganic & medicinal chemistry letters》2012,22(6):2271-2278
Substituted azaquinazolinones were identified as antagonists of the GHSr-1A receptor for the treatment of type II diabetes and obesity. Optimisation for potency and LogD lead to the identification of orally bioavailable, potent antagonists with improved selectivity over hERG. 相似文献
9.
Antiproliferative cardenolide glycosides of Elaeodendron alluaudianum from the Madagascar Rainforest
Yanpeng Hou Shugeng Cao Peggy Brodie Martin Callmander Fidisoa Ratovoson Richard Randrianaivo Etienne Rakotobe Vincent E. Rasamison Stephan Rakotonandrasana Karen TenDyke Edward M. Suh David G.I. Kingston 《Bioorganic & medicinal chemistry》2009,17(6):2215-2218
Bioassay-guided fractionation of an ethanol extract of a Madagascar collection of Elaeodendron alluaudianum led to the isolation of two new cardenolide glycosides (1 and 2). The 1H and 13C NMR spectra of both compounds were fully assigned using a combination of 2D NMR experiments, including 1H–1H COSY, HSQC, HMBC, and ROESY sequences. Both compounds 1 and 2 were tested against the A2780 human ovarian cancer cell line and the U937 human histiocytic lymphoma cell line assays, and showed significant antiproliferative activity with IC50 values of 0.12 and 0.07 μM against the A2780 human ovarian cancer cell line, and 0.15 and 0.08 μM against the U937 human histiocytic lymphoma cell line, respectively. 相似文献
10.
Yanpeng Hou Shugeng Cao Peggy J. Brodie Martin W. Callmander Fidisoa Ratovoson Etienne A. Rakotobe Vincent E. Rasamison Michel Ratsimbason John N. Alumasa Paul D. Roepe David G.I. Kingston 《Bioorganic & medicinal chemistry》2009,17(7):2871-2876
Bioassay-guided fractionation of an ethanol extract of a Madagascar collection of the bark of Scutia myrtina led to the isolation of three new anthrone–anthraquinones, scutianthraquinones A, B and C (1–3), one new bisanthrone–anthraquinone, scutianthraquinone D (4), and the known anthraquinone, aloesaponarin I (5). The structures of all compounds were determined using a combination of 1D and 2D NMR experiments, including COSY, TOCSY, HSQC, HMBC, and ROESY sequences, and mass spectrometry. All the isolated compounds were tested against the A2780 human ovarian cancer cell line for antiproliferative activities, and against the chloroquine-resistant Plasmodium falciparum strains Dd2 and FCM29 for antiplasmodial activities. Compounds 1, 2 and 4 showed weak antiproliferative activities against the A2780 ovarian cancer cell line, while compounds 1–4 exhibited moderate antiplasmodial activities against P. falciparum Dd2 and compounds 1, 2, and 4 exhibited moderate antiplasmodial activities against P. falciparum FCM29. 相似文献