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1.
An investigation of the seeds of the Madagascan Meliaceae Quivisia papinae has yielded quivisianthone, a novel evodulone group limonoid, together with the known azadiradione and two novel derivatives: 6 alpha-hydroxyazadiradione and 7-deacetyl-7-angeloyl-6 alpha-hydroxyazadiradione. Quivisianthone is the first reported evodulone group limonoid possessing both a ring A lactone and an azadiradione-type ring D. 相似文献
2.
A potent and selective nonpeptide antagonist of CXCR2 inhibits acute and chronic models of arthritis in the rabbit 总被引:7,自引:0,他引:7
Podolin PL Bolognese BJ Foley JJ Schmidt DB Buckley PT Widdowson KL Jin Q White JR Lee JM Goodman RB Hagen TR Kajikawa O Marshall LA Hay DW Sarau HM 《Journal of immunology (Baltimore, Md. : 1950)》2002,169(11):6435-6444
Much evidence implicates IL-8 as a major mediator of inflammation and joint destruction in rheumatoid arthritis. The effects of IL-8 and its related ligands are mediated via two receptors, CXCR1 and CXCR2. In the present study, we demonstrate that a potent and selective nonpeptide antagonist of human CXCR2 potently inhibits (125)I-labeled human IL-8 binding to, and human IL-8-induced calcium mobilization mediated by, rabbit CXCR2 (IC(50) = 40.5 and 7.7 nM, respectively), but not rabbit CXCR1 (IC(50) = >1000 and 2200 nM, respectively). These data suggest that the rabbit is an appropriate species in which to examine the anti-inflammatory effects of a human CXCR2-selective antagonist. In two acute models of arthritis in the rabbit induced by knee joint injection of human IL-8 or LPS, and a chronic Ag (OVA)-induced arthritis model, administration of the antagonist at 25 mg/kg by mouth twice a day significantly reduced synovial fluid neutrophils, monocytes, and lymphocytes. In addition, in the more robust LPS- and OVA-induced arthritis models, which were characterized by increased levels of proinflammatory mediators in the synovial fluid, TNF-alpha, IL-8, PGE(2), leukotriene B(4), and leukotriene C(4) levels were significantly reduced, as was erythrocyte sedimentation rate, possibly as a result of the observed decreases in serum TNF-alpha and IL-8 levels. In vitro, the antagonist potently inhibited human IL-8-induced chemotaxis of rabbit neutrophils (IC(50) = 0.75 nM), suggesting that inhibition of leukocyte migration into the knee joint is a likely mechanism by which the CXCR2 antagonist modulates disease. 相似文献
3.
Five 3-hydroxy-type homoisoflavonoids, 3,5-dihydroxy-7,8-dimethoxy-3-(3',4'-dimethoxybenzyl)-4-chromanone, 3,5-dihydroxy-7-methoxy-3-(3',4'-dimethoxybenzyl)-4-chromanone, 3,5-dihydroxy-7,8-dimethoxy-3-(3'-hydroxy-4'-methoxybenzyl)-4-chromanone, 3,5,6-trihydroxy-7-methoxy-3-(3'-hydroxy-4'-methoxybenzyl)-4-chromanone and 3,5,7-trihydroxy-3-(3'-hydroxy-4'methoxybenzyl)-4-chromanone in addition to the nortriterpenoid, 15-deoxoeucosterol, have been isolated from the dichloromethane extract of the bulbs of Pseudoprospero firmifolium, the sole representative of the tribe Pseudoprospereae of the subfamily Hyacinthoideae of the Hyacinthaceae. 相似文献
4.
An investigation of the seeds of the Madagascan Meliaceae Quivisia papinae has yielded five mexicanolide group limonoids, together with two known mexicanolide limonoids and two known triterpenoids. Quivisianolide A 9 possesses a hitherto unreported 9alpha,11alpha-epoxide ring, quivisianolide B 10 the corresponding delta(9(11)) double bond, and quivisianone 11 is a 17-keto seco-ring D compound. 相似文献
5.
The chloroform and ethyl acetate extracts of the leaves of Teclea natalensis have yielded two furoquinoline alkaloids, 6-[(2,3-epoxy-3-methylbutyl)oxy]-4,7-dimethoxyfuro[2,3-b]quinoline and 4,7-dimethoxy-6-[(3-methyl-2-butenyl)oxy]furo[2,3-b]quinoline, and the known alkaloids 4,7-dimethoxy-8-[(3-methyl-2-butenyl)oxy]furo[2,3-b]quinoline, flindersiamine and dictamnine. 相似文献
6.
Moses K. Langat Neil R. Crouch Leena Pohjala Päivi Tammela Peter J. Smith Dulcie A. Mulholland 《Phytochemistry letters》2012,5(3):414-418
Two new ent-kauren-19-oic acid derivatives, ent-14S*-hydroxykaur-16-en-19-oic acid and ent-14S*,17-dihydroxykaur-15-en-19-oic acid together with eleven known compounds ent-kaur-16-en-19-oic acid, ent-kaur-16-en-19-al, ent-12β-hydroxykaur-16-en-19-oic acid, ent-12β-acetoxykaur-16-en-19-oic acid, 8R,13R-epoxylabd-14-ene, eudesm-4(15)-ene-1β,6α-diol, (?)-7-epivaleran-4-one, germacra-4(15), 5E,10(14)-trien-9β-ol, acetyl aleuritolic acid, β-amyrin, and stigmasterol were isolated from the stem bark of Croton pseudopulchellus (Euphorbiaceae). Structures were determined using spectroscopic techniques. Ent-14S*-hydroxykaur-16-en-19-oic acid, ent-kaur-16-en-19-oic acid, ent-12β-hydroxykaur-16-en-19-oic acid, ent-12β-acetoxykaur-16-en-19-oic acid and 8R,13R-epoxylabd-14-ene were tested for their effects on Semliki Forest virus replication and for cytotoxicity against human liver tumour cells (Huh-7 strain) but were found to be inactive. Ent-kaur-16-en-19-oic acid, the major constituent, showed weak activity against the Plasmodium falciparum (CQS) D10 strain. 相似文献
7.
Neil A. Koorbanally Neil R. Crouch Avinash Harilal Bavani Pillay Dulcie A. Mulholland 《Biochemical Systematics and Ecology》2006
We report on the first phytochemical investigation of a member of the African genus Resnova (Hyacinthoideae: Hyacinthaceae). From the dichloromethane extract of the bulbs of both Resnova humifusa and Eucomis montana (Hyacinthoideae: Hyacinthaceae) a novel 3-benzyl-4-chromanone homoisoflavonoid, 5,6-dimethoxy-7-hydroxy-3-(4′-hydroxybenzyl)-4-chromanone, was isolated. A further 11 known homoisoflavonoids were also identified, the 12 in total presenting a clear biosynthetic sequence. Eight of the 12 compounds found were common to both species. 相似文献
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9.
Lainé DI Yan H Xie H Davis RS Dufour J Widdowson KL Palovich MR Wan Z Foley JJ Schmidt DB Hunsberger GE Burman M Bacon AM Webb EF Luttmann MA Salmon M Sarau HM Umbrecht ST Landis PS Peck BJ Busch-Petersen J 《Bioorganic & medicinal chemistry letters》2012,22(9):3366-3369
A novel series of N-substituted tropane derivatives was characterized as potent muscarinic acetylcholine receptor antagonists (mAChRs). Kinetic washout studies showed that the N-endosubstituted analog 24 displayed much slower reversibility at mAChRs than the methyl-substituted parent molecule darotropium. In addition, it was shown that this characteristic appeared to translate into enhanced which duration of action in a mouse model of bronchonstriction. 相似文献
10.
Yonghui Wang Jakob Busch-Petersen Feng Wang Terence J. Kiesow Todd L. Graybill Jian Jin Zheng Yang James J. Foley Gerald E. Hunsberger Dulcie B. Schmidt Henry M. Sarau Elizabeth A. Capper-Spudich Zining Wu Laura S. Fisher Michael S. McQueney Ralph A. Rivero Katherine L. Widdowson 《Bioorganic & medicinal chemistry letters》2009,19(1):114-118
A series of N-arylpiperazine camphor sulfonamides was discovered as novel CXCR3 antagonists. The synthesis, structure–activity relationships, and optimization of the initial hit that resulted in the identification of potent and selective CXCR3 antagonists are described. 相似文献