In Vitro Platelet-Activating Factor Receptor Binding Inhibitory Activity of Pinusolide Derivatives: A Structure−Activity Study

Han, Byung Hoon; Yang, Hyun Ok; Kang, Young‐Hwa; Suh, Dae-Yeon; Go, Hyun Jung; Song, Wan-Jin; Kim, Yong Chul; Park, Man Ki

doi:10.1021/jm970569j

Cited by 19 publications

(11 citation statements)

References 24 publications

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“…A number of terpenes and flavonoids were reported as chemical constituents of this tree (Zhu et al, 2004;Koo et al, 2002;Sung et al, 1998;Yang et al, 1995). In addition, several diterpenes have been reported to exert the neuroprotective activity, platelet activating factor receptor binding inhibitory activity and anticancer activity (Kosuge et al, 1985;Han et al, 1998;Koo et al, 2002). In the present study, we further attempted to investigate the antifibrotic constituents of B. orientalis using an immortalized rat hepatic stellate HSC-T6 cell line as an in vitro assay system.…”

Section: Introductionmentioning

confidence: 90%

Antifibrotic activity of diterpenes from Biota orientalis leaves on hepatic stellate cells

et al. 2008

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Antifibrotic effect of twelve diterpenes (1-12) from the 90% methanolic fraction of Biota orientalis leaves was evaluated employing HSC-T6 cells by assessing cell proliferation and morphological change. Among these diterpenes, totarol (8) and isopimara-8(14),15-dien-19-oic acid (9) dramatically reduced cell proliferation in dose-and time-dependent manner. Furthermore, treatment with these compounds resulted in the different pattern of morphological changes of HSC-T6 cells. Taken together, antiproliferative activity of diterpenes from B. orientalis might suggest therapeutic potentials against liver fibrosis.

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Section: Introductionmentioning

confidence: 90%

Antifibrotic activity of diterpenes from Biota orientalis leaves on hepatic stellate cells

et al. 2008

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“…To investigate the structure-activity relationship and find derivatives with improved pharmacological profiles, 17 pinusolide derivatives were prepared and tested for their ability to inhibit the PAF receptor binding. The results demonstrated that the carboxymethyl ester group at C-19, the integrity of the alpha, beta unsaturated butenolide ring, and the exocyclic olefinic function of pinusolide are all necessary for its maximum PAF receptor binding inhibitory activity [195][196][197][198].…”

Section: Anti-paf Activitymentioning

confidence: 99%

“…Biota orientalis) Anti-PAF activity, antimalarial [148,[195][196][197][198] Thuja standishii (Gord) Carr. cytotoxicity [137,138] Cyperaceae…”

Section: Species Activities Referencesmentioning

confidence: 99%

Labdanes of Natural Origin-Biological Activities (1981-2004)

Chinou

2005

CMC

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Terpenoids is a class of natural compounds found in higher plants, mosses, liverworts, algae and lichens, as well as in insects, microbes or marine organisms. Through centuries many of these compounds have been used as ingredients of perfumes, drugs, narcotics or pigments. Labdanes, belonging to the bicyclic diterpenoids group, have been found as secondary metabolites in tissues of fungi, insects, marine organisms, and in essential oils, resins and tissues of higher plants. The diterpenes of labdane type, have been reported to have broad spectrum of biological activities. In this study, the reported bioactivities and/or uses of them, the last two decades (1981-2004), are selected as an attempt to underline their role in nature.

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“…Pinusolide and its derivative, 15-methoxypinusolidic acid (15-MPA) are diterpenoid constituents of B. orientalis. Pinusolide has been reported to exhibit anti-aggregation effects by binding and inhibiting platelet activating factor (Han et al, 1998;Kim et al, 1999). In addition, pinusolide and 15-MPA attenuate neurotoxic effects of glutamate or staurosporin in primary rat cortical cells by reducing nitric oxide (NO) production, exerting the potent antioxidant and antiapoptotic activities (Koo et al, 2002(Koo et al, , 2006(Koo et al, , 2007.…”

Section: Introductionmentioning

confidence: 99%

Suppression of adipocyte differentiation by 15-methoxypinusolidic acid through inhibition of PPARγ activity

et al. 2010

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Pinusolide and its derivative, 15-methoxypinusolidic acid (15-MPA) are diterpenoid compounds isolated from Biota orientalis, which has been used as a Korean folk medicine for treating inflammatory disorders. Pinusolide and 15-MPA suppress nitric oxide generation by suppressing inducible nitric oxide synthase and exerted anti-inflammatory functions, whereas other functions and regulatory mechanisms are largely unknown. In this study, we investigated whether pinusolide and 15-MPA modulate adipocyte differentiation from pre-adipocytes 3T3-L1 cells. We found that 15-MPA, not pinusolide, suppressed adipocyte differentiation in a dose-dependent manner, as revealed by lipid droplet formation and expression of adipogenic genes such as adiponectin and aP2. 15-MPA did not affect mRNA and protein levels of PPARgamma, a key adipogenic transcription factor, whereas transcriptional activity of PPARgamma was significantly attenuated by 15-MPA. While aP2 promoter activity was increased by ectopic overexpression of PPARgamma or by rosiglitazone-induced endogenous PPARgamma activation, PPARgamma-induced aP2 promoter activity was inhibited in the presence of 15-MPA. These results suggest that 15-MPA suppresses adipocyte differentiation through the inhibition of PPARgamma-dependent adipogenic gene expression.

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In Vitro Platelet-Activating Factor Receptor Binding Inhibitory Activity of Pinusolide Derivatives: A Structure−Activity Study

Cited by 19 publications

References 24 publications

Antifibrotic activity of diterpenes from Biota orientalis leaves on hepatic stellate cells

Antifibrotic activity of diterpenes from Biota orientalis leaves on hepatic stellate cells

Labdanes of Natural Origin-Biological Activities (1981-2004)

Suppression of adipocyte differentiation by 15-methoxypinusolidic acid through inhibition of PPARγ activity

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