Isolation, Structural Elucidation, and Cytotoxicity of Three New ent-Kaurane Diterpenoids from Isodon japonica var. glaucocalyx

Liang, Hongye; Zhang, Yunxiao; Hai, Guangfan; Bai, Su-Ping; Yuan, Ye; Ye, Dandan; Zhou, Nan-Qian

doi:10.1055/s-0033-1350998

Cited by 4 publications

(5 citation statements)

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“…GLH contains the same antitumor pharmacophore of cyclopentanone, conjugated with an exomethylene group in the structure as glaucocalyxin A. However, GLH exhibits higher inhibitory proliferation activities than its parent compound glaucocalyxin A, with 50% inhibitory concentration (IC 50 ) value of 1.97 μM against HepG 2 cell line in our early studies (16). This suggests that the hydroxyl groups of protocatechuic aldehyde enhance the antitumor activities of GLH.…”

Section: Discussionmentioning

confidence: 90%

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Anti-Hepatoma Activity of a Novel Compound Glaucocalyxin H In Vivo and In Vitro

et al. 2014

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Abstract. Glaucocalyxin H (GLH) is a new compound isolated from a traditional Chinese medical herb Isodon japonica var. glaucocalyx which has been used for folk medicine. This study was carried out for the first time to investigate the potential role of GLH in anti-hepatoma activity and underlying mechanisms in it. GLH could inhibit the growth of tumor in mice and induce HepG 2 cells to death as assessed by the tumor reduction assay, toxic assay, morphological change, and survival rate assay. Many antitumor drugs originated from plants could inhibit the growth of tumor by inducing cells to apoptosis. The morphological changes of HepG 2 cells treated with different concentrations of GLH under fluorescence and electron microscope and apoptotic rates were detected to verify its effect on apoptosis. As shown in the study, GLH could induce HepG 2 cells to apoptosis in a dose-dependent manner. Bcl 2 and Bax proteins played important roles in apoptosis and the disequilibrium between Bcl 2 and Bax might result in apoptosis. The expression of Bax protein was upregulated and Bcl 2 protein was downregulated in HepG 2 cells treated with GLH assessed by Western blotting, and they were in a dose-dependent manner. Taken together, GLH can inhibit the growth of hepatoma cells in vivo and in vitro by inducing cell apoptosis due to the decreased Bcl 2 and increased Bax proteins suggesting that GLH could be a potential candidate as an anti-hepatoma agent for the therapeutic treatment of hepatoma.

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Section: Discussionmentioning

confidence: 90%

“…glaucocalyx in our laboratory (16). The structural elucidation demonstrated that GLH is an acetal derivative of the two hydroxyl groups of glaucocalyxin A with the aldehyde group of protocatechuic aldehyde (Fig.…”

Section: Introductionmentioning

confidence: 83%

Anti-Hepatoma Activity of a Novel Compound Glaucocalyxin H In Vivo and In Vitro

et al. 2014

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“…Isodon henryi is a medicinal herb has the properties of clearing heat, detoxifying, reducing swelling, and dispersing stasis. 9,10 Its leaves are traditionally boiled in water to create tea for the treatment of CP with definite effect. Early on, we carried out a rigorous investigation of the chemical makeup of I. henryi, from which 26 diterpenes were extracted and produced, of which 6 were shown to be the plant's primary constituents.…”

Section: Introductionmentioning

confidence: 99%

“…Isodon henryi is a medicinal herb has the properties of clearing heat, detoxifying, reducing swelling, and dispersing stasis 9,10 . Its leaves are traditionally boiled in water to create tea for the treatment of CP with definite effect.…”

Section: Introductionmentioning

confidence: 99%

Rabdosichuanin C inhibits productions of pro‐inflammatory mediators regulated by NF‐κB signaling in LPS‐stimulated RAW264.7 cells

Lingxia,

Hong,

Man

et al. 2023

J of Cellular Biochemistry

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Chronic pharyngitis (CP) is an inflammatory disease of the pharyngeal mucosa and its lymphatic tissues that is difficult to treat clinically. However, research on the exact therapeutic agents and molecular mechanisms of CP is still unclear. In this study, we investigated Rabdosichuanin C (RC) to attenuate lipopolysaccharide (LPS)‐induced inflammatory damage in RAW264.7 cells by a combination of targeted virtual screening and in vitro activity assay and further clarified its molecular mechanism of action centering on the IκB/nuclear factor kappa B (NF‐κB) pathway. Molecular docking and pharmacophore simulation methods were used to screen compounds with IκB inhibitory effects. Expression of genes and proteins related to the IκB/NF‐κB signaling pathway by RC in LPS‐induced inflammatory injury model of RAW264.7 cells was detected by PCR, enzyme‐linked immunosorbent assay, and Western blot. The docking of RC with IκB protein showed good binding energy, and pharmacophore simulations further confirmed the active effect of RC in inhibiting IκB protein. RC intervention in LPS‐induced RAW264.7 cells significantly reduced the expression levels of inflammatory factors tumor necrosis factor‐α, interleukins‐6, iNOS, and CD‐86 at the messenger RNA and protein levels, downregulated IκB, p65 protein phosphorylation levels, and significantly inhibited IκB/NF‐κB signaling pathway activation. Virtual screening provided us with an effective method to rapidly identify compounds RC that target inhibit the action of IκB, and the activity results showed that RC inhibits NF‐κB signaling pathway activation. It is suggested that RC may play a role in the treatment of CP by inhibiting the IκB/NF‐κB signaling pathway.

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“…Phytochemical analysis of I. japonicus var. glaucocalyx collected from different regions led to the identification of several diterpenoids [9][10][11][12][13][14][15]. Glaucocalyxin A (ent-kaurane diterpenoid), the main constituent in I. japonicus var.…”

Section: Introductionmentioning

confidence: 99%