Bioactivity evaluations of betulin identified from the bark of Betula platyphylla var. japonica for cancer therapy

So, Hae Min; Eom, Hee Jeong; Lee, Dahae; Kim, Sil; Kang, Ki Sung; Lee, Il Kyun; Baek, Kwan-Hyuck; Park, Jun Yeon; Kim, Ki‐Hyun

doi:10.1007/s12272-018-1064-9

Cited by 54 publications

(35 citation statements)

References 41 publications

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“…As part of our ongoing research to identify bioactive components from Korean natural resources [22][23][24], we explored the potential bioactive constituents of garlic. The phytochemical analysis of the methanolic (MeOH) extract of garlic led to the isolation of six compounds: Three eugenol diglycosides (1-3) and three β-carboline alkaloids (4-6).…”

Section: Introductionmentioning

confidence: 99%

Anti-adipogenic Effect of β-Carboline Alkaloids from Garlic (Allium sativum)

Baek

Nam

et al. 2019

Foods

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Garlic (Allium sativum L.) is utilized worldwide for culinary and medicinal use and has diverse health benefits. As part of our ongoing research to identify bioactive components from natural resources, phytochemical analysis of the methanolic extract of garlic led to the isolation and characterization of six compounds: Three eugenol diglycosides (1-3) and three β-carboline alkaloids (4-6). In particular, the absolute configurations of β-carboline alkaloids (5 and 6) were established by gauge-including atomic orbital nuclear magnetic resonance chemical shift calculations, followed by DP4+ analysis. Here, we evaluated the effects of compounds 1-6 on 3T3-L1 preadipocyte adipogenesis and lipid metabolism. 3T3-L1 adipocyte differentiation was evaluated using Oil Red O staining; the expression of adipogenic genes was detected using RT-qPCR. Among compounds 1-6, (1R,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid (6) inhibited 3T3-L1 preadipocyte adipogenesis and reduced the expression of adipogenic genes (Fabp4, PPARγ, C/EBPβ, Adipsin, and Adipoq). Moreover, it markedly decreased the actylation of α-tubulin, which is crucial for cytoskeletal remodeling during adipogenesis. Anti-adipogenic effects were observed upon treatment with compound 6, not only during the entire process, but also on the first two days of adipogenesis. Additionally, treatment with compound 6 regulated the expression of genes involved in adipocyte lipid metabolism, decreasing the lipogenic gene (SREBP1) and increasing lipolytic genes (ATGL and HSL). We provide experimental evidence of the health benefits of using (1R,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid obtained from garlic to prevent excessive adipogenesis in obesity.

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Section: Introductionmentioning

confidence: 99%

Anti-adipogenic Effect of β-Carboline Alkaloids from Garlic (Allium sativum)

Baek

Nam

et al. 2019

Foods

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“…As part of the continuing research into bioactive compounds from Korean medicinal plant sources [13][14][15][16][17], the MeOH extract of the aerial portion of L. cuneata was found to exhibit cytotoxic effects on human ovarian carcinoma cells [5]. In our recent study, bioassay-guided fractionation of the MeOH extract using repeated chromatography resulted in the isolation of (−)-9 -O-(α-l-rhamnopyranosyl)lyoniresinol, which inhibited the proliferation of A2780 human ovarian carcinoma cells through the induction of apoptosis [5].…”

Section: Introductionmentioning

confidence: 99%

Aviculin Isolated from Lespedeza cuneata Induce Apoptosis in Breast Cancer Cells through Mitochondria-Mediated Caspase Activation Pathway

Lee

et al. 2020

Molecules

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The global incidence of breast cancer has increased. However, there are many impediments to the development of safe and effective anticancer drugs. The aim of the present study was to evaluate the effect of aviculin isolated from Lespedeza cuneata (Dum. Cours.) G. Don. (Fabaceae) on MCF-7 human breast cancer cells and determine the underlying mechanism. Using the bioassay-guided isolation by water soluble tetrazolium salt (WST-1)-based Ez-Cytox assay, nine compounds (four lignan glycosides (1–4), three flavonoid glycosides (5–7), and two phenolic compounds (8 and 9)) were isolated from the ethyl acetate (EA) fraction of the L. cuneata methanolic extract. Of these, aviculin (2), a lignan glycoside, was the only compound that reduced metabolic activity on MCF-7 cells below 50% (IC50: 75.47 ± 2.23 μM). The underlying mechanism was analyzed using the annexin V Alexa Fluor 488 binding assay and Western blotting. Aviculin (2) was found to induce apoptotic cell death through the intrinsic apoptosis pathway, as indicated by the increased expression of initiator caspase-9, executioner caspase-7, and poly (ADP-ribose) polymerase (PARP). Aviculin (2)-induced apoptotic cell death was accompanied by an increase in the Bax/Bcl-2 ratio. These findings demonstrated that aviculin (2) could induce breast cancer cell apoptosis through the intrinsic apoptosis pathway, and it can therefore be considered an excellent candidate for herbal treatment of breast cancer.

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“…As part of our continuing projects to explore biologically active, unique natural products from diverse natural sources [18][19][20][21][22], we recently took note of Ulmus davidiana var. japonica, the root barks of which have been used as a Korean traditional medicine for various therapeutic purposes including gastroenteric disorders and inflammatory disorders [23][24][25][26].…”

Section: Introductionmentioning

confidence: 99%

(–)-Catechin-7-O-β-d-Apiofuranoside Inhibits Hepatic Stellate Cell Activation by Suppressing the STAT3 Signaling Pathway

Park

Kim

Jeong

et al. 2019

Cells

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Hepatic fibrosis is characterized by the abnormal deposition of extracellular matrix (ECM) proteins. During hepatic fibrogenesis, hepatic stellate cell (HSC) activation followed by chronic injuries is considered a key event in fibrogenesis, and activated HSCs are known to comprise approximately 90% of ECM-producing myofibroblasts. Here, we demonstrated that (-)-catechin-7-O-β-d-apiofuranoside (C7A) significantly inhibited HSC activation via blocking the signal transducer and activator of transcription 3 (STAT3) signaling pathway. This is the first study to show the hepatic protective effects of C7A with possible mechanisms in vitro and in vivo. In our bioactivity screening, we figured out that the EtOH extract of Ulmus davidiana var. japonica root barks, which have been used as a Korean traditional medicine, inhibited collagen synthesis in HSCs. Four catechins isolated from the EtOAc fraction of the EtOH extract were compared with each other in terms of reduction in collagen, which is considered as a marker of hepatic protective effects, and C7A showed the strongest inhibitory effects on HSC activation in protein and qPCR analyses. As a possible mechanism, we investigated the effects of C7A on the STAT3 signaling pathway, which is known to activate HSCs. We found that C7A inhibited phosphorylation of STAT3 and translocation of STAT3 to nucleus. C7A also inhibited expressions of MMP-2 and MMP-9, which are downstream genes of STAT3 signaling. Anti-fibrotic effects of C7A were evaluated in a thioacetamide (TAA)-induced liver fibrosis model, which indicated that C7A significantly inhibited ECM deposition through inhibiting STAT3 signaling. C7A decreased serum levels of aspartate amino transferase and alanine transaminase, which were markedly increased by TAA injection. Moreover, ECM-associated proteins and mRNA expression were strongly suppressed by C7A. Our study provides the experimental evidence that C7A has inhibitory effects on HSC activation after live injury and has preventive and therapeutic potentials for the management of hepatic fibrosis.

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Bioactivity evaluations of betulin identified from the bark of Betula platyphylla var. japonica for cancer therapy

Cited by 54 publications

References 41 publications

Anti-adipogenic Effect of β-Carboline Alkaloids from Garlic (Allium sativum)

Anti-adipogenic Effect of β-Carboline Alkaloids from Garlic (Allium sativum)

Aviculin Isolated from Lespedeza cuneata Induce Apoptosis in Breast Cancer Cells through Mitochondria-Mediated Caspase Activation Pathway

(–)-Catechin-7-O-β-d-Apiofuranoside Inhibits Hepatic Stellate Cell Activation by Suppressing the STAT3 Signaling Pathway

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