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Quan, Khong Trong,Park, Hyun-Soo,Oh, Joonseok,Park, Hyun Bong,Ferreira, Daneel,Myung, Chang-Seon,Na, MinKyun American Chemical Society and American Society of 2016 Journal of natural products Vol.79 No.10
<P>The abnormal proliferation and migration of vascular smooth muscle cells (VSMCs) are associated with cardiovascular diseases and related complications. Such deleterious proliferation and migration events are triggered by cytokines and growth factors, and among them, platelet-derived growth factor (PDGF) is recognized as the most potent inducer. Despite the genus Rubia being researched to identify valuable commercial and medicinal virtues, Rubia philippinensis has rarely been investigated. Nine arborinane-type triterpenoids (1-9) were identified from this underutilized plant species. In particular, 4 was identified as the first arborinane derivative carrying a ketocarbonyl motif at C-19. The presence of the cyclopentanone moiety and the associated configurational assignment were determined by utilizing NOE and coupling constant analysis. These compounds were assessed for their inhibitory potential on PDGF-induced proliferation and the migration of VSMCs. Treatment with 5 mu M compound 5 (62.6 +/- 10.7%) and compound 9 (41.1 +/- 4.7%) impeded PDGF-stimulated proliferation without exerting cytotoxicity. Compound 7 exhibited antimigration activity in a dose-dependent manner (38.5 +/- 3.0% at 10 mu M, 57.6 +/- 3.2% at 30 mu M). These results suggest that the arborinane-type triterpenoids may be a pertinent starting point for the development of cardiovascular drugs capable of preventing the intimal accumulation of VSMCs.</P>
An, Younju,Quan, Khong Trong,Gwak, Jungsug,Ju, Bong Gun,Na, MinKyun,Oh, Sangtaek Elsevier 2018 Food and chemical toxicology Vol.118 No.-
<P><B>Highlights</B></P> <P> <UL> <LI> Digiferrol is a novel activator of the p53 pathway. </LI> <LI> Digiferrol stabilizes p53 protein in the nucleus. </LI> <LI> Digiferrol induces cell cycle arrest at G2/M phase in colon cancer cells. </LI> <LI> Digiferrol promotes apoptosis and autophagy in colon cancer cells. </LI> </UL> </P>
Oh, Joonseok,Quan, Khong Trong,Lee, Ji Sun,Park, InWha,Kim, Chung Sub,Ferreira, Daneel,Thuong, Phuong Thien,Kim, Young Ho,Na, MinKyun American Chemical Society and American Society of 2018 Journal of natural products Vol.81 No.11
<P>Hydrogen bonding is a vital feature of a large ensemble of chemical structures. Soluble epoxide hydrolase (sEH) has been targeted for development of the treatment for inflammation-associated diseases. Compounds <B>1</B> and <B>2</B> were purified from <I>Rubia philippinensis</I>, and their structures were established via physical data analysis. Compound <B>1</B> possesses intramolecular hydrogen bonding, sufficiently robust to transfer heteronuclear magnetization via a nonbonded interaction. The bonding strength was assessed using the <SUP>1</SUP>H NMR chemical shift temperature coefficients (−1.8 ppb/K), and the heteronuclear coupling constants were measured. The stereochemical details were investigated using interproton distance analysis and ECD. Purified compounds displayed moderate sEH-inhibitory activity.</P> [FIG OMISSION]</BR>
Park, Hyun-Soo,Quan, Khong Trong,Han, Joo-Hui,Jung, Sang-Hyuk,Lee, Do-Hyung,Jo, Eunji,Lim, Tae-Wan,Heo, Kyung-Sun,Na, MinKyun,Myung, Chang-Seon Wiley (Blackwell Publishing) 2017 British journal of pharmacology Vol.174 No.22
<P>These findings suggest that rubiarbonone C inhibits the proliferation and migration of VSMCs by inhibiting the FAK, MAPK and STAT3 signalling pathways. Therefore, rubiarbonone C could be a good candidate for the treatment of cardiovascular disease.</P>
Le, Vu Ngoc Han,Zhao, Yan,Cho, Chong Woon,Na, MinKyun,Quan, Khong Trong,Kim, Jang Hoon,Hwang, Sung Yeoun,Kim, Sang Wook,Kim, Kyung Tae,Kang, Jong Seong Elsevier 2018 Journal of chromatography. B, Analytical technolog Vol.1102 No.-
<P><B>Abstract</B></P> <P>Nardostachyos Radix et Rhizoma (NR) is a valuable medicinal herb widely used in Korea, India, and China for the treatment of many diseases. Desoxo-narchinol A (DA) and nardosinonediol (ND) are the two main bioactive compounds belonging to the sesquiterpene group. Desoxo-narchinol A possesses anti-inflammatory activity while ND exhibits anti-depressant and cardioprotective activities. A pharmacokinetic study is important to decide whether the isolated compounds or the NR extract have better pharmacological activity. Hence, we developed an analytical method for studying the pharmacokinetics of DA and ND after oral administration of the pure compounds and herbal extract. An optimized liquid chromatography-mass spectrometry method (LC-MS/MS) with solid-phase extraction (SPE) for sample preparation was developed. A ZORBAX Extend C18 column (2.1 × 50 mm, 3.5 μm) was used under gradient elution with acetonitrile and 0.1% formic acid in water as the mobile phase. Validation experiments assessing accuracy, precision, and stability were satisfactory; the lower limit of quantification was 5 ng/mL. For the pharmacokinetic study, three groups of rats were administrated pure DA, pure ND, or NR extract orally. Concentrations of DA and ND in their plasma were determined by the developed method. Pharmacokinetic parameters, including the time to achieve maximum plasma concentration (<I>T</I> <SUB> <I>max</I> </SUB>) and the area under the plasma concentration curve from time zero to infinity (<I>AUC</I> <SUB>0–∞</SUB>), were compared for the herbal extract and pure compounds. The <I>T</I> <SUB> <I>max</I> </SUB> of the pure compound and the NR extract for DA was 7.50 and 8.33 min, respectively, compared to 5.00 and 5.83 min for the pure compound and the NR extract for ND, respectively. The <I>AUC</I> <SUB>0–∞</SUB> of the pure compound and the NR extract for DA was 156.34 and 133.90 μg min/mL, respectively, and that for the NR extract for ND was 6.42 and 4.15 μg min/mL, respectively. LC-MS/MS was used to determine DA and ND in rat plasma. The pharmacokinetic profile of each pure compound and those in the extract were characterized and compared.</P>
Extract of Curcuma zedoaria R. prevents atherosclerosis in apolipoprotein E-deficient mice
Ki Mo Kim,Joo Young Lee,Byeong Hwa Jeon,Khong Trong Quan,MinKyun Na,Kung-Woo Nam,Sungwook Chae 한국영양학회 2021 Nutrition Research and Practice Vol.15 No.3
BACKGROUND/OBJECTIVES: Curcuma zedoaria R. (Zingiberaceae) has been used to treat headache, fever, and hypertension-related symptoms in Asian countries, including Korea, China, and Japan. We investigated whether dietary intake of a C. zedoaria extract (CzE) affected atherosclerosis in vivo. MATERIALS/METHODS: Apolipoprotein E-deficient (ApoE<SUP>−/−</SUP>) mice (n = 32) were fed a normal diet (ND), a high-cholesterol diet (HCD), an HCD containing CzE (100 mg/kg/day), or an HCD containing simvastatin (10 mg/kg/day) for 12 weeks. The anti-atherosclerotic effects were evaluated by observing changes in fatty streak lesions, immunohistochemical analysis, ex vivo fluorescence imaging, lipid profiles, and western blot analysis. RESULTS: The CzE-fed group showed a 41.6% reduction of atherosclerosis. Furthermore, CzE significantly reduced the levels of serum triglyceride, high-density lipoprotein, the chemokine (C-X3-C-motif ) ligand 1, the adhesion molecules vascular cell adhesion molecule-1, intracellular adhesion molecule-1, and E-selectin; down-regulation of tumor necrosis factor-α, interleukin-6, high mobility group box-1, and cathepsin levels in the aortic sinuses and aortas of ApoE<SUP>−/−</SUP> mice were also observed. CONCLUSIONS: The results suggest that the inclusion of a water extract of C. zedoaria in a HCD is closely correlated with reducing the risk of vascular inflammatory diseases in an ApoE mouse model.
Alam, Md Badrul,Bajpai, Vivek K.,Ra, Jeong-Sic,Lim, Ji-Young,An, Hongyan,Shukla, Shruti,Quan, Khong Trong,Khan, Imran,Huh, Yun Suk,Han, Young-Kyu,Na, MinKyun,Lee, Sang-Han Pergamon 2019 Food and Chemical Toxicology Vol. No.
<P><B>Abstract</B></P> <P>This study assesses the ability of anthraquinone derivative, 2-methyl-1,3,6-trihydroxy-9,10-anthraquinone (MTAQ) to decrease postprandial hyperglycemia or enhance glucose uptake and to elucidate the underlying molecular mechanism. We investigated α-glucosidase inhibition, glucose uptake, and translocation of glucose transporter 4 (GLUT4) in C2C12 myotubes. The data indicate that MTAQ strongly inhibited α-glucosidase activity in a concentration-dependent manner, with an IC<SUB>50</SUB> value of 6.49 ± 1.31 μM, and functioned as a reversible competitive inhibitor, with a dissociation constant of 41.88 μM. Moreover, MTAQ significantly augmented basal and insulin-stimulated glucose uptake as well as translocation of GLUT4 to the plasma membrane. It also stimulated the phosphorylation of insulin receptor β isoform, insulin receptor substrate-1,3-phosphoinositide-dependent protein kinase 1, and protein kinase B (AKT). A pretreatment with an AKT inhibitor, LY294002, attenuated the ability of MTAQ to activate an insulin-like signaling pathway and to enhance basal and insulin-stimulated glucose uptake and stimulate GLUT4 translocation to the plasma membrane. These findings reveal the fact that MTAQ may have potential for the development of new antidiabetic drugs to manage blood glucose levels.</P>