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Zhi-Ning Huang,Han Liang,Hong Qiao,Bao-Rui Wang,Ning Qu,Hua Li,Run-Run Zhou,Li-Juan Wang,Shan-Hua Li,Fu-Nan Li 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.12
Guided by bioisosterism and pharmacokinetic parameters, we designed and synthesized a series of novel benzamide derivatives. Preliminary in vitro studies indicated that compounds 10b and 10j show significant inhibitory bioactivity in HepG2 cells (IC50 values of 0.12 and 0.13 μM, respectively). Compounds 10b and 10j induced the expression of HIF-1α protein and downstream target gene p21, and upregulated the expression of cleaved caspase-3 to promote tumor cells apoptosis.
Cytotoxic Isoflavanones from Uraria clarkei
Huang, Xiang-Zhong,Bai, Xi-Shan,Liang, Hui,Wang, Chao,Li, Wen-Juan,Guo, Jun-Ming,Jiang, Zhi-Yong Korean Chemical Society 2013 Bulletin of the Korean Chemical Society Vol.34 No.5
Two new isoflavanones, (3R) 5,7,3',4'-tetrahydroxy-2'-methoxyisoflavanone (1) and (3R) 5',8-di-(${\gamma}$,${\gamma}$-dimethylallyl)-2',5-dihydroxyl-4',7-dimethoxyl-isoflavanone (2), were isolated from Uraria clarkei, together with two known compounds dalbergioidin (3), 5,7-dihydroxy-2',4'-dimethoxyisoflavanone (4). The structures involving the absolute configuration of the new compounds were well elucidated by MS, IR, UV, CD, 1D and 2D NMR analyses. Cytotoxicity of the four compounds were assessed, results suggested that compound 2 possessed well cytotoxic activity, against the Hela, K562, and HL60 cell lines with $IC_{50}$ values of 28.0, 40.6 and $35.1{\mu}M$, respectively.
Remarkable impact of amino acids on ginsenoside transformation from fresh ginseng to red ginseng
Zhi Liu,Xin Wen,Chong-Zhi Wang,Wei Li,Wei-Hua Huang,Juan Xia,Chang-Chun Ruan,Chun-Su Yuan 고려인삼학회 2020 Journal of Ginseng Research Vol.44 No.3
Background: Amino acids are one of the major constituents in Panax ginseng, including neutral aminoacid, acidic amino acid, and basic amino acid. However, whether these amino acids play a role in ginsenosideconversion during the steaming process has not yet been elucidated. Methods: In the present study, to elucidate the role of amino acids in ginsenoside transformation fromfresh ginseng to red ginseng, an amino acids impregnation pretreatment was applied during thesteaming process at 120 C. Acidic glutamic acid and basic arginine were used for the acid impregnationtreatment during the root steaming. The ginsenosides contents, pH, browning intensity, and free aminoacids contents in untreated and amino acidetreated P. ginseng samples were determined. Results: After 2 h of steaming, the concentration of less polar ginsenosides in glutamic acidetreatedP. ginseng was significantly higher than that in untreated P. ginseng during the steaming process. However,the less polar ginsenosides in arginine-treated P. ginseng increased slightly. Meanwhile, free aminoacids contents in fresh P. ginseng, glutamic acid-treated P. ginseng, and arginine-treated P. ginsengsignificantly decreased during steaming from 0 to 2h. The pH also decreased in P. ginseng samples at hightemperatures. The pH decrease in red ginseng was closely related to the decrease in basic amino acidslevels during the steaming process. Conclusion: Amino acids can remarkably affect the acidity of P. ginseng sample by altering the pH value. Theywere the main influential factors for the ginsenoside transformation. These results are useful in elucidatingwhy andhowsteaming induces the structural change of ginsenoside in P. ginseng and also provides an effectiveand green approach to regulate the ginsenoside conversion using amino acids during the steaming process.
Remarkable impact of amino acids on ginsenoside transformation from fresh ginseng to red ginseng
Liu, Zhi,Wen, Xin,Wang, Chong-Zhi,Li, Wei,Huang, Wei-Hua,Xia, Juan,Ruan, Chang-Chun,Yuan, Chun-Su The Korean Society of Ginseng 2020 Journal of Ginseng Research Vol.44 No.3
Background: Amino acids are one of the major constituents in Panax ginseng, including neutral amino acid, acidic amino acid, and basic amino acid. However, whether these amino acids play a role in ginsenoside conversion during the steaming process has not yet been elucidated. Methods: In the present study, to elucidate the role of amino acids in ginsenoside transformation from fresh ginseng to red ginseng, an amino acids impregnation pretreatment was applied during the steaming process at 120℃. Acidic glutamic acid and basic arginine were used for the acid impregnation treatment during the root steaming. The ginsenosides contents, pH, browning intensity, and free amino acids contents in untreated and amino acid-treated P. ginseng samples were determined. Results: After 2 h of steaming, the concentration of less polar ginsenosides in glutamic acid-treated P. ginseng was significantly higher than that in untreated P. ginseng during the steaming process. However, the less polar ginsenosides in arginine-treated P. ginseng increased slightly. Meanwhile, free amino acids contents in fresh P. ginseng, glutamic acid-treated P. ginseng, and arginine-treated P. ginseng significantly decreased during steaming from 0 to 2h. The pH also decreased in P. ginseng samples at high temperatures. The pH decrease in red ginseng was closely related to the decrease in basic amino acids levels during the steaming process. Conclusion: Amino acids can remarkably affect the acidity of P. ginseng sample by altering the pH value. They were the main influential factors for the ginsenoside transformation. These results are useful in elucidating why and how steaming induces the structural change of ginsenoside inP. ginseng and also provides an effective and green approach to regulate the ginsenoside conversion using amino acids during the steaming process.
Cytotoxic Isoflavanones from Uraria clarkei
Xiang-Zhong Huang,Xi-Shan Bai,Hui Liang,Chao Wang,Wen-Juan Li,Junming Guo,Zhi-Yong Jiang 대한화학회 2013 Bulletin of the Korean Chemical Society Vol.34 No.5
Two new isoflavanones, (3R) 5,7,3',4'-tetrahydroxy-2'-methoxyisoflavanone (1) and (3R) 5',8-di-(γ,γ- dimethylallyl)-2',5-dihydroxyl-4',7-dimethoxyl-isoflavanone (2), were isolated from Uraria clarkei, together with two known compounds dalbergioidin (3), 5,7-dihydroxy-2',4'-dimethoxyisoflavanone (4). The structures involving the absolute configuration of the new compounds were well elucidated by MS, IR, UV, CD, 1D and 2D NMR analyses. Cytotoxicity of the four compounds were assessed, results suggested that compound 2 possessed well cytotoxic activity, against the Hela, K562, and HL60 cell lines with IC50 values of 28.0, 40.6 and 35.1 μM, respectively.
김길남,신운철,윤철남,송혜승,Zhi-Juan Huang,Qiu-Ying Huang,Chaoliang Lei 한국응용곤충학회 2019 Journal of Asia-Pacific Entomology Vol.22 No.2
The oriental armyworm, Mythimna separata Walker, is an important insect pest in eastern Asia. Green (520 nm) light with an exposure time of > 30 min can result in a stronger phototactic response than the wavelengths of other lights in M. separata moths. The present study was mainly focused to estimate the activities of several enzymes (such as glyceraldehyde-3-phosphate dehydrogenase (GAPDH), glycerol-3-phosphate dehydrogenase (GPDH), lactate dehydrogenase (LDH) and 3-hydroxyacyl-CoA dehydrogenase (HOAD)) involved in the energy metabolism and a ratio of HOAD to GAPDH activity in M. separata moths exposed to the green light for different exposure times. Our results showed that when M. separata moths were exposed to the green light for 30 min, the activities of the two enzymes (GPDH and HOAD) and as well as the ratio of HOAD to GAPDH activity were significantly elevated. The activity of LDH was significantly increased in the moths exposed for 60 min. Furthermore, significant differences in enzyme activities between the male and female moths were recorded in 45 min exposure time group of the GAPDH, all light treatment groups of the LDH, and 45 min group of the ratio of HOAD to GAPDH activity, respectively. We suggest that when M. separata adult moths are exposed to the green light, these enzymes can be activated to produce energy for starting the phototactic behavior to the green light. Our findings may provide a theoretical basis for elucidating a reason of the phototactic behavior of nocturnal moths.
( Ru Zhang ),( Xue-mei Huang ),( Hui-juan Yan ),( Xin-yi Liu ),( Qi Zhou ),( Zhi-yong Luo ),( Xiao-ning Tan ),( Bian-ling Zhang ) 한국미생물생명공학회(구 한국산업미생물학회) 2019 Journal of microbiology and biotechnology Vol.29 No.3
To investigate a novel β-glucosidase from Bifidobacterium breve ATCC 15700 (BbBgl) to produce compound K (CK) via ginsenoside F2 by highly selective and efficient hydrolysis of the C-3 glycoside from ginsenoside Rd, the BbBgl gene was cloned and expressed in E. coli BL21. The recombinant BbBgl was purified by Ni-NTA magnetic beads to obtain an enzyme with specific activity of 37 U/mg protein using pNP-Glc as substrate. The enzyme activity was optimized at pH 5.0, 35°C, 2 or 6 U/ml, and its activity was enhanced by Mn<sup>2+</sup> significantly. Under the optimal conditions, the half-life of the BbBgl is 180 h, much longer than the characterized β-glycosidases, and the Km and V<sub>max</sub> values are 2.7 mM and 39.8 μmol/mg/min for ginsenoside Rd. Moreover, the enzyme exhibits strong tolerance against high substrate concentration (up to 40 g/l ginsenoside Rd) with a molar biotransformation rate of 96% within 12 h. The good enzymatic properties and gram-scale conversion capacity of BbBgl provide an attractive method for large-scale production of rare ginsenoside CK using a single enzyme or a combination of enzymes.
Shao-Mei Yang,Fu-Nan Li,Zhi-Ning Huang,Zhong-Shi Zhou,Jin Hou,Man-Yi Zheng,Li-Juan Wang,Yu Jiang,Xin-Yi Zhou,Qiu-Yue Chen,Shan-Hua Li 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.10
To identify novel therapeutic agents to treatcancer, we synthesized a series of diaryl ether derivatives. Structure–activity relationship studies revealed that thepresence of a chlorine or hydroxyl at the para-position onthe phenyl ring (5h or 5k) significantly enhanced antitumoractivity. Compound 5h had stronger growth inhibitory activityin HepG2, A549, and HT-29 cells than compound 5k,with IC50 values of 2.57, 5.48, and 30.04 lM, respectively. Compound 5h also inhibited the growth of other cells lines,including Hep3B, PLC/PRF5, SMMC-7721, HeLa, andA375, with IC50 values of 2.76, 4.26, 29.66, 18.86, and10.21 lM, respectively. The antitumor activity of compound5h was confirmed by a colony forming assay. Further,our results indicated that the antitumor activity ofcompound 5h may be mediated by enhancing expression ofp21 and cl-caspase3, and leading to apoptosis of cancercells.