Preparation and Antitumor Activity of a Tamibarotene-Furoxan Derivative

Wang, Xue-Jian,Duan, Yu,Li, Zong-Tao,Feng, Jin-Hong,Pan, Xiang-Po,Zhang, Xiu-Rong,Shi, Li-Hong,Zhang, Tao Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.15

Multi-target drug design, in which drugs are designed as single molecules to simultaneously modulate multiple physiological targets, is an important strategy in the field of drug discovery. QT-011, a tamibarotene-furoxan derivative, was here prepared and proposed to exert synergistic effects on antileukemia by releasing nitric oxide and tamibarotene. Compared with tamibarotene itself, QT-011 displayed stronger antiproliferative effects on U937 and HL-60 cells and was more effective evaluated in a nude mice U937 xenograft model in vivo. In addition, QT-011 could release nitric oxide which might contribute to the antiproliferative activity. Autodocking assays showed that QT-011 fits well with the hydrophobic pocket of retinoic acid receptors. Taken together, these results suggest that QT-011 might be a highly effective derivative of tamibarotene and a potential candidate compound as antileukemia agent.

Construction of Modified Bacillus thuringiensis cry1Ac Genes for Transgenic Crop Through Multi Site-directed Mutagenesis

Hong Guang Xu,Jong Yul Roh,Yong Wang,Jae Young Choi,Hee Jin Shim,Qin Liu,Xue Ying Tao,Soo Dong Woo,Byung Rae Jin,Yeon Ho Je 한국잠사학회 2009 International Journal of Industrial Entomology Vol.19 No.1

The newly cloned Bacillus thuringiensis cry1-5 gene showed high activity to both Plutella xylostella and Spodoptera exigua, while cry1Ac only showed high activity against P. xylostella but low to S. exigua. Through the alignment of amino acid sequences between Cry1Ac and Cry1-5, we found 12 different residues in domain I (6 residues) and domain II (6 residues). In this study, the modified cry1Ac gene, which is constructed according to a crop-preferring codon usage, was used as a template to construct mutant B. thuringiensis cry1Ac genes based on cry1-5 gene through multi site-directed mutagenesis. Total 63 various mutant cry genes were obtained at 12 positions randomly. Among them, ten mutant cry genes, whose domain I was totally converted and domain II was randomly, were selected to express in baculovirus expression system as a polyhedrin fusion form. The recombinant proteins were 95 kDa in size and were stably activated as 65 kDa by trypsin. The expressed mutant Cry proteins were applied to bioassays against P. xylostella and S. exigua. All mutants showed high insecticidal activity both to P. xylostella and S. exigua similar to cry1-5. These results suggest that these mutant cry genes might be expected of desirable cry genes for introduction to transgenic crops.

Clinical Value of Eukaryotic Elongation Factor 2 (eEF2) in Non-small Cell Lung Cancer Patients

Sun, Hong-Gang,Dong, Xue-Jun,Lu, Tao,Yang, Ming-Feng,Wang, Xing-Mu Asian Pacific Journal of Cancer Prevention 2013 Asian Pacific journal of cancer prevention Vol.14 No.11

Background: The purpose of this study was to evaluate a new type of tumor biomarker, eukaryotic elongation factor 2 (eEF2), in serum for the early diagnosis, confirmative diagnosis as well as assessment of treatment of non-small cell lung cancer (NSCLC). Methods: 130 patients with NSCLC and 50 healthy individuals undergoing physical examination in our hospital provided the observation and healthy control groups. An enzyme linked immune sorbent assay (ELISA) method was applied to determine serum eEF2 levels. Serum neuron specific enolase (NSE) and squamous cell carcinoma antigen (SCC) levels in the observation group were assessed with an automatic biochemical analyzer. Results: The median levels of eEF2 in the serum of NSCLC patients was found to be significantly higher than the healthy control group (p < 0.01) and it was markedly higher in stages III, IV than stages I, II (p < 0.05). eEF2 was higher with tumor size ${\geq}2$ cm than <2 cm (P< 0.01). Furthermore, two weeks after surgery patients showed a significant trend for eEF2 decrease (p < 0.05). Conclusions: The eukaryotic elongation factor 2 (eEF2) has certain clinical values for early diagnosis, verification, and prognosis as well as classification of lung cancer patients.

Effect of Growth on Fatty Acid Composition of Total Intramuscular Lipid and Phospholipids in Ira Rabbits

Shan Xue,Zhi-Fei He,Jingzhi Lu,Xiaoqi Tao,Li Zheng,Yuejie Xie,Xia Xiao,Rong Peng,Hong-Jun Li 한국축산식품학회 2015 한국축산식품학회지 Vol.35 No.1

The changes in fatty acid composition of total intramuscular lipid and phospholipids were investigated in the longissimusdorsi, left-hind leg muscle, and abdominal muscle of male Ira rabbits. Changes were monitored at 35, 45, 60, 75, and 90 d. Analysis using gas chromatography identified 21 types of fatty acids. Results showed that the intramuscular lipid increasedand the intramuscular phospholipids (total intramuscular lipid %) decreased in all muscles with increasing age (p<0.05). Anabundant amount of unsaturated fatty acids, especially polyunsaturated fatty acids, was distributed in male Ira rabbits atdifferent ages and muscles. Palmitic acid (C16:0), stearic acid (C18:0), oleic acid (C18:1), linoleic acid (C18:2), and arachi-donic acid (C20:4) were the major fatty acids, which account to the dynamic changes of the n-6/n-3 value in Ira rabbit meat.

Pharmacokinetic Behavior of Gentiopicroside From Decoction of Radix Gentianae,

Chang-hong Wang,Xue-mei Cheng,Yu-qi He,Kenneth N. White,S. W. Annie Bligh,Christopher J. Branford-White,Zheng-tao Wang 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.9

The pharmacokinetics in rats of gentiopicroside (GPS) from orally administered decoctions of Radix Gentianae (DRG) and Gentiana macrophlla (DGM) were compared with that of GPS alone administered at 150 mg/kg orally and 30 mg/kg intravenously. The metabolic profile of GPS after intravenous injection could be fitted to two-compartment model whereas oral administration decoctions DRG or DGM, or GPS alone, could all be fitted to a one-compartment model. After oral administration of GPS alone, GPS was absorbed quickly and reached a maximum plasma concentration (Cmax) value, 5.78 ± 2.24 µg/mL within 0.75 ± 0.62 h. The plasma level of GPS declined with a T1/2ke, 3.35 ± 0.76 h. After oral administration of decoctions DRG and DGM, GPS was absorbed and reached significantly higher maximum concentrations of 10.53 ± 3.20 µg/mL (p < 0.01) and 7.43 ± 1.64 µg/mL (p < 0.05) at later time points 1.60 ± 0.76 (p < 0.01) and 2.08±0.74 h (p < 0.05), for DRG and DGM respectively, compared with oral GPS alone. Significantly larger AUC values were found for decoctions of GPS (83.49 ± 20.8 µg·h/mL for DRG and 59.43 ± 12.9 µg·h/mL for DGM) compared with oral GPS alone (32.67 ± 12.9 µg·h/mL). The results demonstrate that the bioavailability of GPS was markedly improved when administered as a decoction than as purified GPS. The decoction from Radix Gentianae provided 2.5 times better bioavailability and that from Gentiana macrophlla 1.8 times higher. The study confirms the importance of careful pharmacokinetic analysis in the characterization of herbal medicines when applied for future clinical applications.

Pharmacokinetic Behavior of Gentiopicroside From Decoction of Radix Gentianae, Gentiana Macrophylla After Oral Administration in Rats: a Pharmacokinetic Comaprison with Gentiopicroside after Oral and Intravenous Administration Alone

Wang, Chang-Hong,Cheng, Xue-Mei,He, Yu-Qi,White, Kenneth N.,Bligh, S.W.Annie,Branford-White, Christopher J.,Wang, Zheng-Tao 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.9

The pharmacokinetics in rats of gentiopicroside (GPS) from orally administered decoctions of Radix Gentianae (DRG) and Gentiana macrophlla (DGM) were compared with that of GPS alone administered at 150 mg/kg orally and 30 mg/kg intravenously. The metabolic profile of GPS after intravenous injection could be fitted to two-compartment model whereas oral administration decoctions DRG or DGM, or GPS alone, could all be fitted to a one-compartment model. After oral administration of GPS alone, GPS was absorbed quickly and reached a maximum plasma concentration ($C_{max}$) value, 5.78 ${\pm}$ 2.24 ${\mu}g/mL$ within 0.75 ${\pm}$ 0.62 h. The plasma level of GPS declined with a $T_{1/2ke}$, 3.35 ${\pm}$ 0.76 h. After oral administration of decoctions DRG and DGM, GPS was absorbed and reached significantly higher maximum concentrations of 10.53 ${\pm}$ 3.20 ${\mu}g/mL$ (p < 0.01) and 7.43 ${\pm}$ 1.64 ${\mu}g/mL$ (p < 0.05) at later time points 1.60 ${\pm}$ 0.76 (p < 0.01) and 2.08${\pm}$0.74 h (p < 0.05), for DRG and DGM respectively, compared with oral GPS alone. Significantly larger AUC values were found for decoctions of GPS (83.49 ${\pm}$ 20.8 ${\mu}g{\cdot}h/mL$ for DRG and 59.43 ${\pm}$ 12.9 ${\mu}g{\cdot}h/mL$ for DGM) compared with oral GPS alone (32.67 ${\pm}$ 12.9 ${\mu}g{\cdot}h/mL$. The results demonstrate that the bioavailability of GPS was markedly improved when administered as a decoction than as purified GPS. The decoction from Radix Gentianae provided 2.5 times better bioavailability and that from Gentiana macrophlla 1.8 times higher. The study confirms the importance of careful pharmacokinetic analysis in the characterization of herbal medicines when applied for future clinical applications.

Effect of structural phase transformations under pressure on electronic and optical properties of CuInS2

Bo Gao,Hong-Tao Xue,Fu-Ling Tang,Yu-Wen Cheng 한국물리학회 2017 Current Applied Physics Vol.17 No.11

First-principles plane-wave calculations were employed to study the phase transitions, electronic and optical properties of chalcopyrite CuInS2 (CIS) under pressure, which is a promising semiconductor compound material for nonlinear optical, photovoltaic and bio-applications. From the variations of Gibbs free energy and volume with pressure, we confirmed an experimentally found phase transformation of CIS from tetragonal I42d structure into the cubic Fm3m phase. It occurs at 7.9 GPa with a volume reduction of 15.6%, which are comparable with the experimental values of 9.5 GPa and 12%. A new possible phase transition of CIS from the cubic Fm3m structure to the orthorhombic Cmcm structure under higher pressure was predicted occurring at 49.6 GPa with a volume reduction about 0.64%. Using the more accurate HSE06 functional, we found that the growth rate of energy gap with pressure (dEg/dP) for the I42d phase is about 24.8 meV/GPa, very close to the experimental value of 24 meV/GPa. The calculated electronic properties for Fm3m and Cmcm phases show that CIS is a metallic material under high pressure, rather than a semiconductor. The optical absorption spectra indicate that with the increase of pressure the absorption edge of CIS becomes smaller while the optical energy gap is larger.

Identification and Characterization of Alternaria iridiaustralis Causing Leaf Spot on Iris ensata in China

( Huan Luo ),( Ya Qun Tao ),( Xiao Yan Fan ),( Sang Keun Oh ),( Hong Xue Lu ),( Jian Xin Deng ) 한국균학회 2018 Mycobiology Vol.46 No.2

In 2016, a severe leaf spot disease was found on Iris ensata Thumb. in Nanjing, China. The symptom was elliptical, fusiform, or irregularly necrotic lesion surrounded by a yellow halo, from which a small-spored Alternaria species was isolated. The fungus was identified as Alternaria iridiaustralis based on morphological characteristics. The pathogenicity tests revealed that the fungus was the causal pathogen of the disease. Phylogenic analyses using sequences of ITS, gpd, endoPG, and RPB2 genes confirmed the morphological identification. This study is the first report of A. iridiaustralis causing leaf spots on I. ensata in China.

Impact of Caspase-8 (CASP8) -652 6N Del and D302H Polymorphisms on Prostate Cancer in Different Ethnic Groups

Zhang, Cheng-Dong,Li, Hong-Tao,Liu, Kun,Lin, Zhi-Di,Peng, Qi-Liu,Qin, Xue,He, Min,Wu, Hua,Mo, Zeng-Nan,Yang, Xiao-Li Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.18

Background: Despite evidence suggesting roles for caspase-8 (CASP8) -652 6N del and D302H polymorphisms in prostate cancer (PCa), the association of these polymorphisms with PCa risk remains inconclusive. Therefore, a meta-analysis was performed to more precisely estimate the association of CASP8 -652 6N del and D302H polymorphisms with PCa susceptibility. Materials and Methods: A comprehensive literature search was conducted to identify all case-control studies of CASP8 D302H and -652 6N del polymorphisms and PCa risk. Odds ratios (ORs) and 95% confidence intervals (CIs) were used to assess the strength of the association and the precision of the estimate, respectively. Results: Nine -625 6N del studies and 4 D302H studies were included. CASP8 -652 6N del and D302H polymorphisms were not significantly associated with PCa risk in the overall analyses. However, in the subgroup analysis stratified by ethnicity, -625 6N del was significantly associated with PCa risk in the East Asian and Indian populations under the recessive model. Furthermore, the subgroup analysis strongly suggested that D302H was associated with lower PCa risk in the Non-Indian population under the dominant model. Conclusions: In our meta-analysis, ethnic-specific differences were evident in the association of CASP8-625 6N del and D302H polymorphisms with PCa risk.

Two new ursane-type triterpenoid saponins from Elsholtzia bodinieri

Jin-Dong Zhong,Xue-Wei Zhao,Xuan-Qin Chen,Hong-Mei Li,Chin-Ho Chen,Xue-Shan Xia,Rong-Tao Li 대한약학회 2016 Archives of Pharmacal Research Vol.39 No.6

Two new ursane-type triterpenoid saponins,bodiniosides M (1) and N (2), along with three knownsaponins, oblonganosides I (3), pseudobuxussaponin B (4)and bodinioside A (5), were isolated from the aerial partsof Elsholtzia bodinieri. The structures of compounds 1 and2 were characterized by spectroscopic data as well as acidhydrolysis and GC analysis as 3-O-b-D-xylopyranosyl-19ahydroxy-23-acetoxy-urs-12(13)-en-28-oic acid 28-O-a-Lrhamnopyranosyl-(1-2)-b-D-glucopyranoside and 3-O-b-Dglucopyranosyl-2a,19a-dihydroxy-urs-12(13)-en-28,20blactone. Compounds 1 and 5 exhibited potent anti-HCVactivities in vitro with a selective index of 6.53 and 4.41,respectively.