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Design, synthesis and evaluation of 5-substituted 1-H-tetrazoles as potent anticonvulsant agents
Aimei LIAO,Tiantian Wang,Bangrong Cai,Yi Jin,천승훈,ChangJu Chun,Zengtao Wang 대한약학회 2017 Archives of Pharmacal Research Vol.40 No.4
A series of 5-substituted 1-H-tetrazoles weredesigned and synthesized as potent anticonvulsant agents. Their preliminary anticonvulsant activities were evaluatedusing maximal electroshock and subcutaneouspentylenetetrazole (scPTZ) seizure tests. Neurotoxicity wasdetermined using rotarod test. The results indicated that thecompound 2j in scPTZ model exhibited the ED50 values of83.3 mg/kg, superior to the standard drug ethosuximidewith the maximum activity. In addition, compound 2kshowed the most potent activity in MES model with ED50value of 9.6 mg/kg and TD50 value of 189.5 mg/kg afterintraperitoneal injection in mice, and displayed a highprotective index (TD50/ED50) of 19.7 compared to referenceantiepileptic drugs.
( Bangrong Cai ),( Aimei Liao ),( Kyung-ku Lee ),( Jae-sam Ban ),( Hyun-sam Yang ),( Young Jun Im ),( Changju Chun ) 전남대학교 약품개발연구소 2016 약품개발연구지 Vol.25 No.-
A series of methotrexate-diosgenin conjugates was designed and synthesized to enhance the passive internalization of methotrexate (MTX) in to transport-resistant cells. The inhibitory effects of these con-jugates on dihydrofolate reductase (DHFR), and their anti-proliferation behaviors against a transport-resistant breast cancer cell line, MDA-MB-231, were investigated. All of the synthesized conjugates retained an ability to inhibit DHFR after the diosgenin substitution. The MTX conjugates were much more potent against methotrexate-resistant MDA-MB-231 cells than MTX. Conjugate 18, containing a disulfide bond, exhibited the most potent anti-proliferative and DHFR inhibitory effects (IC<sub>50</sub>=4.1 μM and 17.21 nM, respectively). Anti-proliferative activity was higher in the conjugate with a longer space linker (conjugate 21) than those with shorter linkers (conjugates 19 and 20). These results suggest that dios-genin conjugation of MTX may be an effective way to overcome its transport resistance in cancer cells. ⓒ 2016 Elsevier Inc. All rights reserved.
Xinlong Wan,홍미연,Aimei LIAO,김만일,김기경,한연수,김익수 한국곤충학회 2012 Entomological Research Vol.42 No.1
In the present study, we report the 16 823-bp long complete mitochondrial genome (mitogenome) of a carabid beetle, Damaster mirabilissimus mirabilissim (Coleoptera: Carabidae), which is endangered in Korea. The gene arrangement of D. m. mirabilissim mitogenome is identical to the most common type found in insects. The start codon of the D. m. mirabilissim COI gene is a typicalATN codon. On the other hand, the initiation codon for ND1 gene is TTG, instead of ATN. All transfer RNAs (tRNAs) exhibit a stable canonical clover-leaf structure, except for tRNASer(AGN), the dihydrouridine arm of which forms a simple loop. The 1703-bp long A+T-rich region is the second longest among the complete adephagan mitogenome sequences, next to Macrogyrus oblongus belonging to Gyrinoidea. One of the unusual features of the genome is the presence of a tRNALeu(UUR)-like sequence in the A+T-rich region. This sequence displays the proper anticodon sequence and the potential to form secondary structures, but also harbors many mismatches in the stems.
Joong Won Park,Sun Young Park,Min Jee Kim,Jeong Sun Park,Ah Rha Wang,Aimei Liao,Tae Hwa Kang,Hae Chul Park,Iksoo Kim 한국응용곤충학회 2011 한국응용곤충학회 학술대회논문집 Vol.2011 No.05
The leaf beetle, Chrysolina aurichalcea (Coleoptera: Chysomelidae), is a pest damaging plants of Compositae. In order to understand the genetic diversity and geographic variation of the species we sequenced a portion of mitochondrial COI gene (658 bp) and complete nuclear internal transcribed spacer 2 (ITS2) collected from seven Korean localities. A total of 18 haplotypes (BARCA01 ~ BARCA18), with the maximum sequence divergence of 3.04% (20 bp) were obtained from COI gene sequence, whereas 17 sequence types (ITS2CA01 ~ ITS2CA17), with the maximum sequence divergence of 2.013% (9 bp) were obtained from ITS2, indicating substantially larger sequence divergence in mitochondrial gene sequence. Phylogenetically, the mitochondrial DNA has shown several haplotypes formed independent groups with substantially high node support (≥ 90%), whereas no such grouping was evidenced for ITS2, indicating different behaviors of the two molecules. Such difference may reflect a diverse dynamics of the species such as biogeographic history, mating behaviors, and also possibly different mode of inheritance of the two molecules, but requires further scrutinized examination of the dataset. In terms of population genetic perspective, overall no population subdivision was detected from both molecules, except for locality 7 (Eocheong islet) from mitochondrial DNA. As more scrutinized analysis is performed, further fruitful inference on the geographic contour of the species might be available.