Ryu, Jae-Chun Kim, Youn-Jung Kim, Mi-Soon Kim, Min-Ji Sarma, Sailendra Nath Jung, Sang-Hun 2024-01-21T04:13:39Z 2024-01-21T04:13:39Z 2021-09-03 2005-09-30 1738-642X https://pubs.kist.re.kr/handle/201004/136118 To develop the novel anti-allergic drug, many sophoricoside derivatives were synthesized. Among these derivatives, JSH-II-3, VI-3, VII-3, VIII-3, VII-20 and VII-20 (sodium salt) were selected and subjected to high throughput toxicity screening (HTTS) because they revealed strong IL-5 inhibitory activity and limitation of quantity. Single cell gel electrophoresis (Comet) assay, mouse lymphoma thymidine kinase (tk(+/-)) gene assay (MOLY), chromosomal aberration assay in mammalian cells and Ames reverse mutation assay in bacterial system were used as simplified, inexpensive, short-term in vitro screening tests in our laboratory. Through the primary screening using the comet assay, we could choose the first candidates of sophoricoside derivatives with no genotoxic potentials as JSH-VI-3, VII-3, VII-20 and VII-20 (sodium salt). Also JSH- VII-3, VII-20 and VII-20 (sodium salt) are non-mutagenic in MOLY assay, while JSH-II-3 is mutagenic at high concentration with the presence of metabolic activation system in both comet assay and MOLY assay. The selected derivatives (JSH-VI-3, VII-3, VII-20 and VII-20 (sodium salt) are not mutagenic in S. typhimurium TA98 and TA100 strains both in the presence and absence of metabolic activation. From results of chromosomal aberration assay, 6 h treatment of JSH-VI-3, VII-3 and VII-20 (sodium salt) were not revealed clastogenicity both in the presence and absence of S-9 mixture. Therefore, we suggests that JSH-VI-3, VII-3, VII-20 and VII-20 (sodium salt), as the optimal candidates with both no genotoxic potential and IL-5 inhibitory effects must be chosen. To process the development into new anti-inflammatory drug of these derivatives, further investigation will need. English KOREAN SOCIETY TOXICOGENOMICS & TOXICOPROTEOMICS-KSTT IN-VITRO AIRWAY HYPERRESPONSIVENESS ASSAY CARCINOGENS MUTAGENS IL-5 ANALOGS Genotoxicity on structural derivatives of sophoricoside, a component of Sophora japonica, in bacterial and mammalian cells Article 1 MOLECULAR & CELLULAR TOXICOLOGY, v.1, no.3, pp.179 - 188 MOLECULAR & CELLULAR TOXICOLOGY 1 3 179 188 scie 000243595800006 Biochemistry & Molecular Biology Toxicology Biochemistry & Molecular Biology Toxicology Article IN-VITRO AIRWAY HYPERRESPONSIVENESS ASSAY CARCINOGENS MUTAGENS IL-5 ANALOGS sophoricoside derivatives genotoxicity comet assay MOLY assay chromosomal aberration assay Ames reverse mutation assay anti-inflammatory effect