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Sulfur and nitrogen-containing compounds from the whole bodies of Blaps japanensis.
- Source :
-
Bioorganic chemistry [Bioorg Chem] 2020 Sep; Vol. 102, pp. 104086. Date of Electronic Publication: 2020 Jul 10. - Publication Year :
- 2020
-
Abstract
- Pipajiains H-J (1-3), three new phenolic derivatives with an unusual sulfone group, pipajiamides A-C (4-6), three new amide derivatives, pipajiaine A (7), one new imidazole analogue, and pipajiaine B (8), a pair of new pyrrolidine derivatives, along with three known compounds were isolated from the insect Blaps japanensis. Their structures were identified by spectroscopic and computational methods. Chiral HPLC was used to separate the (-)- and (+)-antipodes of 4 and 8. Biological activities of all the new compounds against extracellular matrix in rat renal proximal tubular cells, human cancer cells (A549, Huh-7, and K562), COX-2, ROCK1, and JAK3 were evaluated. The results show that compounds 2, (+)-4, and (-)-4 are active against kidney fibrosis, whereas, compound 9 is active toward human cancer cells, inflammation, and JAK3 kinase.<br />Competing Interests: Declaration of Competing Interest The authors declare no conflict of interest.<br /> (Copyright © 2020 Elsevier Inc. All rights reserved.)
- Subjects :
- Animals
Cells, Cultured
Density Functional Theory
Dose-Response Relationship, Drug
Fibrosis drug therapy
Humans
Janus Kinase 3 antagonists & inhibitors
Janus Kinase 3 metabolism
Molecular Structure
Nitrogen Compounds chemistry
Nitrogen Compounds isolation & purification
Protein Kinase Inhibitors chemistry
Protein Kinase Inhibitors isolation & purification
Rats
Structure-Activity Relationship
Sulfur chemistry
Sulfur isolation & purification
rho-Associated Kinases antagonists & inhibitors
rho-Associated Kinases metabolism
Coleoptera chemistry
Nitrogen Compounds pharmacology
Protein Kinase Inhibitors pharmacology
Sulfur pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1090-2120
- Volume :
- 102
- Database :
- MEDLINE
- Journal :
- Bioorganic chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 32688114
- Full Text :
- https://doi.org/10.1016/j.bioorg.2020.104086