ABSTRACT
By introducing octyloxy to C-3 and alkyl groups to C-8 of jatrorrhizine, a series of 3-octyloxy-8-alkyljatrorrhizine derivatives were synthesized and their antimicrobial activities were evaluated in vitro. The results indicated that the derivatives exhibited high antimicrobial activities, especially against Gram-positive bacteria. The 3-octyloxy-8-butyljatrorrhizine displayed the highest antimicrobial activity in all compounds. Their structure-activity relationships were discussed.
Subject(s)
Bacteria/drug effects , Berberine , Candida tropicalis/drug effects , Drugs, Chinese Herbal , Berberine/analogs & derivatives , Berberine/chemical synthesis , Berberine/chemistry , Berberine/pharmacology , Drugs, Chinese Herbal/chemical synthesis , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/pharmacology , Microbial Sensitivity Tests , Molecular Structure , Ranunculaceae/chemistryABSTRACT
The compounds 3-ethoxy- ( 2), 3-butoxy- ( 3), 3-hexyloxy- ( 4), 3-octyloxy- ( 5), 3-decyloxy- ( 6) and 3-dodecyloxyjatrorrhizine chlorides ( 7) were synthesized and tested for their antimicrobial activity in vitro to evaluate structure-activity relationships. Substitution of the H with alkyl groups at C-3-OH led to significant changes in the antimicrobial activity. The antimicrobial activity of the substituted derivatives was 32 - 1000 times higher than that of jatorrhizine ( 1), which increased as the aliphatic chain was elongated and then decreased slightly when the alkyl chain exceeded eight carbon atoms. 3-Octyloxyjatrorrhizine ( 5) displayed the highest antimicrobial activity of all compounds. The LD (50) values of compounds 1 - 7 were more than 6000 mg/kg body weight, showing a low toxicity. The toxicities of compounds 2 - 7 were slightly lower than that of ( 1).
Subject(s)
Anti-Infective Agents/analysis , Berberine/analogs & derivatives , Berberine/analysis , Coptis/chemistry , Drugs, Chinese Herbal/chemistry , Microbial Sensitivity Tests , Toxicity TestsABSTRACT
OBJECTIVE: An intrinsically colored machinable glass-ceramic containing tetrasilicic fluormica as the predominant crystal phase was studied, which was used in molar crown in dental CAD/CAM system. METHODS: Orthogonal design analysis was used to select appropriate base formula, coloration and heat treatment process. RESULTS: Factors influencing the color appearance of mica glass ceramic were nucleation agent and the ratio of Mg(2+) to K(+) in base formula; Cerium oxide (CeO(2)) was used as the main coloration; The preferred heat treatment was 650 degrees C for 1 h and 1,000 degrees C or 1,050 degrees C for 3 h - 4 h. CONCLUSIONS: This mica glass-ceramic could provide 4 to 5 color appearance for dental use, it showed excellent machinability which was eminently suitable for use in dental CAD/CAM system.
