ABSTRACT
AIM@#To study the bufadienolides in the Chinese traditional drug "Ch'an Su" and their cytotoxic activity.@*METHOD@#Various chromatographic techniques were used to isolate the constituents, and their structures were elucidated through physical and spectroscopic data.@*RESULTS@#Twenty compounds were isolated, and eighteen were evaluated in vitro for their cytotoxic activity against A-549 and K-562 cells.@*CONCLUSION@#Compound 1 (bufalin 3β-acrylic ester) was a new bufadienolide and exhibited the most potent activity against the two tumor cell lines with IC50 values of 7.16 and 6.83 nmol · L(-1). The relationships between structure and activity are discussed.
Subject(s)
Humans , Amphibian Venoms , Chemistry , Pharmacology , Therapeutic Uses , Antineoplastic Agents , Chemistry , Pharmacology , Therapeutic Uses , Biological Products , Chemistry , Pharmacology , Therapeutic Uses , Bufanolides , Chemistry , Pharmacology , Therapeutic Uses , Inhibitory Concentration 50 , K562 Cells , Medicine, Chinese Traditional , Molecular Structure , Neoplasms , Drug Therapy , Structure-Activity RelationshipABSTRACT
AIM: To examine the effect of acrylic ester and thermosol respectively as pressure sensitive adhesive matrix of zhitong huoxue extract ( Rhizoma Corydalis,Radix aconiti,Radix Paeoniae alba,Radix et notoginseng ginseng,etc) on the dissolution of effective constituent from zhitong huoxue extract.METHODS: The in vitro release experiment was carried out on Permcell diffusion cell,HPLC method was applied to determining the cumulative elease rate of tetrahydropalmatine,aconitine,paeoniflorin and ginsenoside Rg_1 from zhitong huoxue pressure sensitive adhensive.RESULTS: The acrylic ester matrix had sound controlled release profile in vitro of alkaloid components.In KT-A thermosol matrix,the in vitro release rate proved to be inversely proportional to the molecular weight (R = 0.91 ) of the effective constituents,while the 2501 s matrix presented a steadily cumulative release rate over 12 h (30% -43% ).CONCLUSION: Good release rates are observed with effective constituent with small molecular weight,adhesive composition of matrix has an obvious effect on the in vitro release behavior of zhitong huoxue extract.
ABSTRACT
AIM:To examine the effect of acrylic ester and thermosol respectively as pressure sensitive adhesive matrix of zhitong huoxue extract(Rhizoma Corydalis,Radix aconiti,Radix Paeoniae alba,Radix et notoginseng ginseng,etc)on the dissolution of effective constituent from zhitong huoxue extract.METHODS:The in vitro release experiment was carried out on Permcell diffusion cell,HPLC method was applied to determining the cumulative elease rate of tetrahydropalmatine,aconitine,paeoniflorin and ginsenoside Rg_1 from zhitong huoxue pressure sensitive adhensive.RESULTS:The acrylic ester matrix had sound controlled release profile in vitro of alkaloid components.In KT-A thermosol matrix,the in vitro release rate proved to be inversely proportional to the molecular weight(R= 0.91)of the effective constituents,while the 2501 s matrix presented a steadily cumulative release rate over 12 h(30%-43%).CONCLUSION:Good release rates are observed with effective constituent with small molecular weight,adhesive composition of matrix has an obvious effect on the in vitro release behavior of zhitong huoxue extract.