N-Terminal Acylation of Somatostatin Analog with Long Chain Fatty Acids Enhances Its Stability and Anti-Proliferative Activity in Human Breast Adenocarcinoma Cells

The anti-proliferative activity of the somatostatin analog RC-160 is limited by its short serum half life. To circumvent this limitation, fatty acids of chain lengths ranging from 4 to18 were individually conjugated to the N-terminal residue of RC-160. The lipophilized derivatives of RC-160 were syn...

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Veröffentlicht in:	Biological & pharmaceutical bulletin 2002, Vol.25(1), pp.29-36
Hauptverfasser:	Dasgupta, Piyali, Singh, Anu, Mukherjee, Rama
Format:	Artikel
Sprache:	eng
Schlagworte:	Acylation Adenocarcinoma - drug therapy anti-proliferative activity Antineoplastic agents Antineoplastic Agents, Hormonal - chemical synthesis Antineoplastic Agents, Hormonal - chemistry Antineoplastic Agents, Hormonal - pharmacology Binding, Competitive - drug effects Biological and medical sciences Breast Neoplasms - drug therapy Cell Division - drug effects Chemotherapy Cyclic AMP - metabolism Endopeptidases - metabolism Enzyme Inhibitors - pharmacology Fatty Acids - chemistry Female Freeze Drying Guanosine 5'-O-(3-Thiotriphosphate) - metabolism Half-Life Hormone Antagonists - chemical synthesis Hormone Antagonists - chemistry Hormone Antagonists - pharmacology Hormones. Endocrine system Humans lipophilization Medical sciences Pharmacology. Drug treatments protease resistance Protein-Tyrosine Kinases - antagonists & inhibitors Protein-Tyrosine Kinases - metabolism RC-160 serum resistance Signal Transduction - drug effects signaling mechanism Somatostatin - analogs & derivatives Somatostatin - chemistry Somatostatin - pharmacology Structure-Activity Relationship Tumor Cells, Cultured
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Zusammenfassung:	The anti-proliferative activity of the somatostatin analog RC-160 is limited by its short serum half life. To circumvent this limitation, fatty acids of chain lengths ranging from 4 to18 were individually conjugated to the N-terminal residue of RC-160. The lipophilized derivatives of RC-160 were synthesized, purified and characterized. The anti-proliferative activity of lipophilized-RC-160 on the human breast carcinoma cell line MCF-7, was evaluated in vitro. The long chain lipopeptides like pamitoyl-RC-160 exhibited significantly higher anti-proliferative activity on MCF-7 cells (p
ISSN:	0918-6158 1347-5215
DOI:	10.1248/bpb.25.29