A Lipophilic Pt(IV) Oxaliplatin Derivative Enhances Antitumor Activity

Side effects and acquired resistance by cancer cells limit the use of platinum anticancer drugs. Modification of oxaliplatin (OXA) into a lipophilic Pt­(IV) complex [Pt­(DACH)­(OAc)­(OPal)­(ox)] (<b>1</b>), containing both lipophilic and hydrophilic axial ligands, was applied to improve performance and facilitate incorporation into polymeric nanoparticles. Complex <b>1</b> exhibited unique potency against a panel of cancer cells, including cisplatin-resistant tumor cells. [Pt­(DACH)­(OAc)­(OPal)­(ox)] incorporated nanoparticles (<b>2</b>) presented a mean diameter of 146 nm with encapsulation yields above 95% as determined by HPLC. Complexes <b>1</b> and <b>2</b> showed enhanced <i>in vitro</i> cellular Pt accumulation, DNA platination, and antiproliferative effect compared to OXA. Results of an orthotopic intraperitoneal model of metastatic ovarian cancer (SKOV-3) and a xenograft subcutaneous model of colon (HCT-116) tumor in SCID-bg mice showed that the activity of <b>1</b> and <b>2</b> significantly decreased tumor growth rates compared to control and OXA treatment groups. Consequently, these findings warrant further development toward clinical translation

A Lipophilic Pt(IV) Oxaliplatin Derivative Enhances Antitumor Activity

Side effects and acquired resistance by cancer cells limit the use of platinum anticancer drugs. Modification of oxaliplatin (OXA) into a lipophilic Pt­(IV) complex [Pt­(DACH)­(OAc)­(OPal)­(ox)] (<b>1</b>), containing both lipophilic and hydrophilic axial ligands, was applied to improve performance and facilitate incorporation into polymeric nanoparticles. Complex <b>1</b> exhibited unique potency against a panel of cancer cells, including cisplatin-resistant tumor cells. [Pt­(DACH)­(OAc)­(OPal)­(ox)] incorporated nanoparticles (<b>2</b>) presented a mean diameter of 146 nm with encapsulation yields above 95% as determined by HPLC. Complexes <b>1</b> and <b>2</b> showed enhanced <i>in vitro</i> cellular Pt accumulation, DNA platination, and antiproliferative effect compared to OXA. Results of an orthotopic intraperitoneal model of metastatic ovarian cancer (SKOV-3) and a xenograft subcutaneous model of colon (HCT-116) tumor in SCID-bg mice showed that the activity of <b>1</b> and <b>2</b> significantly decreased tumor growth rates compared to control and OXA treatment groups. Consequently, these findings warrant further development toward clinical translation

Biliary tract intraductal papillary mucinous neoplasm: A brief report and review of literature

Biliary Tract Intraductal Papillary Mucinous Neoplasm (BT-IPMN) is a very rare entity, gradually emerging into attention as sporadic cases are being reported worldwide. In this brief report we discuss about such an entity from our part of the world, based on a case from our institution. A 47-year-old female was referred to our department with jaundice, intermittent fever with chills and rigor of 6 weeks duration. Initial evaluation revealed obstructive jaundice with distended gall bladder. Imaging with ultrasonogram (USG) and magnetic resonance imaging (MRI) showed hugely dilated intra and extrahepatic biliary radicles with multiple and diffuse soft tissue lesions filling the common bile duct (CBD) extending to the ductal system of left lobe of liver. A side viewing endoscopy demonstrated mucin extruding from a prominent ampulla of Vater. The patient was managed successfully by left hepatectomy with pancreaticoduodenectomy (HPD). Gross pathological examination of the specimen showed marked dilatation of intra and extra hepatic bile ducts with multiple polypoidal lesions and plenty of mucin filling the entire biliary ductal system. Histopathology revealed predominantly intraductal papillary mucinous adenocarcinoma at the hilum extending to left bile duct with diffuse dysplastic changes throughout the biliary tree. Thus the clinical, radiological and pathological features of this lesion clearly fit into the diagnosis of BT-IPMN, which is slowly being established as a definite clinical entity with features much similar to its pancreatic counterpart