Structure-activity relationship of diosgenin derivatives as Bcl-2 antagonists / 药学学报

The purpose of this paper is to clarify the structure-activity relationship of anti-tumor activity of diosgenin derivatives in vitro. Study has found that diosgenin can inhibit the reproduction of tumor cells by inducing apoptosis and the main target spot of this effect is Bcl-2. Based on the characteristics of pharmacophoric points' of the three-dimensional pharmacophore for Bcl-2 inhibitors, we have docked lots of diosgenin derivatives with Bcl-2, then synthesized 31 compounds of them, finally assessed the anti-tumor activity of the diosgenin derivatives in vitro against A375, A549, HepG-2 and K562. Preliminary studies of SAR have indicated that the aliphatic esters, and aromatic esters of diosgenin without F ring have no anti-tumor activity in vitro. The triazole bromides of diosgenin all achieve fairly good anti-tumor activity in vitro, and those with larger hydrophobic group have the better activity. The stronger is the hydrogen bonding interaction and dipole-dipole interaction of the heterocyclic of diosgenin and diosgenin without F ring and the acid ester of diosgenin without F ring, the better is the activity of derivatives.

Diagnosis and treatment of primary liver cancer with cancer thrombus of the bile duct / 中国普通外科杂志

Objective To study the diagnosis and treatment of primary liver cancer(PLC) with bile duct cancer thrombus (BDT). Methods The clinical data of 21 patients with PLC and BDT admitted in the past 8 years were analyzed retrospectively . Results The major clinical manifestations were the symptoms of primary liver cancer and obstructive jaundice. The correct diagnosis rate was 76.2% before operation. The diagnosis rate of B-us, CT, MRI, ERCP and PTC was 14.3%, 9.52%, 14.3%, 71.4% and 100% respectively. The operative procedures included hepatectomy with removal of BDT ( n =10), hepatectomy combined with extrahepatic bile duct resection ( n =5), thrombectomy through choledochotomy with TACE ( n =3), removal of BDT with HAI ( n =3). The 3,5-year survival rate were 43.20% and 24.60% respectively. Conclusions Multi-examinations should be applied in the diagnosis of PLC with BDT. The comprehensive therapy including surgery and other therapies must be adoptted for PLC with BDT.