Structurally diverse cucurbitane-type triterpenoids from the tubers of Hemsleya chinensis with cytotoxic activity.

Ten previously undescribed cucurbitane-type triterpenoids, namely hemslyencins A-F (1-6) and hemslyencosides A-D (7-10), together with twenty previously reported compounds (11-30), were isolated from the tubers of Hemsleya chinensis. Their structures were elucidated by unambiguous spectroscopic data (UV, IR, HR-ESI-MS, 1D and 2D NMR data). Hemslyencins A and B (1 and 2) possessing unique 9, 11-seco-ring system with a six-membered lactone moiety, were the first examples among of the cucurbitane-type triterpenoids, and hemslyencins C and D (3 and 4) and hemslyencoside D (10) are the infrequent pentacyclic cucurbitane triterpenes featuring a 6/6/6/5/6 fused system. The cytotoxic activities of all isolated compounds were evaluated against MCF-7, HCT-116, HeLa, and HepG2 cancer cells, and their structure-activity relationships (SARs) was discussed as well. Compounds 17, 25, and 26 showed significant cytotoxic effects with IC50 values ranging from 1.31 to 9.89 µM, among which compound 25 induced both apoptosis and cell cycle arrest at G2/M phase in a dose dependent manner against MCF-7 cells.

Five New C21 -Steroidal Sapogenins from the Acid Hydrolysate of Cynanchum otophyllum Roots.

Five new C21 -steroidal sapogenins (1-5) named cynotogenins J-N, were isolated from the acid hydrolysate of Cynanchum otophyllum roots. Their structures were established by extensive spectroscopic analysis (UV, IR, HR-ESI-MS, and NMR). Most notably, compounds 1-3 harboring a rare 5ß,6ß-epoxy group in the C21 -steroidal skeleton of Cynanchum plants. All compounds were evaluated for their cytotoxicities against multiple cancer cell lines, in which compounds 5 showed weak cytotoxicity against HepG2 cancer cells with IC50 values of 44.90 µM.

Design, Synthesis and Anticancer Activity of Novel Steroidal Derivatives with D-Ring Fused or Substituted N-Heterocyclic Systems.

A series of novel D-ring fused or substituted steroidal N-heterocycles were synthesized, and their chemical structures were characterized by spectroscopic analysis. The anticancer activity of these compounds against four human cancer cell lines (MCF-7, H1299, HeLa and HepG2) were evaluated and the structure-activity relationship (SAR) was also investigated. Compound 3c displayed significant inhibitory activity on the four cancer cells with IC50 values ranging from 3.88 to 10.05 µM. Overall, these studies indicated that construction of N-heterocyclic system with D-ring substituted containing a double bond at C-16 and C-17 or D-ring fused with [17,16-d]azolo[1,5-a]pyrimidine could be a promising strategy to improve antitumor activity for steroids deserved further investigation.

Thymoquinone Attenuates Brain Injury via an Anti-oxidative Pathway in a Status Epilepticus Rat Model.

AIM: Status epilepticus (SE) results in the generation of reactive oxygen species (ROS), which contribute to seizure-induced brain injury. It is well known that oxidative stress plays a pivotal role in status epilepticus (SE). Thymoquinone (TQ) is a bioactive monomer extracted from black cumin (Nigella sativa) seed oil that has anti-inflammatory, anti-cancer, and antioxidant activity in various diseases. This study evaluated the protective effects of TQ on brain injury in a lithium-pilocarpine rat model of SE and investigated the underlying mechanism related to antioxidative pathway. METHODS: Electroencephalogram and Racine scale were used to value seizure severity. Passive-avoidance test was used to determine learning and memory function. Moreover, anti-oxidative activity of TQ was observed using Western blot and super oxide dismutase (SOD) activity assay. RESULTS: Latency to SE increased in the TQ-pretreated group compared with rats in the model group, while the total power was significantly lower. Seizure severity measured on the Racine scale was significantly lower in the TQ group compared with the model group. Results of behavioral experiments suggest that TQ may also have a protective effect on learning and memory function. Investigation of the protective mechanism of TQ showed that TQ-pretreatment significantly increased the expression of Nrf2, HO-1 proteins and SOD in the hippocampus. CONCLUSION: These findings showed that TQ attenuated brain injury induced by SE via an anti-oxidative pathway.

Mifepristone in combination with prostaglandins for termination of 10-16 weeks' gestation: a systematic review.

OBJECTIVES: Medical regimens using mifepristone in combination with prostaglandins have been widely available for women undergoing termination of pregnancy (TOP) at 10-16 weeks' gestation in China. We undertook a systematic review to compare different regimens of mifepristone with prostaglandins for TOP at 10-16 weeks' gestation. METHODS: We searched multiple electronic databases for English and Chinese language reports (1990-2007) including MEDLINE, the Cochrane Library and the Chinese Biomedical Literature Database. Included were trials comparing mifepristone with prostaglandins (misoprostol, gemeprost or carboprost (PG05)) to each other for women at 10-16 weeks' gestation. Outcomes were successful abortion rates, induction-to-expulsion time, blood loss and side effects. Data were processed with RevMan 5 software. RESULTS: Nineteen trials comparing mifepristone with prostaglandin (misoprostol and PG05) were found of which 14 contributed to meta-analyses (4206 women). The quality of reports was poor. The effectiveness of vaginal mifepristone/misoprostol was super than mifepristone/PG05 (RR 1.14, 95%CI 1.05-1.22) as was induction-to-expulsion time, blood loss and side effects. When comparing misoprostol/mifepristone 150mg to misoprostol/mifepristone 200mg, no difference in TOP success rates were found (RR 0.98, 95%CI 0.96-1.01). Misoprostol vaginally compared to orally significantly increased the TOP success rate (RR 1.12, 95%CI 1.01-1.24). Gastrointestinal symptoms and fever occurred more often in misoprostol oral group (RR 1.67, 95%CI 1.46-1.91). CONCLUSIONS: Medical regimens of mifepristone/prostaglandins were effective and safe for TOP at 10-16 weeks' gestation. Misoprostol was super than PG05, and misoprostol vaginally was found to have better effectiveness than misoprostol orally. Further research should evaluate the relative effectiveness of medical methods compared to surgery.

[Detection of human parvovirus B19 nonstructural protein DNA by nested- polymerase chain reaction in pregnant women].

OBJECTIVE: To explore the sensitivity and specificity of the new nested-polymerase chain reaction (nested-PCR) assay in the detection of human parvovirus B19 (HPV B19) nonstructural protein DNA and the applicability of this technique in detecting the gravida infected with parvovirus B19. METHODS: Evaluating the new nested-polymerase chain reaction assay by routine process, and compared with the general nested-PCR in detecting structural protein DNA. Then, the two techniques were used to detect human parvovirus B19 structural protein and nonstructural protein DNA in gravida serum and pregnant tissue of 30 cases. RESULTS: The sensitivity of the new method was 0.005 fg which was similar to the general nested-polymerase chain reaction assay, and the detection results of other viruses and human genome DNA were all negative. The positive rates of structural protein DNA and nonstructural protein DNA in gravida sera were 26.7% and 33.3%, respectively. And the difference was non significant in statistics. At the same time, both of these two positive rates in placenta and villus were 26.7%. CONCLUSIONS: The new nested-polymerase chain reaction assay was a sensitive, specific and convenient method in detecting human parvovirus B19 infection, and the detection of nonstructural protein DNA paves the way for the following study on the disease mechanisms of B19.