Carbon-carbon bond activation by B(OMe)3/B2pin2-mediated fragmentation borylation.

Selective carbon-carbon bond activation is important in chemical industry and fundamental organic synthesis, but remains challenging. In this study, non-polar unstrained Csp2-Csp3 and Csp2-Csp2 bond activation was achieved by B(OMe)3/B2pin2-mediated fragmentation borylation. Various indole derivatives underwent C2-regioselective C-C bond activation to afford two C-B bonds under transition-metal-free conditions. Preliminary mechanistic investigations suggested that C-B bond formation and C-C bond cleavage probably occurred in a concerted process. This new reaction mode will stimulate the development of reactions based on inert C-C bond activation.

New clerodane diterpenoids from the roots of Polyalthia laui.

Five new clerodane diterpenoids, polylauiester A (1), (4→2)-abeo-2,13-diformyl-cleroda-2,12E-dien-14-oic acid (2) and polylauiamides B-D (3-5), together with 11 known clerodane diterpenoids (6-16), were isolated from the roots of Polyalthia laui. Among them, polylauiester A (1) represents the first example of a novel norclerodane diterpenoid only containing 17 carbon atoms on the carbon skeleton, and polylauiamide B (3) is an unusual diterpenoid with a p-substituted benzene ring as a substituent. Their structures were elucidated by extensive spectroscopic methods, and the relative configuration of polylauiamide B (3) was further confirmed by the single crystal X-ray diffraction method. Biological evaluation of new compounds against human Hela, MCF-7 and A549 human cancer cell lines showed that all compounds displayed weak cytotoxicities against various human cancer cell lines in the range of IC50 at 25.01-39.31µM.

cDNA cloning and localization of Sp3111 (also called Ms4a14) in the rat testis.

With tetraspanning topology, members of the membrane-spanning four-domain subfamily A (MS4A) may facilitate signaling or ion channel functions in many tissues. In this study, we report the cloning of a full-length cDNA from rat testis, designated Ms4a14 (Sp3111), which encodes the MS4A protein with 1139 amino acid residues. In situ hybridization and immunohistochemical analyses indicate that Ms4a14 is predominantly expressed from round spermatids to spermatozoa at specific stages in the rat testis at both the mRNA and protein level. Immunofluorescence analysis revealed that MS4A14 (SP3111) is located in the acrosome and the midpiece of the flagellum in mature sperm. Previously, we explored and reported the involvement of MS4A14 in reproductive functions, using antibody blockage during IVF and a transgenic RNA interference method in a mouse model. Our results suggested that MS4A14 is involved in fertilization and zygote division. As MS4A14 protein exists in mammals, such as humans, cows, dogs, and rodents, MS4A14 may play a ubiquitous role in mammalian reproduction.

[Clinical observation on treatment of advanced gastric cancer by combined use of Shenqi Fuzheng injection, docetaxel, flurouracil and calcium folinate].

OBJECTIVE: To investigate the effects of Shenqi Fuzheng injection (SQFZI) combined with docetaxcl, flurouracil and calcium folinate in treating advanced gastric carcinoma, and to evaluate the action of SQFZI for enhancing therapeutic effect and alleviating adverse reaction of chemotherapy. METHODS: Sixty advanced gastric cancer patients were assigned to two groups randomly, the control group treated with chemotherapy alone and the treated group treated with SQFZI combined chemotherapy. Chemotherapy regimens (TFC) was given to all patients consisting of docetaxel 75 mg/m2 intravenous dripping on the 1st day, flurouracil (5-FU) 350 mg/m2 and calcium folinate (CF) 120 mg/m2 intravenous dripping with micro-pump continuously from day 1 to 5, for 21-28 days as a cycle. To patients in the treated group, starting from 3 days before chemotherapy, SQFZI 250 mL was dripped every day for 14 successive days. The clinic effects were evaluated after two-cycle treatment. RESULTS: The short-term effective rate was 40.0% in the treated group and 33.3% in the control group. As compared with those in the control group, patients in the treated group after treatment had a higher Karnofsky score (chi2 = 7.21, P < 0.05) and body weight (chi2 = 11.47, P < 0.05), lesser adverse reactions in decreasing of peripheral blood leucocyte, damage of peripheral nerve, adverse reaction of gastrointestinal tract, as well as better immune function. CONCLUSION: SQFZI could effectively improve the clinical symptoms induced by chemotherapy regimen TFC, alleviate the adverse reaction, raise patients' quality of life and their immune function.

[Clinical study on the antioxidant effect of methylene blue in vivo].

OBJECTIVE: To investigate the relationship of oxygen free radical (OFR) with per-oxidative injury of erythrocyte induced by intravenous procaine in vivo and the effect of methylene blue (MB) in removal of nitric oxide (NO) and peroxynitrite (ONOO(-)). METHODS: Forty patients undergoing elective surgery were divided randomly into intravenous procaine anesthesia (IPA) group and fentanyl group. Blood sample was taken before anesthesia (T0), 120 minutes (T1) and 180 minutes (T2) after IPA and 30 minutes after treatment with MB (1-2 mg/kg, T3) to determine the changes in the levels of NO, OFR, lipid peroxide (LPO), superoxide dismutase (SOD), catalase (CAT), NADH-Cyt b5-reductase (Cyt b5-R) and methemoglobin (MHb). RESULTS: Compared with T0, the levels of NO, OFR, LPO, MHb in IPA group were significantly increased at T1,T2. At same time SOD, CAT and Cyt b5-R were significantly decreased. NO, OFR, MHb, SOD, CAT and Cyt b5-R were all reduced to the normal levels at T3. No changes in any determined parameters in fentanyl group during anesthesia. CONCLUSION: It is indicated that the metabolites of procaine consist of a large quantity of NO:ONOO(-), producing per-oxidative injury to erythrocyte. MB is effective in eliminating OFR in vivo, protecting tissue cells. It may act as an antioxidant drug in the treatment of critical illness.