Effect and mechanism of gerbeloid J from Gerbera piloselloides (L.) Cass. on cycle and apoptosis of breast cancer cells / 药学学报

Breast cancer has become the most prevalent malignant tumor among women, putting the health of women at serious risk. Screening for lead compounds in the active ingredients of plant that are effective and less toxic continues to be an important strategy for treating breast cancer. Gerbeloid J, a coumarin isolated from Gerbera piloselloides (L.) Cass., showed significant anti-cancer activity. But there is no report on the effect and mechanism of gerbeloid J on cycle and apoptosis of breast cancer. By using the CCK-8, clone formation, and PI staining assays, the effects of gerbeloid J on the proliferation of MCF-7 and MDA-MB-231 cells were assessed in this study. The effects of gerbeloid J on the apoptosis and mitochondrial function of MCF-7 and MDA-MB-231 cells were assessed using DAPI, Annexin V/TO-PRO-3, Rhod-2 AM, TMRM, DCFDA staining assays, and Western blot. The results demonstrated that gerbeloid J regulated the P21/CDC25C/CDK-1/cyclin B1 pathway and arrested the cell cycle at G2/M phase to suppressed the proliferation of MCF-7 and MDA-MB-231 cells. Additionally, gerbeloid J induced apoptosis through the stimulation of mitochondrial calcium excess, reduction of mitochondrial membrane potential, and promotion of ROS generation, and its mechanism was related to the activation of mitochondrial apoptotic pathway. In conclusion, by regulating the P21/CDC25C/CDK-1/cyclin B1 pathway and activating the mitochondrial apoptosis pathway, gerbeloid J could cause breast cancer cell cycle arrest and apoptosis, which might offer a promising candidate for the creation of new drugs against breast cancer.

A new pair of coumarin-like enantiomeric isomers from Gerbera piloselloides / 药学学报

Ten compounds were isolated from the 95% ethanol extract of the whole plant of Gerbera piloselloides by silica gel column chromatography, MCI column chromatography and semi-preparative HPLC methods. Their structures were identified on the basis of physicochemical properties, spectral data (UV, IR, MS and NMR), circular dichroism (CD) spectra and single crystal X-ray diffraction analysis as 3′R-gerpilosecoumarin A (1a), 3′S-gerpilosecoumarin A (1b), gymnastone (2), gerberinside (3), divaricataester C (4), luteolin (5), caffeic acid methyl ester (6), ethyl chlorogenate (7), 6-(β-D-glucopyranosyloxy)-7-methoxy-5-benzoranpropanoic acid methyl ester (8) and glucozaluzanin C (9). Among them, new compounds 1a and 1b were new compounds and optical enantiomers, which were obtained by chiral resolution, and their absolute configurations were determined by quantum chemical calculation ECD. Compounds 1 and 1a/1b significantly increased the survival of IEC-6 in rat small intestinal crypt epithelial cells after LPS injury.

Effect of high-frequency electric lacrimal duct plasty and annular lacrimal drainage tube implantation combined with acupuncture on upper lacrimal duct obstruction / 国际眼科杂志(Guoji Yanke Zazhi)

·AIM:To investigate the clinical effect of high-frequency electric lacrimal duct plasty and annular lacrimal drainage tube implantation combined with acupuncture on upper lacrimal duct obstruction. ·METHODS:A total of 86 patients (102 eyes) with upper lacrimal duct obstruction who were treated in our department from July 2013 to June 2016 were 26 males(28 eyes) and 60 females(74 eyes). The treatment was high-frequency electric lacrimal duct plasty and annular lacrimal drainage tube implantation, combined with traditional Chinese medicine acupuncture plus oral medicine made by our department for 30d, followed up for 6mo after surgery to observe the effect. ·RESULTS:A total of 86 eyes(84.3%) were cured in 102 eyes,12 eyes (11.8%) were improved, 4 eyes (3.9%) were ineffective,and the total effective rate was 96.1%. Intraoperative complications: 1)orbital hemorrhage in 2 eyes, maybe caused by vessel injury at the front of ethmoidal sinus, the blood was stopped after press, the operation went successfully after 5d; 2) lacrimal duct rupture in 3 eyes, all because of uncareful operation or weak compliance;3)the duct was hard to implanted in 3 eyes and iatrogenic sinus occurred, we suggested them went to superior hospital. Postoperative complications:1) lacrimal duct rupture without epiphora in 3 eyes(2.9%);2)the duct draw out in 5 eyes (3.9%), the duct was draw and fixed to nasal vestibule, in other 4 eyes (4.9%) with fully draw out,in one of the 4,the duct was replaced and in the rest 3 of the 4, no treatment; 3) irritation symptoms at inner canthus in 11 eyes (10.8%) with symptomatic treatment; 4 ) granulation tissue hyperplasia in 2 eyes (2.0%), one of them near the lacrimal punctum was cut and disappeared after tobramycin dexamethasone eye drops,one in the lacrimal ductile, the duct was draw and after tobramycin dexamethasone eye drops or compound neomycin sulfate eye drops the hyperplasia did not enlarge, but the lacrimal passage irrigation was failed. ·CONCLUSION:It is effective of high-frequency electric lacrimal duct plasty and annular lacrimal drainage tube implantation combined with acupuncture on upper lacrimal duct obstruction.

Expression of thrombomodulin, endothelial protein C receptor in lung tissue of acute paraquat poisoned rats and intervention of sodium dimercaptopropane sulfonate / 中华劳动卫生职业病杂志

<p><b>OBJECTIVE</b>To observe the expression and effect of thrombomodulin (TM) mRNA and endothelial protein C receptor (EPCR) mRNA in lung tissue of acute paraquat poisoned rats, and intervention of sodium dimercaptopropane sulfonate (Na-DMPS).</p><p><b>METHODS</b>Eighty male SD rats were randomizedly divided into four groups: the normal control group (n=8), the Na-DMPS control group (n=8, administered with 200 mg/kg Na-DMPS intraperitoneally), the PQ group (n=32, administered with 20 mg/kg 1% PQ intraperitoneally), the NA-DMPS protected group (n=32, administered with 200 mg/kg Na-DMPS intraperitoneally before with 20 mg/kg 1% PQ). The expression of TM mRNA and EPCR mRNA in the PQ group and the Na-DMPS protected group was evaluated at the six hour, on the first, third and seventh day.</p><p><b>RESULTS</b>The expression of TM mRNA and EPCR mRNA in lung tissue of poisoned rats, was significantly increased and reached the peak at the six hour, was decreased slowly on the first day, and returned to normal level on the seventh day. In the Na-DMPS protected group, at the six hour and on the first day, the expression of TM mRNA (1.071 +/- 0.097, 1.055 +/- 0.051) was less than that in the PQ group (P<0.05 or P<0.01). EPCR mRNA (0.678 +/- 0.005), (0.650 +/- 0.007) at the six hour and on the first day in the Na-DMPS protected group was less than that in the PQ group (P<0.05 or P<0.01).</p><p><b>CONCLUSION</b>The expression of TM mRNA and EPCR mRNA of rats after PQ intoxication is increased, and can significantly be decreased after administered with Na-DMPS.</p>

Oxidative stress of acute paraquat poisoned rats and sodium dimercaptopropane sulfonate intervention / 中华劳动卫生职业病杂志

<p><b>OBJECTIVE</b>to study the oxidative stress of rats with acute paraquat poisoning and the intervention of Sodium Dimercaptopropane Sulfonate (NA-DMPS).</p><p><b>METHODS</b>Eighty male SD rats were randomizedly divided into: the normal control group (n=8), NA-DMPS control group (n=8), the PQ group (n=32, the rats were intraperitoneally injected with 1% PQ solution at the dosage of 20 mg/kg) and the NA-DMPS protected group (n=32). The rats in the groups of normal and NA-DMPS control were sacrificed 1d after administration of NS or NA-DMPS. And the rats in the PQ group and the NA-DMPS protected group were sacrificed at 6h, 1, 3, 7d after poisoning. Samples of serum, bronchoalveolar lavage fluid (BALF) and lung tissue were gathered. The MDA and CAT in serum, BALF and lung homogenate, the glutathione (GSH) in serum and BALF were measured. And the expression of Nuclear factor E2-related factor 2 (Nrf2) mRNA in lung was tested with RT-PCR.</p><p><b>RESULTS</b>Compared with the normal control group, the activities of MDA and CAT in serum, BALF and lung homogenate are higher in both groups of PQ and NA-DMPS protected. And compared with the PQ group, the activities of MDA in serum, BALF and lung homogenate of the NA-DMPS protected group decreased significantly at 6h, 1d after poisoning, whereas the activities of CAT are higher at 6h, 1, 3d in serum and 1, 3d in BALF and lung homogenate (P<0.05 or P<0.001). The serum GSH at 6h, 3d of the NA-DMPS protected group [(730.07 +/- 16.23), (793.66 +/- 7.40)] were higher than those in the PQ group. And the BALF GSH at 1, 3d of the NA-DMPS protected group [(609.75 +/- 6.74), (631.83 +/- 12.03)] were also markedly higher than the PQ group (P<0.05 or P<0.001). The expression of NRF2 mRNA of the lung at 1, 3, 7d in the PQ group [(0.71 +/- 0.061), (1.023 +/- 0.158), (0.969 +/- 0.046)] and the NA-DMPS protected group [(1.005 +/- 0.06), (1.464 +/- 0.166), (1.066 +/- 0.191)] were significantly higher than those in the control groups. Compared with the PQ group, the expression of NRF2 mRNA of the lung increased markedly in the NA-DMPS protected group at 1, 3d (P<0.01).</p><p><b>CONCLUSION</b>Na-DMPS decreases the activity of MDA and increases the activity of CAT, GSH and the expression of Nrf2 mRNA. NA-DMPS can protected rats from PQ intoxication by improving the balance of redox reaction.</p>