Ten compounds, including five steroidal saponins and five flavonol glycosides, were isolated from the whole plant of Solanum coagulans by means of column chromatographies over silica gel, ODS, Sephadex LH-20, and preparative HPLC. Based on analysis of MS and NMR spectroscopic data, their structures were established as anguiviosides XV (1), smilaxchinoside A (2), methylprotodioscin (3), protodioscin (4), solamargine (5), 3', 4', 5-trihydroxy-7-methoxy-6-C-β-D-glucopyranoside (6), brainoside B (7), camsibriside A (8), kampferol 3-O-(2"-β-D-galactopyranosyl)-β-D-glucopyranoside (9), and quercetin-3-O-(2"-β-D-galactopyranosyl)-β-D-glucopyranoside (10). All the compounds were first isolated from this plant. In the in vitro assays, compounds 4 and 5 showed cytotoxic activity against SMCC-7721 and NCI-H460.
Cell Line, Tumor ; Flavonols ; chemistry ; isolation & purification ; pharmacology ; Humans ; Saponins ; chemistry ; isolation & purification ; pharmacology ; Solanum ; chemistry

Phellinus is a kind of rare medicinal fungus that has a variety of physiological activities include anti-cancer, anti-liver fibrosisa, antioxidant and so on. Phellinus contains polysaccharides, steroids, terpenoids, flavonoids, pyrone, furan, alkaloids and other substances. Polysaccharide extracts of phellinus showed obvious antitumor effect and has been a hot research field in recent years. It was also found other extracts of phellinus such as ethyl acetate extract exhibited anticancer activity. Thus, the antitumor effect of different extract, especially the anti-cancer mechanism were discussed in this review.
Antineoplastic Agents ; pharmacology ; Basidiomycota ; Cytokines ; analysis ; Neoplasm Metastasis ; prevention & control

Objective To comparative the expression of suppressors of cytokine signaling 3 (SOCS3) in placental tissues between premature delivery and term delivery,and to evaluate the significance of SOCS3 in premature-delivered placental tissues.Meth ods Retrospective analysis was made on 30 patients who had spontaneous premature delivery and 30 pregnant women with normal delivery from February 2013 to October 2013 in our hospital.Reverse transcription and polymerase chain reaction (RT-PCR) was used to detect the mRNA expressions of SOCS3,interferon-α(IFN-α),and interleukin-10 (IL-10).Western-blot was used to detect protein expression of SOCS3,and to analyze the balance of Th1/Th2.Results PCR detection showed that SOCS3-mRNA in the control group was significantly lower than that in the experimental group (P ＜ 0.01).Western-blot test showed that SOCS3 protein expression in the control group was significantly lower than that in the experimental group (P ＜ 0.01).The expression of SOCS3 gene was consistent with its protein expression.PCR detected the significant increase of IFN-α with the secretion of Th1 cytokine,significant decrease of IL-10 with secretion of Th2 cytokine (P ＜ 0.05),and the balance deviation of Th1/Th2 toward Th1.Conclusions SOCS3 is associated with premature delivery,which mechanism might be involved in regulation of the immune balance through janus kinase/signal transducer and activator of transcription (JAK/STAT) signaling pathways.

Abnormalities, Multiple ; genetics ; Chromosome Deletion ; Chromosome Mapping ; Chromosomes, Human, Pair 9 ; genetics ; Growth Disorders ; genetics ; Humans ; Infant, Newborn ; Male

Background and purpose:Axillary lymph node metastasis of breast cancer has an important significance in prognosis and treatment of breast cancer. This study was to investigate the correlation between axillary lymph node metastasis and ultrasonographic characteristics of axillary lymph node combined with immunohistochemistry in breast cancer patients.Methods:A total number of 366 breast cancer patients were selected in this study. Seven hundred and twenty-eight axillary lymph nodes were collected. With ultrasonography, the maximum cortex thickness, the ratio of the height to the length, the ratio of the cortex to the medulla and blood lfow of axillary lymph nodes were observed, in order to study the correlation between these indicators and axillary lymph node metastasis combined with the postoperative immunohistochemical results.Results:According to univariate analysis, axillary lymph node maximum cortex thickness, the ratio of the height to the length, characteristics of blood flow and the positive expression rate of p53 were related to axillary lymph node metastasis (P<0.05). Multivariate logistic regression analysis and receiver operating characteristic (ROC) curve showed that axillary lymph node maximum cortex thickness was the best indicator to determine axillary lymph node metastasis. The positive expression rate of p53 in patients with maximum cortex thickness >3 mm (42.78%) of axillary lymph node was signiifcantly higher than that in patients with maximum cortex thickness≤3 mm (25.82%) (P<0.01).Conclusion:Ultrasonographic characteristics of axillary lymph node and immunohistochemistry method are closely correlated with axillary lymph node metastasis in patients with breast cancer, which is important in diagnostic and treatment in clinic.

AIM: To observe the clinical effect of the tonifying kidney pills with mingmuwuzi treating evaporative dry eyes.METHODS: This study adopted the positive drug control,prospective study,random number remainder grouping method to 65 cases of outpatient patients diagnosed with evaporative dry eyes which were divided into the treatment group 32 cases (64 eyes) and the control group 33 cases (66 eyes).The treatment group took the decoction of kidney pills with mingmuwuzi,combined with sodium hyaluronate eye drops.The control group simply use sodium hyaluronate eye drops,both group were set to 4wk for a course of treatment.To observe the symptoms and signs of two groups before and after the treatment,the change of the evaluation index and curative effect were evaluated.RESULTS: The effectiveness of the treatment group was 87.5%,the control group was 78.8%,the difference was statistically significant (z=-3.149,P<0.05).CONCLUSION: The treatment of the kidney pills with mingmuwuzi combined with sodium hyaluronate eye drops to evaporative dry eyes is more effective than the simple use of sodium hyaluronate eye drops.

Aged ; CDX2 Transcription Factor ; Cysts ; metabolism ; pathology ; surgery ; Diagnosis, Differential ; Female ; Homeodomain Proteins ; metabolism ; Humans ; Keratin-20 ; metabolism ; Mucous Membrane ; pathology ; Peritoneal Neoplasms ; metabolism ; pathology ; surgery ; Pseudomyxoma Peritonei ; metabolism ; pathology ; surgery ; Rupture ; Splenic Neoplasms ; metabolism ; pathology ; surgery

CD38 is a multifunctional enzyme expressed in a variety of mammalian tissues, its catalytic activity was involved in a wide range of physiological processes. Based on the reported inhibitor of human CD38 NADase, 33 purine derivatives were designed and synthesized. The biological activity assay showed that compounds 20 and 38 exhibited almost the same extent of inhibitory activities on human CD38 NADase as the lead compound H2. The results also revealed that small substituents at C-6 of purine ring gave no obvious effect on inhibitory activity, but phenylpropionyl moiety at N-2 could affect the binding mode of the compound with CD38. This study provides a reliable basis for future rational design of inhibitors for CD38.
ADP-ribosyl Cyclase 1 ; antagonists & inhibitors ; Enzyme Inhibitors ; chemical synthesis ; chemistry ; Humans ; Purines ; chemical synthesis ; chemistry

To study the interaction of drugs of different properties, namely puerarin, borneol and catalpol in the process of in- clusion, in order to explore the inclusion regularity of multi-component and multi-property traditional Chinese medicine compound in- clusions. With HP-β-CD as the inclusion material, the freeze-drying method was used to prepare the inclusion. The inclusion between puerarin, borneol and catalpol was tested by measuring the inclusion concentration, DSC and X-ray diffraction. According to the find- ings, when insoluble drugs puerarin and borneol were included simultaneously, and puerarin was overdosed, puerarin included was almost equal to puerarin included, and borneol was not included. When puerarin was under-dosed, and HP-β-CD was overdosed, borne- ol was included, and the simultaneous inclusion was lower than the separate inclusion of borneol. When water-soluble drug catalpol was jointly included with puerarin or borneol, the simultaneous inclusion was almost the same with their separate inclusion, without charac- teristic peak of catalpol in DSC and X-ray diffraction patterns. There is a competition in the simultaneous inclusion between water-solu- ble drugs puerarin and borneol and a stronger competition in puerarin. The water-soluble drug catalpol could be included with HP-β-CD with no impact on the inclusion of puerarin or borneol.
2-Hydroxypropyl-beta-cyclodextrin ; Bornanes ; chemistry ; therapeutic use ; Brain Ischemia ; drug therapy ; Drug Compounding ; methods ; Freeze Drying ; Iridoid Glucosides ; chemistry ; therapeutic use ; Isoflavones ; chemistry ; therapeutic use ; Solubility ; beta-Cyclodextrins ; chemistry

This study is to investigate the sedative and hypnotic effects of a novel compound H1208. The sedative activity of H1208 was investigated by recording the spontaneous locomotor activity of mice. The hypnotic property was evaluated by the latency and duration of sleep (loss of righting reflex) in mice and the effect of hypnotics on sleep pattern of electroencephalogram were studied in conscious, freely moving mice with chronically implanted electrodes. The brain monoamine neurotransmitters levels in mice were measured by high performance liquid chromatography-electrochemical detection. The spontaneous locomotor activity was decreased by 56.7% and 80.2% in H1208 (5 and 25 mg x kg(-1), ip) treated mice, respectively. The loss of righting reflex was directly induced in mice after H1208 (60 mg x kg(-1), ip) administration. The non-rapid eye movement sleep increased significantly by 131% and 259%, respectively, within 3 hours after H1208 (30 and 60 mg x kg(-1), ip) administration. However, the rapid eye movement sleep decreased significantly. The contents of DA in the striatum and cortex and 5-HT in the cortex decreased significantly. These results demonstrated that H1208 has potent sedative and hypnotic effects, which may be closely related to the decreased contents of DA and 5-HT in mouse brain.
Animals ; Brain ; drug effects ; physiology ; Dopamine ; metabolism ; Electroencephalography ; Hypnotics and Sedatives ; pharmacology ; Mice ; Motor Activity ; drug effects ; Serotonin ; metabolism ; Sleep ; drug effects