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

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.

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.

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

AIMTo investigate the enhancing effect on insulin absorption through GI. tract in mice by using the Ulex europaeus agglutinin I (UEA1) modified liposomes as the carrier.

METHODSUEA1 modified phosphatidylethanolamine (PE) was prepared by conjugating method of 1-ethyl-3-(3'-dimethylaminopropyl) carbodiimide (EDC), then the modified compound (PE-UEA1) was incorporated into the conventional liposomes of insulin to obtain UEA1 modified liposomes. The agglutination test was performed to examine the UEA1 biological activities after synthesis and modification. When liposomes were applied to healthy mice or diabetic mice at insulin dose of 350 u x kg(-1) orally, the hypoglycemic effect was investigated according to the blood glucose level determination.

RESULTSThe blood glucose levels of the healthy mice reduced by UEA1 modified liposomes were (84 +/- 15)% at 4 h, (78 +/- 11)% at 8 h and (90 +/- 12)% at 12 h after oral administration. The conventional liposomes and saline showed no effect. The blood glucose levels of the diabetic mice reduced by UEA1 modified liposomes were (73 +/- 7)% at 4 h, (74 +/- 9)% at 8 h, (86 +/- 9)% at 12 h after oral administration.

CONCLUSIONThe UEA1 modified liposomes promote the oral absorption of insulin due to the specific-site combination on M cell membrane.

Administration, Oral ; Animals ; Blood Glucose ; metabolism ; Diabetes Mellitus, Experimental ; blood ; Drug Carriers ; Drug Delivery Systems ; Hypoglycemic Agents ; administration & dosage ; pharmacokinetics ; Insulin ; administration & dosage ; pharmacokinetics ; Intestinal Absorption ; drug effects ; Liposomes ; Mice ; Phosphatidylethanolamines ; chemistry ; Plant Lectins ; chemistry ; isolation & purification ; pharmacology ; Plants, Medicinal ; chemistry ; Ulex ; chemistry

AIMTo investigate the enhancing effect on insulin absorption through GI tract in mice by using tomato lectin (TL) modified liposomes as the carrier.

METHODSTL-phosphatidylethanolamine (PE) conjugate (TL-PE) was synthesized by using carbodiimide cross-linking method, then the compound was incorporated into the conventional liposomes of insulin. The agglutination test was performed to examine TL biological activities after synthesis and incorporation. When TL modified liposomes were administrated orally to the normal mice or diabetic mice at insulin dose of 350 u x kg(-1), the hypoglycemic effect was determinated according to the blood glucose level.

RESULTSThe blood glucose levels of the normal mice were reduced by modified liposomes. The glucose levels were (85 +/- 5)% at 4 h, (54 +/- 11)% at 8 h, (57 +/- 6)% at 12 h postdose compared with the glucose levels prior to oral administration respectively. However, the conventional liposomes and saline have no hypoglycemic effect. The blood glucose levels of the diabetic mice were obviously reduced by TL modified liposomes, the glucose levels were (38 +/- 13)% at 4 h, (50 +/- 15)% at 8 h, (50 +/- 16)% at 12 h respectively.

CONCLUSIONTL modified liposomes promote the oral absorption of insulin due to the specific-site combination on GI cell membrane.

Administration, Oral ; Animals ; Blood Glucose ; metabolism ; Delayed-Action Preparations ; Diabetes Mellitus, Experimental ; blood ; metabolism ; Drug Carriers ; Drug Delivery Systems ; Hypoglycemic Agents ; administration & dosage ; pharmacokinetics ; pharmacology ; Insulin ; administration & dosage ; pharmacokinetics ; pharmacology ; Intestinal Absorption ; drug effects ; Intestine, Small ; metabolism ; Liposomes ; Mice ; Phosphatidylethanolamines ; chemistry ; Plant Lectins ; chemistry ; pharmacology ; Technology, Pharmaceutical ; methods