OBJECTIVETo investigate the chemical constituents of Ilex pernyi.

METHODThe chemical constituents were isolated by various column chromatographic methods. The structures were identified by spectral data.

RESULTEight triterpenoid compounds were isolated and identified as ursolic acid (1), lupeol (2), alpha-amyrin (3), uvaol (4), 3beta-hydroxyurs-11-ene-13beta-olide (5), pomolic acid (6), lup-20 (29)-ene-3beta, 24-diol (7), 3beta, 23-dihydroxy-urs-12-en-28-oic acid (8).

CONCLUSIONThe eight compounds were obtained from this plant for the first time.

Ilex ; chemistry ; Oleanolic Acid ; analogs & derivatives ; chemistry ; isolation & purification ; Plant Leaves ; chemistry ; Plants, Medicinal ; chemistry ; Triterpenes ; chemistry ; isolation & purification

AIMTo study the chemical composition of Tripterygirm wilfordii Hook. f.

METHODSColunm chromatography was used to separate the chemical constituents. UV, IR, MS, HRMS, 1HNMR, 13CNMR (COM and OFR), 1H-1H COSY, 1H-13C COSY, NOESY and COLOC spectra were used to determine the structures of the isolated constituents.

RESULTSTwo sesquiterpene alkaloids were isolated and their structures were elucidated as wilforgine and wilfordlongine on the basis of spectral evidence.

CONCLUSIONWilfordclonine is a new sesquiterpene alkaloid.

Lactones ; chemistry ; isolation & purification ; Molecular Structure ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Pyridines ; chemistry ; isolation & purification ; Tripterygium ; chemistry

OBJECTIVETo observe the effects of Bushen Tongmai Recipe (, BSTMR) on mRNA and protein expressions of protein kinase B alpha (PKB alpha) in hepatic, adipose, muscular, and ovarian tissues of polycystic ovary (PCO) rats with insulin resistance (IR) and to explore the possible molecular mechanism of BSTMR in treating IR and ovulation dysfunction.

METHODSFemale 22-day-old SD rats were injected subcutaneously with sodium prasterone sulfate (9 mg.100g(-1).d(-1)) for 20 days and fed with high-fat diet for 80 days to induce PCO rats with IR. Then, the PCO rats were randomly divided into the model group (n=23) and the treated group (n=21). The treated group was administered with BSTMR for 2 weeks. Meanwhile, a group with 15 rats of the same age was used as the control group. The histological changes in the ovaries were examined. Fasting blood glucose (FBG) was determined by the glucose oxidase method. Serum fasting insulin (Fins) was determined by radioimmunoassay (RIA). The mRNA level of PKBalpha was measured by reverse transcription polymerase chain reaction (RT-PCR). Immunohistochemistry staining and Western blot analysis were employed to detect the protein expression in target tissues.

RESULTSCompared with the control group, the ovaries in the model group showed multiple follicular cysts, levels of FBG and Fins in the model group increased markedly (P<0.05 or P<0.01, respectively), and the insulin sensitive index (ISI) decreased obviously (P<0.01). The mRNA and protein expressions of PKBalpha in target tissues in the model group were dramatically lower than those in the control group (P<0.05 or P<0.01). Compared with the model group, the stratum granulosum of the ovarian follicle in the treated group increased markedly, the level of Fins in the treated group decreased obviously (P<0.01), ISI in the treated group improved markedly (P<0.01), and the mRNA and protein expressions of PKBalpha in target tissues of the treated rats were elevated significantly (P<0.05 or P<0.01).

CONCLUSIONBSTMR could improve IR and ovulation dysfunction in PCO rats with IR, and its molecular mechanisms might be closely related with the elevation of mRNA and protein expressions of PKBalpha in target tissues of PCO rats with IR.

Animals ; Blood Glucose ; drug effects ; metabolism ; Blotting, Western ; Drugs, Chinese Herbal ; pharmacology ; therapeutic use ; Fasting ; blood ; Female ; Gene Expression Regulation, Enzymologic ; drug effects ; Insulin ; blood ; Insulin Resistance ; physiology ; Organ Specificity ; drug effects ; Ovary ; drug effects ; enzymology ; pathology ; Polycystic Ovary Syndrome ; blood ; drug therapy ; enzymology ; physiopathology ; Proto-Oncogene Proteins c-akt ; genetics ; metabolism ; RNA, Messenger ; genetics ; metabolism ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo investigate the role of microtubule-actin crosslinking factor 1 (MACF1) in the response of glioma cells to temozolomide (TMZ).

METHODSTMZ was applied to a human gliomablastoma cell line (U87) and changes in the protein expression and cellular localization were determined with Western blot, RT-PCR, and immunofluorescence. The responses of the cells with MACF1 expression knockdown by RNA interference to TMZ were assessed. TMZ-induced effects on MACF1 expression were also assessed by immunohistochemistry in a nude mouse model bearing human glioblastoma xenografts.

RESULTSTMZ resulted in significantly increased MACF1 expression (by about 2 folds) and changes in its localization in the gliomablastoma cells both in vitro and in vivo (P<0.01). Knockdown of MACF1 reduced the proliferation (by 45%) of human glioma cell lines treated with TMZ (P<0.01). TMZ-induced changes in MACF1 expression was accompanied by cytoskeletal rearrangement.

CONCLUSIONMACF1 may be a potential therapeutic target for glioblastoma.

Qizhu, the dried rhizome of Atractylodes macrocephala in Compositae family, is the representative wild variety of Atractylodis Macrocephalae Rhizoma (Baizhu) with modern excellent quality. Through textual research of materia medica works and modern studies, the medication methods between Qizhu and ancient Baizhu were systematically compared. Focusing on seven key issues, this paper systematically summarized the medicinal history, characters, cultivation and other related contents of Qizhu, in order to provide a basis of Qizhu in the recovery and development of its own Daodi-status, and further serve the industrial development of this herb. The name, harvesting time, processing method and other issues had undergone a relatively complicated evolution process. At present, acknowledged points are as following：①The distribution areas of Qizhu include southern areas of the Yangtze River in Anhui province and its surrounding regions. ②Harvesting time is late October. ③Qizhu can be dried in the shade or micro-hot dried after being wrapped with absorbent paper, later it can be divided into two commercial specifications. ④In addition to cutting, there is still a lack of other processing methods. ⑤The superior characters of Qizhu contain white, less oil, fragrant smell and sweet taste and so on. ⑥The history of Qizhu as a genuine medicinal material can be traced back to the Ming dynasty.

Objective To investigate the regulatory role of recombinant Trichinella spiralis cysteine protease inhibitors (rTs-Cys) in induction of polarization of bone marrow-derived macrophages (BMDMs) in vitro. Methods BMDMs were captured and cultured in conditioned medium for 7 days. Then, mature BMDMs were harvested and assigned into four groups. Cells in Group A (negative control) were given 10 ng/mL IFN-γ combined with 100 ng/mL LPS, cells in Group B (positive control) were treated with IL-4 and IL-10 (at 10 ng/mL both), and cells in Group C (recombinant protein alone) were stimulated with 1 μg/mL rTs-Cys, while cells in Group D (protein co-culture) were simultaneously treated with 1 μg/mL rTs-Cys, 10 ng/mL IFN-γ and 100 ng/mL LPS. Cells and culture supernatant were collected 24 hour post-treatment, and the proportions of F4/80⁺, CD11b⁺, CD206⁺ and CD11c⁺ cells were detected by flow cytometry. The levels of interleukin IL-6 (IL-6), tumor necrosis factor-α (TNF-α), IL-10 and transforming growth factor-β (TGF-β) in the cell culture supernatant were measured by ELISA and the CD86⁺ and CD206⁺ phenotypes were identified by immunofluorescent staining. Results Flow cytometry detected no significant difference in the proportion of F4/80⁺ CD11b⁺ CD11c⁺ cells among the four groups (F = 46.184, P < 0.001), and a lower proportion of F4/80⁺ CD11b⁺ CD11c⁺ cells was seen in groups C and D than in group A (all P values < 0.001). There was a significant difference in the proportion of F4/80⁺ CD11b⁺ CD206⁺ cells among the four groups (F = 11.032, P < 0.001), and a greater proportion of F4/80⁺ CD11b⁺ CD206⁺ cells was seen in groups C and D than in group A (all P values < 0.01). Immunofluorescent staining showed higher CD206⁺ expression and lower CD86⁺ expression in groups C and D than in Group A. There were significant differences in the IL-6 and (F = 3.950, P < 0.001) and TNF-α (F = 205.827, P < 0.001) levels in the cell culture supernatants among the four groups, and significantly lower IL-6 and TNF-α levels were measured in groups C and D than in Group A (both P < 0.05). There were significant differences in the IL-10 and (F = 8.274, P < 0.001) and TGF-β (F = 13.559, P < 0.01) levels in the cell culture supernatants among the four groups, and greater IL-10 and TGF-β levels were measured in Group C than in Group A (both P values < 0.01). In addition, the TGF-β level was significantly higher in Group D than in Group A (P < 0.05); however, there was no significant difference in the IL-10 level between groups D and A (P > 0.05). Conclusion rTs-Cys may induce the polarization of BMDMs to antiinflammatory M2 macrophages in vitro and inhibit the activation of M1 macrophages.