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The phytochemical investigation of the methanol extract of Ixeris sonchifolia led to the isolation and identification of nine analogs, including one new guaiane-type sesquiterpenoid, named ixerinoid A (1). The structure of 1 was determined by extensive analysis of the 1 D and 2 D nuclear magnetic resonance spectroscopic data, as well as quantum chemical calculations. Additionally, all the isolates were tested for their neuroprotective activity using the oxygen-glucose deprivation/reperfusion-induced SH-SY5Y cell injury model. Compounds 3, 5, 6, 8, and 9 displayed remarkable protective effects at concentrations of 1, 5, and 10 μM, respectively.

Xiaokeyinshui extract combination (XEC), originating from a traditional Chinese formula Xiaokeyinshui (XKYS) recorded in ancient Bencao, has been reported to exert significant hypoglycemic effects. However, the chemical profiles, metabolic transformation and pharmacokinetic behavior of XEC in vivo were unclear. The research was to investigate the chemical constituents, metabolic profiles and pharmacokinetic behavior of XEC. A UPLC-QE-Orbitrap-HRMS qualification method was developed to identify the chemical constituents in XEC and xenobiotics of XEC in plasma, urine, feces and bile of rats after oral administration. A LC-MS quantification method was established and applied for the pharmacokinetic studies of major active compounds of XEC in normal and T

The phytochemical investigation of the methanol extract of

Background Shedan has a long history of application in Traditional Chinese medicine (TCM), however, Shedan from different original source has been indiscriminately used. So far, there is still a lack of an effective tool to differentiate the original source of Shedan medicinal materials, which brings great risk to the safety and effectiveness of clinical applications. Hence, it is imperative to develop a practicable approach to identify Shedan medicinal materials. Methods The specificity of two pairs of primers, including Folmer’s universal primers and a pair of originally designed primers COISNFF/COISNFR, was tested to screen the more specific primers for further origin identification of Shedan. A total of 253 fresh snake gallbladder samples from 31 morphologically identified snake species were collected and authenticated. Moreover, 51 fresh snake bile samples and 17 fresh bile samples from five other common domestic poultry and livestock (cattle, chicken, duck, pig and sheep) were collected and distinguished using the more specific primers. Additionally, a total of 195 market Shedan samples randomly selected from 18 batches of Shedan medicinal materials were investigated. Sequence definition was executed by querying sequence similarities in GenBank and the Barcode of Life Data System (BOLD), respectively. Results It turned out that the standard COI barcode obtained by COISNFF/COISNFR primers, rather than Folmer’s universal primers, can distinguish all the testing samples from each other in fresh Shedan samples, and COISNFF/COISNFR primers were also specific to snake species and the other four animal species except duck. In terms of market Shedan, 84.6% (165/195) samples can be attributed to 13 snake species from four families and 4.6% (9/195) can be attributed to adulterated chicken species. Conclusion The COI-based DNA barcoding was practicable for species identification of Shedan used in traditional Chinese medicine. The original source of current market Shedan, including adulterated species, has been preliminarily clarified, which provides a foundation for quality control of Shedan medicinal materials.

Extensive phytochemical investigation on the methanol extract of the inflorescences, twigs, and leaves of Brucea javanica led to the isolation and identification of 27 triterpenoids, including 21 previously undescribed ones, named brujavanoids A-U (1-21). Their structures were determined based on comprehensive spectroscopic analysis and single-crystal X-ray diffraction. Of these compounds, brujavanoid A (1) represents the first apotirucallane-type triterpenoid with a novel 19(10 → 9)abeo motif, and brujavanoids B and C (2-3) are the first apotirucallane-type triterpenoids with a rarely occurring 14-hydorxy-15,16-epoxy fragment. All the isolates were evaluated for their anti-inflammatory effect in an LPS-activated RAW264.7 cells model. Furthermore, the most active one, brujavanoid E (5), can suppress the transcriptional expression of typical pro-inflammatory mediators and inhibit the nuclear translocation of NF-κB p65 in the LPS- activated RAW264.7 cells.

A new phenolic glycoside, chinenside A (

Buxaustroines A-N (

Hedyotis hedyotidea has been traditionally used for the treatment of arthritis, cold, cough, gastro-enteritis, headstroke, etc. But few studies have screened the active compounds from extracts of H. hedyotidea. In this study, the structure of the chemical constituents from stems of H. hedyotidea were determined and the immunosuppressive activity of the compounds was evaluated. The compounds were separated and purified with silica gel, gel column chromatographies and preparative HPLC, and their structures were identified by spectral methods such as MS and NMR. Eleven compounds were obtained and identified as(6S,9S) -vomifoliol (1), betulonic acid (2), betulinic acid (3), betulin(4), 3-epi-betulinic acid (5), ursolic acid (6), β-sitosterol (7), stigmast-4-en-3-one (8), 7β-hydroxysitosterol (9), (3β,7β) -7-methoxystigmast-5-en-3-ol (10) and morindacin (11). This is the first report of compounds 1, 2, 4, 8, 9, 10 and 11 from H. hedyotidea. Compounds 1, 2 and 8-11 were firstly isolated from the genus Hedyotis, and compounds 9 and 10 were isolated from the family Rubiaceae for the first time. The immunosuppressive activity of these compounds was tested using the lymphocyte transsormationtest. Compounds 4, 6 and 9 showed significant immunosuppressive activity.

A new compound named 1-hydrate, 3-deoxy- α - d -tagatofuranose was isolated from Swertia punicea Hemsl. The structure of compound was determined by 1D and 2D NMR, HRESIMS techniques.

Two rare new chiratane-type triterpenoids, kouitchenoids A and B (1, 2), together with oleanolic acid (3) and ursolic acid (4), were isolated from ethanol extract of Swertia kouitchensis. The new structures were determined by the analysis of MS and NMR data. In addition, compounds 1–4 showed moderate inhibitory activity against the α-glucosidase (with IC50 values ranging from 1,812 to 2,027 μM).

The present study was to investigate the anti-diabetic activities ofSwertia bimaculata. Based on the glucose consumption ofS. bimaculataextractsand different fractions (petroleum, dichloromethane, ethyl acetate,n-butanol and water extracts) in 3T3-L1 adipocyte assay, ethanol (ETH) and dichloromethane (DTH) extracts had the most effective potency. Furthermore, ETH, DTH and corymbiferin (the most abundant component of DTH) were evaluated for anti-diabetic effects in high fat and sucrose fed combined with low dose streptozocin induced diabetic rats. DTH and corymbiferin displayed remarkable anti-diabetic activities. The fasting blood glucose levels were significantly decreased, while the serum insulin levels were obviously increased. The oral glucose tolerance was also improved. The lowed serum total cholesterol, low density lipoprotein (LDL) and triglyceride levels and increased ratio of HDL (high density lipoprotein)/LDL were observed. The insulin sensitivity was improved on the basis of increased expressions of insulin-receptor substrate-2, phosphatidylinositol 3-kinase and Ser/Thr kinase AKT2. And also DTH and corymbiferin improved antioxidant capacity and carbohydrate metabolism in diabetic rats, along with the improvement of histopathology of livers and pancreaticβcells. Corymbiferin was one of active constituents, responsible for anti-diabetic properties. Therefore,S. bimaculatacould be considered as an alternative agent against diabetes mellitus.

Liriopes Radix, which is regarded as both drug and healthy diet, is drunk as tea and used in traditional Chinese medicine to treat diabetes. Based on our previous studies, investigated the hypoglycemic effects and explored the mechanisms of total polysaccharides from Liriope spicata var. prolifera (Liriopes Radix) in a diabetic rat model.TLSP reduced hyperglycemia in diabetic rats. The oral glucose tolerance test showed that TLSP could improve the glucose tolerance of diabetic rats. Damage to liver and pancreas tissue was inhibited after treatment with TLSP. Moreover, TLSP increased glycogen content, glucokinase (GK) and glycogen synthetase (GS) activities, and suppressed the elevation of glucose-6-phosphatase (G6Pase) and glycogen phosphorylase (GP) activities in liver. Compared with the diabetic control group, GK and GS mRNA expression were significantly elevated, while G6Pase and GP mRNA expression were decreased in TLSP groups. In addition, TLSP could inhibit glycogen synthase kinase-3β expression and increase insulin receptor, insulin receptor substrate-1, phosphoinositide 3-kinase, protein kinase B and glucose transport protein-4 expression in liver.TLSP showed hypoglycemic function. Improvement of glucose metabolism and insulin-signaling transduction were possible mechanisms.

To study the chemical constituents from Schisandra glaucescens.The chemical constituents were separated and purifed with silica gel, gel column chromatography preparative HPLC, and their structures were identified by such spectral methods as MS and NMR.Twelve compounds were separated from petroleum ether fractions, and identified as t-cadinol (1), alpha-cadinol (2), torreyol (3), (+)-ent-epicubenol (4), ent-T-muurolol (5), (-)-15-hydroxycalamenene (6), (-)-cubebol (7), 4-epi-cubebol (8), caryophyllenol-I (9), caryophyllenol-II (10), oxyphyllenodiols A (11), caryolane-1,9/3-diol (12).Compounds 4, 6-12 were separated from the genus for the first time, while compounds 1-12 were separated from this plant for the first time.

Two new flavan-4-ol glycosides, (2R,4S)-6,8-dimethyl-7-hydroxy-4'-methoxy-4,2''-oxidoflavan-5-O-beta-D-6''-O-acetyl-glucopyranoside (1) and (2R,4S)-5,7-O-beta-D-di-glucopyranosyloxy-4'-methoxy-6,8-dimethyl-4,2''-oxidoflavane (2), were isolated from the rhizomes of Abacopteris penangiana. Their structures were elucidated by spectroscopic methods. Compounds 1 and 2 showed significant anticancer activities against HeLa and L929 cell lines in vitro.

To compare the difference of anther and pollen growth between Liriope spicata var. prolifera and L. spicate, and investigate the mechanism of the sterility of Liriope spicata var. prolifera.A comparative study on anther and pollen growth process was carried out between L. spicata var. prolifera and L. spicata by means of paraffin section.In L. spicata, the tapetum was secretory tapetum and began to degrade during dyad stage. The cells of tapetum and middle layer disappeared thoroughly when pollens were fully mature at 3-celled stage. In L. spicata var. prolifera, the degradation of the tapetum took place at the early time of meiosis stage and the tapetum cells inflated like vacuolization. The mononuclear pollens were abortive, which eventually formed abnormal pollens.The pollen abortion of L. spicata var. prolifera is associated with tapetum heteroplasia and degradation in advance.

To investigate the effects of anti-sense peptide nucleic acids (PNAs) targeting Ki-67 gene on modulation of the proliferation and apoptosis of human renal carcinoma cell lines, human renal carcinoma cell line 786-0 cells were treated with anti-sense PNAs at different concentrations (1.0 micromol/L, 2.0 micromol/L, 10.0 micromol/L). The Ki-67 expression of 786-0 cells was detected by immunohistochemical technique and Western blot method respectively. The proliferation of 786-0 cells was studied by cell growth curves and 3H-thymidine incorporation. The apoptosis of 786-0 cells was detected by TUNEL assay. The control groups were treated with anti-sense oligonucleotide (ASODNs) targeting Ki-67 gene. Our results showed that the Ki-67 expression of 786-0 cells treated with anti-sense PNAs (16.9+/-0.7) was significantly inhibited as compared with that of the control groups (28.6+/-0.4) (P0.01). The Ki-67 protein rate of 786-0 cells treated with anti-sense PNAs (42.1 +/-2.2) was significantly reduced when compared with that of the control groups (83.6+/- 1.4) (P0.01). Proliferation of 786-0 cells treated with anti-sense PNAs (20.7+/- 1.5) was significantly inhibited as compared with that of the control groups (58.6+/- 1.4) (P0.01). The apoptosis rate of 786-0 cells treated with anti-sense PNAs (28.7+/- 2.3) was significantly increased higher compared with that of the control groups (13.8 +/- 1.0) (P0.01). From these finds we are led to conclude that anti-sense PNAs targeting Ki-67 gene have stronger effects on the inhibition of the proliferation and induction of apoptosis of human renal carcinoma cells than ASODNs targeting Ki-67 gene. The strategies using anti-sense PNAs targeting Ki-67 gene may be a promising approach for the treatment of renal cell carcinoma.

We treated in vitro human renal carcinoma cells (cell line 786-0) with the lipid-delivered peptide nucleic acids (PNAs) against Ki-67 gene. Corresponding control groups were treated with the antisense oligonucleotides (ASOs) of the same nucleobase sequence, and with mismatched PNAs. In cells treated by anti- Ki-67 PNAs, the Ki-67 expression rate, Ki-67 protein level, cell growth and the DNA synthesis-indicative 3 H-thymidine incorporation rate were lower than in the ASO-treated groups, and reduced significantly compared to untreated controls, whereas the rate of apoptosis was markedly increased by PNA treatment. We conclude that anti- Ki-67 PNA has more strong (than ASO) and dose-dependent effects on the proliferation and apoptosis of human renal carcinoma cells. Our results indicate that the strategy of using PNA against the Ki-67 gene might be a promising approach in renal carcinoma therapy.

To offer evidences for quality control of medicinal Asteropyrum plants.Pharmacognostic studies were made through field collection, market investigation, document utilization, comparative morphology and histology.The shape and properties, microscopic characteristics in root, rhizome, leaves were worked out.Asteropyrum can be distinguished from close relative Coptis plants by microscopic and histology characteristics. Two species in Asteropyrum can also be identified by microscopic and histology characteristics, and the morphological and histology characteristics can be used as evidences for quality control of medicinal Asteropyrum plants.

AIM: To confirm the therapeutic effect of Zijin capsule on liver fibrosis in rat model. METHODS: Model group: Bovine serum albumin (BSA) Freund’s incomplete adjuvant 0.5 mL was injected subdermally at d1 d15 d22 d29 and d36 for primary sensitization. Seven days after the fifth injection, BSA antibody in the serum was detected by double agar diffusion method. Normal saline of 0.4 mL was injected through cauda vein to BSA antibody-positive rat twice a week for fifteen times. Traditional Chinese medicine (TCM) decoction group and Zijin capsule group: In the attack injection period, Chinese medicinal decoction or Zijin capsule was given ig, the others were the same as in the model group. NS was used in the control group. The collagen content of rat liver was determined by Bergman’s method and expressed as x- ± s. The liver pathological changes were divided into four grades and expressed as the avarage of the total rank sum. RESULTS: The collagen content (mg/g) of the liver in the control group (7.2 ± 1.9) was significantly lower than that in the other groups; it was higher in the model group (31.7 ± 16.6) than that in the two therapeutic groups; and lower in Zijin capsule group (9.7 ± 2.8) than that in the TCM decoction group (11.5 ± 5.3). The pathological changes were more aggravated in the model group (37.4) than those in the two therapeutic groups; and more severe in the TCM decoction group (30.2) than in the Zijin capsule group (22.9). CONCLUSION: The therapeutic effect of Zijin capsule on the model was confirmed.

We studied the effects of two xanthones compounds isolated from Swertia punicea Hemsl (from Geutianaceae), swertianolin (I) and bellidifolin (II), on Hepatitis B surface antigen (HBsAg) and e antigen (HBeAg) in cultured human hepatocellular carcinoma cell line (HepG 2 ). The HepG 2 cells were first cultured for 24h, various concentrations of these two xanthones were then added to the culture medium. The culture medium containing the two xanthones was exchanged once every 4 days. After 8 days, the cytotoxic activities of these two xanthones were assessed by cytopathic effect. The HepG 2 cells were then treated with the two compounds at a concentration of swertianolin (1.6, 3.1, 6.2, 12.5, 25 m g/ml) and bellidifolin (2.0, 3.9, 7.8, 25.5, 31.2 m g/ml). Four or eight days later, the culture medium was collected and the expression of HBsAg and HBeAg were determined by radioimmunoassay. Our results show that swertianolin can suppress the expression of HBeAg with IC 50 of 8.0 m g/ml, while bellidifolin can inhibit the expression of HBsAg with IC 50 of 13 m g/ml at the eighth days. The Therapeutic Index for swertianolin and bellidifolin are 6.2 and 6.8, respectively. Our findings suggest that swertianolin and bellidifolin have anti-HBV activities in vitro.