Vitellaria paradoxa nutshells from seven sub-Saharan countries as potential herbal medicines for treating diabetes based on chemical compositions, HPLC fingerprints and bioactivity evaluation / 中国天然药物

The aim of the study was to determine the feasibility of the Vitellaria paradoxa nutshell as a new medicinal resource for treating diabetes. A total of forty-one compounds were identified by HPLC-DAD-Q-TOF-MS and phytochemical methods in V. paradoxa nutshell methanol extract. Based on HPLC fingerprints, four characteristic constituents were quantified and the origin of twenty-eight V. paradoxa nutshells from seven sub-Saharan countries was compared, which were classified into three groups with chemometric method. Twenty-eight samples contained high total phenolic content, and exhibited moderate-higher antioxidant activity and strong α-glucosidase inhibitory activity. Furthermore, all fractions and isolated compounds were evaluated for their antioxidant and α-glucosidase inhibitory activities, and α-glucosidase inhibitory action mechanism of four characteristic constituents including protocatechuic acid, 3, 5, 7-trihydroxycoumarin, (2R, 3R)-(+)-taxifolin and quercetin was investigated via molecular docking method, which were all stabilized by hydrogen bonds with α-glucosidase. The study provided an effective approach to waste utilization of V. paradoxa nutshell, which would help to resolve waste environmental pollution and provide a basis for developing potential herbal resource for treating diabetes.

Activation of farnesoid X receptor by GW4064 inhibits invasive growth of colon cancer cells and expression of stromal cell-derived factor 1 / 第二军医大学学报

Objective To explore the mechanism by which specific agonist of farnesoid X receptor (FXR) GW4064 inhibits the growth and invasion of colon cancer cells. Methods Human colon cancer cell lines HT-29 were in vitro cultured. After treatment with GW4064 of 0, 0.1, 1, 3, 5, 7 and 10 μmol/L for 72 h, cell viability was measured by MTT assay. After treatment with GW4064 of 0, 1 and 5 μmol/L for 24 h, the cell morphology was observed under phase contrast microscope, and the mRNA expression levels of FXR and stromal cell-derived factor 1 (SDF-1) were detected by PCR. After treatment with GW4064 of 0 and 1 μmol/L for 24 h, the cell invasive ability was detected by cell scratch test. After treatment with GW4064 of 0, 1, 5 and 7 μmol/L for 24 h, the SDF-1 expression in the culture medium was detected by ELISA. Nude mouse. tumorigenesis model was established by subcutaneous inoculation of HT-29 cells. After intragastric administration with GW4064 or DMSO for 16 d, the tumor growth and the mRNA expression of FXR and SDF-1 in the tumors were determined. ResultsGW4064 inhibited the growth of HT-29 cells in a dose-dependent manner, and there was significant difference in the cell viability of HT-29 cells between the GW4064 groups (1, 3, 5, 7 and 10 μmol/L) and the control group (0 μmol/L, all P<0.05). After treatment with GW4064, phase contrast microscopy showed contracted and rounded colon cancer cells and slender cells transforming into epidermoid cells. The cell scratch test showed that the invasion ability of the colon cancer cells was significantly reduced after treatment with GW4064 compared with the control group (0 μmol/L, P<0.05). PCR results showed that the mRNA expression level of FXR was increased in a dose-dependent manner after GW4064 treatment, while the expression of SDF-1 mRNA changed in the opposite way. ELISA results showed that the SDF-1 expression in the cell culture supernant was decreased with the increase of GW4064 concentrations, and there were significant differences between the GW4064 (1, 5 and 7 μmol/L) groups and the control group (0 μmol/L, P<0.05). GW4064 significantly reduced tumor size compared with the control group (DMSO, P<0.05). In addition, the mRNA expression of FXR in the tumors was increased, and the mRNA expression of SDF-1 was decreased. ConclusionThe activation of FXR can inhibit the invasive growth of colon cancer cells and the expression of SDF-1.

Identification of metabolites and pharmacokinetics of mogrol in rat plasma / 药学学报

Mogrol is the aglycone of seven kinds of mogrosides and siamenoside I. Mogrol has drawn more attention in recent years for its anti-leukemia and anti-diabetes activities. An ultra-high performance liquid chromatography/quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF/MS) method was applied to identify the main metabolites of mogrol in rat plasma. A liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for determination of the main components in rat plasma. After an oral administration of 100 mg·kg-1 mogrol in rats, 13 metabolites were detected along the main component of parent drug in the plasma. The major metabolites were oxidated and dehydrogenated products. In this study, mogrol was quantitative analyzed using lithium carbonate reagent with high sensitivity. The assay was linear in concentration range 5.00-1 000 ng·mL-1 with intra-and inter-day precision within 9.3% and accuracy in range of -4.5% to 2.9%. Mogrol was absorbed into the blood very fast after oral administration, and the time to reach maximum concentration (tmax) was 1.67 h. The half-life (t1/2) of mogrol in rats was 2.34 h, and the oral absolute bioavailability was 3.5%.

Comparison of anesthetic effect of different anesthetic drugs in the pediatric tonsilloadenoiectomy / 天津医药

Objective To investigate different anesthetic effects of remifentanil, sufentanil, and fentanyl in the pediatric tonsilloadenoiectomy. Methods Totally 210 cases of tonsilloadenoiectomy enrolled in our institution from March 2016 to February 2017 were selected as study objects. Children were divided randomly into three groups, with 70 cases in each group, including remifentanil group, sufentanil group, and fentanyl group. Child patients in the remifentanil group were induced by remifentanil with 1μg/kg, and were maintained with 0.1μg · kg-1 · min-1. Remifentanil was withdrawn 5 minutes before the end of operation. Child patients in the sufentanil group were induced by sufentanil with 0.2 μg/kg, and were maintained with 0.1 μg · kg-1 · h-1. Sufentanil was withdrawn 30 minutes before the end of operation. Child patients in the fentanyl group were induced by fentanyl with 2μg/kg, and were maintained with 1μg·kg-1·h-1. Fentanyl was withdrawn 30 minutes before the end of operation. During the anesthesia, the indexes of heart rate (HR), mean arterial pressure (MAP), and oxygen saturation were recorded in the three groups. The time of eyelash reflex disappearance, pain reflex disappearance, postoperation eye open, and extubation were also recorded. The incidences of perioperative adverse events were compared between the three groups. Results HR and MAP at time points of anesthesia induction, 5 minutes after anesthesia induction, and 10 minutes after anesthesia induction were higher in the remifentanil group than those in the other two groups (P<0.05). And the differences of the above indexes at all time points between sufentanil group and fentanyl group showed no statistical significance (P>0.05). The time of pain reflex disappearance, postoperation eye open, and extubation were higher in the fentanyl group than those in the other two groups (P<0.05). And the differences of the above indexes between sufentanil group and remifentanil group showed no statistical significance (P>0.05). Incidence rate of postoperative agitation was higher in the remifentanil group than that in the other two groups (P<0.01). And the difference of incidence rate of postoperative agitation between the sufentanil group and fentanyl group showed no statistical significance ( P>0.05). Conclusion The effect of sufentanil is better than remifentanil and fentanyl in the anesthesia of pediatric tonsilloadenoiectomy, with fast effect, fast analepsia, stable haemodynamics, and low incidence rate of postoperative agitation.

Morphological and TLC identification on Tibetan medicine Asteris Flos / 中国中药杂志

Tibetan medicine Asteris Flos is the flowers of Aster souliei, A. flaccidus, and A. asteroides, with the function of clearing away heat and toxic matter, relieving cough, and removing phlegm. In order to control the quality of Asteris Flos, the morphological and chemical methods were established for identification of three origins. The morphological features of three species were described and photographed, and the microscopic characteristics of three drug powders were also described in detail and pictured. The results showed that three origins of Asteris Flos could be easily distinguished by their macro- and micro-morphologic features, and a key for distinguishing the three origins was given. Moreover, a TLC method, with apigenin-7-O-β-D-glucurono pyranoside and chlorogenic acid as chemical references, was also established for the identification of three origins. The results showed that the TLC chromatograms of the flowers of A. souliei and A. flaccidus were very similar, but different from that of A. asteroides. The established macroscopic, powder microscopic and TLC methods for identification of three origins of AF were simple, accurate, and reproducible, and also effective and easy to operate.

Microscopic and polariscopic characteristics of 30 medicinal plants of Polygonum / 药学学报

Polygonum L. s. str., belonging to Polygonaceae family, is a big genus with abundant medicinal plants. More than 10 plants are specified in Chinese Pharmacopoeia and many local medicinal standards and over 50 species are used as folk medicines. Owing to the similar morphologies and very small flowers and fruits, they are uneasily identified and often confused with each other and misused clinically. In order to provide a basis for identification of Polygonum s. str. plants, a histological study on stems and leaves of 30 species from Polygonum was undertaken by a routine/polarized light microscopy for the first time. The results showed that: (1) the transverse sections of stems of Polygonum are relatively similar, sclerenchyma such as xylem and fibres with strong polarization effects; (2) the surface views of leaves of Polygonum are distinguishable on distributions and types of stomata, with or without attachments (such as glandular hairs/scales or non-glandular hairs) and the polariscopic features of epidermal cell walls, stomata and cell contents. Observed under polarized light, it was found for the first time that stomata on leaf surface of some plants have a Maltese-cross effect with the arms of the cross intersecting at the stomatal opening. As a result, a key combining the microscopic and polariscopic characteristics of the stems as well as leaves was provided for identifying the 30 medicinal plants of Polygonum. The polarized light microscopic method was proven to be one of the quick, simple and effective techniques for the identification of medicinal plants and botanic crude materials.

Effects of bile acids on expression of interleukin-6 and cell viability in QBC939 cell line / 中华外科杂志

<p><b>OBJECTIVE</b>To research the effects of bile acids on the expression of interleukin-6 (IL-6) and the cell viability in QBC939 cell line.</p><p><b>METHODS</b>Human cholangiocarcinoma cells were stimulated with 800 µmol/L bile acid (CA), 100 µmol/L deoxycholate (DCA), 100 µmol/L chenodeoxycholic acid (CDCA), 1200 µmol/L gly acid (GCA), 200 µmol/L glycodeoxycholic acid (GDCA) and 300 µmol/L gly chenodeoxycholic acid (GCDCA).MTT assay and ELISA were used to detect the cell viability and the expression of IL-6 at 24 h, 48 h and 72 h.</p><p><b>RESULTS</b>Treated by DCA, CDCA and GCDCA for 48 hours, the cell viability ratios changed to 0.61, 0.58 and 1.26, which were significant differences between control group and treated groups. And after 72 hours, the viability ratios of group CA, group DCA, group CDCA, group GCA, group GDCA and group GCDCA turned into 0.48, 0.50, 0.42, 1.29, 1.30 and 1.41. The differences of cell viability between bile acid-treated groups and control group were significant (P < 0.05). The expression of IL-6 in control group at 48 h and 72 h was (198 ± 32) ng/L and (323 ± 34) ng/L, while treated by CA, DCA, CDCA, GCA, GDCA and GCDCA respectively for 48 hours, the expression of IL-6 altered to (106 ± 33) ng/L, (88 ± 29) ng/L, (116 ± 54) ng/L, (413 ± 21) ng/L, (587 ± 32) ng/L and (366 ± 30) ng/L. After 72 hours, the expression of IL-6 of each bile acid-treated groups as above was (123 ± 66) ng/L, (45 ± 21) ng/L, (74 ± 45) ng/L, (792 ± 13) ng/L, (1310 ± 22) ng/L and (845 ± 18) ng/L, respectively. The differences between each bile acid-treated group and control group were significant (P < 0.05).</p><p><b>CONCLUSIONS</b>Free bile acids (CA, DCA and CDCA) can inhibit the expression of IL-6 and the cell viability, while glycine conjugates (GCA, GDCA and GCDCA) can promote the expression of IL-6 and the cell viability. Bile acids can change tumor cell viability via IL-6 pathway.</p>

Phenolic components from herbs of Dendrobium aphyllum / 中国中药杂志

<p><b>OBJECTIVE</b>To study the phenolic constituents of Dendrobium aphyllum.</p><p><b>METHOD</b>Various chromatographic techniques were used to isolate and purify the constituents, their physico-chemical properties and spectral data were employed to elucidate their structures.</p><p><b>RESULT</b>Nine bibenzyls and two benzylethanyl compounds were isolated and identified as: moscatilin (1), gigantol (2), batatasin (3), tristin (4), 3, 5, 4'-trihydroxylbibenzyl (5), 3, 5-dimethoxyl-4, 4'-dihydroxylbibenzyl (6), moscatin (7), 2, 4, 7-trihydroxyl-9, 10-dihydrophenanthrene (8), hircinol (9), 2-(4-hydroxyphenyl) ethyl-beta-D-glucopyranoside, salidroside (10) and p-hydroxylbenzylacetic acid (11).</p><p><b>CONCLUSION</b>All compounds were obtained firstly from the plant, and the compounds 10 and 11 were isolated in this genus for the first time.</p>

HPLC fingerprint of Herba Senecionis Scandentis and its ESI-MS analysis / 中国中药杂志

<p><b>OBJECTIVE</b>To study and establish the fingerprints of Herba Senecionis Scandentis by RP-HPLC and LC-MS.</p><p><b>METHOD</b>C18 column was used in the HPLC separation. The mobile phase was composed of acetonitrile and 0.03% phosphoric acid with gradient elution. The flow rate was 1.0 mL m x min(-1) and detection wavelength was 254 nm.</p><p><b>RESULT</b>Under this selected chromatographic condition, good HPLC fingerprints of Senecio scandens were obtained.</p><p><b>CONCLUSION</b>HPLC fingerprint facilitate the evaluation of the quality of Herba Senecionis Scandentis.</p>

Alkaloid and sesquiterpenes from the root tuber of Curcuma longa / 药学学报

One new quinoline alkaloid and seven known bisabolane sesquiterpenes: 2-(2'-methyl-1'-propenyl)-4, 6-dimethyl-7-hydroxyquinoline (1), 2, 5-dihydroxybisabola-3, 10-diene (2), 4, 5-dihydroxybisabola-2,10-diene (3), turmeronol A (4), bisacurone (5), bisacurone A (6), bisacurone B (7) , bisacurone C (8), as well as dehydrozingerone (9) and zingerone (10) were isolated from the root tuber of Curcuma longa. Their structures were identified by spectral evidence. Compound 1 is a new compound, compounds 6 -8 were isolated from this plant for the first time and compounds 9 - 10 from Curcuma for the first time.

Study on chemical constituents from stem of Dendrobium aphyllum / 中国中药杂志

<p><b>OBJECTIVE</b>To study the active constituents of Dendrobium aphyllum.</p><p><b>METHOD</b>Various chromatographic techniques were used to isolate and purify the constituents, their physico-chemical properties and spectral data are determinated to elucidate the structure.</p><p><b>RESULT</b>Eight compounds were isolated and identified as: 4'-methoxyl-tricin (1), tricin (2), 7, 3', 5'-tri-O-methyl-tricetin (3), syringic acid (4), ( + )-syring-aresinol (5), D-allitol (6), sucrose (7), icariside D2 (8).</p><p><b>CONCLUSION</b>Compounds 1-3, 6-8 were isolated from genus Dendrobium for the first time, additionally, the others were obtained firstly from the plant.</p>

Studies on chemical constituents of Dendrobium crystallinum / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Dendobium crystallinum.</p><p><b>METHOD</b>Compounds were isolated and purified by silica gel and Sephadex LH-20 column chromatography. Their structures were identified by physicochemical properties and spectral analyses.</p><p><b>RESULT</b>Nine compounds were obtained and identified as: 4, 4'-dihydroxy-3, 5-dimethoxybi-benzyl (1), gigantol (2), naringenin (3) , p-hydroxybenzoic acid (4), n-tetracosyl trans-p-cou-marate (5), n-octacosy trans-p-coumarate (6), n-hexacosyl trans-ferulate (7), stigmasterol (8), daucosterol (9).</p><p><b>CONCLUSION</b>All these compounds were obtained from this plant for the first time, compounds 1 and 4 were isolated firstly from the genus.</p>

Study on chemical constituents in roots and rhizomes of Ligularia duciforms II / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents in roots and rhizomes of Ligularia duciforms.</p><p><b>METHOD</b>90% ethanol extract was isolated and purified by silica gel and sephadex LH-20 column chromatography, the structures of compounds were identified by physicochemical properties and spectral analysis.</p><p><b>RESULT</b>Nine compounds were isolated and identified as lupeol (1), isoscopoletin (2), isoline (3), duciformine (4), (2S, 3S, 4R)-sphinganine-(2'R)-delta5',6' (E)-2'-hydroxytetracosanoylamino (5), tetracosanoic acid (6), tetracosanoicacid glyceride (7), (E)-docosyl ferulate (8), (E)-docosyl caffeate (9).</p><p><b>CONCLUSION</b>Compounds 1, 2, 5-7 were isolated for the first time from this plant, and the compound 2, 5-7 were isolated firstly from the genus Ligularia.</p>

Studies on constituents of Dendrobium gratiosissimum / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of Dendrobium gratiosissimum.</p><p><b>METHOD</b>The constituents were isolated and purified by silica gel, Sephadex LH-20 colum chromatography, and the structures were identified by physicochemical properties and spectral data.</p><p><b>RESULT</b>Nine compounds were obtained as: 3,5,4'-trihydroxybibenzyl (1), 3,4'-dihydroxy-5-methoxybibenzyl (2), 3,4-dihydroxy-4', 5-dimethoxybibenzyl (3), apigenin (4), p-hydroxybenzaldehyde (5), defuscin (6), n-octacostyl ferulate (7), beta-sitosterol (8) and daucosterol (9).</p><p><b>CONCLUSION</b>All these compounds were obtained from this plant for the first time, and compounds 2, 4 and 5 were isolated firstly from this genus.</p>

Studies on chemical constituents in roots of Rumex dentatus / 中国中药杂志

<p><b>OBJECTIVE</b>To investigate the active constituents from Rumex dentatus.</p><p><b>METHOD</b>Compounds were isolated by silica gel, Sephadex LH -20 and ODS column chromatography and identified by chemical and spectroscopic methods.</p><p><b>RESULT</b>Ten compounds were obtained and identified as helonioside A (1), gallic acid (2), isovanillic acid (3), p-hydroxycinnamic acid (4), succinic acid (5), n-butyl-beta-D-fructopyranoside (6), quercetin (7), hexadecanoic acid 2, 3-dihydroxy propyl ester (8), beta-sitosterol (9) and daucosterol (10).</p><p><b>CONCLUSION</b>Compounds 1, 3-6 and 8 were isolated from the genus of Rumex for the first time.</p>

Studies on constituents in herb of Senecio scandens / 中国中药杂志

<p><b>OBJECTIVE</b>To isolate the constituents of Senecio scandens and determine their structures.</p><p><b>METHOD</b>Componds were isolated and purified by silica gel column chromatography and the structures were identified by spectroscopic methods.</p><p><b>RESULT</b>Nine compounds were isolated as lupenone (1) , oleanane (2) , beta-sitosterol (3) , daucosterol (4) , adonifoline (5) , phydroxy benzeneacetic acid (6) , 2-(1,4-dihydroxy-cyclohexanyl) -acetic acid (7), hyperoside (8), linarin (9).</p><p><b>CONCLUSION</b>These compounds were obtained from S. scandens for the first time except 4 and 6.</p>

Terpenoid compounds isolated from Ligularia sagitta / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents of radix and rhizome of Ligularia sagitta.</p><p><b>METHOD</b>Isolation and purification were carried out on the column chromatography of silica gel and sephadex LH -20. The structures were identified by spectral analysis.</p><p><b>RESULT</b>Seven terpenoid compounds were isolated from the radix and rhizome of L. sagitta. Five of them are sesquiterpenoids, the structures were determined as 7alpha-hydroxy-9(10) -ene-1, 8-dioxo-6, 7-dihydrofuranoeremophilane (1), 1p, 10P3-epoxy-6beta, 8 beta-dihydroxy-eremophil7 (11) -en-12, 8alpha-olide (2) , 1-oxo-9-desoxycacalol (3), benzofuranoeremophil-l-ene (4) and bakkenolide (5); other two compounds belong to triterpenoid. 3p, 16P3-dihydroxy-12-oleanen-28-al (6) and lupeol (7).</p><p><b>CONCLUSION</b>Compoundsl-3 and 6 were: isolated from L. sagitta for the first time, and compounds 3 and 6 were obtained from Ligularia for the first time.</p>

The chemical constituents of Ligularia pleurocaulis / 药学学报

<p><b>AIM</b>To study the chemical constituents of the underground part of Ligularia pleurocaulis (Franch.) Hand-Mazz.</p><p><b>METHODS</b>The dried roots and rhizomes of L. pleurocaulis were extracted with methanol. Isolation and purification were performed by silica gel column chromatography and recrystallization etc. Structures of the pure compounds were established on basis of spectral analysis.</p><p><b>RESULTS</b>Twelve compounds were obtained from L. pleurocaulis, they were 6-angeloyloxy-furanoligularenone (1), 2-oxo-3-hydroxy-eremophila-1(10),3,7(11),8-tetraen-8,12-olide (2), tiglic acid (3), oleanolic acid (4), lupeol (5), beta-sitosterol (6), daucosterol (7), caffeic acid (8), emodin (9), 7-methoxy-coumarin (10), ferulic acid (11) and 4-hydroxy-2,5-dimethoxy-benzaldehyde (12).</p><p><b>CONCLUSION</b>Compound 1 is a new eremophilane and compound 2 is a new natural compound. All above compounds were obtained for the first time from L. pleurocaulis.</p>

Study on the chemical constituents in roots and rhizomes of Ligularia duciforms / 中国中药杂志

<p><b>OBJECTIVE</b>To study the chemical constituents in roots and rhizomes of ligularia duciforms.</p><p><b>METHOD</b>The compounds were isolated by column chromatography, the structures were identified by physicochemical properties and spectral analysis.</p><p><b>RESULT</b>Six compounds were isolated and identified as caffeic acid (I), (E)-docosyl-3, 4-dihydroxycinnamate (II), (E)-docosyl 3-methoxy-4-hydroxyferulate (III, beta-amyrone (IV), beta-sitosterol (V), and daucosterol (VI).</p><p><b>CONCLUSION</b>All the compound were isolated for the first time from the plant, and the compound II and IV were isolated firstly from the genus Ligularia.</p>