Barbaloin attenuates pulmonary fibrosis through TGF-ß1/Smads/p38 pathway.

OBJECTIVES: Barbaloin is one of the main bioactive ingredients extracted from Aloe vera, which has the property of protecting the lung from LPS-induced acute injury; however, the anti-pulmonary fibrosis effect of barbaloin is still unknown. Herein, we present novel data showing the anti-pulmonary fibrosis effect of barbaloin and revealing the possible molecular mechanism. METHODS: In vivo experiment, oral administration of barbaloin was investigated through paraquat-induced pulmonary fibrosis in mice. In vitro experiment, epithelial-mesenchymal transition (EMT) process and TGF-ß1 pathway were investigated in A549 cells for exploring the anti-fibrosis molecular mechanism of barbaloin. KEY FINDINGS: Results showed that barbaloin could improve pulmonary fibrosis through improving physiological routine indexes and histopathological lesions of mice in a dose-dependent manner. Hydroxyproline, collagen I, N-cadherin and α-SMA levels were significantly suppressed. Besides, pro-inflammatory cytokines were also improved. In vitro experiment, barbaloin could inhibit the process of EMT through repressing α-SMA, collagen I and N-cadherin and increasing E-cadherin. In addition, barbaloin could repress the expression of p-Smad2/3 and then suppress the process of EMT through intervening TGF-ß1-induced canonical pathway. Moreover, MMP-2 and MMP-9 were also inhibited by barbaloin via repressing phosphorylation of p38 through TGF-ß1-induced non-canonical axis. CONCLUSIONS: Our findings reveal the anti-pulmonary fibrosis effect of barbaloin in vivo and in vitro for the first time. These results indicate that barbaloin may be a promising clinical candidate drug against pulmonary fibrosis.

Identification and Attribution of Chemical Constituents in Naizilai Granules by UHPLC-Q-Orbitrap-MS / 中国实验方剂学杂志

Objective:Ultra-high performance liquid chromatography-quadrupole/orbitrap high resolution mass spectrometry （UHPLC-Q-Orbitrap-MS） was used to rapidly analyze and assign the chemical constituents of Naizilai granules. Method:An ACQUITY UPLC BEH Shield RP C₁₈ column （2.1 mm×100 mm， 1.7 µm） was selected for chromatographic analysis， the mobile phase was 0.1% formic acid aqueous solution （A） and acetonitrile （B） for gradient elution （0-3 min， 1%B； 3-16 min， 1%-11%B； 16-30 min， 11%-34%B； 30-37 min， 34%-52%B； 37-42 min， 52%-100%B； 42-44 min， 100%B）， flow rate was 0.3 mL·min^-1 and the column temperature was 35 ℃. Mass spectrometry data of Naizilai granules were collected in positive and negative ion modes， the chemical constituents of this preparation were speculated and identified according to the precise molecular weight， secondary fragmentation and other information， combined with reference substance and literature data. Result:A total of 175 compounds were identified and speculated， including 72 flavonoids， 77 organic acids， 15 sesquiterpenes， 6 coumarins and 5 other compounds. Among these identified chemical constituents， there were 154 from <italic>Artemisia rupestris</italic>， 64 from <italic>Hyssopus cuspidatus</italic>， 33 from <italic>Cordia dichotoma</italic>， 42 from <italic>Viola tianshanica</italic>， 56 from <italic>Lactuca sativa</italic>， 65 from <italic>Mentha haplocalyx</italic>， 78 from <italic>Matricaria chamomilla</italic>， 28 from <italic>Ziziphus jujuba</italic>， 7 of which were common components of these eight herbs. Conclusion:The established analytical method can realize the rapid and accurate identification of the chemical constituents in Naizilai granules， and basically covers the main constituents of each medicinal material in the formula， so as to provide a basis for improving the quality evaluation system of the preparation and lay a foundation for elucidating the pharmacodynamic mechanism.

Chemical constituents and their pharmacological activities of plants from Cichorium genus / 中草药·英文版

Plants of genus Cichorium are famous due to their therapeutic and medicinal properties. They are used as traditional medicine and edible food. To date, several scholars concentrated on compounds belonging to coumarins, flavonoids, sesquiterpenoids, triterpenoids, steroids, organic acids and other chemical constituents. Pharmacological effects such as photo-protective, hepatoprotective, anti-diabetic and lipid lowering, antioxidant, anti-inflammation, antifungal, antimalarial, increased bone mineral density, as well as vasorelaxant and antitumour activity were wildly reported. In this study, botanical resources, ethnopharmacological application, chemical constituents and bioactivities, as well as safety and toxicity of clinical applications of genus Cichorium were reviewed, which may provide a reliable basis for further development and utilization of Cichorium genetic resources.

Isochlorogenic acid A promotes melanin synthesis in B16 cell through the ß-catenin signal pathway.

Isochlorogenic acid A, also called 3,5-dicaffeoylquinic acid (3,5-diCQA), is a widespread phenolic compound in the plant. Recent studies have shown that it has antioxidant and anti-inflammatory activity. In addition, oxidative stress and inflammation induced by solar ultraviolet radiation is a very significant reason for skin depigmentation. Therefore, in this study, we evaluated the effect of 3,5-diCQA on B16 cells and explored its molecular mechanism. Results showed that 3,5-diCQA upregulated intracellular melanin production in a time- and dose-dependent manner. Tyrosinase (TYR) activity was also increased after treatment with 3,5-diCQA in a dose-dependent manner. Expressions of TYR, TYR-related protein1, TYR-related protein2, and microphthalmia-associated transcription factor were upregulated in a dose-dependent manner after 48 h of treatment with 3,5-diCQA. Results also showed that 3,5-diCQA promoted the phosphorylation of Akt at Thr308 and glycogen synthase kinase-3ß at Ser 9. Moreover, 3,5-diCQA increased the content of ß-catenin in cell cytoplasm and nucleus by reducing the content of phosphorylated ß-catenin (p-ß-catenin). All these results suggest that 3,5-diCQA may mediate the acceleration of melanin synthesis by the ß-catenin signal pathway.

Alkaloids of Nitraria sibirica Pall. decrease hypertension and albuminuria in angiotensin II-salt hypertension / 中国天然药物

In traditional Chinese medicine, Nitraria sibirica Pall. (Nitrariaceae) is used to treat hypertension. This study determined the effects of the total alkaloids of the leaves of Nitraria sibirica (NSTA) on blood pressure and albuminuria in mice treated with angiotensin II and a high-salt diet (ANG/HS). Adult mice were divided into three groups: control; infused with angiotensin II and fed a diet containing 4% NaCl (ANG/HS; and ANG/HS plus injection of NSTA (1 mg·kg(-1)·d(-1), i.p.). After treatment of these regimens, daily water and food intake, kidney weight, blood pressure, urinary albumin excretion, renal concentrations of inflammatory markers, including soluble intercellular adhesion molecule-1 (sICAM-1) and monocyte chemoattractant protein-1 (MCP-1), and the expression of renal fibrosis markers were determined. Compared to the control group, the ANG/HS group had higher blood pressure and urinary albumin excretion. Treatment with NSTA in ANG/HS mice for three weeks significantly reduced blood pressure and urinary albumin excretion. ANG/HS treatment caused elevated levels of sICAM-1 and MCP-1, as well as increased fibrosis markers. Concurrent treatment with ANG/HS and NSTA attenuated the levels and expression of renal inflammatory and fibrosis markers. Treatment with NSTA effectively reduces hypertension-induced albuminuria through the reduction of renal inflammatory and fibrosis markers.

[Effects of pomegranate flowers polyphenols on liver PON expression of diabetes combining non-alcoholic fat liver diseases rats].

To investigate the protective effects and possible mechanism of pomegranate flowers polyphenols (PFP) on liver function of rats with diabetes combining non-alcoholic fat liver diseases, diabetes combining nonalcoholic fat liver disease model rats were established with high calorie feeding and small dose intraperitoneal injection of streptozotocin (STZ). Model rats were randomly divided into: model group, metformin group, pomegranate flowers polyphenols low, medium and high dose group (75, 150 and 300 mg x kg(-1)). After four weeks treatment, the levels of FPG, blood fat profiles and serum insulin, ALT, AST levels, SOD and MDA in the liver and serum separately were analyzed with biochemical methods. Paraoxonase (PON1 and PON3) mRNA and protein expression in liver were checked by RT-PCR and immunohistochemical method. Pathological changes of the liver were observed. FPG, IRI, non-HDL-C and transaminase significantly reduced and HDL-C raised in the each PFP dose group; Furthermore, compared with model group, fat drops in liver cells significantly reduced, antioxidant ability enhanced, PON1 mRNA and protein expression level in liver increased significantly. The protective effects of PFP against diabetes combining non-alcoholic fat liver diseases rats might through the increase liver PON1 mRNA and protein expression further enhanced the body antioxidant capacity and reduced IRI so as to ameliorate the rat hepatic steatosis.

[Effects of two different extracts of total saponins from Cicer arietinum on kidney of T2DM rats].

Protective effects of two different extracts of TSCA (total saponins from Cicer arietinum) were studied on kidney of T2DM rats. The diabetic model group was established with high calorie feeding and small dose injection of streptozotocin (STZ, 45 mg x kg(-1)). DM rats were randomly assigned to model group (feed with propylene glycol 1 mL/100 g), TSCA high dose group (300 mg x kg(-1)), TSCA low dose group (100 mg x kg(-1)) and normal control group (feed with propylene glycol 1 mL/100 g). After four weeks treatment with TSCA I and II, the levels of FPG FIns, BUN, Scr, ATII, ET-1, TXB2 and 6-keto-PGF1alpha in blood and the activities of SOD, GSH-PX and MDA in kidney were analyzed by biochemical methods. After four weeks treatment with TSCA II, the levels of FPG FIns, BUN, Scr, ATII and ET-1 were reduced significantly; and the ratios of TXB2 to 6-keto-PGF1alpha and SOD were effectively alleviated in TSCA II group. While there is no significant change on FPG and BUN in comparison to the rats treated with TSCA I, Scr, ATII, ET-I, GSH-PX and SOD were alleviated. The results suggest that TSCA II could be used to reduce FPG and FIns. According to the result of vasoactive substances index, TSCA II is more effective than TSCA I on renal protection of DM rats.

[Analysis of essential oil extracted from Lactuca sativa seeds growing in Xinjiang by GC-MS].

OBJECTIVE: To analyze the components of essential oil from Lactuca sativa seeds growing in Xinjiang. METHODS: The components of essential oil from Lactuca sativa seeds were analyzed by gas chromatography-mass spectrometry (GC-MS). RESULTS: 62 components were identified from 71 separated peaks,amounting to total mass fraction 95.07%. The dominant compounds were n-Hexanol (36.31%), n-Hexanal (13.71%), trans-2-Octen-l-ol (8.09%) and 2-n-Pentylfuran (4.41%). CONCLUSION: The research provides a theoretical basis for the exploitation and use of Lactuca sativa seeds resource.

Simultaneous determination of contents of sophoridine, oxymatrine and oxysophocarpine in seed of Sophora alopecuroides by HPLC / 中国中药杂志

<p><b>OBJECTIVE</b>To develop a HPLC method for simultaneous determination of the contents of sophoridine, oxymatrine and oxysophocarpine in seed of Sophora alopecuroides.</p><p><b>METHOD</b>Chromatographic condition included a Phenomenex Gemini C18 (4.6 mm x 250 mm, 5 microm) column and thmobile phase consisting of a mixture of methanol-0.2% phosphatic acid (7:93). The detection wavelength was at 205 nm. The flow rate was 1.0 mL x min(-1) and column temperature was set at 30 degrees C.</p><p><b>RESULT</b>All calibration curves showed good linearity (r > or = 0.9997) within test ranges. The mean recoveries were 100.0%, 97.0% and 97.0% respectively.</p><p><b>CONCLUSION</b>This method is simple, rapid and accurate, and suitable for quality control of S. alopecuroides seed.</p>