Hepatoprotective activity of Zha Xun and its different solvent-eluting components / 药学学报

A pharmacophore-based study was conducted to investigate the therapeutic activity of the traditional Tibetan medicine Zha Xun (ZX) in liver diseases. In the present study, the protective effect of ZX on the acute liver injury induced by concanavalin A (ConA) and 0.15% carbon tetrachloride (0.15% CCl4) in ICR mice was evaluated, and the results showed that ZX significantly reduced serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) in the ConA-induced acute immune liver injury model and the CCl4-induced acute oxidative liver injury model (P < 0.05). Subsequently, the protective effects of aqueous, 95% ethanol, 60% ethanol and 30% ethanol eluting fractions of ZX, and fulvic acid, the main water-soluble constituent of ZX, were evaluated against acute oxidative liver injury induced by 0.15% CCl4 in mice. The results showed that different solvent-eluting fractions of ZX showed certain hepatoprotective activities, among which the aqueous extract of ZX and 30% ethanol extract of ZX significantly reduced the serum levels of ALT, AST, and lactate dehydrogenase (LDH) in mice (P < 0.05), and the serum levels of LDH in mice were significantly reduced by fulvic acid (P < 0.05), which showed significant hepatoprotective activity. The protective activities and preliminary mechanisms of the total extract of ZX, the aqueous extract of ZX, the 30% ethanol extract of ZX, and fulvic acid against hepatocellular injury in vitro were further evaluated by using the H2O2-induced hepatocellular injury model. The results showed that the components could significantly inhibit H2O2-induced hepatocellular injury, reduce the levels of ALT, alkaline phosphatase (ALP), and LDH, improve the survival rate of hepatocellular cells, and reduce the content of intracellular reactive oxygen species (ROS) in cell culture. At the same time, it can inhibit hepatocyte apoptosis by increasing the expression ratio of Bcl-2/BAX protein and decreasing the expression ratio of cleaved caspase-3/pro caspase-3 protein. The present study showed that ZX has clear hepatoprotective activity in vitro and in vivo, and the different solvent elution fractions of ZX showed certain hepatoprotective activity, among which the aqueous extract of ZX, 30% ethanol extract of ZX had better hepatoprotective activity, and the activity of 60% ethanol extract of ZX was stronger than that of 95% ethanol extract of ZX. The activity of ZX and its water-soluble elution site exerted hepatoprotective effects by inhibiting hepatocyte apoptosis and oxidative stress. The animals used in this experiment and related disposal meet the requirements of animal welfare, and have been reviewed and approved by the Laboratory Animal Management and Use Committee of the Institute of Materia Medica, Chinese Academy of Medical Sciences (approval number: 00004018).

Straw Incorporation with Nitrogen Amendment Shapes Bacterial Community Structure in an Iron-Rich Paddy Soil by Altering Nitrogen Reserves.

Incorporation of crop straw into the soil along with inorganic fertilization is a widespread agricultural practice and is essential in nutrient-scarce soils, such as iron-rich (ferruginous) paddy soils. The responses of soil bacterial communities to straw incorporation under different nitrogen inputs in iron-rich soils remain unclear. Therefore, 6000 kg ha-1 dry wheat (Triticum aestivum L. cv. Zhengmai 12) straw was applied to a rice paddy with and without nitrogen amendment (0, 80, 300, and 450 kg ha-1 N as urea), to investigate its effects on soil fertility and bacterial community structure. Organic matter, total nitrogen, and water contents tended to decrease in straw-incorporated soils with different nitrogen inputs. Proteobacteria was the dominant bacterial phylum across all treatments (26.3-32.5% of total sequences), followed by Chloroflexi, Acidobacteria, and Nitrospirae. Up to 18.0% of all the taxa in the bacterial communities were associated with iron cycling. Straw incorporation with nitrogen amendment increased the relative abundance of iron oxidizers, Gallionellaceae, while decreasing the relative abundance of iron reducers, Geobacteraceae. Bacterial community composition shifted in different treatments, with total nitrogen, water, and Fe(III) contents being the key drivers. Straw incorporation supplemented by 300 kg ha-1 N increased bacterial richness and enhanced all the predicted bacterial functions, so that it is recommended as the optimal nitrogen dosage in practice.

Zenglv Fumai Granule protects cardiomyocytes against hypoxia/reoxygenation-induced apoptosis via inhibiting TRIM28 expression.

Myocardial ischemia/reperfusion (MIR) injury, which occurs following acute myocardial infarction, can cause secondary damage to the heart. Tripartite interaction motif (TRIM) proteins, a class of E3 ubiquitin ligases, have been recognized as critical regulators in MIR injury. Zenglv Fumai Granule (ZFG) is a clinical prescription for the treatment of sick sinus syndrome, a disease that is associated with MIR injury. The present study aimed to investigate the effect of ZFG on MIR injury and to determine whether ZFG exerts its effects via regulation of TRIM proteins. In order to establish an in vitro MIR model, human cardiomyocyte cell line AC16 was cultured under hypoxia for 5 h and then under normal conditions for 1 h. Following hypoxia/reoxygenation (H/R) treatment, these cells were cultured with different ZFG concentrations. ZFG notably inhibited H/R-induced cardiomyocyte apoptosis. The expression levels of four TRIM proteins, TRIM7, TRIM14, TRIM22 and TRIM28, were also detected. These four proteins were significantly upregulated in H/R-injured cardiomyocytes, whereas their expression was inhibited following ZFG treatment. Moreover, TRIM28 knockdown inhibited H/R-induced cardiomyocyte apoptosis, whereas TRIM28 overexpression promoted apoptosis and generation of reactive oxygen species (ROS) in cardiomyocytes. However, the effects of TRIM28 overexpression were limited by the action of ROS inhibitor N-acetyl-L-cysteine. In addition, the mRNA and protein levels of antioxidant enzyme glutathione peroxidase (GPX)1 were significantly downregulated in H/R-injured cardiomyocytes. TRIM28 knockdown restored GPX1 protein levels but had no effect on mRNA expression levels. Co-immunoprecipitation and ubiquitination assays demonstrated that TRIM28 negatively regulated GPX1 via ubiquitination. In sum, the present study revealed that ZFG attenuated H/R-induced cardiomyocyte apoptosis by regulating the TRIM28/GPX1/ROS pathway. ZFG and TRIM28 offer potential therapeutic options for the treatment of MIR injury.

Chemical constituents of Artemisia lactiflora(II) / 中国中药杂志

To study the chemical constituents of Artemisia lactiflora. The compounds were isolated by column chromatography with silica gel, C18 reverse-phase silica gel, semi-preparative HPLC, and their structures were elucidated on the basis of spectral analysis. Twelve compounds were isolated from alcohol extracts of A. lactiflora and identified as 7-hydroxycoumarin (1), 7-methoxycoumarin (2), balanophonin (3), aurantiamide (4), aurantiamide acetate (5), isovitexin (6), kaempferol-3-O-beta-D-rutinoside (7), rutin (8), caffeic acid ethyl ester (9), quercetin (10), methyl 3, 5-di-O-caffeoyl quinate (11) and methyl 3, 4-di-O-caffeoyl quinate (12), respectively. Compounds 3-12 were obtained from this plant for the first time.

The analgesic and anti-rheumatic effects of Thladiantha dubia fruit crude polysaccharide fraction in mice and rats.

ETHNOPHARMACOLOGICAL RELEVANCE: The fruit of Thladiantha dubia has been used in Chinese manchu nationality folk medicine for treatment of various pains, such as rheumatic pain, lumbocrural pain, and dysmenorrhea. The aim of the present study was to evaluate the anti-rheumatic effect of Thladiantha dubia fruit crude polysaccharide (TF-P) fraction in rats. MATERIALS AND METHODS: TF-P was evaluated in mice for analgesic activity using acetic acid-induced abdominal contractions test and for anti-inflammatory activity using xylene-induced ear oedema model. Moreover, rheumatoid arthritis (RA) was induced by injection of CFA into the subplantar surface of the hind paw of the male Wistar rats. Joint swelling was measured. In order to evaluate the effect of TF-P on disease progression, proinflammatory mediators (TNF-α and IL-2), and antioxidant indicators (SOD, MDA, and NO) were determined in rats induced by CFA. Pathologic changes of RA in rats were also observed under light microscope. RESULTS AND CONCLUSIONS: In the present study, TF-P at the dose of 200mg/kg (according to the clinical traditional dosage) significantly reduced writhings and stretchings induced by the acetic acid in mice. TF-P significantly inhibited xylene-induced ear oedema in mice, compared with control group. TF-P significantly inhibited inoculated and non-inoculated joint swellings in rats induced by CFA. TF-P had no effect of body weight in rats. The histopathological analysis suggested that TF-P obviously alleviated the degree of RA rats. TF-P treated rats preserved a nearly normal histological architecture of the joint. Results of the present study confirm the use of Thladiantha dubia traditionally for the treatment of painful and inflammatory conditions. Those results suggest TF-P has protective and therapeutic effects on RA rats induced by CFA.

The anti-hyperplasia of mammary gland effect of Thladiantha dubia root ethanol extract in rats reduced by estrogen and progestogen.

AIM OF THE STUDY: Thladiantha dubia (Cucurbitaceae) has been used in Chinese manchu nationality folk medicine for treatment of various diseases, such as scrofula, carbuncle, lactation deficiency, etc. Its effects include softening hard masses, heat-clearing and detoxifying, reducing swelling, eliminating carbuncle, and promoting lactation. It has a history of use in the treatment of breast disorders and as an agent to increase lactation. The aim of the present study was to evaluate the anti-hyperplasia of mammary (HMG) effect of T. dubia root ethanol extract (TD-E) in estrogen combined with progestogen induced HMG rats. MATERIALS AND METHODS: Forty virgin female Wistar rats were randomly divided into blank control, HMG model, Rupixiao Tablet (RPXT, positive control), and TD-E groups, 10 in each. Injection of estrogen and progestogen were given to establish rat models of HMG, RPXT and TD-E were given at the same time. Changes of nipple heights were measured; uterus and ovary index were calculated; sex hormone levels (LH, E(2), and P) in serum were estimated. Pathologic changes of MG in rats were also observed under light microscope. RESULTS AND CONCLUSION: TD-E could decrease the increased nipple height, reduce the numbers of MG lobules and relieve the pathologic changes of HMG in rats. It could also decrease E(2) and LH levels in serum compared with the control group, nipple height, uterus index, and the levels of E(2) and LH in the HMG model group increased significantly, the level of P decreased significantly. Compared with the HMG model group, nipple height, uterus index, and the levels of E(2) and LH in the TD-E group decreased, and no obvious effect on P content. The histopathological analysis suggested that TD-E obviously alleviated the degree of HMG. Those results suggest TD-E has protective and therapeutic effects on HMG rats induced by estrogen and progestogen.

The hepatoprotective and antifibrotic effects of Saururus chinensis against carbon tetrachloride induced hepatic fibrosis in rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Saururus chinensis (Lour.) Baill (Saururaceae) has been used in Chinese folk medicine for treatment of various diseases, such as edema, jaundice, gonorrhea, antipyretic, diuretic, and antiinflammatory agents. AIM OF THE STUDY: Our aim was to evaluate the hepatoprotective and antifibrotic effects of Saururus chinensis extract (SC-E) in carbon tetrachloride (CCl(4)) induced liver fibrosis rats. MATERIALS AND METHODS: The SC-E (70 mg/kg) was administrated via gavage once a day starting from the onset of CCl(4) treatment (14 weeks) for subsequent 8 weeks. Evaluated with liver index, serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), hyaluronic acid (HA), hepatic malondialdehyde (MDA) content, and superoxide dismutase (SOD) activity, total cholesterol (TC), triglyceride (TG), total lipoprotein (TP), albumin (ALB), hydroxyproline (HYP), total antioxidant capacity (T-AOC), laminin (LN), type III collagen terminal peptide (PC-IIINP), and type IV collagen (IV-C), as well as with histopathologic changes of liver. RESULTS: SC-E effectively reduced the elevated levels of liver index, serum ALT, AST, HA, and hepatic MDA contents, enhance the reduced hepatic SOD activity in CCl(4)-treated rats. The histopathological analysis suggested that SC-E obviously alleviated the degree of liver fibrosis induced by CCl(4). CONCLUSIONS: Those results suggest SC-E has protective and therapeutic effects on liver fibrosis induced by CCl(4).

[Diterpenes constituents of Tripterygium wilfordii].

AIM: To study the chemical constituents of Tripterygium wilfordii Hook. F. METHODS: Various column chromatographies with silica gel were used for the isolation and purification. The structures of compounds were established on the basis of its IR, MS, UV, 1H NMR, 13C NMR and HRMS, 1H-1H COSY, 1H-13C COSY and NOESY. RESULTS: Four diterpenoids were isolated: 16-hydroxytriptolide (I), triptolidenol (II), tripdiolide (III), 2-epitripdiolide (IV). CONCLUSION: Compound IV is a new diterpenoid.

Diterpenes constituents of Tripterygium wilfordii / 药学学报

<p><b>AIM</b>To study the chemical constituents of Tripterygium wilfordii Hook. F.</p><p><b>METHODS</b>Various column chromatographies with silica gel were used for the isolation and purification. The structures of compounds were established on the basis of its IR, MS, UV, 1H NMR, 13C NMR and HRMS, 1H-1H COSY, 1H-13C COSY and NOESY.</p><p><b>RESULTS</b>Four diterpenoids were isolated: 16-hydroxytriptolide (I), triptolidenol (II), tripdiolide (III), 2-epitripdiolide (IV).</p><p><b>CONCLUSION</b>Compound IV is a new diterpenoid.</p>

[Anti-lipid peroxidaton of the water extract from cornu cervi pantotrichum].

OBJECTIVE: To investigate the anti-lipid peroxidation of the water extract from Cornu Cervi Pantotrichum (WECCP) in vitro. METHODS: The lipid peroxidation (malondialdehyde formation) in microsomes of rat brain, liver and kidney induced by NADPH-Vit C and cyctein-Fe2+, and the superoxide anion radical production (reduced cytochrome c formation) in xanthine-xanthine oxidase system in vitro were evaluated. RESULTS: The lipid peroxidation (MDA formation) in microsomes of rat brain, liver and kidney induced by NADPH-Vit C and cyctein-Fe2+, O2 production(reduced cytochrome c formation) in xanthine-xanthine oxidase system were significantly inhibited by WECCP. CONCLUSION: WECCP exhibits an antioxidant activity.

[Isolation and structure of wilfordlonging from Tripterygium wilfordii Hook. f].

AIM: To study the chemical composition of Tripterygirm wilfordii Hook. f. METHODS: Colunm 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. RESULTS: Two sesquiterpene alkaloids were isolated and their structures were elucidated as wilforgine and wilfordlongine on the basis of spectral evidence. CONCLUSION: Wilfordclonine is a new sesquiterpene alkaloid.

Isolation and structure of wilfordlonging from Tripterygium wilfordii Hook. f / 药学学报

<p><b>AIM</b>To study the chemical composition of Tripterygirm wilfordii Hook. f.</p><p><b>METHODS</b>Colunm 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.</p><p><b>RESULTS</b>Two sesquiterpene alkaloids were isolated and their structures were elucidated as wilforgine and wilfordlongine on the basis of spectral evidence.</p><p><b>CONCLUSION</b>Wilfordclonine is a new sesquiterpene alkaloid.</p>