Synergistic effects of Cortex Mori alkaloids combined with Simvastatin in rats with hyperlipidaemia / 中国临床药理学与治疗学

AIM: To explore the lipid lowering effect of Cortex Mori alkaloids combined with simvastatin on hyperlipidemia rats. METHODS: Hyperlipidemia model was established by feeding golden hamsters with high-fat diet for 6 weeks, and 40 golden hamsters were randomly divided into normal group, model group, Cortex Mori alkaloids group (CMA, 25 mg•kg-1•d-1),simvastatin group (15 mg•kg-1•d-1) and combination group (Cortex Mori alkaloids, 25 mg•kg-1•d-1, simvastatin 15 mg•kg-1•d-1). 2 weeks after the intragastric administration, cardiac blood sampling was used to determine the blood biochemical indexes such as TG,TC,LDL-C,HDL-C, as well as the levels of ALT,AST,CRP, NO,Lp-PLA2.Liver HE staining was used to observe pathological changes, and liver cell lipid deposition was observed by oil red O staining. RESULTS:Compared with the model group, TC levels in combination group were significantly reduced (P<0.05), LDL-C levels in simvastatin group and the combination group were significantly reduced (P<0.05).The level of NO in the combined group was significantly increased (P<0.05), and the difference was statistically significant compared with that in Cortex Mori alkaloids group and simvastatin group (P<0.05).The levels of CRP were significantly decreased in Cortex Mori alkaloids group, simvastatin group and the combination group (P<0.05).The level of Lp-PLA2 in combination group was significantly reduced (P<0.05). The results of liver HE staining and oil red O staining showed that both of them could improve the hepatic lesion and lipid deposition after drug treatment, and the improvement of the combination group was better than that of the two groups alone. CONCLUSION: Simvastatin combined with Cortex Mori alkaloids can effectively decrease lipid level and inflammatory level of golden hamstrel with hyperlipidemia.Cortex Mori alkaloids can be used as the auxiliary drug of simvastatin, which is expected to provide a new choice for clinical treatment of hyperlipidemia.

Effect of polyphenol from Cortex Mori on melanogenesis of B16 cells and its mechanism / 中国药理学通报

Aim To investigate the inhibitory effect of polyphenol from Cortex Mori( CMP) on melanogenesis in mouse melanoma B16 cells and its possible mecha- nism. Methods Melanoma B16 cells with high ex-pression melanin were induced by α-melanocyte-stimu-lating hormone ( α-MSH) to establish cell model. Cell viability was detected by MTT assay. The melanin syn-thesis and tyrosinase activity were measured by NaOH and L-Dopa assays, respectively. The tyrosinase (TYR), tyrosinase-related protein-1 (TRP-1), tyrosi-nase-related protein-2 ( TRP-2 ) and microphthalmia associated transcription factor ( MITF ) protein and mRNA levels were measured by Western blot and qRT-PCR, respectively. Results CMP could inhibit the melanin synthesis and tyrosinase activity in α-MSH stimulated B16 cells in a dose-dependent manner ( P<0.05) . The melanin content and tyrosinase activity significantly decreased by 52.95% , 32.85% at 20 mg ·L-1of CMP, respectively. Treatment of 100 mg· L-1of arbutin reduced the melanin content and tyrosi- nase activity by 17.29% , 16.75% , respectively. Based on the results of this study, CMP showed a stronger anti-melanogenesis activity than that of positive control arbutin. After treated by CMP, the protein and mRNA levels of TYR, TRP-1, TRP-2 and MITF were significantly inhibited compared to the α-MSH group ( P<0.05) . Conclusions CMP could suppress the melanogenesis in α-MSH stimulated B16 cells, and its mechanism may be related to its regulation of the pro-tein and mRNA expressions of TYR, TRP-1, TRP-2 and MITF, and the inhibition of tyrosinase activity.

Virtual Screening ofα-glycosidase Inhibitors in Cortex mori and Folium mori / 中国药房

OBJECTIVE:To virtually screen potential α-glycosidase inhibitor ingredients from C. mori and F. mori,and to pro-vide reference for finding out new typeα-glycosidase inhibitor ingredient. METHODS:Surflex-Dock module of Sybyl-x 2.0 molecu-lar simulation software was used to perform the docking of small molecule compound,which was from the ingredients of C. mori and F. mori as ligand stated in literatures,with α-glycosidase. Total score of affinity scoring function was equal to 7 as the thresh-old value,to judge potential α-glycosidase inhibitor ingredient in C. mori and F. mori. RESULTS:After 70 small molecule com-pounds docked with α-glycosidase, 10 compounds showed binding activity (Total score≥7.00). Among them, moracin M-3′-O-β-D-glucopyranoside,5,7,2′-trihydroxyflavanone-4′-O-β-D-glucoside,mulberroside A,resveratrol-4,3′-di-O-β-D-gluco-pyranoside and 1,4-dideoxy-1,4-imino-(2-O-β-D-glucopyranosyl)-D-arabinitol had higher binding activity with α-glycosidase(Total score>8.00). CONCLUSIONS:Multi-constituents of C. mori and F. Mori show potential α-glycosidase inhibitory activity. The method is a kind of highly targeted,rapid and efficient approach to discover α-glycosidase inhibitor from traditional Chinese medi-cine.

Study on Quality Standard of Feireqingjie Oral Liquid / 中国中医药信息杂志

Objective To study the quality control method of Feireqingjie Oral Liquid. Methods UV was used to determine the content of total flavonoid. Cortex Mori was identified qualitatively by TLC. Pheretima was identified qualitatively by PC. Results Total flavonoid showed a good linear relationship in the range of 0.005 26-0.052 60 mg/mL, r=0.999 8. The average recovery rate was 98.65%, RSD=0.28% (n=6). The TLC spot of Cortex Mori was coincident with the standard reference, and Pheretima showed the same color as the reference in PC, with no interference of negative control. Conclusion The method is convenient, accurate and can be used as one of the quality control methods of Feireqingjie Oral Liquid.

Influence of Processing Method on Chemical Composition of Cortex Mori radicis

Cortex Mori radicis (CMR) is a traditional medicine using in the treatment of cough due to heat phlegm. The material consists of Cortex Mori radicis harvesting from the mulberry of four, five, seven and ten years in Hai Duong, Lao Cai, Lam Dong province and bought in Lan Ong street (Ha Noi) and pure honey. CMR is processed by mixing with honey and roasted. CMR with before and after processing also consist of uniform chemical components: flavonoids, tanin, total nitrogen reduced sugars, amino acids and organic acids of the remedy. The contents of flavonoid and tanin in raw CMR and processing CMR does not alter significantly.

Influence of Cortex mori on the Capsaicin-induced Neurogenic Inflammation / 대한해부학회지

The root bark of mulberry (Morus alba L. Cortex Mori and other plant of the genus Morus) has been used as an antiphlogistic, diuretic, and expectorant in herbal medicine, and the crude drug is known as "Sangbaikpi" in Korea. Capsaicin, a neurotoxin extracted from a red peppers, has selective effects on peptide-containing C-fiber and induces the release of neuropeptides from sensory nerve ending. But, any reports about the influences of Cortex mori (CM) on the capsaicin-induced neurogenic inflammation were not found, and the precise mechanism of capsaicin-induced neurogenic inflammation remains incompletely understood. The purpose of this study was to determine whether CM could inhibit the capsaicin-induced cutaneous reaction, and to find out its action mechanism. For this purpose, influences of CM on the capsaicin-induced cutaneous reaction (vascular permeability) in back skin of Sprague-Dawley rat, capsaicin-induced histamine release, calcium influx and the change of intracellular cAMP level in rat peritoneal mast cell were estimated. Results obtained were as follows; 1. Pretreatment of CM inhibited remarkably the capsaicin-induced cutaneous reaction. 2. The capsaicin-induced histamine release was inhibited by pretreatment with CM. 3. Capsaicin-induced calcium influx into mast cell was also inhibited by pretreatment with CM. 4. Capsaicin-induced decrease of cAMP level in the mast cell was inhibited significantly by pretreatment with CM. These results suggest that CM contains some substances with an anti-neurogenic inflammatory activity which inhibit the capsaicin-induced cutaneous reaction through the mechanism of mast cell stabilization.

Inhibitory Effect of Cortex mori on the Colchicine-induced Mast Cell Activation / 대한해부학회지

Cortex mori (Morus alba L. : Sangbaikpi), the root barks of mulberry tree, has been used as an antiphlogistic, diuretic, and expectorant in herbs. Previous studies have demonstrated that the phenolic extracts of Cortex mori have hypotensive, hypoglycemic, antifungal, antiviral, antiinflammatory, and anticancer effects, and the hot water extract from Cortex mori has the inhibitory effects on compound 48/80-induced mast cell degranulation and histamine release from rat mast cells (RMCs). Colchicine, an alkaloid found in the crocuslike plant, has been known as an inhibitor of mitosis and microtubule assembly by formation of tubulin-colchicine complex. The purpose of this study was to examine the effect of Cortex mori on the colchicine-induced mast cell degranulation, histamine release, and calcium uptake as a part of the study of the role of microtubules in the mast cell secretory process and the inhibitory mechanism of Cortex mori. The results were summarized as follows. Cortex mori sigificantly inhibited the colchicine-induced cytomorphologi-cal changes of RMCs such as displacement of the nucleus to the periphery, pronounced anisodiametry of the cytoplasm, stubby or broad cytoplasmic mass. Colchicine induced histamine release from RMCs and calcium uptake into RMCs, but it was not significantly , compared to those of negative control group. Cortex mori inhibited the colchicine-induced histamine release from RMCs and calcium uptake into RMCs. Above results, it is suggested that Cortex mori has an activity to inhibit the colchicine-induced cytomorphological changes by inhibition of calcium uptake into the mast cells.

Inhibitory Effect of Polysaccharide Fraction from Cortex Mori on Compound 48/80-Induced Mast Cell Activation / 대한면역학회지

Cortex mori (Morus alba L.: Sangbaikpi), the root bark of mulberry tree, has been used as an antiphlogistic, diuretic, and expectorant in herbal medicine. Previous studies have demonstrated that the phenolic extract of Cortex mori have hypotensive, hypoglycemic, antifungal, antiviral, antiinflammatory, and anticancer effects, and the hot water extract from Cortex mori has inhibitory effects on compound 48/80- induced mast cell degranulation and histamine release from rat peritoneal mast cells (RPMCs). This study was perforrned to investigate the effects of polysaccharide fraction from Cortex mori (PFCM) on compound 48/80-induced degranulation, histamine release, calcium influx, changes of intracellular cAMP and cGMP level, and morphological changes of RPMCs. The results were summarized as follows. 1) Compound 48/80-induced cytomorphological changes such as swelling, degranulation, intracellular vacuoles, and interrupted cell boundary were significantly inhibited by pretreatment with either hot water or polysaccaride fractions frorn Cortex mori (PFCM), 2) the compound 48/80-induced histamine release from RPMCs pretreated with PFCM was significantly inhibited, compared to that of control without PFCM pretreatment, 3) the PFCM inhibited remarkably the compound 48/80-induced calcium influx into the RPMCs, 4) the PFCM increased significantly the intracellular cAMP levels and decreased the intracellular cGMP levels of RPMCs, compared to those of normal control, and 5) the compound 48/80-induced cAMP levels of RPMCs pretreated with PFCM were significantly increased, compared to those of positive control without PFCM, and the compound 48/80-induced cGMP levels of RPMCs pretreated with PFCM were remarkably decreased, compared to those of positive control without PFCM. From the above results, it is suggested that PFCM have an activity to inhibit the compound 48/80-induced mast cell activation.

Inhibitory effect of Cortex mori on the substance P-induced mast cell degranulation, granular leukocyte infiltraion, and vascular permeability in vivo / 대한해부학회지

Cortex mori (Morus alba L.), the root bark of mulberry tree, has been used as an antiphlogistic, diuretic, and expectorant in herbal medicine. It has been reported tha hot water extract of Cortex mori has an inhibitory effect on substance P- and compound 48/80-induced mast cell degranulation and histamine release from rat peritoneal mast cells. Substance P (SP), a decapeptide which is present in sensory neurons, is believed to be a major mediator of neurogenic inflammations. N-terminal peptide of SP causes mast cell degranulation and its C-terminal peptide directly activates vascular endothelial cells to increase the vascular permeability. It has recently been shown that SP induces leukocyte infiltration in the skin, which is mediated through mast cell degranulation. The purpose of this study was to investigate whether Cortex mori could inhibit SP-induced leukocyte infiltration in mouse skin. Subcutaneous administration of SP (10(-8) to 10(-5) M) induced leukocytes infiltration in the skin of BALB/c mice 8h after the injection. Leukocyte infiltration of mouse skin was associated with mast cell degranulation which was induced by SP1-9 (10(-7) to 10(-5) M), but not by SP6-11 (10(-7) to 10(-5) M) which was found to increase the vascular permeability of endothelial cells in mouse skin. However, SP6-11 (10(-7) to 10(-5) M) enhanced SP1-9-induced leukocyte infiltration in the skin without any significant increase in mast cell degranulation. Cortex mori (10 mg/ml) inhibited SP- and SP1-9-induced mast cell degranulation, but did not inhibite SP6-11-induced increase in vascular perameability. Taken together, the data indicate that the hot water extract of Cortex mori contains some substances with an activity to inhibit SP-induced leukocyte infiltration in to the mous skin. These activity of Cortex mori is likely due to the inhibition of release of chemical mediators from the mast cells which participate in neurogenic inflammations.

Determination of scopoletin in Cortex Mori from different sources / 中草药

Object To study the contents and the determinating method of scopoletin in Cortex Mori from different sources.Methods Scopoletin was determined by HPLC.The mobile phase was MeOH-H 2O-HAc (40∶60∶0.25).Detection wavelength was at 354 nm.Results The average recovery was 98.88% with RSD=1.91% and the linear range was 0.025 6—0.128 ?g.The highest content of scopoletin was 0.017 3% and the lowest content was 0.002% from different producing areas.Conclusion The method is easy, accurate, reliable with good reproducibility and high sensitivity.

Study on Vasodilating Mechanism of the Acetone Extract from Cortex Mori / 中药新药与临床药理

Objective To study the vasodilating effect of the acetone- extract (AE) from Cortex Mori (CM) and its vasodilating mechanism. Methods Guinea pig models with contraction of mesentery blood capillary induced by noradrenalin were used to study the in- vivo vasodilating effects of AE from CM. In- vitro effect of AE from CM on rat thoracic aortic ring was observed. The contents of nitric oxide (NO), nitric oxide synthase (NOS), constitutive NOS(cNOS) and inducible (iNOS) in plasma and aortic tissue were determined by method of nitroreductase chromatometry. Results AE from CM had vasodilating effect on the contracti on of mesentery blood capillary in guinea pigs and the contraction of rat thoracic aortic ring induced by 10? mol/L phenylephrine, even under the condition of pre- treating with glibenclamide (1 ? mol/L) or propranolol (3 ? mol/L). When the endothelium of the rat thoracic aortic ring was removed, AE from CM had not vasodilating effect but constrictive effect. AE from CM could also increase the contents of NO, NOS and cNOS in the aortic tissue and had no obvious effect on the NO content in plasma and iNOS in aortic tissue of rats. Conclusion The vasodilating mechanism of AE from CM may be related to promoting the release of NO from endothelium of blood vessel and synthesis of NOS and cNOS in aortic tissue.

Determination of depressor constituent sanggenon of Cortex Mori in different sources / 中成药

Objective:To study the contents and determinate method of Sanggenon C of Cortex Mori in different sources.Methods:Sanggenon C was determined by HPLC. The mobile phase was methanol water(75∶25). Detection wavelength was at 280nm.Results:The average recovery was 96.94% with RSD = 1.72% and the linear range was 0.32～4.80?g. The highest content of Sanggenon C was 0.55% and the lowest content was 0.02% from different producing area. Conclusion: The method is accurate and reliable with good reproducibility.

Comparison of two determination methods of 1-deoxynojirimycin in Cortex Mori / 中成药

0.05). CONCLUSION: Two methods are of good reproducibility and sensitivity, and can be used for the quality control of DNJ in Cortex Mori.

Comparison of Scopoletin Contents in Cortex Mori Processed by Different Methods and Picking Periods / 中成药

Objective: To study the best gathering period and processing method of Cortex Mori.Methods: A HPLC method was used to determine the content of scopoletin. Results: The scopoletin contents in Cortex Mori picked in Jan., Feb. Apr., Jul. and Aug. were higher than that picked in the other months. The scopoletin content in Cortex mori of which rough barks were unremoved was higher than that of which rough barks were removed.Conclusion: Spring and Summer are the best gathering periods, but the processing method shouldn't be stricthy limited.