Content of L-carnitine and its acylates in plasma of patients with diabetes and diabetes complications / 中国药理学通报

Aim To investigate the changes of content of L-carnitine (LC ), acetyl-L-carnitine (ALC ) and propionyl-L-carnitine (PLC )in patients with diabetes and its complications.Methods By replicating meth-od of pre-column derivatization HPLC,the contents of plasma LC,ALC,PLC were detercted in normal sub-jects and in patients of diabetes mellitus,diabetic reti-nopathy, diabetic nephropathy, diabetic peripheral neuropathy,diabetic hypertension,diabetic coronary heart disease.Results The concentration of LC in normal subjects and in patients of diabetes mellitus, diabetic retinopathy, diabetic nephropathy, diabetic peripheral neuropathy,diabetic hypertension,diabetic coronary heart disease were (41.01 ±8.05 )μmol · L-1 ,(36.72 ±8.23 )μmol · L-1 ,(33.3 1 ±6.26 )μmol·L-1 ,(33.81 ±5.61 )μmol·L-1 ,(33.57 ± 6.67 )μmol · L-1 , (33.67 ±5.36 )μmol · L-1 , (32.87 ±6.05 )μmol · L-1 respectively.The plasma LC concentration in diabetic group was significantly lower than that of normal control group (P<0.05 ). Moreover,the LC concentration in other groups of dia-betic complications was lower than that in diabetic group, and LC concentration showed no significant difference in various groups of diabetic complications. There was no significant difference in the plasma con-centrations of ALC and PLC of diabetes group and the diabetic complication groups too.Conclusion In Chi-nese normal subjects,patients with diabetes and dia-betic complications,the plasma concentrations of LC in diabetic patients are lower than normal,and plasma concentration of LC in diabetic complications are lower than that in patients with diabetes mellitus.

Meridian Tropism of Polygoni Avicularis Herba by Tissue Distribution of Avicularin in Rats / 中草药·英文版

Objective To observe the meridian tropism of Polygoni Avicularis Herba by tissue distribution of avicularin in rats.Methods Tissue distribution of avicularin in rat following a single iv administration was appointed and observed.HPLC method was established and validated for the determination of avicularin in rat tissues.Results Kidney and bladder were the most important target tissue of avicularin.Conclusion HPLC method is successfully applied to tissues distribution study of avicularin after iv administration to rats,and the results explain Polygoni Avicularis Herba on bladder tropism reasonably.

Advances in algae tool enzymes: alginate lyases / 生物工程学报

Marine can be considered as a rather unexplored source of biological material. Production of algal oligosaccharides by using valuable enzymes from marine origin has become an important way to utilize marine resources. As one of algal tool enzymes, the use of alginate lyases has been focused mainly on development and application of alginate oligosaccharides with bioactive function in recent years. In this paper, we reviewed the research of alginate lyases over the past decade in several aspects, including their origin, diversity, substrate specification, mode of action, structure and catalysis mechanism, assay of enzyme activity, enzyme characterization, as well as our own experience on this subject. At the end of the review, the application prospects of alginate lyases are presented.

The potential molecular targets of marine sulfated polymannuroguluronate interfering with HIV-1 entry. Interaction between SPMG and HIV-1 rgp120 and CD4 molecule.

The potential targets of marine sulfated polymannuroguluronate (SPMG) involved in inhibition of HIV-1 entry were investigated by surface plasmon resonance and flow cytometry. Results indicated that binding of SPMG either to soluble oligomeric rgp120 or to complexed rgp120-sCD4 mainly resided in V3 loop region. In addition, SPMG was shown to be less accessible for sCD4 when sCD4 had pre-interacted with rgp120, though SPMG per se multivalently bound to sCD4 with relatively low affinity. While the pre-incubation of SPMG with rgp120 caused a partial blockade of rgp120 binding to sCD4, suggesting that SPMG either shared common binding sites on gp120 with sCD4 or masked the docking sites of gp120 for sCD4. Taken together, V3 domain was demonstrated to be the major site mediating interaction of SPMG with complexed rgp120-sCD4. It seems likely that SPMG binds to both rgp120 and sCD4, but has less accessibility for sCD4 when sCD4 has already bound to rgp120. Nevertheless, addition of SPMG either prior to or after the interaction of rgp120 with sCD4 may suppress rgp120 binding to sCD4. The exact pattern of this trimolecular complex formation at the cell membrane-anchored virus level requires further clarification.

Comparative study on immunoregulation of sulfated propylene glycol alginate and its fractions / 中国海洋药物

Objective To investigate the influence of sulfated propylene glycol alginate(PSS) and its fractions on the immunoregulation.Methods The immunoregulation activity of PSS and its fractions were investigated by using immunocyte cultivation technique in vitro.The structure activity relationship was analysed on the basis of the structure studies of PSS' fractions.Results The experimental results showed that PSS could improve spleen cell proliferation,enhance macrophage phagocytic function and inhibit T-cell and B-cell proliferation.Conclusion PSS possessed significant immunoregulation effect,whilst the immunocompetence comparison of PSS' fractions proved that the different immunocytes had different requirements for saccharides length.

INHIBITORY EFFECTS OF D-POLYMANNURONIC SULFATE ON PROLIFERATION OF RAT VASCULAR SMOOTH MUSCLE CELLS AND ITS RELATED MECHANISMS OF ACTION IN VITRO / 药学学报

AIM　To investigate the inhibitory effects of D-polymannuronic sulfate (DPS) on the proliferation of rat vascular smooth muscle cells (VSMC) induced by basic fibroblast growth factor (bFGF) or interleukin-1 (IL-1) and its related mechanisms. METHODS　Rat aortic smooth muscle cells pretreated with DPS in concentrations ranging from 0.001 μg*mL-1 up to 100 μg*mL-1 were incubated at 37℃ for 24 h, followed by addition of bFGF (50 ng*mL-1) or IL-1 (50 U*mL-1) for another 24 h. The effects of DPS on the proliferation of VSMC were evaluated by MTT assays. VSMC were pretreated with DPS in concentrations ranging from 0.001 μg*mL-1 up to 1 μg*mL-1, followed by addition of L-NAME (0.1 μg*mL-1) or bFGF (50 ng*mL-1) for 24 h. Supernatant nitric oxide (NO) was determined with NO assay kit, while supernatant angiotensin II (Ang II) and endothelin-1 (ET-1) were measured by radioimmunoassay. RESULTS　DPS exerted antiproliferative effects at concentrations ranging from 0.01 μg*mL-1 to 10 μg*mL-1, and its maximal effect was observed at the concentration of 1 μg*mL-1. Also, the suppressing actions of DPS on the proliferation of VSMC were diminished by increasing the concentrations of bFGF or IL-1. Furthermore, DPS increased NO synthesis and decreased Ang II and ET-1 contents released from VSMC in a concentration-dependent manner. CONCLUSION　DPS afforded the antiproliferative effects on bFGF- or IL-1-treated VSMC and its underlying mechanisms were associated with enhancement of NO synthesis and decrement of Ang II and ET-1 production/release in vitro.

Synthsis of quaternary Ammonium-Glucosamine conjugate / 中国海洋药物

Quaternary ammonium glucosamine conjugatewas prepared by a two step procedure.First,condensation of glucosamine hydrochloride with chloro acetic chloride in the presence of potassium bicarbonate in aqueous medium at 0℃ provided the N chloroacetyl derivative in 74% yield.Subsequent reaction of this intermediate with pyridine at 40℃ for 3 days gave the pyridinium conjugate in 71% yield.The structures of compounds were confirmed by IR,NMR spectra and element analysis.

Preparation and study on the physicochemical characteristics of glycoprotein from Crassostrea gigas / 中国海洋药物

Objective To study the preparation and the physicochemical characteristics of glycoprotein from Crassostrea gigas.Methods Oyster collected in Qingdao was taken as the experiment materials,and was extracted with H2O in low temperature.The extracts were purified using Sephacryl s-100 HR gel chromatography and HPLC.Three glycoprotein F22,F33,F42 were finally isolated from the oyster extracts.Results The physicochemical characteristics of glycoprotein were studied.The results showed that the pI value of F22 was 5.5,relative molecular mass of F22 was 34230Da,the protein contents of F22,F33,F42 were 34.1%,19.7% and 12.5%,the saccharide contents of F22,F33,F42 were 35.9%,28.8% and 40%.Conclusion The research result would be used for the study of bioactive component from Crassostrea gigas.

PREPARATION OF BASIC ALUMINIUM 6-?-(CARBOXYME-THYL)CHITOSAN / 中国海洋药物

Basic aluminium 6 ? (carboxylmethyl) chitosan was prepared by reacting the solution of 6 ? (carb?xylmethyl) chitosan in water with basic aluminium chloride 〔Al(OH) 2Cl〕. The structure of product was confirmed by IR and atomic absoption spectroscopy.

Research on pharmacokinetics of D-polymannuronicate in rats / 中国海洋药物

Objective To investigate the pharmacokinetics of D-polymannuronicate after single and successive administrations for 7 days by means of intravenous injection and intragastric administration.Methods Bioanalysis for the determination of D-polymannuronicate plasma concentration was applied in rats,and parameters of pharmacokinetics were calculated by DAS2.1.1 software.Results The well linearity(r=0.9991) in 0.05～150mg?L~(-1) of plasma concentrations.The recovery rate was between 94.72%～103.21%,the derivations withinday and between-days were less than 15%.Zata were 0.89,1.06,0.93,0.85 h~(-1) and t_(1/2z) were 0.78,0.69,0.75,0.87h corresponding with the four methods of administration.The bioavailabilities were 3%～5%.Conclusion The bioavailability was low.The ends of the elimination of two means of intravenous injection and intragastric administration were same. There was no significant difference in pharmacokinetic parameters of single and successive administrations.

Analysis of the UV absorbing constituents of the metabolites from UV-B tolerance bacteria and study on its anti-ultraviolet mechanism / 中国海洋药物

Objective The anti-UV-B radiation mechanism of UV-B tolerance strain KFS-9 was studied from the profile of metabolites.Methods The compounds were separated by column chromatography and their structures were elucidated based on GC-MS,LC-TOF-MS,EI-MS and NMR analyses.Results Three unsaturated fatty acids(identified as 9-hexadecenoic acid,9,12-octadecadienoic acid and 11-octadecenoic acid) and 1,2-benzenedicarboxylic acid able to absorb ultraviolet were isolated from the petroleum ether extract of the fermentation liquid of Pantoea agglomerans KFS-9.Fraction(Ⅱ) was isolated from the ethyl acetate extract and was composed of 2,3-butanediol and a series of high unsaturated aroma compounds.Fraction(Ⅱ) had a wide absorption peak,and it could protect E.coli from UV-B damage in some sense.Conclusion Strain KFS-9 produced metabolites that were able to absorb UV to build a natural barrier and so improved the tolerance to UV radiation.The UV-B radiation protection test to the E.coli also showed fraction(Ⅱ) was not the only protector,and there definitely existedother materials and mechanism to protect the strain.

Effects of D-Polymannuronic sulfate on potential-dependent and/or receptor-operated calcium channel in rat aortic rings / 中国海洋药物

The effects of D-polymannuronic sulfate (DPS) on the norepinephrine (NA) or potassium chloride (KCL)-induced contraction of rat aortic rings were studied in this paper. The results showed that DPS at the final concentration of Img ? L-1 inhibited the contraction of aortic rings e-voked by NA or KCL and shift doseresponse curves for NA or KCL to the right in a non-parallel fa-sion and depressed their maximal response, implicating that DPS afforded the noncompetitive antagonism on contraction of rat aortic rings induced by NA or KCL. This finding suggested that DPS exerted an inhibitory action of potential-dependent calcium channel and that of receptor-operated calcium channel in vascular smooth muscle.

Comparative study on the effect of polysaccharide sulfate and amlodipine for renal hemodynamics in dogs / 中国海洋药物

To comparative study the effect of polysaccharide sulfate (PSS) and amlodipine on renal hemodynamics in dogs. The kidney was denervated, PSS or amlodipine was injected through renal artery. Renal hemodynamic parameters, including mean arterial pressure, renal blood flow, glomerular filtration, urine flow, et al, were measured. Both PSS and amlodipine significantly increased renal blood flow and urine flow (P

The antihypertensive effect of marine sulfated polysaccharide AHD and its related mechanisms of action / 中国海洋药物

The antihypertensive effect of marine sulfated polysaccharide AHD and its underlying mechanisms were studied in renovascular hypertensive rats (RHR) [two-kidney one clip,Goldblatt(2-K 1C)J. AHD were given orally at doses of 12.5, 25,50mg?kg～-1 once a day for five weeks,simultaneously wity the initiation of the establishment of renovascular hypertensive model. Serum nitric oxide(NO) was determined with NO kit,and plasma Angiotensin E (Ang Ⅱ ) and Eneothelin (ET) Were measured by radioimmumoassays. The results indicated that AHD decreased arteial blood pressure in a dose-dependent manner. Moreover, nitric oxide (NO) contents in serum were dose-dependently elevated,accompanied by dramatic reduction in Ang Ⅱ and ET contents. These findings suggested that AHD exerted its hypotensive activity by enhancing tye release of NO,followed by reduction in production of boty ANG Ⅱ and ET in vivo.

IDENTIFICATION OF NEUTRAL MONOSACCHARIDES IN GLY-COSAMINOGLYCAN FROM THE BAY SCALLOP ARGOPECTEN IRRADIANS BY GAS CHROMATOGRAPHY / 中国海洋药物

The glycosaminoglycan (GAG), isolated from Bay scallop Argopectenirradians, contains neutral monosaccharides besides hexosamines and hexosuronic acids. The monosaccharides obtained by alcoholysis with HCI-methylalcohol from the sample of GAG was trimethylsilanized with hexamethyldisilan and chlortrimethylsilan (HMDS ' TMCS = 2 : 1). And the trimethylsilyl derivatives of monosaccharides was determined by gas chro-matography. Compared the gas chromatography of the sample with that of standard monosaccharides, it was found that the GAG of the Bay scallop contains five neutral monosaccharides, viz glucose, galactose, xylose, fucose and rhamnose.

IDENTIFICATION OF GLYCOSAMINOGLYCAN FROM THE BAY SCALLOP ARGOPECTEN IRRADIAUS BY AGAROSE GEL ELEC-TROPHORESIS / 中国海洋药物

Fraction F3-3-3 of glycosaminoglycan was isolated from the leftover bits of Bay scallop Argopecten irradiaus . Infrared spectra of F3-3-3 was similar to that of heparin. Agarose gel electrophoresis of this fraction was performed in the system of barbital buffer (0. 06 mol/L,pH 8. 6). It was found that F3-3-3 showed single band in the electrophoresis. Compared with the agarose gel electrophoresis of standard glycosaminoglycan, such as heparin, hyaluronic acid and chondroitin 6-sulfate, it indicated that the relative migration rate of the fraction was close to that of heparin.

DISTRIBUTION OF SELENIUM ASSOCIATED WITH BIOCHEMICAL FRACTIONS IN BLUE MUSSEL AND BAY SCALLOP / 中国海洋药物

Concentration,biochemical fractions of selenium have been investigated in the tissue organs of Blue mussel ( Mytilus edulis ) and Bay scallop ( Argopecten trradiaus ). It is found by determination that the selenium concentration in the mantle is higher than in other tissue organs of the Blue mussel and Bay scallop. Selenium is predominantely associated with amino acids and proteins. 64. 4 per cents to 70. 4 per cents of selenium was associated with insoluble proteins in the mantle of the Blue mussel and Bay scallop.

A SURVEY OF THE METHODS OF EXTRACTION, ISOLATION AND DETERMINATION FOR GLYCOSAMINOGLYCANS / 中国海洋药物

The studies on glycosaminogiycans (GAG) from animals are carrying out extensively in the fields of biology.biochemistry and medicine. The methodology of GAG researches has been developed rapidly at present. The researches of GAG have just begun in China. Synthesizing a large number of references,this paper gives a brief introduction on the methods of extraction isolation and determination for GAG. And the latest methods and developing tendency are summarized as well.

CONCENTRATION AND DISTRIBUTION OF SELENIUM IN 12 kinds of SEAWEEDS / 中国海洋药物

Concentration and distribution of selenium have been investigated in 12 kinds of seaweeds. It is found by determination that the selenium concentration in Phaeophyta is lower than in Chlorophyta and Rhodophyta. Selenium is predominately associated with amino acids and proteins.

A new sesquiterpene lactone from root of Baccaurea ramiflora / 中草药

Objective To study the chemical constituents in the root of Baccaurea ramiflora.Methods Various chromatographic techniques were used to separate and purify the constituents.The structures of the compounds were elucidated by physicochemical properties and spectral analyses(UV,IR,ESI-MS,1H-NMR,13C-NMR,Dept90,Dept135,1H-1H COSY,1H-1H NOESY,HMQC,HMBC).Results A new compound was isolated and idertified.Conclusion This compound is a novel compound and named as epidihydrotutin.