AIM To investigate the effect of Boschniakiarossica（BR）extract on expression of GST-P,p53 and p21<sup>ras</sup>proteins in early stage of chemicalhepatocarcinogenesis in rats and its anti-inflammatory ac...AIM To investigate the effect of Boschniakiarossica（BR）extract on expression of GST-P,p53 and p21<sup>ras</sup>proteins in early stage of chemicalhepatocarcinogenesis in rats and its anti-inflammatory activities.METHODS The expression of tumor marker-placental form glutathione S-transferase（GST-P）,p53 and p21<sup>ras</sup>proteins were investigated byimmunohistochemical techniques and ABCmethod.Anti-inflammatory activities of BR werestudied by xylene and croton oil-induced mouseear edema,carrageenin,histamine and hotscald-induced rat pow edema,adjuvant-inducedrat arthritis and cotton pellet-induced mousegranuloma formation methods.RESULTS The 500 mg/kg of BR-H<sub>2</sub>O extractfractionated from BR-Methanol extract hadinhibitory effect on the formation of DEN-inducedGST-P-positive foci in rat liver（GST-P stainingwas 78% positive in DEN+AAF group vs 20%positive in DEN+AAF+BR group,P【0.05）andthe expression of mutant p53 and p21<sup>ras</sup>proteinwas lower than that of hepatic preneoplasticlesions（33% and 22% positive respectively inDEN+AAF group vs negative in DEN+AAF+BRgroup）.Both CH<sub>2</sub>Cl<sub>2</sub> and H<sub>2</sub>O extracts from BRhad anti-inflamatory effect in xylene and crotonoil-induced mouse ear edema（inhibitory rateswere 26%-29% and 35%-59%,respectively）. BR-H<sub>2</sub>O extract exhibited inhibitory effect incarrageenin,histamine and hot scald-inducedhind paw edema and adjuvant-induced arthritis inrats and cotton pellet-induced granulomaformation in mice.CONCLUSION BR extract exhibited inhibitory effect on formation of preneoplastic hepatic foci in early stage of rat chemical hepato-carcinogenesis. Both CH<sub>2</sub>CI<sub>2</sub> and H<sub>2</sub>O extracts from BR exerted anti-inflammatory effect in rats and mice.展开更多
The anti-fungal activities of synthesized pyridinyl-pyrazole-carbox amide derivatives 1a^1c were investigated via theoretical parameters. The obtained results in present paper were compared with the reported experimen...The anti-fungal activities of synthesized pyridinyl-pyrazole-carbox amide derivatives 1a^1c were investigated via theoretical parameters. The obtained results in present paper were compared with the reported experimental results. Experimental results show that derivative 1a has the highest and derivative 1c the lowest anti-fungal activity. The interactions of derivatives 1a^1c with Ge-nanotube（6, 6） were investigated, and also quantum molecular descriptors of derivatives 1a^1c were calculated. Results show that, derivatives 1a^1c can interact with Ge-nanotube（6, 6） effectively, and their adsorptions were exothermic and possible from the theoretical viewpoint. The absolute ΔEad and ΔGad values of derivative 1a on Ge-nanotube（6, 6） were higher than the absolute ΔEad and ΔGad values of 1 b and 1c. Derivative 1a has the highest absolute μ, ω and ΔN values. The theoretical and experimental trends of anti-fungal activity of derivatives 1a^1c were similar, successfully.展开更多
fter the alcoholic group of serine located in the binding site of Anti-HumanIgM(Fcμ) (Rabbit IgG) was selectively activated by phenylmethylsulfonyl fluoride(PMSF) and displaced with hydrogen selenide(H2Se) , the seri...fter the alcoholic group of serine located in the binding site of Anti-HumanIgM(Fcμ) (Rabbit IgG) was selectively activated by phenylmethylsulfonyl fluoride(PMSF) and displaced with hydrogen selenide(H2Se) , the serine residue was con-verted to selenocysteine(SeCys). Because SeCys is a catalytic group of glutathioneperoxidase (GPX), the mutated antibody has the GPX activity which is seventytimes more than that of PZ51, the best GPX mimic in the world. Moreover, themutated antibody remains its original antibody titer.展开更多
The management, control and elimination of tuberculosis (TB) have been difficult with the advent of HIV and cases of multidrug resistant (MDR-TB) tuberculosis. The cases of multidrug resistance to rifampicin and isoni...The management, control and elimination of tuberculosis (TB) have been difficult with the advent of HIV and cases of multidrug resistant (MDR-TB) tuberculosis. The cases of multidrug resistance to rifampicin and isoniazid pose greater challenges on first line and second line drugs to eliminate TB. The study is aimed at establishing anti-tuberculosis activity of <i>Tetrapleura tetraptera</i> against <i>Mycobacterium tuberculosis</i> and MDR-TB and the phytochemical present. The leaves of <i>Tetrapleura tetraptera </i>were collected, weighed, dried and pulverized to powder. The pulverized leaves of <i>Tetrapleura tetraptera </i>were subjected to 70% methanol extraction and screened for phytochemical. The crude extract was further purified into fractions using silica gel and thin layer chromatography techniques.<i> M. tuberculosis</i> and MDR-TB were obtained from positive acid fast bacilli sputa of TB patients and confirmed using GeneXpert to differentiate genotypic drug susceptible <i>M. tuberculosis</i> and MDR-TB. The sputa were digested using sodium hydroxide-cysteine technique and cultured in Middlebrook 7H9. The crude extract and fractions were screened for anti-tuberculosis activity using tetrazolium microtitre plate assay. The results showed that <i>Tetrapleura tetraptera crude </i>had activities against <i>M. tuberculosis</i> at 7.4 ± 0 mg/ml and 27.5 ± 0 mg/ml for MDR-TB. One of the fractions inhibited the growth of <i>M. tuberculosis </i>at 0.24 ± 0 mg/ml and MDR-TB at 0.89 ± 0 mg/ml. The phytochemical screened includes tannins, alkaloids, saponins, flavonoids, phenols and resins. <i>T. tetraptra </i>possesses anti-tuberculosis potential at low concentration on MDR-TB and can be a lead compound in drug development for the treatment of tuberculosis and multidrug resistant tuberculosis.展开更多
Lectins are the carbohydrate-binding proteins of non-immune origin which have been the subject of intense investigation over the last few decades owing to the variety of interesting biological properties. Most of the ...Lectins are the carbohydrate-binding proteins of non-immune origin which have been the subject of intense investigation over the last few decades owing to the variety of interesting biological properties. Most of the lectins which have been purified and characterized from plants have been obtained from dicotyledons. In the present study a lectin was purified from tubers of a monocot plant Arisaema utile (AUL) Schott by affinity chromatography on asialofetuin-linked amino activated silica beads. AUL gave a single band in SDS-PAGE at pH 8.3 corresponding to subunit Mr 13.5 kDa. The native molecular mass of AUL was 54 kDa suggesting a homotetrameric structure. AUL gave multiple bands in isoelectric focusing and in native PAGE at pH 8.3. AUL was inhibited by N-acetyl-D-lactosamine (Lac NAc), a disaccharide and asialofetuin, a complex desialylated serum glycoprotein. When treated with denaturing agents, the lectin was stable in the presence of urea (3 M), thiourea (4 M) and guanidine HCl (4 M). AUL was a glycoprotein with a carbohydrate content of 1.2%. Complete loss of activity was observed upon modification of tryptophan residues of the lectin. The activity was reduced to 25% after modification of tyrosine. Chemical modification of arginine, histidine, serine and cysteine residues of AUL did not affect its activity. Using Far UV CD spectra the estimated secondary structure was 37% α-helix, 25% β-sheet and 38% random contributions. The lectin showed potent mitogenic response towards human lymphocytes. In vitro anti-proliferative assay using 11 human cancer cell lines resulted in 50% inhibition of six cell lines viz. SW-620, HCT-15, SK-N-SH, IMR-32, Colo-205 and HT-29 at 38, 42, 43, 49, 50 and 89 &#181;g/ml, respectively.展开更多
基金the National Natural Science Foundation of China,No.39660021
文摘AIM To investigate the effect of Boschniakiarossica（BR）extract on expression of GST-P,p53 and p21<sup>ras</sup>proteins in early stage of chemicalhepatocarcinogenesis in rats and its anti-inflammatory activities.METHODS The expression of tumor marker-placental form glutathione S-transferase（GST-P）,p53 and p21<sup>ras</sup>proteins were investigated byimmunohistochemical techniques and ABCmethod.Anti-inflammatory activities of BR werestudied by xylene and croton oil-induced mouseear edema,carrageenin,histamine and hotscald-induced rat pow edema,adjuvant-inducedrat arthritis and cotton pellet-induced mousegranuloma formation methods.RESULTS The 500 mg/kg of BR-H<sub>2</sub>O extractfractionated from BR-Methanol extract hadinhibitory effect on the formation of DEN-inducedGST-P-positive foci in rat liver（GST-P stainingwas 78% positive in DEN+AAF group vs 20%positive in DEN+AAF+BR group,P【0.05）andthe expression of mutant p53 and p21<sup>ras</sup>proteinwas lower than that of hepatic preneoplasticlesions（33% and 22% positive respectively inDEN+AAF group vs negative in DEN+AAF+BRgroup）.Both CH<sub>2</sub>Cl<sub>2</sub> and H<sub>2</sub>O extracts from BRhad anti-inflamatory effect in xylene and crotonoil-induced mouse ear edema（inhibitory rateswere 26%-29% and 35%-59%,respectively）. BR-H<sub>2</sub>O extract exhibited inhibitory effect incarrageenin,histamine and hot scald-inducedhind paw edema and adjuvant-induced arthritis inrats and cotton pellet-induced granulomaformation in mice.CONCLUSION BR extract exhibited inhibitory effect on formation of preneoplastic hepatic foci in early stage of rat chemical hepato-carcinogenesis. Both CH<sub>2</sub>CI<sub>2</sub> and H<sub>2</sub>O extracts from BR exerted anti-inflammatory effect in rats and mice.
文摘The anti-fungal activities of synthesized pyridinyl-pyrazole-carbox amide derivatives 1a^1c were investigated via theoretical parameters. The obtained results in present paper were compared with the reported experimental results. Experimental results show that derivative 1a has the highest and derivative 1c the lowest anti-fungal activity. The interactions of derivatives 1a^1c with Ge-nanotube（6, 6） were investigated, and also quantum molecular descriptors of derivatives 1a^1c were calculated. Results show that, derivatives 1a^1c can interact with Ge-nanotube（6, 6） effectively, and their adsorptions were exothermic and possible from the theoretical viewpoint. The absolute ΔEad and ΔGad values of derivative 1a on Ge-nanotube（6, 6） were higher than the absolute ΔEad and ΔGad values of 1 b and 1c. Derivative 1a has the highest absolute μ, ω and ΔN values. The theoretical and experimental trends of anti-fungal activity of derivatives 1a^1c were similar, successfully.
文摘fter the alcoholic group of serine located in the binding site of Anti-HumanIgM(Fcμ) (Rabbit IgG) was selectively activated by phenylmethylsulfonyl fluoride(PMSF) and displaced with hydrogen selenide(H2Se) , the serine residue was con-verted to selenocysteine(SeCys). Because SeCys is a catalytic group of glutathioneperoxidase (GPX), the mutated antibody has the GPX activity which is seventytimes more than that of PZ51, the best GPX mimic in the world. Moreover, themutated antibody remains its original antibody titer.
文摘The management, control and elimination of tuberculosis (TB) have been difficult with the advent of HIV and cases of multidrug resistant (MDR-TB) tuberculosis. The cases of multidrug resistance to rifampicin and isoniazid pose greater challenges on first line and second line drugs to eliminate TB. The study is aimed at establishing anti-tuberculosis activity of <i>Tetrapleura tetraptera</i> against <i>Mycobacterium tuberculosis</i> and MDR-TB and the phytochemical present. The leaves of <i>Tetrapleura tetraptera </i>were collected, weighed, dried and pulverized to powder. The pulverized leaves of <i>Tetrapleura tetraptera </i>were subjected to 70% methanol extraction and screened for phytochemical. The crude extract was further purified into fractions using silica gel and thin layer chromatography techniques.<i> M. tuberculosis</i> and MDR-TB were obtained from positive acid fast bacilli sputa of TB patients and confirmed using GeneXpert to differentiate genotypic drug susceptible <i>M. tuberculosis</i> and MDR-TB. The sputa were digested using sodium hydroxide-cysteine technique and cultured in Middlebrook 7H9. The crude extract and fractions were screened for anti-tuberculosis activity using tetrazolium microtitre plate assay. The results showed that <i>Tetrapleura tetraptera crude </i>had activities against <i>M. tuberculosis</i> at 7.4 ± 0 mg/ml and 27.5 ± 0 mg/ml for MDR-TB. One of the fractions inhibited the growth of <i>M. tuberculosis </i>at 0.24 ± 0 mg/ml and MDR-TB at 0.89 ± 0 mg/ml. The phytochemical screened includes tannins, alkaloids, saponins, flavonoids, phenols and resins. <i>T. tetraptra </i>possesses anti-tuberculosis potential at low concentration on MDR-TB and can be a lead compound in drug development for the treatment of tuberculosis and multidrug resistant tuberculosis.
文摘Lectins are the carbohydrate-binding proteins of non-immune origin which have been the subject of intense investigation over the last few decades owing to the variety of interesting biological properties. Most of the lectins which have been purified and characterized from plants have been obtained from dicotyledons. In the present study a lectin was purified from tubers of a monocot plant Arisaema utile (AUL) Schott by affinity chromatography on asialofetuin-linked amino activated silica beads. AUL gave a single band in SDS-PAGE at pH 8.3 corresponding to subunit Mr 13.5 kDa. The native molecular mass of AUL was 54 kDa suggesting a homotetrameric structure. AUL gave multiple bands in isoelectric focusing and in native PAGE at pH 8.3. AUL was inhibited by N-acetyl-D-lactosamine (Lac NAc), a disaccharide and asialofetuin, a complex desialylated serum glycoprotein. When treated with denaturing agents, the lectin was stable in the presence of urea (3 M), thiourea (4 M) and guanidine HCl (4 M). AUL was a glycoprotein with a carbohydrate content of 1.2%. Complete loss of activity was observed upon modification of tryptophan residues of the lectin. The activity was reduced to 25% after modification of tyrosine. Chemical modification of arginine, histidine, serine and cysteine residues of AUL did not affect its activity. Using Far UV CD spectra the estimated secondary structure was 37% α-helix, 25% β-sheet and 38% random contributions. The lectin showed potent mitogenic response towards human lymphocytes. In vitro anti-proliferative assay using 11 human cancer cell lines resulted in 50% inhibition of six cell lines viz. SW-620, HCT-15, SK-N-SH, IMR-32, Colo-205 and HT-29 at 38, 42, 43, 49, 50 and 89 &#181;g/ml, respectively.
