Two new dimeric naphthoquinones, 5′,8′-dihydroxy-6,6′-dimethyl-7,3′-binaphthyl-1,4,1′,4′-tetraone(1; Di-naphthodiospyrol D) and 5′,8′-dihydroxy-5,8-dimethoxy-6,6′-dimethyl-7,3′-binaphthyl-1,4,1′,4′-tetraon...Two new dimeric naphthoquinones, 5′,8′-dihydroxy-6,6′-dimethyl-7,3′-binaphthyl-1,4,1′,4′-tetraone(1; Di-naphthodiospyrol D) and 5′,8′-dihydroxy-5,8-dimethoxy-6,6′-dimethyl-7,3′-binaphthyl-1,4,1′,4′-tetraone(2; Di-naphthodiospyrol E), along with known naphthoquinones diospyrin(3) and 8-hydroxy diospyrin(4) were isolated from the chloroform fraction of extract of Diospyros lotus roots. Their structures were elucidated by advanced spectroscopic analyses, including HSQC, HMBC, NOESY, and J-resolved NMR experiments. The fractions and compounds 1-4 were evaluated for urease activity and phosphodiesterase-Ⅰ, carbonic anhydrase-Ⅱ and α-chymotrypsin enzyme inhibitory activities. Compounds 1 and 2 and their corresponding fractions showed significant and selective inhibitory effects on urease activities. The IC_(50) values of 1 and 2 were 260.4 ± 6.37 and 381.4 ± 4.80 μmol·L-1, respectively, using thiourea(IC_(50) = 21 ± 0.11 μmol·L^(-1)) as the standard inhibitor. This was the first report demonstrating that the naphthoquinones class showed urease inhibition.展开更多
Carbonic anhydrase Ⅱ (CAⅡ) is an important enzyme complex with Zn2+,which is involved in many physiological and pathological processes, such as calcification, glaucoma and tumorigenicity. In order to search for nove...Carbonic anhydrase Ⅱ (CAⅡ) is an important enzyme complex with Zn2+,which is involved in many physiological and pathological processes, such as calcification, glaucoma and tumorigenicity. In order to search for novel inhibitors of CAⅡ, inhibition assay of carbonic anhydrase Ⅱ was performed, by which seven natural phenolic compounds, including four phenolics (grifolin, 4-O-methyl-grifolic acid, grifolic acid, and isovanillic acid) and three flavones (eriodictyol, quercetin and puerin A), showed in-hibitory activities against CAⅡ with IC50s in the range of 6.37-71.73 μmol/L. Grifolic acid is the most active one with IC50 of 6.37 μmol/L. These seven phenolic compounds were proved to be novel natural carbonic anhydrase Ⅱ inhibitors, which were obtained in flexible docking study with GOLD 3.0 soft-ware. Results indicated that the aliphatic chain and polar groups of hydroxyl and carboxyl are impor-tant to their inhibitory activities, providing a new insight into study on CA Ⅱ potent inhibitors.展开更多
采用扫描电镜观察了不同碱度(0、2、4 g/L Na HCO_3)胁迫对尼罗罗非鱼(Oreochromis niloticus)鳃离子细胞形态变化的影响,并采用免疫组化技术观察了鳃、肾、肠中4个HCO_3^-转运因子碳酸酐酶(CAⅡ、CAⅣ)、碳酸氢钠协同转运载体(SLC4A4)...采用扫描电镜观察了不同碱度(0、2、4 g/L Na HCO_3)胁迫对尼罗罗非鱼(Oreochromis niloticus)鳃离子细胞形态变化的影响,并采用免疫组化技术观察了鳃、肾、肠中4个HCO_3^-转运因子碳酸酐酶(CAⅡ、CAⅣ)、碳酸氢钠协同转运载体(SLC4A4)、Cl^-/HCO_3^-离子交换体(SLC26A6)的阳性反应变化。扫描电镜结果表明,鳃离子细胞分布在鳃小片基部。根据其表面开孔形状和尺寸,可分为Ⅰ型、Ⅱ型、Ⅲ型和Ⅳ型4种亚型,各亚型离子细胞的开孔尺寸随碱度胁迫强度增高呈正比增大,Ⅲ型离子细胞开孔尺寸变化最明显(P<0.01);离子细胞总数目也随碱度升高而增加,Ⅲ型离子细胞数目上升最为显著(P<0.01)。免疫组化结果表明,在淡水、碱水组中,CAⅡ、CAⅣ、SLC4A4、SLC26A6在鳃小片基部和肾中均有阳性反应,且随着碱度升高,阳性反应增强,但在肠道中未观察到阳性反应。本研究结果初步表明,尼罗罗非鱼可通过鳃离子细胞形态和数量调节适应碱度变化,鳃和肾为主要应答调节器官。展开更多
目的探讨碳酸酐酶Ⅱ(CAⅡ)的表达与结直肠癌(CRC)的发生、发展,以及临床病理特征的关系。方法 Western Blot法检测CAⅡ在12对新鲜配对的CRC和远癌黏膜中的表达。再以免疫组织化学法检测CAⅡ在配对的64对远癌结直肠黏膜和CRC,20个转移淋...目的探讨碳酸酐酶Ⅱ(CAⅡ)的表达与结直肠癌(CRC)的发生、发展,以及临床病理特征的关系。方法 Western Blot法检测CAⅡ在12对新鲜配对的CRC和远癌黏膜中的表达。再以免疫组织化学法检测CAⅡ在配对的64对远癌结直肠黏膜和CRC,20个转移淋巴结及27个息肉中的表达,比较各组间表达的差异。分析CAⅡ表达与CRC的部位、分化及临床病理分期间的关系。结果 Western Blot检测显示远癌黏膜CAⅡ/tubulin灰度比为2.48±1.68,癌组织为1.33±1.28,两者差异有统计学意义(P=0.027)。免疫组化显示CAⅡ的表达评分远癌黏膜为(2.81±0.48)分,息肉(包括增生性息肉和腺瘤)为(2.56±0.51)分,CRC为(1.30±0.89)分;按上述3种组织的顺序评分逐步显著降低(P<0.05)。在转移淋巴结中为(1.35±0.67)分,表达与配对原发灶相似(P>0.05)。CAⅡ的表达在不同部位和分化程度的CRC间差异无统计学意义(P>0.05),Ⅲ,Ⅳ期表达与Ⅰ,Ⅱ期无统计学差异(P>0.05)。结论 CAⅡ在CRC中表达的下调,是CRC发生中的早期事件,与分化、分期和转移无关。展开更多
基金supported by the Education Commission of Pakistan(No.112-26510-2PS1-258)
文摘Two new dimeric naphthoquinones, 5′,8′-dihydroxy-6,6′-dimethyl-7,3′-binaphthyl-1,4,1′,4′-tetraone(1; Di-naphthodiospyrol D) and 5′,8′-dihydroxy-5,8-dimethoxy-6,6′-dimethyl-7,3′-binaphthyl-1,4,1′,4′-tetraone(2; Di-naphthodiospyrol E), along with known naphthoquinones diospyrin(3) and 8-hydroxy diospyrin(4) were isolated from the chloroform fraction of extract of Diospyros lotus roots. Their structures were elucidated by advanced spectroscopic analyses, including HSQC, HMBC, NOESY, and J-resolved NMR experiments. The fractions and compounds 1-4 were evaluated for urease activity and phosphodiesterase-Ⅰ, carbonic anhydrase-Ⅱ and α-chymotrypsin enzyme inhibitory activities. Compounds 1 and 2 and their corresponding fractions showed significant and selective inhibitory effects on urease activities. The IC_(50) values of 1 and 2 were 260.4 ± 6.37 and 381.4 ± 4.80 μmol·L-1, respectively, using thiourea(IC_(50) = 21 ± 0.11 μmol·L^(-1)) as the standard inhibitor. This was the first report demonstrating that the naphthoquinones class showed urease inhibition.
基金Supported by the National Natural Science Foundation of China (Grant No. 30725048)the Foundation of Chinese Academy of Sciences (West Light Program)
文摘Carbonic anhydrase Ⅱ (CAⅡ) is an important enzyme complex with Zn2+,which is involved in many physiological and pathological processes, such as calcification, glaucoma and tumorigenicity. In order to search for novel inhibitors of CAⅡ, inhibition assay of carbonic anhydrase Ⅱ was performed, by which seven natural phenolic compounds, including four phenolics (grifolin, 4-O-methyl-grifolic acid, grifolic acid, and isovanillic acid) and three flavones (eriodictyol, quercetin and puerin A), showed in-hibitory activities against CAⅡ with IC50s in the range of 6.37-71.73 μmol/L. Grifolic acid is the most active one with IC50 of 6.37 μmol/L. These seven phenolic compounds were proved to be novel natural carbonic anhydrase Ⅱ inhibitors, which were obtained in flexible docking study with GOLD 3.0 soft-ware. Results indicated that the aliphatic chain and polar groups of hydroxyl and carboxyl are impor-tant to their inhibitory activities, providing a new insight into study on CA Ⅱ potent inhibitors.
文摘采用扫描电镜观察了不同碱度(0、2、4 g/L Na HCO_3)胁迫对尼罗罗非鱼(Oreochromis niloticus)鳃离子细胞形态变化的影响,并采用免疫组化技术观察了鳃、肾、肠中4个HCO_3^-转运因子碳酸酐酶(CAⅡ、CAⅣ)、碳酸氢钠协同转运载体(SLC4A4)、Cl^-/HCO_3^-离子交换体(SLC26A6)的阳性反应变化。扫描电镜结果表明,鳃离子细胞分布在鳃小片基部。根据其表面开孔形状和尺寸,可分为Ⅰ型、Ⅱ型、Ⅲ型和Ⅳ型4种亚型,各亚型离子细胞的开孔尺寸随碱度胁迫强度增高呈正比增大,Ⅲ型离子细胞开孔尺寸变化最明显(P<0.01);离子细胞总数目也随碱度升高而增加,Ⅲ型离子细胞数目上升最为显著(P<0.01)。免疫组化结果表明,在淡水、碱水组中,CAⅡ、CAⅣ、SLC4A4、SLC26A6在鳃小片基部和肾中均有阳性反应,且随着碱度升高,阳性反应增强,但在肠道中未观察到阳性反应。本研究结果初步表明,尼罗罗非鱼可通过鳃离子细胞形态和数量调节适应碱度变化,鳃和肾为主要应答调节器官。
文摘目的探讨碳酸酐酶Ⅱ(CAⅡ)的表达与结直肠癌(CRC)的发生、发展,以及临床病理特征的关系。方法 Western Blot法检测CAⅡ在12对新鲜配对的CRC和远癌黏膜中的表达。再以免疫组织化学法检测CAⅡ在配对的64对远癌结直肠黏膜和CRC,20个转移淋巴结及27个息肉中的表达,比较各组间表达的差异。分析CAⅡ表达与CRC的部位、分化及临床病理分期间的关系。结果 Western Blot检测显示远癌黏膜CAⅡ/tubulin灰度比为2.48±1.68,癌组织为1.33±1.28,两者差异有统计学意义(P=0.027)。免疫组化显示CAⅡ的表达评分远癌黏膜为(2.81±0.48)分,息肉(包括增生性息肉和腺瘤)为(2.56±0.51)分,CRC为(1.30±0.89)分;按上述3种组织的顺序评分逐步显著降低(P<0.05)。在转移淋巴结中为(1.35±0.67)分,表达与配对原发灶相似(P>0.05)。CAⅡ的表达在不同部位和分化程度的CRC间差异无统计学意义(P>0.05),Ⅲ,Ⅳ期表达与Ⅰ,Ⅱ期无统计学差异(P>0.05)。结论 CAⅡ在CRC中表达的下调,是CRC发生中的早期事件,与分化、分期和转移无关。
