A method to extract crude heparin sodium from pig intestinal mucosa by dialysis and spray drying was established. The pig intestinal mucosa was treated in the following steps: enzymolysis, resin exchange adsorption-wa...A method to extract crude heparin sodium from pig intestinal mucosa by dialysis and spray drying was established. The pig intestinal mucosa was treated in the following steps: enzymolysis, resin exchange adsorption-washing, elution, pressure filtration, dialysis, spray drying. Activity of the product was measured using a heparin anti-IIa factor assay kit. The yield of crude heparin obtained by this method was 2.79% higher than that of oven drying method;the production of 1 kg crude heparin sodium saved 43.4 pigs small intestine. The activity was 98.48 ± 2.49 IU/mg (n = 5), 15.18 IU/mg higher than that obtained by oven drying method. The product is pale white powder, attractive color and easy to dissolve.展开更多
Platinum-based chemotherapeutic drugs such as cisplatin, carboplatin and oxaliplatin are widely applied for the treatment of various types of tumors. However, poor solubility, serious side effects, and more importantl...Platinum-based chemotherapeutic drugs such as cisplatin, carboplatin and oxaliplatin are widely applied for the treatment of various types of tumors. However, poor solubility, serious side effects, and more importantly, the intrinsic and acquired resistance limit their clinical applications. These factors motivate scientists to design and synthesize novel and more potent analogues lacking disadvantages of clinical platinum drugs. Platinum (IV) complexes are one of representatives. In this review, we summarized the investigations undertaken into Platinum (IV) antitumor compounds since Rosenberg first noted their antitumor activity. The synthesis method and mechanism of action of Platinum (IV) complexes are outlined, as well as their chemical and pharmacological properties. Recent advances in Platinum (IV) anticancer agents that have been in clinical trials and photoactivatable Platinum (IV) complexes are also summarized, and the purpose here is to provide insight into the requirements for the antitumor activity of Platinum (IV) complexes and a basis for progressing in a new platinum compound.展开更多
The development of multiple drug resistance(MDR) to chemotherapy and subsequent treatment failures are major obstacles in cancer therapy. An attractive option for combating MDR is inhibiting the expression of P-glycop...The development of multiple drug resistance(MDR) to chemotherapy and subsequent treatment failures are major obstacles in cancer therapy. An attractive option for combating MDR is inhibiting the expression of P-glycoprotein(P-gp) in tumor cells. Here, we report a novel chemosensitizing agent, XMD8-92,which can down-regulate P-gp. To enhance the specificity of MDR chemotherapy, a promising nanotheranostic micelle system based on poly(ethylene glycol)-blocked-poly(L-leucine)(PEG-b-Leu) was developed to simultaneously carry the anticancer drug doxorubicin, chemosensitizing agent XMD8-92, and superparamagnetic iron oxide nanoparticles(SPIOs). Featured with MDR environmentally responsive dual-targeting capability, controllable drug delivery, and efficient magnetic resonance(MR) imaging characteristics, the prepared nanotheranostics(DXS@NPs) showed outstanding in vitro cytotoxicity on MDR cells(SCG 7901/VCR) with only 53% of cells surviving compared to 90% of DOX-treated cells.Furthermore, efficient tumor inhibition and highly reduced systemic toxicity were exhibited by MDR tumor-bearing mice treated with DXS@NPs. Overall, the environmentally responsive dual-targeting nanotheranostics represent a promising approach for overcoming cancer MDR.展开更多
Background and Aims: Chronic hepatitis B virus(HBV)in-fection remains a major public health problem globally.Here,we describe the baseline characteristics and treatment pro-files of HBV-infected patients recruited to ...Background and Aims: Chronic hepatitis B virus(HBV)in-fection remains a major public health problem globally.Here,we describe the baseline characteristics and treatment pro-files of HBV-infected patients recruited to the China Registry of Hepatitis B.Methods: Inclusion criteria were patients with different stages of chronic HBV infection and complete key data.Exclusion criteria were patients with hepatocellular car-cinoma.The baseline clinical,laboratory and treatment pro-files were analyzed.Results: Finally,40,431 patients were included.The median age was 43 years,with 65.2%being men and 51.3%being positive for hepatitis B e antigen(HBeAg).The most common initial diagnosis was chronic hep-atitis B(81.0%),followed by cirrhosis(9.3%),inactive carrier of hepatitis B surface antigen(HBsAg)(6.7%),and immune tolerant phase of hepatitis B infection(3.0%).Among the 21,228 patients who were on treatment,88.0%,10.0%and 2.0%received nucleos(t)ide analogues(NAs),interferon or combination of NAs and interferon,respectively.The propor-tion of patients who received preferred NAs(entecavir or te-nofovir disoproxil fumarate)had increased from 13.5%in 2003 to 79.7%in 2016.Conclusions: We concluded that middle-aged men accounted for most of the patients with chronic hepatitis B in this cross-sectional study.About half of the patients were HBeAg-positive.NAs were the most com-monly used therapy,and use of the preferred NAs had steadily increased in the past decade.展开更多
An oxidative tandem(4+2)-cyclization/aromatization of N-aryl glycine derivatives with electron-deficient alkenes was first achieved using Ru(bpy)_(3)Cl_(2) as a photocatalyst and TBHP as an oxidant in combination with...An oxidative tandem(4+2)-cyclization/aromatization of N-aryl glycine derivatives with electron-deficient alkenes was first achieved using Ru(bpy)_(3)Cl_(2) as a photocatalyst and TBHP as an oxidant in combination with visible-light irradiation by blue LEDs.One-electron oxidation and the followingα-deprotonation of glycine derivatives affordα-amino alkyl radicals,which were then trapped by electrophilic maleimides.As an atom-economic and efficient method,a variety of pyrrolo[3,4-c]quinoline-1,3-diones have been obtained in good yields under mild reaction conditions.展开更多
文摘A method to extract crude heparin sodium from pig intestinal mucosa by dialysis and spray drying was established. The pig intestinal mucosa was treated in the following steps: enzymolysis, resin exchange adsorption-washing, elution, pressure filtration, dialysis, spray drying. Activity of the product was measured using a heparin anti-IIa factor assay kit. The yield of crude heparin obtained by this method was 2.79% higher than that of oven drying method;the production of 1 kg crude heparin sodium saved 43.4 pigs small intestine. The activity was 98.48 ± 2.49 IU/mg (n = 5), 15.18 IU/mg higher than that obtained by oven drying method. The product is pale white powder, attractive color and easy to dissolve.
文摘Platinum-based chemotherapeutic drugs such as cisplatin, carboplatin and oxaliplatin are widely applied for the treatment of various types of tumors. However, poor solubility, serious side effects, and more importantly, the intrinsic and acquired resistance limit their clinical applications. These factors motivate scientists to design and synthesize novel and more potent analogues lacking disadvantages of clinical platinum drugs. Platinum (IV) complexes are one of representatives. In this review, we summarized the investigations undertaken into Platinum (IV) antitumor compounds since Rosenberg first noted their antitumor activity. The synthesis method and mechanism of action of Platinum (IV) complexes are outlined, as well as their chemical and pharmacological properties. Recent advances in Platinum (IV) anticancer agents that have been in clinical trials and photoactivatable Platinum (IV) complexes are also summarized, and the purpose here is to provide insight into the requirements for the antitumor activity of Platinum (IV) complexes and a basis for progressing in a new platinum compound.
基金supported by the National Basic Research Development Program of China(2017YFA0205201 and 2018YFA0107301)the National Natural Science Foundation of China(81422023,81871404,81603015,U1705281,and U1505221)+1 种基金the Fundamental Research Funds for the Central Universities(20720160065,and 20720150141)the Program for New Century Excellent Talents in University,China(NCET-13-0502)
文摘The development of multiple drug resistance(MDR) to chemotherapy and subsequent treatment failures are major obstacles in cancer therapy. An attractive option for combating MDR is inhibiting the expression of P-glycoprotein(P-gp) in tumor cells. Here, we report a novel chemosensitizing agent, XMD8-92,which can down-regulate P-gp. To enhance the specificity of MDR chemotherapy, a promising nanotheranostic micelle system based on poly(ethylene glycol)-blocked-poly(L-leucine)(PEG-b-Leu) was developed to simultaneously carry the anticancer drug doxorubicin, chemosensitizing agent XMD8-92, and superparamagnetic iron oxide nanoparticles(SPIOs). Featured with MDR environmentally responsive dual-targeting capability, controllable drug delivery, and efficient magnetic resonance(MR) imaging characteristics, the prepared nanotheranostics(DXS@NPs) showed outstanding in vitro cytotoxicity on MDR cells(SCG 7901/VCR) with only 53% of cells surviving compared to 90% of DOX-treated cells.Furthermore, efficient tumor inhibition and highly reduced systemic toxicity were exhibited by MDR tumor-bearing mice treated with DXS@NPs. Overall, the environmentally responsive dual-targeting nanotheranostics represent a promising approach for overcoming cancer MDR.
文摘Background and Aims: Chronic hepatitis B virus(HBV)in-fection remains a major public health problem globally.Here,we describe the baseline characteristics and treatment pro-files of HBV-infected patients recruited to the China Registry of Hepatitis B.Methods: Inclusion criteria were patients with different stages of chronic HBV infection and complete key data.Exclusion criteria were patients with hepatocellular car-cinoma.The baseline clinical,laboratory and treatment pro-files were analyzed.Results: Finally,40,431 patients were included.The median age was 43 years,with 65.2%being men and 51.3%being positive for hepatitis B e antigen(HBeAg).The most common initial diagnosis was chronic hep-atitis B(81.0%),followed by cirrhosis(9.3%),inactive carrier of hepatitis B surface antigen(HBsAg)(6.7%),and immune tolerant phase of hepatitis B infection(3.0%).Among the 21,228 patients who were on treatment,88.0%,10.0%and 2.0%received nucleos(t)ide analogues(NAs),interferon or combination of NAs and interferon,respectively.The propor-tion of patients who received preferred NAs(entecavir or te-nofovir disoproxil fumarate)had increased from 13.5%in 2003 to 79.7%in 2016.Conclusions: We concluded that middle-aged men accounted for most of the patients with chronic hepatitis B in this cross-sectional study.About half of the patients were HBeAg-positive.NAs were the most com-monly used therapy,and use of the preferred NAs had steadily increased in the past decade.
基金We thank the National Natural Science Foundation of China(No.21961033)for financially supporting this work.
文摘An oxidative tandem(4+2)-cyclization/aromatization of N-aryl glycine derivatives with electron-deficient alkenes was first achieved using Ru(bpy)_(3)Cl_(2) as a photocatalyst and TBHP as an oxidant in combination with visible-light irradiation by blue LEDs.One-electron oxidation and the followingα-deprotonation of glycine derivatives affordα-amino alkyl radicals,which were then trapped by electrophilic maleimides.As an atom-economic and efficient method,a variety of pyrrolo[3,4-c]quinoline-1,3-diones have been obtained in good yields under mild reaction conditions.
