2016 Vol. 34, No. 2
Display Method:
2016, 34(2): 97-102.
doi: 10.3969/j.issn.1006-0111.2016.02.001
Abstract:
With the development of science and the progress of age, medicinal chemistry is not only limited to the lead discovery and the structure-activity relationship studies, but also finding the target of bioactive small molecule drugs has become a tough issue to be solved. The identification and validation of bioactive small molecule targets has become the most critical and difficult task, which plays a decisive role in academic and pharmaceutical research. Herein we summarize the current methods for target identification of small molecules,and mainly discuss about the target identification method by the chemical probes. Recent cases of successful application were also introduced to demonstrate the strategy of probe synthesis and design.
With the development of science and the progress of age, medicinal chemistry is not only limited to the lead discovery and the structure-activity relationship studies, but also finding the target of bioactive small molecule drugs has become a tough issue to be solved. The identification and validation of bioactive small molecule targets has become the most critical and difficult task, which plays a decisive role in academic and pharmaceutical research. Herein we summarize the current methods for target identification of small molecules,and mainly discuss about the target identification method by the chemical probes. Recent cases of successful application were also introduced to demonstrate the strategy of probe synthesis and design.
Progress on nano-sized drug delivery system reversing tumor and multidrug resistance of osteosarcoma
2016, 34(2): 103-105.
doi: 10.3969/j.issn.1006-0111.2016.02.002
Abstract:
Multidrug resistance(MDR) of tumor cell is the major problem for chemotherapy. However, there is no effective strategy to overcome MDR due to the complicated mechanism. The nano-sized drug delivery system could target to the tumor cell. Moreover, it could delivery different kinds of drugs. Therefore, the nano-sized drug delivery system has become a promising approach to reverse MDR. The nano-sized drug delivery system which is applied to treat the MDR of tumor(osteosarcoma) was summarized and the reverse mechanism was discussed.
Multidrug resistance(MDR) of tumor cell is the major problem for chemotherapy. However, there is no effective strategy to overcome MDR due to the complicated mechanism. The nano-sized drug delivery system could target to the tumor cell. Moreover, it could delivery different kinds of drugs. Therefore, the nano-sized drug delivery system has become a promising approach to reverse MDR. The nano-sized drug delivery system which is applied to treat the MDR of tumor(osteosarcoma) was summarized and the reverse mechanism was discussed.
2016, 34(2): 106-109.
doi: 10.3969/j.issn.1006-0111.2016.02.003
Abstract:
Triazoles are the most widely used antifungal drugs in clinic with broad spectrum and high efficacy, which targets sterol 14α-demethylase(CYP51), an enzyme expressed by the gene EGR 11, which is a key enzyme in the fungi ergosterol biosynthesis. On the one hand, the CYP51 belongs to a transmembrane protein. It is difficult to get the exact functional structure conformation which becomes a big challenge for the development of new drugs. On the other hand, it becomes consensus that EGR11 exon mutation cause CYP51 structural change is one of the major reasons for antifungal drugs resistance. Therefore, study of the structural changes toward the antifungal drug resistance is quite important. The review authors have summarized the research progress on CYP51 over the recent years.
Triazoles are the most widely used antifungal drugs in clinic with broad spectrum and high efficacy, which targets sterol 14α-demethylase(CYP51), an enzyme expressed by the gene EGR 11, which is a key enzyme in the fungi ergosterol biosynthesis. On the one hand, the CYP51 belongs to a transmembrane protein. It is difficult to get the exact functional structure conformation which becomes a big challenge for the development of new drugs. On the other hand, it becomes consensus that EGR11 exon mutation cause CYP51 structural change is one of the major reasons for antifungal drugs resistance. Therefore, study of the structural changes toward the antifungal drug resistance is quite important. The review authors have summarized the research progress on CYP51 over the recent years.
2016, 34(2): 110-113,128.
doi: 10.3969/j.issn.1006-0111.2016.02.004
Abstract:
Fluconazole, the third generation of triazole-antifungal drug, becomes the first choice in the treatment of fungal infection due to its broad antifungal spectrum, good water solubility and low toxicity. With an increasingly drug-resistant strain, developing new fluconazole derivatives is becoming an attractive topic. This review mainly indicates that people can get new fluconazole derivatives used by clinic through structural modification of fluconazole, which will give clues for advanced research.
Fluconazole, the third generation of triazole-antifungal drug, becomes the first choice in the treatment of fungal infection due to its broad antifungal spectrum, good water solubility and low toxicity. With an increasingly drug-resistant strain, developing new fluconazole derivatives is becoming an attractive topic. This review mainly indicates that people can get new fluconazole derivatives used by clinic through structural modification of fluconazole, which will give clues for advanced research.
2016, 34(2): 114-115,134.
doi: 10.3969/j.issn.1006-0111.2016.02.005
Abstract:
Oridonin is an en-kaurene diterpenoids compound which was found to have effect on tumor in vitro. But the clinical application has been limited because of poor water solubility, low bioavailability and oral absorption. Many scholars conducted a large number of structure modification researches of oridonin to search for new diterpenes with higher bio-activities and better bio-availabilities, and to develop new antitumor drugs. In this paper, studies on this aspect of oridonin were reviewed.
Oridonin is an en-kaurene diterpenoids compound which was found to have effect on tumor in vitro. But the clinical application has been limited because of poor water solubility, low bioavailability and oral absorption. Many scholars conducted a large number of structure modification researches of oridonin to search for new diterpenes with higher bio-activities and better bio-availabilities, and to develop new antitumor drugs. In this paper, studies on this aspect of oridonin were reviewed.
2016, 34(2): 116-118,173.
doi: 10.3969/j.issn.1006-0111.2016.02.006
Abstract:
Pathogenic Candida albicans has a high degree of adaptability to environment, which is evidenced by its adaptability to various conditions, including its symbiosis with the host, growth in host tissues during invasion, and survival under antifungal treatment. The growth and reproduction of C. albicans is accompanied with metabolism process. C. albicans can use a wide range of carbon and nitrogen sources, and it is sensitive to the alteration of nutrition. Recent studies reveal that the environment affects the metabolism of C. albicans, whilst C. albicans regulates its metabolism to adapt to the environment. Therefore, further study on the relationship between metabolism and high adaptability of C. albicans is helpful to discover novel antifungal targets.
Pathogenic Candida albicans has a high degree of adaptability to environment, which is evidenced by its adaptability to various conditions, including its symbiosis with the host, growth in host tissues during invasion, and survival under antifungal treatment. The growth and reproduction of C. albicans is accompanied with metabolism process. C. albicans can use a wide range of carbon and nitrogen sources, and it is sensitive to the alteration of nutrition. Recent studies reveal that the environment affects the metabolism of C. albicans, whilst C. albicans regulates its metabolism to adapt to the environment. Therefore, further study on the relationship between metabolism and high adaptability of C. albicans is helpful to discover novel antifungal targets.
2016, 34(2): 119-123.
doi: 10.3969/j.issn.1006-0111.2016.02.007
Abstract:
The inflammation and apoptosis were vital important in the progress and recovery in myocardial infarction. Apoptosis was regulated by inflammation though TNF-α, CHOP, IL-10 and α7nAChR signal pathways and influenced the severity of the inflammation via feedback regulation. Inflammation and apoptosis affected myocardial infarction size and cardiac function recovery together. Inhibition of inflammation, reducing apoptosis had been proved to be the important parts in prevention of ventricular remodeling and regulating cardiac dysfunction after myocardial infarction, which had broad prospects.
The inflammation and apoptosis were vital important in the progress and recovery in myocardial infarction. Apoptosis was regulated by inflammation though TNF-α, CHOP, IL-10 and α7nAChR signal pathways and influenced the severity of the inflammation via feedback regulation. Inflammation and apoptosis affected myocardial infarction size and cardiac function recovery together. Inhibition of inflammation, reducing apoptosis had been proved to be the important parts in prevention of ventricular remodeling and regulating cardiac dysfunction after myocardial infarction, which had broad prospects.
Advances on the research of the pharmacological activity mechanism and toxicology of Glaucocalyxin A
2016, 34(2): 124-128.
doi: 10.3969/j.issn.1006-0111.2016.02.008
Abstract:
Glaucocalyxin A(GLA) is a kind of diterpenoid enantiomers with organic chemical structure of en-15-oxo-16-kaurene. It has various pharmacological activities, such as cardiovascular and endothelium cellular protection, anti-blood coagulation, anti-Hepatitis B Virus(HBV), anti-tumor, anti-bacteria, anti-inflammation, hypoxic tolerance, immunomodulation and Ca2+ concentration regulation effect, where as its in vivo safety is quite good. As a folk medicine, it is conventionally used to treat hepatitis, gastritis, mastitis, stomachache and arthralgia. It is also used for ischemic and/or hypoxic cardio-cerebrovascular diseases such as coronary heart diseases, stenocardia and chronic cerebral circulation insufficiency in clinic. This review gives a summary of the pharmacological effects, biological mechanism, and toxicity of Glaucocalyxin A.
Glaucocalyxin A(GLA) is a kind of diterpenoid enantiomers with organic chemical structure of en-15-oxo-16-kaurene. It has various pharmacological activities, such as cardiovascular and endothelium cellular protection, anti-blood coagulation, anti-Hepatitis B Virus(HBV), anti-tumor, anti-bacteria, anti-inflammation, hypoxic tolerance, immunomodulation and Ca2+ concentration regulation effect, where as its in vivo safety is quite good. As a folk medicine, it is conventionally used to treat hepatitis, gastritis, mastitis, stomachache and arthralgia. It is also used for ischemic and/or hypoxic cardio-cerebrovascular diseases such as coronary heart diseases, stenocardia and chronic cerebral circulation insufficiency in clinic. This review gives a summary of the pharmacological effects, biological mechanism, and toxicity of Glaucocalyxin A.
2016, 34(2): 129-134.
doi: 10.3969/j.issn.1006-0111.2016.02.009
Abstract:
Objective 3,4-Methylenedioxyphenethylamine and caffeic acid derivatives have been proven previously in our group to produce activity against drug resistant fungi synergistic with fluconazole(FCZ). The two pharmacophores were coupled by amino acids as linkers in this project in order to design and synthesize the novel compounds and investigate the activity against drug resistant fungi in vitro. Methods 3,4-Methylenedioxyphenethylamine initially reacted with Boc-protected amino acids, following deprotection and coupling reaction with caffeic acid, to get nine title compounds. All title compounds as well as four intermediates were subjected to antifungal activity screening for fluconazole resistant Candida albicans in vitro. Results Nine title compounds showed synergistic antifungal activity for drug resistant Candida albicans with fluconazole at a concentration range of 0.5-2.0μg/ml. Among them, compounds 3b, 3f, 3g and 3i showed the higher activity with the same MIC80 value of 0.5μg/ml, which is comparable to those of the control compounds 7b and 5. Conclusion Linking 3,4-methylenedioxyphenethylamine and caffeic acid with piperidine-4-carboxylic acid(3b), valine(3g), leucine(3f) and isoleucine(3i) led to novel compounds with high synergistic antifungal activity against drug resistant Candida albicans combined with fluconazole.
Objective 3,4-Methylenedioxyphenethylamine and caffeic acid derivatives have been proven previously in our group to produce activity against drug resistant fungi synergistic with fluconazole(FCZ). The two pharmacophores were coupled by amino acids as linkers in this project in order to design and synthesize the novel compounds and investigate the activity against drug resistant fungi in vitro. Methods 3,4-Methylenedioxyphenethylamine initially reacted with Boc-protected amino acids, following deprotection and coupling reaction with caffeic acid, to get nine title compounds. All title compounds as well as four intermediates were subjected to antifungal activity screening for fluconazole resistant Candida albicans in vitro. Results Nine title compounds showed synergistic antifungal activity for drug resistant Candida albicans with fluconazole at a concentration range of 0.5-2.0μg/ml. Among them, compounds 3b, 3f, 3g and 3i showed the higher activity with the same MIC80 value of 0.5μg/ml, which is comparable to those of the control compounds 7b and 5. Conclusion Linking 3,4-methylenedioxyphenethylamine and caffeic acid with piperidine-4-carboxylic acid(3b), valine(3g), leucine(3f) and isoleucine(3i) led to novel compounds with high synergistic antifungal activity against drug resistant Candida albicans combined with fluconazole.
2016, 34(2): 135-137.
doi: 10.3969/j.issn.1006-0111.2016.02.010
Abstract:
Objective To improve the synthesis process of chlorine f(1). Methods A "one-pot" method was applied to prepare Photosensitizer component(1), using pheophorbide a(3) as raw material by oxidating and cracking of the E-ring of(3) with bubbling oxygen in alcoholic solution of potassium hydroxide at 0℃ followed by refluxing in nitrogen atmosphere. In order to obtain the optimal synthetic procedure, the orthogonal experimental design of L9(34) was adopted to investigate three different levels of four main factors i.e. ring opening reaction time, alcoholic variety, alkali concentration and refluxing reaction time. Results The target compound(1) was optimizedly synthesized through treatment of raw material(3) with bubbling oxygen in 25% ethanol solution of potassium hydroxide at 0℃ for 30 min, followed by refluxing in nitrogen atmosphere for 20 min in yield of 40.8%. Conclusion The procedure developed has some advantages of simple and safty operation, and high synthetic yield.
Objective To improve the synthesis process of chlorine f(1). Methods A "one-pot" method was applied to prepare Photosensitizer component(1), using pheophorbide a(3) as raw material by oxidating and cracking of the E-ring of(3) with bubbling oxygen in alcoholic solution of potassium hydroxide at 0℃ followed by refluxing in nitrogen atmosphere. In order to obtain the optimal synthetic procedure, the orthogonal experimental design of L9(34) was adopted to investigate three different levels of four main factors i.e. ring opening reaction time, alcoholic variety, alkali concentration and refluxing reaction time. Results The target compound(1) was optimizedly synthesized through treatment of raw material(3) with bubbling oxygen in 25% ethanol solution of potassium hydroxide at 0℃ for 30 min, followed by refluxing in nitrogen atmosphere for 20 min in yield of 40.8%. Conclusion The procedure developed has some advantages of simple and safty operation, and high synthetic yield.
2016, 34(2): 138-141,166.
doi: 10.3969/j.issn.1006-0111.2016.02.011
Abstract:
Objective To investigate the secondary metabolites of the South China Sea spine body sponge Acanthella cavernosa. Methods The acetone extract of A. cavernosa was isolated and purified by repeated column chromatography on silica gel, sephadex LH-20, and high-performance liquid chromatography(HPLC). Structures were determined by spectroscopic analysis and comparison with reported data. Results Nine compounds were isolated. Their structures were determined as kalihinol E(1), kalihinol A(2), 10-epi-kalihinol X(3), 10-epi-kalihinol I(4), 1H-indole-3-carboxylic acid methyl ester(5), 1H-indole-3-carboxylic acid(6), 3-buten-2-one,4-(2,3,6-trimethylphenyl)-(3E)(7), aristolone(8), and 5α, 8α-epidioxy-(22E, 24R)-erost-6, 22-dien-3β-ol(9). Conclusion Compounds 5 to 8 were isolated from the sponge of genus Acanthalla for the first time.
Objective To investigate the secondary metabolites of the South China Sea spine body sponge Acanthella cavernosa. Methods The acetone extract of A. cavernosa was isolated and purified by repeated column chromatography on silica gel, sephadex LH-20, and high-performance liquid chromatography(HPLC). Structures were determined by spectroscopic analysis and comparison with reported data. Results Nine compounds were isolated. Their structures were determined as kalihinol E(1), kalihinol A(2), 10-epi-kalihinol X(3), 10-epi-kalihinol I(4), 1H-indole-3-carboxylic acid methyl ester(5), 1H-indole-3-carboxylic acid(6), 3-buten-2-one,4-(2,3,6-trimethylphenyl)-(3E)(7), aristolone(8), and 5α, 8α-epidioxy-(22E, 24R)-erost-6, 22-dien-3β-ol(9). Conclusion Compounds 5 to 8 were isolated from the sponge of genus Acanthalla for the first time.
2016, 34(2): 142-147,170.
doi: 10.3969/j.issn.1006-0111.2016.02.012
Abstract:
Objective To screen the formulation of self-microemulsifying drug delivery system(SMEDDS) for sirolimus(SRL) and prepare the SRL-SMEDDS pellets. Methods Co-emulsifier, oil phase and emulsifier were chosen by solubility test and ternary phase diagrams, central composite design and response surface method were adopted to screen and optimize the preparation and formulation of liquid SRL-SMEDDS. The selected liquid SRL-SMEDDS formulations were prepared into pellets by extrusion-spheronization method. Results The final pellets from liquid SRL-SMEDDS formulation:SRL 0.4%, Labrafil M1944CS 9.3%, Cremophor EL 15.9%, Transcutol P 8.0%, MCC 49.8%, lactose 13.3%, CMS-Na 3.3%. Dissolution test showed superphosphate(SSP) in the dissolution water is much greater than the commercially available sirolimus tablets; while in 0.4% SDS solution, the two formulations showed similar dissolution. Conclusion SMEDDS can improve the dissolution of SRL in vitro.
Objective To screen the formulation of self-microemulsifying drug delivery system(SMEDDS) for sirolimus(SRL) and prepare the SRL-SMEDDS pellets. Methods Co-emulsifier, oil phase and emulsifier were chosen by solubility test and ternary phase diagrams, central composite design and response surface method were adopted to screen and optimize the preparation and formulation of liquid SRL-SMEDDS. The selected liquid SRL-SMEDDS formulations were prepared into pellets by extrusion-spheronization method. Results The final pellets from liquid SRL-SMEDDS formulation:SRL 0.4%, Labrafil M1944CS 9.3%, Cremophor EL 15.9%, Transcutol P 8.0%, MCC 49.8%, lactose 13.3%, CMS-Na 3.3%. Dissolution test showed superphosphate(SSP) in the dissolution water is much greater than the commercially available sirolimus tablets; while in 0.4% SDS solution, the two formulations showed similar dissolution. Conclusion SMEDDS can improve the dissolution of SRL in vitro.
2016, 34(2): 148-152.
doi: 10.3969/j.issn.1006-0111.2016.02.013
Abstract:
Objective To prepare a novel drug delivery system camptothecin loaded nanogel(CPT-PPO gel), and investigate its contents, physical and chemical properties and in vitro transdermal permeability. Methods The solvent evaporation method was utilized to prepare core-shell nano-drug delivery systems(CPT-PLGA-PAMAM, CPT-PP), in which the Poly lactic-co-glycolic acid(PLGA) was used to load camptothecin as the nucleus and the polyamidoamine(PAMAM) G3.0 was wrapped in the surface of PLGA as the shell. Then the oleic acid(OA) was connected to CPT-PP to obtain the surface modified drug delivery system(CPT-PLGA-PAMAM OA, CPT-PPO). HPLC was used to determine the content of camptothecin in nanoparticles, transmission electron microscopy was applied to identify the nanoparticles morphology, and laser analyzer was used to determine the particle size. The hydroxypropyl methylcellulose(HPMC) was added as the base for the preparation of the nanogel(CPT-PPO gel) at last. The Franz-diffusion cell was used to determine the permeation rate of nanogel in vitro. Results The resulting CPT-PPO gel was stable at 4℃, the average particle size was(246.7±5.4) nm and the encapsulation efficiency was up to(78.7±6.9)%. Comparing to the normal gel,(CPT gel), the cumulative penetration amount and the retention amount in the skin of the nanogels(CPT-PPO gel,CPT-PP gel) were significant higher(P<0.01), the retention and cumulative penetration amount of CPT-PPO gel was significant higher than that of CPT-PP gel(P<0.05). Conclusion After modified by OA, CPT-PPO gel can increase the cumulated amount and absorption in skin and can be used as a carrier of CPT in the new formulation for topical treatment of psoriasis.
Objective To prepare a novel drug delivery system camptothecin loaded nanogel(CPT-PPO gel), and investigate its contents, physical and chemical properties and in vitro transdermal permeability. Methods The solvent evaporation method was utilized to prepare core-shell nano-drug delivery systems(CPT-PLGA-PAMAM, CPT-PP), in which the Poly lactic-co-glycolic acid(PLGA) was used to load camptothecin as the nucleus and the polyamidoamine(PAMAM) G3.0 was wrapped in the surface of PLGA as the shell. Then the oleic acid(OA) was connected to CPT-PP to obtain the surface modified drug delivery system(CPT-PLGA-PAMAM OA, CPT-PPO). HPLC was used to determine the content of camptothecin in nanoparticles, transmission electron microscopy was applied to identify the nanoparticles morphology, and laser analyzer was used to determine the particle size. The hydroxypropyl methylcellulose(HPMC) was added as the base for the preparation of the nanogel(CPT-PPO gel) at last. The Franz-diffusion cell was used to determine the permeation rate of nanogel in vitro. Results The resulting CPT-PPO gel was stable at 4℃, the average particle size was(246.7±5.4) nm and the encapsulation efficiency was up to(78.7±6.9)%. Comparing to the normal gel,(CPT gel), the cumulative penetration amount and the retention amount in the skin of the nanogels(CPT-PPO gel,CPT-PP gel) were significant higher(P<0.01), the retention and cumulative penetration amount of CPT-PPO gel was significant higher than that of CPT-PP gel(P<0.05). Conclusion After modified by OA, CPT-PPO gel can increase the cumulated amount and absorption in skin and can be used as a carrier of CPT in the new formulation for topical treatment of psoriasis.
2016, 34(2): 153-157.
doi: 10.3969/j.issn.1006-0111.2016.02.014
Abstract:
Objective To prepare paeoniflorin gastric floating tablets and to optimize the formulation. Methods Gastric floating tablets were prepared by wet granulation, with floating performance and in vitro cumulative release rate as evaluat indicators, single factor tests and orthogonal design test were adopted for the optimal formulation. Results With HPMC K4M 20% as reinforcing materials, NaHCO3 15% as gas agent, PVPP 7% as the release of accelerator, lactose as a filler, the obtained gastric floating tablet can immediately play bleaching, continued to float more than 12 hours, and the cumulative release rate was more than 90%. Conclusion The optimal formulation of paeconiflorin floating tablet has achieved a sustained and slow release request floating, the operability is good.
Objective To prepare paeoniflorin gastric floating tablets and to optimize the formulation. Methods Gastric floating tablets were prepared by wet granulation, with floating performance and in vitro cumulative release rate as evaluat indicators, single factor tests and orthogonal design test were adopted for the optimal formulation. Results With HPMC K4M 20% as reinforcing materials, NaHCO3 15% as gas agent, PVPP 7% as the release of accelerator, lactose as a filler, the obtained gastric floating tablet can immediately play bleaching, continued to float more than 12 hours, and the cumulative release rate was more than 90%. Conclusion The optimal formulation of paeconiflorin floating tablet has achieved a sustained and slow release request floating, the operability is good.
2016, 34(2): 158-162.
doi: 10.3969/j.issn.1006-0111.2016.02.015
Abstract:
Objective To improve the hydrophobic properties of the ordered mesoporous carbon nanoparticles(MCN) by PVP or DSPE-mPEG2000 modification, and to compare the effect on the dispersion and cytotoxicity of MCN before and after modification. Methods MCN was synthesized by low concentration hydrothermal method. The surface was modified by PVP or DSPE-mPEG2000. The properties of the materials were characterized by transmission electron microscopy(TEM), scanning electron microscopy(SEM), nitrogen sorption analysis, particle size and infrared spectroscopy(IR). The effect on the dispersion of MCN was investigated. CCK-8 method was used to investigate the cytotoxicity of the materials. Flow cytometry was used to investigate the effect of cell oxidative stress. Results The distribution of synthesized MCN was uniform, with average particle size about 90 nm. The particle size and Zeta potential increased slightly after surface modification, while the dispersibility was significantly improved. No significant difference was observed in the toxicity of L929 and HeLa cells before and after modification. However, the modified MCN showed significant effect of reducing production of cellular reactive oxygen species. Conclusion Ordered mesoporous carbon nanoparticles with surface modified by PVP or DSPE-mPEG2000 provide good biocompatibility and can significantly reduce oxidative stress.
Objective To improve the hydrophobic properties of the ordered mesoporous carbon nanoparticles(MCN) by PVP or DSPE-mPEG2000 modification, and to compare the effect on the dispersion and cytotoxicity of MCN before and after modification. Methods MCN was synthesized by low concentration hydrothermal method. The surface was modified by PVP or DSPE-mPEG2000. The properties of the materials were characterized by transmission electron microscopy(TEM), scanning electron microscopy(SEM), nitrogen sorption analysis, particle size and infrared spectroscopy(IR). The effect on the dispersion of MCN was investigated. CCK-8 method was used to investigate the cytotoxicity of the materials. Flow cytometry was used to investigate the effect of cell oxidative stress. Results The distribution of synthesized MCN was uniform, with average particle size about 90 nm. The particle size and Zeta potential increased slightly after surface modification, while the dispersibility was significantly improved. No significant difference was observed in the toxicity of L929 and HeLa cells before and after modification. However, the modified MCN showed significant effect of reducing production of cellular reactive oxygen species. Conclusion Ordered mesoporous carbon nanoparticles with surface modified by PVP or DSPE-mPEG2000 provide good biocompatibility and can significantly reduce oxidative stress.
2016, 34(2): 163-166.
doi: 10.3969/j.issn.1006-0111.2016.02.016
Abstract:
Objective To determine the concentration of eupatilin and arteanoflavone in Artemisia anomala by high performance liquid chromatography(HPLC). Methods Artemisia anomala was extracted by ultrasonic for 60 minutes with 10 times volume of methanol. The HPLC was performed on a SHISEIDO MG-C18 column(3.0 mm×100 mm, 3μm). The mobile phase was a mixture of acetonitrile(ACN) and 0.1% formic acid(40:60, V/V). The detection wavelength was 350 nm, the column temperature was 25℃ and the injection volumn was 5μl. Results Eupatilin and arteanoflavone were separated at baseline within 15min with good linearity. The method validation results show that the precisions, repeatability and stability were all in the normal range. The low,medium and high level recoveries of eupatilin were 100.26%,99.58%,102.24%,and those of arteanoflavone were 99.09%,101.12%,101.43%,respectively. Conclusion The method was rapid, simple, reproductive and accurate. It can be used to control the quality of Artemisia anomala.
Objective To determine the concentration of eupatilin and arteanoflavone in Artemisia anomala by high performance liquid chromatography(HPLC). Methods Artemisia anomala was extracted by ultrasonic for 60 minutes with 10 times volume of methanol. The HPLC was performed on a SHISEIDO MG-C18 column(3.0 mm×100 mm, 3μm). The mobile phase was a mixture of acetonitrile(ACN) and 0.1% formic acid(40:60, V/V). The detection wavelength was 350 nm, the column temperature was 25℃ and the injection volumn was 5μl. Results Eupatilin and arteanoflavone were separated at baseline within 15min with good linearity. The method validation results show that the precisions, repeatability and stability were all in the normal range. The low,medium and high level recoveries of eupatilin were 100.26%,99.58%,102.24%,and those of arteanoflavone were 99.09%,101.12%,101.43%,respectively. Conclusion The method was rapid, simple, reproductive and accurate. It can be used to control the quality of Artemisia anomala.
2016, 34(2): 167-170.
doi: 10.3969/j.issn.1006-0111.2016.02.017
Abstract:
Objective To establish a quality standard of Weinaxin granular. Methods Pinelliae Rhizoma,Poria,Glycyrrhizae, Radix Angelicae,Aurantii Fructus were identified by TLC,and the assay of Narigin in Aurantii Fructus was performed by reverse phase HPLC. Results Pinelliae Rhizoma,Poria,Glycyrrhizae,Radix Angelicae,Aurantii Fructus can be identified by TLC. The HPLC method for Narigin shows a baseline separation with a linear calibration curve in the range of 0.0844~0.2954μg(r=0.9993). The average recovery of the method was 98.74%.The RSD was 1.20%(n=6). Conclusion This method was reliable and accurate,can be used for the quality control of this product.
Objective To establish a quality standard of Weinaxin granular. Methods Pinelliae Rhizoma,Poria,Glycyrrhizae, Radix Angelicae,Aurantii Fructus were identified by TLC,and the assay of Narigin in Aurantii Fructus was performed by reverse phase HPLC. Results Pinelliae Rhizoma,Poria,Glycyrrhizae,Radix Angelicae,Aurantii Fructus can be identified by TLC. The HPLC method for Narigin shows a baseline separation with a linear calibration curve in the range of 0.0844~0.2954μg(r=0.9993). The average recovery of the method was 98.74%.The RSD was 1.20%(n=6). Conclusion This method was reliable and accurate,can be used for the quality control of this product.
2016, 34(2): 171-173.
doi: 10.3969/j.issn.1006-0111.2016.02.018
Abstract:
Objective To optimize novel triazole antifungal compounds synthesis of key intermediates. Methods The orthogonal experimental design is used, emphasizing on four factors including the reaction temperature, the weight ratio of material, reaction time and solvent on the yield. Results The effect of reaction temperature on the reaction yield is the most significant, followed by reaction time; the weight ratio of material and solvent on the yield impact is not obvious. Conclusion The new technology has several advantages and yields up to about 50%, less reactive impurities, easy post processing.
Objective To optimize novel triazole antifungal compounds synthesis of key intermediates. Methods The orthogonal experimental design is used, emphasizing on four factors including the reaction temperature, the weight ratio of material, reaction time and solvent on the yield. Results The effect of reaction temperature on the reaction yield is the most significant, followed by reaction time; the weight ratio of material and solvent on the yield impact is not obvious. Conclusion The new technology has several advantages and yields up to about 50%, less reactive impurities, easy post processing.
2016, 34(2): 174-176,187.
doi: 10.3969/j.issn.1006-0111.2016.02.019
Abstract:
Objective To study the fingerprint of Polygonum cuspidatum from various regions by HPLC and provide technical support for the identification. Methods HPLC conditions:the chromatographic column was Agilent ZORBAX SB-C18(4.6 mm×250 mm, 5μm); the mobile phase was 0.1% formic acid in water and acetonitrile(A-B); gradient elution; the detection wavelength was 306 nm; the flow rate was 1 ml/min; the column temperature was 30℃; injection volume was 20μl. Results The HPLC gradient conditions could effectively separate polydatin, resveratrol, emodin and emodin ether, etc. Conclusion This method is stable, effective and durable, which is instructive to the herbs data identification of Polygonum cuspidatum.
Objective To study the fingerprint of Polygonum cuspidatum from various regions by HPLC and provide technical support for the identification. Methods HPLC conditions:the chromatographic column was Agilent ZORBAX SB-C18(4.6 mm×250 mm, 5μm); the mobile phase was 0.1% formic acid in water and acetonitrile(A-B); gradient elution; the detection wavelength was 306 nm; the flow rate was 1 ml/min; the column temperature was 30℃; injection volume was 20μl. Results The HPLC gradient conditions could effectively separate polydatin, resveratrol, emodin and emodin ether, etc. Conclusion This method is stable, effective and durable, which is instructive to the herbs data identification of Polygonum cuspidatum.
2016, 34(2): 177-178.
doi: 10.3969/j.issn.1006-0111.2016.02.020
Abstract:
Objective To establish a method of microbial limit tests for compound Hongjingtian oral liquid and to perform the validation of the method. Methods The validation on the microbial limit test method was conducted according to the counting method of bacteria,mycetes and yeasts and the control bacteria test method stated in the appendix of China pharmacopoeia(2010 edition). Results The recoveries were over 70% when culture diluting method was used for staphylococcus aureus and routine test method was used for Escherichia coli, Bacillus subtilis,Candida albicans and Aspergillus niger. In the test of positive control bacteria, the growth was detected, while the negative control was no growth detected. Conclusion The microbial limit test for compound Hongjingtian oral liquid is validated in this study. The amount of staphylococcus aureus can be determined using diluted culture method; while the amounts of Escherichia coli, Bacillus subtilis,Candida albicans, Aspergillus niger can be determined by conventional method.
Objective To establish a method of microbial limit tests for compound Hongjingtian oral liquid and to perform the validation of the method. Methods The validation on the microbial limit test method was conducted according to the counting method of bacteria,mycetes and yeasts and the control bacteria test method stated in the appendix of China pharmacopoeia(2010 edition). Results The recoveries were over 70% when culture diluting method was used for staphylococcus aureus and routine test method was used for Escherichia coli, Bacillus subtilis,Candida albicans and Aspergillus niger. In the test of positive control bacteria, the growth was detected, while the negative control was no growth detected. Conclusion The microbial limit test for compound Hongjingtian oral liquid is validated in this study. The amount of staphylococcus aureus can be determined using diluted culture method; while the amounts of Escherichia coli, Bacillus subtilis,Candida albicans, Aspergillus niger can be determined by conventional method.
2016, 34(2): 179-180.
doi: 10.3969/j.issn.1006-0111.2016.02.021
Abstract:
Objective To discuss the measures to prevent adverse events caused by misused hyperosmolar drugs. Methods Clinical pharmacists were involved in the treatment of one case of skin necrosis caused by hyperosmolar arginine infusion, analyzing the cause of the adverse events and proposing solutions and preventative measures. Results Treatment includs external application of Epson salt,debridements,infection prevention and so on were implemented. All bruises were absorbed with good wound healing. Conclusion Clinical pharmacist should play a role in examining prescriptions and ensuring drug safety for patients.
Objective To discuss the measures to prevent adverse events caused by misused hyperosmolar drugs. Methods Clinical pharmacists were involved in the treatment of one case of skin necrosis caused by hyperosmolar arginine infusion, analyzing the cause of the adverse events and proposing solutions and preventative measures. Results Treatment includs external application of Epson salt,debridements,infection prevention and so on were implemented. All bruises were absorbed with good wound healing. Conclusion Clinical pharmacist should play a role in examining prescriptions and ensuring drug safety for patients.
2016, 34(2): 181-183.
doi: 10.3969/j.issn.1006-0111.2016.02.022
Abstract:
Objective To investigate countermeasures and effects of clinical pharmacists participating in the treatment for fluconazole-exposure candidemia, and to provide reference for infectious control in the clinic. Methods Clinical pharmacists used their professional knowledge and suggested utilizing micafungin to treat candidemia, when voriconazole was ineffective in a patient with candidemia and fluconazole exposure history. Results The patient's candida bloodstream infection was finally controlled. Clinical pharmacists were highly complimented from the doctors, nurses and patients. Conclusion Micafungin is effective in treatment of candidemia with a recent(<30 days) fluconazole exposure history. The participation of clinical pharmacists is helpful to develop individual medicinal therapy in clinical treatment and can improve therapeutic effects.
Objective To investigate countermeasures and effects of clinical pharmacists participating in the treatment for fluconazole-exposure candidemia, and to provide reference for infectious control in the clinic. Methods Clinical pharmacists used their professional knowledge and suggested utilizing micafungin to treat candidemia, when voriconazole was ineffective in a patient with candidemia and fluconazole exposure history. Results The patient's candida bloodstream infection was finally controlled. Clinical pharmacists were highly complimented from the doctors, nurses and patients. Conclusion Micafungin is effective in treatment of candidemia with a recent(<30 days) fluconazole exposure history. The participation of clinical pharmacists is helpful to develop individual medicinal therapy in clinical treatment and can improve therapeutic effects.
2016, 34(2): 184-187.
doi: 10.3969/j.issn.1006-0111.2016.02.023
Abstract:
Objective To introduce the process and experience of construction of medical supplies support practice training platform under informatization. Methods To review and comment the structure composition, functions implemented, applications and experience of medical supplies support practice training platform. Results The medical supplies support practice training platform achieved four functions which are indoor deduction, simulation training, drill outdoor, participate in military health service exercise. Conclusion The medical supplies support practice training platform has achieved good effects in teaching and training, which has effectively promoted the teaching and training mode reform aimed at combat requirements.
Objective To introduce the process and experience of construction of medical supplies support practice training platform under informatization. Methods To review and comment the structure composition, functions implemented, applications and experience of medical supplies support practice training platform. Results The medical supplies support practice training platform achieved four functions which are indoor deduction, simulation training, drill outdoor, participate in military health service exercise. Conclusion The medical supplies support practice training platform has achieved good effects in teaching and training, which has effectively promoted the teaching and training mode reform aimed at combat requirements.
2016, 34(2): 188-190,192.
doi: 10.3969/j.issn.1006-0111.2016.02.024
Abstract:
Objective To study the application of outpatient oral antihypertensive drugs in Shanghai Meishan Hospital, and provide a guide for clinical rational drug use. Methods The utilization of antihypertensive drugs in outpatients of our hospital was analyzed statistically by using defined daily dose(DDD) recommended by WHO. Results 1 The most commonly used antihypertensive drugs in outpatients was calcium antagonist(51.98%), followed by angiotensin receptor blockers(16.60%), fixed-dose combination(13.23%), β-blockers(11.93%), diuretics(3.67%), angiotensin-converting enzyme inhibitors(2.40%), and α,β-blockers(0.19%). 2 The combination therapy was fewer in outpatients than monotherapy(32.99% versus 67.01%). Conclusion The application of antihypertensive drugs is basically reasonable in outpatient of our hospital, but the combination therapy was inadequate.
Objective To study the application of outpatient oral antihypertensive drugs in Shanghai Meishan Hospital, and provide a guide for clinical rational drug use. Methods The utilization of antihypertensive drugs in outpatients of our hospital was analyzed statistically by using defined daily dose(DDD) recommended by WHO. Results 1 The most commonly used antihypertensive drugs in outpatients was calcium antagonist(51.98%), followed by angiotensin receptor blockers(16.60%), fixed-dose combination(13.23%), β-blockers(11.93%), diuretics(3.67%), angiotensin-converting enzyme inhibitors(2.40%), and α,β-blockers(0.19%). 2 The combination therapy was fewer in outpatients than monotherapy(32.99% versus 67.01%). Conclusion The application of antihypertensive drugs is basically reasonable in outpatient of our hospital, but the combination therapy was inadequate.
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