2010 Vol. 28, No. 4
Display Method:
2010, 28(4): 241-244.
Abstract:
Ganoderma polysaccharides(GP) contain active substances with remarkable bioactivities such as immunoregulation,anticancer,anti-oxidant,anti-aging and promoting blood circulation by removing blood stasis.Their recent research progress is of great significance and be paid more and more attention.The progress on extraction,isolation and purification,structural analysis and biological activity of GP were summarized and the development prospects were forecasted in this paper.
Ganoderma polysaccharides(GP) contain active substances with remarkable bioactivities such as immunoregulation,anticancer,anti-oxidant,anti-aging and promoting blood circulation by removing blood stasis.Their recent research progress is of great significance and be paid more and more attention.The progress on extraction,isolation and purification,structural analysis and biological activity of GP were summarized and the development prospects were forecasted in this paper.
2010, 28(4): 255-257,290.
Abstract:
Objective To investigate the effect of a single dose of allisartan potassium(ALS3K) on the blood pressure(BP) in spontaneously hypertensive rats(SHR). Methods SHR were randomly divided into seven groups(n=9 per group) and given 0.5%CMC-Na,allisartan 2.5 mg/kg,Losartan potassium 2.5 mg/kg,ALS3K 1.0、2.5、5.0 and 10 mg/kg,respectively.Rats were anesthetized and two catheters were inserted into the lower abdominal aorta via the left femoral artery and the stomach.After 24 h recovery period,the drugs were dissolved in 0.5 % carboxymethylcellulose sodium(CMC) and given via a catheter inserted into the stomach.The BP and HP 1 h before drug administration and 6 h after drug administration were determined in conscious freely moving SHR by computer. Results Compared to before administration,the BP was significantly decreased by ALS3K at the dose of 2.5 mg/kg(SBP/DBP,15/16 mmHg,(P<0.01).Similar Results were found by ALS3K at the dose of 5.0 and 10 mg/kg.The BP had no change in ALS-3(2.5 mg/kg) and Los(2.5 mg/kg) treatment groups.HP had no change in any groups. Conclusion Compared with the basal values,levels of SBP and DBP after drug administration were significantly decreased dose-dependently by ALS3K.In the way of changing the structure,SHR can be given lower dose by ALS3K to get the same BP reduction as ALS-3.
Objective To investigate the effect of a single dose of allisartan potassium(ALS3K) on the blood pressure(BP) in spontaneously hypertensive rats(SHR). Methods SHR were randomly divided into seven groups(n=9 per group) and given 0.5%CMC-Na,allisartan 2.5 mg/kg,Losartan potassium 2.5 mg/kg,ALS3K 1.0、2.5、5.0 and 10 mg/kg,respectively.Rats were anesthetized and two catheters were inserted into the lower abdominal aorta via the left femoral artery and the stomach.After 24 h recovery period,the drugs were dissolved in 0.5 % carboxymethylcellulose sodium(CMC) and given via a catheter inserted into the stomach.The BP and HP 1 h before drug administration and 6 h after drug administration were determined in conscious freely moving SHR by computer. Results Compared to before administration,the BP was significantly decreased by ALS3K at the dose of 2.5 mg/kg(SBP/DBP,15/16 mmHg,(P<0.01).Similar Results were found by ALS3K at the dose of 5.0 and 10 mg/kg.The BP had no change in ALS-3(2.5 mg/kg) and Los(2.5 mg/kg) treatment groups.HP had no change in any groups. Conclusion Compared with the basal values,levels of SBP and DBP after drug administration were significantly decreased dose-dependently by ALS3K.In the way of changing the structure,SHR can be given lower dose by ALS3K to get the same BP reduction as ALS-3.
2010, 28(4): 258-261.
Abstract:
Objective To apply 1HNMR spectroscopic analysis and principal components analysis(PCA) for investigating the difference of blood composition spectrum between hypertension patients with hyperactivity of liver-yang and healthy volunteers,to search possible biomarker,Reveal the nature of syndrome of hyperactivity of liver-yang. Methods Choose typical cases according to the clinic diagnostic criteria for liver-yang hyperactivity hypertension,and analysis the components in the blood of hypertension in the patients with syndrome of ascendant hyperactivity of liver-yang and healthy volunteers by 1HNMR.Track biomarkers and make the possible explanation of the relevant metabolic pathways with pattern recognition by the PCA method. Results The data from the analysis by PCA of the serum samples of hypertension in hypertension patients with syndrome of ascendant hyperactivity of liver-yang and healthy volunteers shows that: two sets of data can be classified in the score plot.There is significant differences existing between the two groups in terms of relative metabolism of body,especially for some amino acid metabolism and Glucose metabolism. Conclusion The metabonomics method,1HNMR combined with PCA pattern recognition,has advantages in studying pathophysiological changes of the body under the complicated conditions.The study provided evidences for probing the essence of the hypertension of syndrome of ascendant hyperactivity of liver-yang and researching the clinical diagnosis of such diseases.
Objective To apply 1HNMR spectroscopic analysis and principal components analysis(PCA) for investigating the difference of blood composition spectrum between hypertension patients with hyperactivity of liver-yang and healthy volunteers,to search possible biomarker,Reveal the nature of syndrome of hyperactivity of liver-yang. Methods Choose typical cases according to the clinic diagnostic criteria for liver-yang hyperactivity hypertension,and analysis the components in the blood of hypertension in the patients with syndrome of ascendant hyperactivity of liver-yang and healthy volunteers by 1HNMR.Track biomarkers and make the possible explanation of the relevant metabolic pathways with pattern recognition by the PCA method. Results The data from the analysis by PCA of the serum samples of hypertension in hypertension patients with syndrome of ascendant hyperactivity of liver-yang and healthy volunteers shows that: two sets of data can be classified in the score plot.There is significant differences existing between the two groups in terms of relative metabolism of body,especially for some amino acid metabolism and Glucose metabolism. Conclusion The metabonomics method,1HNMR combined with PCA pattern recognition,has advantages in studying pathophysiological changes of the body under the complicated conditions.The study provided evidences for probing the essence of the hypertension of syndrome of ascendant hyperactivity of liver-yang and researching the clinical diagnosis of such diseases.
2010, 28(4): 262-264,273.
Abstract:
Objective To investigate variance of apoptosis and correspondingly mechanism in HL-60 cell line in vitro by different combinations adminstration of three drug including cytarabine,daunorubicin and all-trans retinoic acid.Methonds HL-60 cell line was cultured in vitro,cell suspension was divided into different 7 groups which's density was 2.0×105/ml : Group A: control;Group B:Ara-C and ATRA were simultaneous applied in cells for 48 h(Ara-C+ATRA 48 h);Group C: ATRA and Ara-C subsequently administrated respectively for 24 h that is ATRA was applied first for 24 h,then followed by Ara-C for 24 h.Group D: Ara-C and ATRA subsequently administrated respectively for 24 h that is Ara-C was applied first for 24 h,then followed by ATRA for 24 h;Group E: DNR and ATRA simultaneously administrated for 48 h;Group F: DNR and ATRA subsequently administrated respectively for 24 h that is DNR was applied first for 24 h,then followed by ATRA for 24 h.Group G: ATRA and DNR subsequently administrated respectively for 24 h that is ATRA was applied first for 24 h,then followed by DNR for 24 h.All drug concentrations of Ara-C,DNR and ATRA were 1.0×10-7 mol/L.The ratio of apoptosis cells was evaluated by flow cytometry.Anti-apoptosis protein Bcl-2 was checked by Western Blotting. Results The ratio of cell apoptosis in D group increase slightly,the rate of increase in apoptosis was(50±14.7) %,its protein Bcl-2 disappeared.Compared with control group,both two groups including E and G groups caused the apoptosis ratio significant higher.The alive cells' ratio in E group was reduced to the highest degree and the amount of dead cells increased to a degree of(4.00±0.56) %.Anti-apoptosis protein Bcl-2 in E,F,G groups all disappeared. Conclusion Combination DNR and ATRA simultaneously can effectively decrease HL-60 survival.Three ways of combination DNR with ATRA can signifi- cantly cause protein Bcl-2 disappear.But low dose of Ara-C was administrated first then followed by ATRA can not only increase slightly the ratio of apoptosis of HL-60 cell,but also inhibited anti-apoptosis protein Bcl-2 to express and effectively controled the way of HL-60 cell's death to apoptosis,and we concluded that this combination is the most potentiall way.
Objective To investigate variance of apoptosis and correspondingly mechanism in HL-60 cell line in vitro by different combinations adminstration of three drug including cytarabine,daunorubicin and all-trans retinoic acid.Methonds HL-60 cell line was cultured in vitro,cell suspension was divided into different 7 groups which's density was 2.0×105/ml : Group A: control;Group B:Ara-C and ATRA were simultaneous applied in cells for 48 h(Ara-C+ATRA 48 h);Group C: ATRA and Ara-C subsequently administrated respectively for 24 h that is ATRA was applied first for 24 h,then followed by Ara-C for 24 h.Group D: Ara-C and ATRA subsequently administrated respectively for 24 h that is Ara-C was applied first for 24 h,then followed by ATRA for 24 h;Group E: DNR and ATRA simultaneously administrated for 48 h;Group F: DNR and ATRA subsequently administrated respectively for 24 h that is DNR was applied first for 24 h,then followed by ATRA for 24 h.Group G: ATRA and DNR subsequently administrated respectively for 24 h that is ATRA was applied first for 24 h,then followed by DNR for 24 h.All drug concentrations of Ara-C,DNR and ATRA were 1.0×10-7 mol/L.The ratio of apoptosis cells was evaluated by flow cytometry.Anti-apoptosis protein Bcl-2 was checked by Western Blotting. Results The ratio of cell apoptosis in D group increase slightly,the rate of increase in apoptosis was(50±14.7) %,its protein Bcl-2 disappeared.Compared with control group,both two groups including E and G groups caused the apoptosis ratio significant higher.The alive cells' ratio in E group was reduced to the highest degree and the amount of dead cells increased to a degree of(4.00±0.56) %.Anti-apoptosis protein Bcl-2 in E,F,G groups all disappeared. Conclusion Combination DNR and ATRA simultaneously can effectively decrease HL-60 survival.Three ways of combination DNR with ATRA can signifi- cantly cause protein Bcl-2 disappear.But low dose of Ara-C was administrated first then followed by ATRA can not only increase slightly the ratio of apoptosis of HL-60 cell,but also inhibited anti-apoptosis protein Bcl-2 to express and effectively controled the way of HL-60 cell's death to apoptosis,and we concluded that this combination is the most potentiall way.
2010, 28(4): 265-266,270.
Abstract:
Objective To compare the difference of essential oil from Cortex Moutan extracted by different method. Methods Steam distillation and ethyl ehter ultrasonic were used to extract the essential oil from Cortex Moutan which were analyzed by GC-MS. Results The extraction rate of essential oil by steam distillation was 1.2%,and 17 compounds were identified.The extraction rate of essential oil by ethyl ehter ultrasonic was 2.5%,and 20 compounds were identified.There were 5 compounds were extracted by both method. Conclusion The essential oil extracted by two Methods have differences but common characteristics in some way.The ethyl ether ultrasonic had higher extraction rate with more chemical constituents.
Objective To compare the difference of essential oil from Cortex Moutan extracted by different method. Methods Steam distillation and ethyl ehter ultrasonic were used to extract the essential oil from Cortex Moutan which were analyzed by GC-MS. Results The extraction rate of essential oil by steam distillation was 1.2%,and 17 compounds were identified.The extraction rate of essential oil by ethyl ehter ultrasonic was 2.5%,and 20 compounds were identified.There were 5 compounds were extracted by both method. Conclusion The essential oil extracted by two Methods have differences but common characteristics in some way.The ethyl ether ultrasonic had higher extraction rate with more chemical constituents.
2010, 28(4): 267-270.
Abstract:
Objective To study the factors that influence the release of tacrolimus from the thermosensitive ophthalmic gel. Methods The non-membrane model was introduced to observe the influence on the drug release and gel erosion for surface area and shaking frequency. Results The drug release and gel erosion were increased with the rise of surface area and shaking frequency. Conclusion The drug release mainly depends on the gel erosion.
Objective To study the factors that influence the release of tacrolimus from the thermosensitive ophthalmic gel. Methods The non-membrane model was introduced to observe the influence on the drug release and gel erosion for surface area and shaking frequency. Results The drug release and gel erosion were increased with the rise of surface area and shaking frequency. Conclusion The drug release mainly depends on the gel erosion.
2010, 28(4): 271-273.
Abstract:
Objective To study the chemical constituents of Cirsium segestum. Methods Multi-chromatographic Methods including Silica gel column chromatography and Sephadex LH-20 gel permeation were employed for the isolation and purification.The structures were identified on the basis of chemical evidence and spectral data. Results Five compounds were isolated and identified as Caffeic acid(Ⅰ),Chlorogenic acid(Ⅱ),Baicalin(Ⅲ),stigmasterol 3-O-glucopyranoside(Ⅳ),5,8,4'-trihydroxy-7-O-β-D-glucopyranoside(Ⅴ). Conclusion compounds Ⅳ and Ⅴwere isolated from Cirsium segestum for the first time.
Objective To study the chemical constituents of Cirsium segestum. Methods Multi-chromatographic Methods including Silica gel column chromatography and Sephadex LH-20 gel permeation were employed for the isolation and purification.The structures were identified on the basis of chemical evidence and spectral data. Results Five compounds were isolated and identified as Caffeic acid(Ⅰ),Chlorogenic acid(Ⅱ),Baicalin(Ⅲ),stigmasterol 3-O-glucopyranoside(Ⅳ),5,8,4'-trihydroxy-7-O-β-D-glucopyranoside(Ⅴ). Conclusion compounds Ⅳ and Ⅴwere isolated from Cirsium segestum for the first time.
2010, 28(4): 274-278.
Abstract:
Objective To study the bioactive constituents of soft coral Sinularia sp. Methods The compounds were isolated and purified by silica gel,Sephadex LH-20 column chromatography and HPLC.Their chemical structures were identified by spectroscopic analysis. Results Seven sterol compounds were identified that are: ergos-7,24(28)-dien-3β,5α,6β-triol(1),(24R)-ergost-7,22-dien-3β,5α,6β-triol(2),ergost-24(28)-en-3β,5α,6β-triol(3),(24 S)-ergost-7(8)-en-3β,5α,6β-triol(4),23-demethylgorgost-7-en-3β,5α,6β-triol(5),ergosterol peroxide(6),cholesterol(7). Conclusion s All these compounds have the ergost-3β,5α,6β-tiol substructure segment except the common ergosterol peroxide and cholesterol.Preliminary bioactive experiment indicated that these compounds have the effect of antimicrobial activity.
Objective To study the bioactive constituents of soft coral Sinularia sp. Methods The compounds were isolated and purified by silica gel,Sephadex LH-20 column chromatography and HPLC.Their chemical structures were identified by spectroscopic analysis. Results Seven sterol compounds were identified that are: ergos-7,24(28)-dien-3β,5α,6β-triol(1),(24R)-ergost-7,22-dien-3β,5α,6β-triol(2),ergost-24(28)-en-3β,5α,6β-triol(3),(24 S)-ergost-7(8)-en-3β,5α,6β-triol(4),23-demethylgorgost-7-en-3β,5α,6β-triol(5),ergosterol peroxide(6),cholesterol(7). Conclusion s All these compounds have the ergost-3β,5α,6β-tiol substructure segment except the common ergosterol peroxide and cholesterol.Preliminary bioactive experiment indicated that these compounds have the effect of antimicrobial activity.
2010, 28(4): 279-282.
Abstract:
Objective To study the protective effects of Danshensu(Dan) on acute myocardial ischemia in rats. Methods Acute myocardial ischemia rats were induced by injection of Iso and Pit.The height changes of T wave in ECG were examined.The levels of LDH,CK in serum were measured. Results Dan(6、12、24 mg/kg) can significantly inhibit the height changes of T wave,obviously decrease the level of LDH,CK in the serum. Conclusion The Results indicate that Dan has protective effects on acute myocardial ischemia in rats.
Objective To study the protective effects of Danshensu(Dan) on acute myocardial ischemia in rats. Methods Acute myocardial ischemia rats were induced by injection of Iso and Pit.The height changes of T wave in ECG were examined.The levels of LDH,CK in serum were measured. Results Dan(6、12、24 mg/kg) can significantly inhibit the height changes of T wave,obviously decrease the level of LDH,CK in the serum. Conclusion The Results indicate that Dan has protective effects on acute myocardial ischemia in rats.
2010, 28(4): 283-287.
Abstract:
Objective To study the effect and mechanisms of timosaponin B-Ⅱ on depression. Methods The tail suspension test(TST),forced swimming test(FST),open field activity test(OFA),APO-induced synergistic action test,inhibiting reuptake of monoamine neurotransmitters and monoamine oxidase inhibitor(MAOI) test,yohimbine-induced lethality test and 5-HTP-induced head-twitch test were carried out to examine the antidepressant effect and mechanisms of timosaponin B-Ⅱ in rats.Immobility duration in FST and TST,spontaneous activity frequency in OFA,the stereotyped behaviors scores in APO-induced synergistic action test,and mortality in the other tests were observed. Results Timosaponin B-Ⅱ(100、150mg/kg) could effectively shorten the immobility time in TST and FST,but all dosages showed no significant effect on the spontaneous activity frequency in OFA.Timosaponin B-Ⅱ(150 mg/kg) significantly increased the rate of death of injecting dopamine,but had no obvious effect on the inhibiting reuptake of NE.Timosaponin B-Ⅱ(100、150 mg/kg) enhanced the apomorphine-induced stereotypy remarkably,which with statistically significant differences(P<0.05),and increased the head-twitch response evoked by 5-HTP,but had no effect on the yohimbine toxicity. Conclusion Timosaponin B-Ⅱhas significant antidepressant effect which may be related to the potentiation of brain 5-HT nerve system and DA nerve system.
Objective To study the effect and mechanisms of timosaponin B-Ⅱ on depression. Methods The tail suspension test(TST),forced swimming test(FST),open field activity test(OFA),APO-induced synergistic action test,inhibiting reuptake of monoamine neurotransmitters and monoamine oxidase inhibitor(MAOI) test,yohimbine-induced lethality test and 5-HTP-induced head-twitch test were carried out to examine the antidepressant effect and mechanisms of timosaponin B-Ⅱ in rats.Immobility duration in FST and TST,spontaneous activity frequency in OFA,the stereotyped behaviors scores in APO-induced synergistic action test,and mortality in the other tests were observed. Results Timosaponin B-Ⅱ(100、150mg/kg) could effectively shorten the immobility time in TST and FST,but all dosages showed no significant effect on the spontaneous activity frequency in OFA.Timosaponin B-Ⅱ(150 mg/kg) significantly increased the rate of death of injecting dopamine,but had no obvious effect on the inhibiting reuptake of NE.Timosaponin B-Ⅱ(100、150 mg/kg) enhanced the apomorphine-induced stereotypy remarkably,which with statistically significant differences(P<0.05),and increased the head-twitch response evoked by 5-HTP,but had no effect on the yohimbine toxicity. Conclusion Timosaponin B-Ⅱhas significant antidepressant effect which may be related to the potentiation of brain 5-HT nerve system and DA nerve system.
2010, 28(4): 288-290.
Abstract:
Objective To evaluate the efficacy and safety of 0.1% tacrolimus ointment in the treatment of chronic hand eczema in patients. Methods A total of 86 patients with chronic hand eczema applied 0.1%tacrolimus ointment or hydrocortisone butyrate cream twice daily for 4 weeks.Eficacy was evaluated by the use of a standardized hand score(JHS). Results The clinical efficacy rates of 0.1% tacrolimus and hydrocortisone butyrate group in patients were 83.7% and 46.5%,0.1% tacrolimus was significantly more effective than control group in patients with chronic hand eczema(P<0.05).The hand eczema score in 0.1% tarcrolimus ointment group declined significantly compared with control group.The common but temporary side effects in tarcrolimus ointment group included skin itching and burning on the application site. Conclusion s The Results show that 0.1% tacrolimus ointment in the treatment of chronic hand eczema in patients is effective and safe.
Objective To evaluate the efficacy and safety of 0.1% tacrolimus ointment in the treatment of chronic hand eczema in patients. Methods A total of 86 patients with chronic hand eczema applied 0.1%tacrolimus ointment or hydrocortisone butyrate cream twice daily for 4 weeks.Eficacy was evaluated by the use of a standardized hand score(JHS). Results The clinical efficacy rates of 0.1% tacrolimus and hydrocortisone butyrate group in patients were 83.7% and 46.5%,0.1% tacrolimus was significantly more effective than control group in patients with chronic hand eczema(P<0.05).The hand eczema score in 0.1% tarcrolimus ointment group declined significantly compared with control group.The common but temporary side effects in tarcrolimus ointment group included skin itching and burning on the application site. Conclusion s The Results show that 0.1% tacrolimus ointment in the treatment of chronic hand eczema in patients is effective and safe.
2010, 28(4): 291-292,307.
Abstract:
Objective To establish the method for the quantitative determination of total sugar and acidity in milk vetch honey. Methods Ultraviolet spectrophotometry was used to determine the content of total sugar in honey.Potentionmetric titration was used to analyze the total acidity in the honey. Results The total sugar in honey was 541 mg/g which showed a good linear relationship in the range of 26.2～131 μg(r=0.998).The average recovery was 102.1% and RSD was 2.79%.Potentiometric titration was used to control the response end point to avoid indicator errors when the total acidity was determinatd.The accuracy was improve and RSD was 0.92%～2.27%. Conclusion The method is simple,convenient and reliable which could be used for the quality control.
Objective To establish the method for the quantitative determination of total sugar and acidity in milk vetch honey. Methods Ultraviolet spectrophotometry was used to determine the content of total sugar in honey.Potentionmetric titration was used to analyze the total acidity in the honey. Results The total sugar in honey was 541 mg/g which showed a good linear relationship in the range of 26.2～131 μg(r=0.998).The average recovery was 102.1% and RSD was 2.79%.Potentiometric titration was used to control the response end point to avoid indicator errors when the total acidity was determinatd.The accuracy was improve and RSD was 0.92%～2.27%. Conclusion The method is simple,convenient and reliable which could be used for the quality control.
2010, 28(4): 293-295.
Abstract:
Objective To establish a method for determination of adenosine in capsule of Chinese Caterpillar Fungus. Methods HPLC was carried out with Agilent TC-C18(4.6 mm × 250 mm,5 μm);the Mobile phase was acetonitrile-0.01 mol/L potassium dihydrogen phosphate solution(892);the flow rate was 1.0 ml/min;the detection wavelength was 254 nm;the column temperature was 30 ℃;and content calculation was used external standard method. Results The concentration of adenosine in 0.402 4～60.36 μg/ml(r=1) had good linear relationship with peak area;the average recovery was 98.04%(n=6) with RSD of 0.63%. Conclusion This method is simple,reliable and can be used to quality control of adenosine in capsule of Chinese Caterpillar Fungus.
Objective To establish a method for determination of adenosine in capsule of Chinese Caterpillar Fungus. Methods HPLC was carried out with Agilent TC-C18(4.6 mm × 250 mm,5 μm);the Mobile phase was acetonitrile-0.01 mol/L potassium dihydrogen phosphate solution(892);the flow rate was 1.0 ml/min;the detection wavelength was 254 nm;the column temperature was 30 ℃;and content calculation was used external standard method. Results The concentration of adenosine in 0.402 4～60.36 μg/ml(r=1) had good linear relationship with peak area;the average recovery was 98.04%(n=6) with RSD of 0.63%. Conclusion This method is simple,reliable and can be used to quality control of adenosine in capsule of Chinese Caterpillar Fungus.
2010, 28(4): 296-298,312.
Abstract:
Objective Novel 3-substituted quinazolinon compounds were designed and synthesised on the base of the active site of human acrosin. Methods The compounds were designed by computer and chemically synthesised. Results Seven 3-substituted quinazolinon compounds were designed and synthesised,subsequently carried out in vitro anti-acrosin test. Conclusion The Results of anti-acrosin tese in vitro exhibited that all the compounds showed potent anti-acrosin activities.Particularly,compounds 3 g displayed much stronger anti-acrosin activities(229 times) than that of TLCK.
Objective Novel 3-substituted quinazolinon compounds were designed and synthesised on the base of the active site of human acrosin. Methods The compounds were designed by computer and chemically synthesised. Results Seven 3-substituted quinazolinon compounds were designed and synthesised,subsequently carried out in vitro anti-acrosin test. Conclusion The Results of anti-acrosin tese in vitro exhibited that all the compounds showed potent anti-acrosin activities.Particularly,compounds 3 g displayed much stronger anti-acrosin activities(229 times) than that of TLCK.
2010, 28(4): 299-303.
Abstract:
Objective To study of design and synthesis of the novel acyclic nucleoside phosphonates analogues and study their activities of inhibiting HBV. Methods Based on the chemical structure of PMEA,and according to the theory of bioisostere,a 8-aza-6-thiophenyl group was introduced and a series of title compounds were synthesized.All of them were confirmed by IR,1H-NMR and MS.Preliminary pharmacological test of compounds 1a-1e was made on HBV. Results Ten compounds were synthesized.The test Results show the inhibitory rate of 1a-1e compounds on HBsAg and HBeAg is higher than PMEA.The inhibitory rate of compound 1e on HBV-DNA is correspond with PMEA. Conclusion The PMEA derivatives with a 8-aza-6-thiophenyl group have high activity on inhibiting HBsAg,HBeAg and HBV-DNA.
Objective To study of design and synthesis of the novel acyclic nucleoside phosphonates analogues and study their activities of inhibiting HBV. Methods Based on the chemical structure of PMEA,and according to the theory of bioisostere,a 8-aza-6-thiophenyl group was introduced and a series of title compounds were synthesized.All of them were confirmed by IR,1H-NMR and MS.Preliminary pharmacological test of compounds 1a-1e was made on HBV. Results Ten compounds were synthesized.The test Results show the inhibitory rate of 1a-1e compounds on HBsAg and HBeAg is higher than PMEA.The inhibitory rate of compound 1e on HBV-DNA is correspond with PMEA. Conclusion The PMEA derivatives with a 8-aza-6-thiophenyl group have high activity on inhibiting HBsAg,HBeAg and HBV-DNA.
2010, 28(4): 304-307.
Abstract:
Objective To promote safe,effective,economical and proper medication by prescription comment. Methods From August 2007 to October 2008,100 outpatient prescriptions were spot-checked stochastically each month in our hospital which were statistically evaluated. Results The ratio of unqualified Outpatient prescriptions is 2.5%.The ratio of irrational prescriptions is 18%. Conclusion The pharmacists carry out prescription evaluation to monitor the clinical medication tightly,which can enhance the level of clinical medication,guarantee the clinical safety of medication.Through the prescription evaluation,the pharmacists would be encouraged to grasp the professional knowledge and improve the ability of judging unreasonable medication.
Objective To promote safe,effective,economical and proper medication by prescription comment. Methods From August 2007 to October 2008,100 outpatient prescriptions were spot-checked stochastically each month in our hospital which were statistically evaluated. Results The ratio of unqualified Outpatient prescriptions is 2.5%.The ratio of irrational prescriptions is 18%. Conclusion The pharmacists carry out prescription evaluation to monitor the clinical medication tightly,which can enhance the level of clinical medication,guarantee the clinical safety of medication.Through the prescription evaluation,the pharmacists would be encouraged to grasp the professional knowledge and improve the ability of judging unreasonable medication.
2010, 28(4): 313-315.
Abstract:
Objective To enhance the level of safe and rational use of drugs throgh investigating the adverse drug reactions(ADR) cases in our hospital in 2009. Methods 87 ADR cases in our hospital in 2009 were collected which were analyzed according to the patient's age and sex,drug species,route of administration and clinical manifestation etc. Results 51 drug species were involved in 87 ADR cases.54 cases(62.07%)were related to antibacterial agents;6 cases(6.90%) were related to the Chinese herba preparation.61cases(70.11%) were induced by intravenous infusion;the ADR cases of female were more than male with the proportion of 1:0.64;the ADR cases occurred in patients older than 65 years were more than in other age groups;and 57.47% of clinical manifested were skin lesions and accessories injuries. Conclusion The most ADR cases were caused by antibacterial agents through intravenous infusion,which should be taken seriously.
Objective To enhance the level of safe and rational use of drugs throgh investigating the adverse drug reactions(ADR) cases in our hospital in 2009. Methods 87 ADR cases in our hospital in 2009 were collected which were analyzed according to the patient's age and sex,drug species,route of administration and clinical manifestation etc. Results 51 drug species were involved in 87 ADR cases.54 cases(62.07%)were related to antibacterial agents;6 cases(6.90%) were related to the Chinese herba preparation.61cases(70.11%) were induced by intravenous infusion;the ADR cases of female were more than male with the proportion of 1:0.64;the ADR cases occurred in patients older than 65 years were more than in other age groups;and 57.47% of clinical manifested were skin lesions and accessories injuries. Conclusion The most ADR cases were caused by antibacterial agents through intravenous infusion,which should be taken seriously.
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