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ObjectiveTo investigate the effect of Shengjiang Tonglong prescription hollow suppository on rats with prostate hyperplasia， and the effect of the proteins related to phosphoinositide 3-kinase/protein kinase B （PI3K/Akt） signaling pathway in the prostate， thus exploring the mechanism of Shengjiang Tonglong prescription hollow suppository in the treatment of rats with prostate hyperplasia. MethodTen SD male rats were randomly selected from 60 SD male rats to form a sham operation control group， and the rest rats were subcutaneously injected with testosterone propionate for 4 consecutive weeks after castration to induce the rat model of prostatic hyperplasia. According to the random number table method， the 50 rats were randomly divided into a model group， a finasteride group （0.45 mg·kg-1）， and three high， middle， and low-dose Shengjiang Tonglong prescription hollow suppository groups （3.98， 1.99， 0.99 g·kg-1）， with ten rats in each group. After castration for 7 d， the sham operation control group and the model group used the blank hollow suppositories， and the finasteride group and the Shengjiang Tonglong prescription hollow suppository groups used the corresponding hollow suppositories. The drugs were given to the rats by anal plugs continuously for 28 d. The rats were then killed， and the prostate tissues were separated and weighed to observe the effects of drugs on the prostate index of rats in each group. The hematoxylin-eosin （HE） staining was used for the pathological observation of the prostate tissues. The level of dihydrotestosterone （DHT） was detected by enzyme-linked immunosorbent assay （ELISA）. Western blot was used to detect the expression levels of PI3K/Akt signaling pathway protein， B-cell lymphoma-2 （Bcl-2）， cysteine aspartate-specific protease-3 （Caspase-3）， Bcl-2-associated X protein （Bax）， and αB-crystallin （CRYAB） protein in the prostate tissues. ResultAs compared with the sham operation control group， the protein expression levels of prostate index， DHT level， CRYAB， Bcl-2， PI3K， and Akt in the model group were increased， and the protein expression levels of Caspase-3 and Bax were decreased （P<0.05， P<0.01）. As compared with the model group， the prostate index in the high-dose Shengjiang Tonglong prescription hollow suppository group was decreased （P<0.05）， and the level of DHT and the protein expression levels of CRYAB， Bcl-2， PI3K， and Akt in the prostate of the Shengjiang Tonglong prescription hollow suppository groups were decreased， and the protein expression levels of Caspase-3 and Bax were increased （P<0.05， P<0.01）. ConclusionShengjiang Tonglong prescription hollow suppository decreases the expression of CRYAB protein， negatively regulates the PI3K/Akt signaling pathway， down-regulates the level of DHT and the protein expression levels of Bcl-2， PI3K， and Akt， and up-regulates the protein expression levels of Caspase-3 and Bax， thereby inhibiting cell proliferation and promoting cell apoptosis， which plays a therapeutic role in the benign prostate hyperplasia （BPH）. The high-dose Shengjiang Tonglong prescription hollow suppository significantly improves prostatic hyperplasia in rats.
ABSTRACT
ObjectiveTo investigate the effect of Shengjiang Tonglong prescription hollow suppository on rats with prostate hyperplasia， and the effect of the proteins related to phosphoinositide 3-kinase/protein kinase B （PI3K/Akt） signaling pathway in the prostate， thus exploring the mechanism of Shengjiang Tonglong prescription hollow suppository in the treatment of rats with prostate hyperplasia. MethodTen SD male rats were randomly selected from 60 SD male rats to form a sham operation control group， and the rest rats were subcutaneously injected with testosterone propionate for 4 consecutive weeks after castration to induce the rat model of prostatic hyperplasia. According to the random number table method， the 50 rats were randomly divided into a model group， a finasteride group （0.45 mg·kg-1）， and three high， middle， and low-dose Shengjiang Tonglong prescription hollow suppository groups （3.98， 1.99， 0.99 g·kg-1）， with ten rats in each group. After castration for 7 d， the sham operation control group and the model group used the blank hollow suppositories， and the finasteride group and the Shengjiang Tonglong prescription hollow suppository groups used the corresponding hollow suppositories. The drugs were given to the rats by anal plugs continuously for 28 d. The rats were then killed， and the prostate tissues were separated and weighed to observe the effects of drugs on the prostate index of rats in each group. The hematoxylin-eosin （HE） staining was used for the pathological observation of the prostate tissues. The level of dihydrotestosterone （DHT） was detected by enzyme-linked immunosorbent assay （ELISA）. Western blot was used to detect the expression levels of PI3K/Akt signaling pathway protein， B-cell lymphoma-2 （Bcl-2）， cysteine aspartate-specific protease-3 （Caspase-3）， Bcl-2-associated X protein （Bax）， and αB-crystallin （CRYAB） protein in the prostate tissues. ResultAs compared with the sham operation control group， the protein expression levels of prostate index， DHT level， CRYAB， Bcl-2， PI3K， and Akt in the model group were increased， and the protein expression levels of Caspase-3 and Bax were decreased （P<0.05， P<0.01）. As compared with the model group， the prostate index in the high-dose Shengjiang Tonglong prescription hollow suppository group was decreased （P<0.05）， and the level of DHT and the protein expression levels of CRYAB， Bcl-2， PI3K， and Akt in the prostate of the Shengjiang Tonglong prescription hollow suppository groups were decreased， and the protein expression levels of Caspase-3 and Bax were increased （P<0.05， P<0.01）. ConclusionShengjiang Tonglong prescription hollow suppository decreases the expression of CRYAB protein， negatively regulates the PI3K/Akt signaling pathway， down-regulates the level of DHT and the protein expression levels of Bcl-2， PI3K， and Akt， and up-regulates the protein expression levels of Caspase-3 and Bax， thereby inhibiting cell proliferation and promoting cell apoptosis， which plays a therapeutic role in the benign prostate hyperplasia （BPH）. The high-dose Shengjiang Tonglong prescription hollow suppository significantly improves prostatic hyperplasia in rats.
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OBJECTIVE:To prepare Potassium dehydroandrographolide succinate(PDS)hollow suppository and establish a method for its quality control.METHODS:The PDS hollow suppository was prepared with semisynthesis fatty acid glyceride as ground substances and PEG300 or 1,2 propylene glycol as disperse medium.The content of PDS was determined by ultraviolet spectrophotometry at a detection wavelength of 251nm.RESULTS:The linear concentration range of PDS was 6.0～50.0?g?mL-1(r=0.999 9,n=5).The two kinds of PDS hollow suppository were all up to the quality standard.CONCLUSION:This method is reasonable in design and feasible in technology.
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OBJECTIVE:To prepare penciclovir hollow suppository and establish its quality control method.METHODS:Penciclovir hollow suppository was prepared by heat-melting method.The content of penciclovir was determined by HPLC and the stability of the suppository was investigated as well.RESULTS:The preparation was ivory yellow hollow suppository and its property fitted the description of Chinese Pharmacopeia(2005 edition).The linear range of penciclovir was 5.00～100.00 ?g?mL-1(r=0.999 7),and its average recovery was 98.69%(RSD=0.81%).No obvious change was noted for the property of the suppository within 1 year storage under temperature away from light.CONCLUSION:The preparation technique of the penciclovir hollow suppository is simple and feasible,its quality control method is rapid in operation and its determination result is accurate and reliable.
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OBJECTIVE: To prepare diclofenac sodium hollow suppository and establish its quality control. METHODS: The hollow type suppository was prepared with mixed fatty glyceride as the base; the content of diclofenac sodium was deter-mined by ultraviolet spectrophotometry. RESULTS: The linear range of diclofenac sodium was 5～25 ?g?mL-1(r=0.999 7),with an average recovery rate of 102.04%(RSD=1.08%). CONCLUSION: The preparation technology of diclofenac sodium hollow suppository is simple and feasible,and the quality of the suppository is stable and controllable.
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OBJECTIVE:To prepare ofloxacin hollow suppository(OHS) and to observe its in vitro dissolubility.METHODS:OHS was prepared with PEG 6000,PEG 400 and Carbopol-940 as wase material and wax as retardant.The content of ofloxacin in OHS was determined with the first order derivative UV-spectrophotometry.RESULTS:The wax,as a retardant,could retard the release of drug.The in vitro dissolution of OHS revealed the first order dissolution pattern:K0～1=27.81/h,indicating a speedy effect,K2～6=5.94/h,indicating sustained-release effect.CONCLUSION:This preparation is feasible in technology and controllabe in quality.The preparation of OHS extends the kinds of dose-form of ofloxacin
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OBJECTIVE:To prepare and establish quality control for the compo und metronidazole hollow suppository.METHODS:The compound metronidazole hollow suppository was prepared with semisynthesis fatty acid glyceride as ground substance;The contents of metronidazole and ofloxacin were determined by dual-wave length K-ratio method and equivalent absorption dual-wave length method.RESULTS:The detecting concentration linear range of metronidazole and ofloxacin were6.0～18.0?g/ml and3.0～9.0?g/ml respectively,the average recovery were100.98%and99.56%(n=5)respectively,RSD were0.82%?0.80%respectively.CONCLUSION:This method is convenient,accurate and reproducible,which can be used for the quality control of compound metronidazole suppository.
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Objective To observe the effect of Zhipu Hollow Suppository (ZHS) on postoperative ankylenteron in rats,and to investigate the possible mechanism.Methods Forty Wistar rats were randomly divided into model group,ZPS group,positive control group,and blank control group,10 rats in each group.Rats were given corresponding drugs according to the experimental design after modeling.Rats were executed after medication for one week,and the pathologic changes of ileal serosa were observed under scanning electron microscope and the ultrastructure of ileal serosa cells was observed under transmission electron microscope.Results Results of the examination under scanning electron microscope showed that the arrangement of ileal-serosa mesothelial cells in ZHS group was regular,and the network structure arranged spindle-shaped with uniformity size and with the shape close to the normal ones.There was proliferation in mesothelial cells in the exposed base layer.Under the transmission electron microscope,mesothelial cells recovered well and the proliferation of fibroblasts was not obviously in ZHS group,but mesothelial cells disappeared and the secretion of collagen by fibroblasts was actively in the model group.Conclusion ZHS can prevent ankylenteron by promoting the ileal-serosa mesothelial cell proliferation,improving the ileal-serosa ultrastructure and protecting the ileal serosa.