ABSTRACT
OBJEC TIVE To establish the qu ality standard of Hylocereus undatus ，and to provide reference for its quality control. METHODS The sample of H. undatus medicinal materials was collected for character observation ，powder microscopic identification and thin-layer chromatography （TLC）identification. Moisture content ，total ash ，acid-insoluble ash ，water-soluble extracts and alcohol-soluble extracts were determined according to the corresponding methods in the general provisions of the 2020 edition of Chinese Pharmacopoeia （part Ⅳ）. The contents of kaempferol and isorhamnetin in H. undatus were determined by high performance liquid chromatography. RESULTS The medicinal materials of H. undatus were in brown or yellowish brown irregular long bundles ；the calyx tubes were twisted in bundles ；the scales on the outside of the flower were shrunken ，and many stamens were inserted on the inside. The powder was brown-green or brown-yellow ，and pollen grains ，ducts and non-glandular hairs were found.In the TLC diagram of test sample ，fluorescent spots of the same color were displayed on the corresponding position of the chromatogram of substance control （kaempferol， isorhamnetin） and reference material. The moisture content ， total ash ， acid-insoluble ash ，water-soluble extract and alcohol-soluble extract of the 15 batches of samples ranged from 10.70％ to 12.23％， 7.48％ to 11.29％，0.25％ to 0.70％，30.34％ to 49.91％，and 25.27％ to 36.92％，respectively. The average values were 11.44％，9.51％，0.46％，40.13％，32.33％，respectively. The contents of kaempferol and isorhamnetin were 1.787-3.785 and 0.597-2.211 mg/g，respectively. CONCLUSIONS This study add microscopic identification ，TLC identification and inspection items such as moisture content ，ash and extract on the basis of the existing quality standards of H. undatus . It is preliminarily proposed that the moisture content in H. undatus shall not exceed 13.0％ and total ash content shall not exceed 12.0％，and the water-soluble extract and alcohol-soluble extract shall not be less than 30.0％ and 25.0％ respectively；the contents of kaempferol and isorhamnetin shall not be less than 1.780 and 0.590 mg/g，respectively. The established quality standard can be used for quality control of H. undatus .
ABSTRACT
Rosmarinic acid (RA) is a natural polyphenolic compound that exists in many medicinal species of Boraginaceae and Lamiaceae. The previous studies have revealed that RA had therapeutic effects on hepatocellular carcinoma (HCC) in the H22-xenograft models by inhibiting the inflammatory cytokines and NF-κB p65 pathway in the tumor microenvironment. However, its molecular mechanisms of immunoregulation and pro-apoptotic effect in HCC have not been fully explored. In the present study, RA at 75, 150, and 300 mg/kg was given to H22 tumor-bearing mice via gavage once a day for 10 days. The results showed that RA can effectively inhibit the tumor growth through regulating the ratio of CD4⁺/CD8⁺ and the secretion of interleukin (IL)-2 and interferon-γ, inhibiting the expressions of IL-6, IL-10 and signal transducer and activator of transcription 3, thereby up-regulating Bax and Caspase-3 and down-regulating Bcl-2. The underlying mechanisms involved regulation of immune response and induction of HCC cell apoptosis. These results may provide a more comprehensive perspective to clarify the anti-tumor mechanism of RA in HCC.
Subject(s)
Animals , Mice , Apoptosis , Boraginaceae , Carcinoma, Hepatocellular , Caspase 3 , Cytokines , Interleukin-10 , Interleukin-6 , Interleukins , Lamiaceae , STAT3 Transcription Factor , Therapeutic Uses , Tumor MicroenvironmentABSTRACT
OBJECTIVE： To study the anti-gout effect of aqueous extract from the stems and leaves of Erythropalum scandens （ASLE）. METHODS： The mice were randomly divided into normal group， model group， allopurinol group （positive control， 5 mg/kg）， ASLE low-dose， medium-dose and high-dose groups （1 300， 2 600， 5 200 mg/kg， by raw material； similarity hereinafter）， with 10 mice in each group. Except for normal group， other groups were given potassium oxonate intragastrically to induce hyperuricemia model. One hour after modeling， normal group and model group were given constant volume of normal saline intragastrically； administration group was given relevant medicine intragastrically， once a day， for consecutive 7 d. One hour after last administration， the levels of serum uric acid （SUA） and serum creatinine （Scr） were detected by colorimetry assay. Another mice were randomly divided into normal group， model group， indomethacin group （positive control， 7.5 mg/kg）， ASLE low-dose， medium-dose and high-dose groups， with 10 mice in each group. Normal group and model group were given constant volume of normal saline intragastrically； administration group was given relevant medicine intragastrically， once a day， for consecutive 7 d. After last administration， except for normal group， the mice were given sodium microcrystalline urate via toes to induce gouty arthritis model. Before and 1， 2， 4， 6， 8 h after modeling， the circumference of the same part of the inflamed limbs and toes of mice in each group was measured by wire binding method， and the degree of toe swelling was calculated. The number of white blood cell （WBC）， neutrophil （NEU） and lymphocyte （LYM） were detected by animal hematology analyzer. The levels of SUA and Scr were measured by colorimetry assay. The content of NO in toe tissue was determined by Griess method. RESULTS： The experimental results of hyperuricemia model showed that the levels of SUA and Scr in mice were significantly higher in model group than those in normal group （P＜0.01）. Compared with model group， above indexes of mice were decreased significantly in administration group （P＜0.05 or P＜0.01）. The experimental results of gouty arthritis model showed that the level of SUA， the degree of toe swelling （2-8 h）， the number of WBC， NEU and LYM， NO content in model group were increased significantly， compared with normal group （P＜0.05 or P＜0.01）. Compared with model group， the levels of SUA and Scr （ASLE groups）， the degree of toe swelling [indomethacin group， ASLE high-dose group （2-8 h）， ASLE low-dose group （2， 6 h）， ASLE medium-dose group （6 h）]， the number of WBC and NEU （administration groups）， the number of LYM （indomethacin group） and NO content （administration groups except for ASLE low-dose group） were decreased significantly in administration groups （P＜0.05 or P＜0.01）. CONCLUSIONS： The anti-gout effect of ASLE may be associated with promoting uric acid metabolism， anti-inflammatory and improving renal function.
ABSTRACT
The aim of this study was to synthesize 1-(5-(hydroxymethyl)-4-methyl-3-oxo-3,4-dihydro-pyrazin-2-yl) guanidine (mucunaguanide),a pyrazinone alkaloid compound extracted from the seed of Stizotobium cochinchinensis.Starting from benzyloxy acetaldehyde,following four steps in reaction including condensation,cyclization,substitution and hydrogenation reaction,mucunaguanide was synthesized with total yield of 27.9％,and purity of more than 97.5％.Structures of all the intermediates and target compound were confirmed by IR,1H NMR and MS.This synthetic process was characterized with raw materials available,simple in operation with much milder reaction conditions,and was an ideal method of synthesis of this compound.
ABSTRACT
Objective To analyze the chemical constituents of kumquat essential oil(KEO)and the acute toxicity of KEO in mice. Methods The chemical constituents of KEO were analyzed by GC-MS. After preliminary test,KM mice were randomly divided into control and KEO groups with 20 mice in each group(10 male and 10 female). The doses of KEO were designed with ratio 0.758 be?tween the 100%and 0%mortality amount as 10,7.60,5.70,4.40,3.30 and 2.50 ml/kg. The acute toxicity was evaluated by examina?tion of the mice for 14 days after single administration of KEO. Results The principal constituents in KEO wereα-pinene(0.46%),β-phellandrene(0.11%),β-myrcene(2.34%),D-limonene(95.62%),geranyl acetate(0.10%),β-copaene(0.67%),andγ-elemene (0.13%),which accounted for 99.43%of the total chemical content of KEO. The half-lethal dose(LD50)of KEO in mice by the acute toxicity test was 6.24 ml/kg with the 95%confidence limit of(5.39-7.33)ml/kg in female mice and 5.73 ml/kg with the 95%confi?dence limit of(4.91-6.79)ml/kg in male mice. The possible toxic target organs were liver,spleen and gastrointestinal tract. Conclu?sion KEO with the content of D-limonene was obtained from kumquat for the first time,and the toxicity of the KEO was low accord?ing to the toxicity classification standard of World Health Organization.
ABSTRACT
Aim To observe the effects of the L-dopa methyl ester (LDME) on the pattern visual evoked potentials (P-VEP) and the expression of c-fos mRNA in neurons of the visual cortex of kittens with strabismic amblyopia, and explore the therapeutic effect of L-dopa methyl ester on amblyopia and its action mechanism.Methods 30 normal kittens were randomly divided into 6 groups: low dose of L-dopa methyl ester (20 mg·kg~(-1)), medium dose of L-dopa methyl ester (40 mg·kg~(-1)), and high dose of L-dopa methyl ester (80 mg·kg~(-1)),positive control (L-dopa 40 mg·kg~(-1)),normal control, and model control group.The surgery for producing iatrogenic convergent strabismus was performed on 4 weeks old kittens(normal control group excluded). After the confirmation of the development of amblyopia by pattern visual evoked potential,L-dopa methyl ester,L-dopa and normal saline were given to the corresponding animals, respectively. The P-VEP of amblyopia eyes was observed after one month, and the technique of in situ hybridization was used to detect the expression of c-fos mRNA.Results L-dopa methyl ester could reduce obviously the length of P100 peak latency of the cat strabismic amblyopes, and increase the amplitude of P100. The positive staining cells of strabismic cat visual cortex were less than those of normal cats, whose difference was significant (P<0.01).Positive staining cells in the treatment group were significantly increased when compared with that of the model group (P<0.01).Conclusion L-dopa methyl ester can significantly improve the conduction and sensory function in the model of strabismic amblyopia cats. The mechanism may be related to the increased amount of L-dopa methyl ester into the cerebral cortex and regulation of the expression of c-fos mRNA.
ABSTRACT
OBJECTIVE:To optimize the extraction technique for Sidiming capsules.METHODS:The technical conditions for the water decoction and the alcohol precipitation were optimized respectively by the orthogonal experiment design L9(34)with hydrosoluble extract used as the index for the water decoction and the catalpol extract for alcohol precipitation.The content of Catalpol was determined by HPLC.RESULTS:The optimum conditions were as follows:decocting the crude drugs twice with 8-fold water,1 h each time.The physic liquor extracted by water was filtered,mixed and concentrated to 1.0 g?mL-1(crude drug),and then precipitated by 75% concentration of alcohol for 24 h.Then the physic liquor was filtered,concentrated and dried by microwave vacuum concentration dryer to obtain the dry ointment.CONCLUSION:The optimum extraction procedure is stable and reliable,and it can be used as the optimal extraction procedure of Sidiming capsules.
ABSTRACT
OBJECTIVE: To study the inhibitory effects of traditional chinese medicine Compound Liuyuexue (CLYX) on hepatitis B surface antigen(DHBsAg) and hepatitis B e-antigen(DHBeAg).METHODS: One-day old guangxi brown spotted ducks infected with DHBV were used as the hepatitis B virus infected animal model. Positive ducks were detected by PCR at 13 days after the infection of DHBV, and were randomly divided into five groups: the high dose group, middle dose group and low dose group of Compound Liuyuexue(CLYX), model group, and positive control group, with 10 ducks in each group. CLYX was given ig.for 14 days. Serum sampling was scheduled at 0, 7, 14 days respectively and 3 days after drug withdrawal, and the contents of DHBsAg and DHBeAg in serum were measured by ELISA. RESULTS: The serum DHBsAg and DHBeAg contents in high dose and middle dose groups of CLYX were decreased significantly(P
ABSTRACT
OBJECTIVE:To evaluate the bioequivalence of domestic secnidazole tablet,capsule and imported secnidazole tablet in healthy volunteers.METHODS:18healthy volunteers were randomly divided into3groups according to a triple-cross design,all the volunteers were given a single dose of1g secnidazole,the interval for washout period of3times adminis?tration was14days.The plasma drug concentration of secnidazole was determined by HPLC-UV.RESULTS:The main pharmacokinetic parameters of homemade tablet and homemade capsule and imported tablet were as follow,t max were(2.00?1.93),(2.67?2.14)and(1.54?1.53)h respectively,t 1/2 were(28.56?4.98)、(29.69?6.81)and(27.16?5.06)h,C max were(25.50?2.74),(24.27?3.76)and(25.64?4.10)?g/ml respectively.AUC 0～t were(736.03?73.20),(704.78?88.51)and(737.77?76.02)(?g?h)/ml respcetively.AUC 0～∞ were(886.36?114.50),(864.57?172.27)and(870.64?100.21)(?g?h)/ml respectively.The relative bioavailability of homemade tablet was(100.02?6.73)%,and that of homemade capsule was(95.91?10.66)%.CONCLUSION:3preparations of secnidazole are bioequivalent.
ABSTRACT
Aim To observe the protective effects of two flavone morphons on hypoxia/reoxygenation(H/R) injury in myocardial cells and explore the mechanisms.Methods The hypoxia/reoxygenation injury model of cultured neonatal rat cardiomyocytes was developed. The cell morphology,the spontaneous beating,the survival rate,the content of LDH,NOS,T-SOD,MDA and the activity of Na+,K+-ATP,Ca2+,Mg2+-ATP enzyme were determined in the cultured neonatal rat cardiomyocytes injuried by H/R.Results Compared with the model,preconditioning by two flavone morphons enhanced the spontaneous beating and the survival rate. Meanwhile,it increased the activity of T-SOD,Na+,K+-ATP,Ca2+,Mg2+-ATP enzyme and decreased the release of LDH,NOS,MDA(P
ABSTRACT
OBJECTIVE:To study the scavenging action of Longyanshen on O2 ?- and ? OH.METHODS:Spectrophotometry (wavelength 322nm and 536nm)was used to detect the effects of Longyanshen upon O2 ?- and?OHRESULTS:Longyanshen in concentration of 30g/ml could reduce the level of?OH by 284%,and Longyanshen in concentrations of 15g/ml,30g/ml and 60g/ml could decrease the levels of O2 ?- by 441%,630% and 479% and inhibit the generation of O2 ?- by 489%,589%and 675% in vitro,respectivelyCONCLUSION:The results show that Longyanshen could scavenge and inhibit O2 ?- markedly(P
ABSTRACT
OBJECTIVE:To study the effects of LYS polysaccharides on learning & memory and monoamine neurotrans-mitter content in SAMP8 brain.METHODS:50 6-month-old SAMP8 mice were randomized to 5 groups(10 in each group):SAMP8 group,huperzine A control group,low-,mid-and high-dose groups of polysaccharides.Another 10 6-month-old SAMR1 mice were assigned to normal control group.After medication for 40 days,the learning and memory abilities of mice in each group were detected with Morris water maze method.The norepinephrine(NE),dopamine(DA) and 5-HT contents in brain were determined by HPLC.RESULTS:The learning and memory abilities of SAMP8 group decreased significantly,and the NE,DA and 5-HT contents in brain decreased significantly compared with normal group(P
ABSTRACT
OBJECTIVE:To study the protective effects and mechanisms of Longyanshen on chemical liver injury in mice.METHODS:The models of CCl 4 ,TAA and acetaminophen induced acute liver injury in mice were used to study the pro?tective effects of Longyanshen,and relevant parameters were detected and compared.RESULTS:Compared with model group,in Longyanshen group,activity of ALT markedly decreased,the contents of hepatic cyt P 450 ,cyt b 5 increased,the content of MDA in liver tissue significantly decreased,the activities of aniline hydroxylase and aminopurine-N-demethylase increased,the activity of Ca 2+ -ATPase in hepatic cell microsome markedly decreased and the activities of GSH-PX and the content of GSH increased.CONCLUSION:Longyanshen has protective effect on chemical liver injury in mice and the mechanisms may be related to the antioxidative action,inhibiting effect on lipid peroxidation,inducing the activities of hepatic microsomal enzymes and blocking the calcium channel.
ABSTRACT
AIM:To study the isolation and composition of Cliffbean(Millettia pulchra kurz)polysaccharide.METHODS:Cliffbean was extracted by boiling water.The polysaccharide in the filtrate was precipitated fractionally by alcohol.The protein in the product was removed by Sevag method,and was further purified by DEAE ion-exchange cellulose(DEAE-52).The component of the saccharide was determined by GC and TLC.RESULTS:The polysaccharide obtained in this way didn't contain protein and nucleic acid.It showed a single polysaccharide when identified by means of Sephadex G-75 column or High Performance Gel Permeation Chromatography(HPGPC).It was composed of glucose and arabinose.CONCLUSION:Cliffbean polysaccharide was first isolated from its root and was one of the important components.
ABSTRACT
AIM:To study the inhibitory effect of Compound Liuyuexue(Tarphochlamys affinis(Giff) Bremekhu,Herba Hedyotis,Raidx Gardeniae,etc.)(CLYX) on HBV in vitro.METHODS:The serum containing CLYX was added to cultured HepG2.2.15 cells,and HepG2.2.15 cells were cultured in medium containing the serum with CLYX for 72 h and 144 h.The culture media were collected for determining the levels of HBsAg and HBeAg by ELISA.RESULTS:The serum containing CLYX could markedly inhibit HBsAg and HBeAg expressions in the HepG2.2.15 cells(P
ABSTRACT
OBJECTIVE:To establish a method for the assaying of total flavonoids in the extracts of Gynostemma and to provide basis for the study of its internal quality.METHOD:The contents of total flavonoids in6kinds of Gynostemma made from Guangxi were determined by UV-spectrophotometry with a detection wavelength at510nm.RESULTS:Good linear re-lationship with absorbability occurred when the concentration range of rutin was0.0092～0.0553mg/ml(r=0.9999,n=6)and its average recovery was100.8%(RSD=2.25%,n=6).CONCLUSION:The method is simple and accurate,of the testing samples,Gynostemma from Guangxi ranked the first in terms of the content of total flavonoids.
ABSTRACT
OBJECTIVE:To optimize the conditions of the extraction technique for compound Liuyuexue gran?ules.METHODS:The herbs in formulation were first extracted by ethanol percolating,then the dregs were decocted with water to be extracted once more.Taking oleanolic acid and total flavones as evaluation markers,the extraction technique in two-step process was evaluated by orthogonal design.RESULTS:The optimum condition of ethanol percolating process was that the crude herb powder was soaked by8-fold80%ethanol for24hours and the optimum condition of water decocting process was that the dregs were decocted for3times with12-fold water,1.5hour each time.CONCLUSION:The repeated experimental results are stable,and the contents of components for markers are high.The optimum conditions can be used for enlarged pro?duction.
ABSTRACT
OBJECTIVE:To observe the effect of extract of longyanshen(EL)on immunodepression induced by cyclophosphamide in mice.METHODS:The immunodepression was induced by cyclophosphamide,the the different oral doses of EL were given to mice for 30 days,and control group took NS.RESULTS:The different doses of EL could significantly increase the killing function of neutrophil(P
ABSTRACT
Aim To observe the effects of LYS polysaccharides on expressions of APP, PS1, PS2 and ApoE in SAMP8 mouse brain. Methods 50 6-month-old SAMP8 mice were used and divided randomly into 5 groups: SAMP8 untreated control group, huperzine A control group, low-, mid-and high-dose groups of polysaccharides, with 10 mice in each group. 10 6-month-old SAMR1 mice were used as normal control. After each group was treated by corresponding drug for 40 days continuously, the mRNA contents of APP, PS1, PS2 and ApoE in brain tissue were assayed by reverse transcription polymerase chain reaction.Results The low-, mid-and high-dose groups of polysaccharides could reduce the mRNA contents of APP, PS1 and PS2, which showed a dose-effect relationship in some degrees. But it could not affect the content of ApoE. Conclusion LYS polysaccharides could inhibit the expressions of APP, PS1, and PS2 in SAMP8 mouse brain.