New di-spirocyclic labdane diterpenoids from the aerial parts of Leonurus japonicus / 中国天然药物

Phytochemical investigation on the ethanol extract of a well-known medicinal herb Leonurus japonicus, led to the separation of 18 labdane type diterpenoids (1-18). Through comprehensive spectroscopic analyses and quantum chemical calculations, these compounds were structurally characterized as six new interesting 5,5,5-di-spirocyclic ones (1-6), two new (7 and 8) and six known (13-18) interesting 6,5,5-di-spirocyclic ones, a new rare 14,15-dinor derivative (9), and three new ones incorporating a γ-lactone unit (10-12). An in vitro neuroprotective assay in RSC96 cells revealed that compounds 7 and 12 exhibited neuroprotective activity in a concentration-dependent way, comparable to the reference drug N-acetylcysteine.

Study on HPLC fingerprint of Leonurus japonicus granules and the contents of 4 index components / 中国药房

OBJECTIVE To establish HPLC finger print of Leonurus japonicus granules，and to determine the contents of 4 index components such as leonurine hydrochloride ，ferulic acid ，rutin，hyperoside. METHODS The determination was performed on Inertsil TM ODS-3 column with mobile phase consisted of acetonitrile （A）-0.1％ formic acid solution （B）in the form of gradient elution；the flow rate was 1.0 mL/min，the detection wavelength was 280 nm，the column temperature was 25 ℃，and the sample size was 5 µL. Similarity Evaluation System of Chromatogram Fingerprint of TCM （2012 edition）was used for establishing the HPLC fingerprints of 10 batches of L. japonicus granules and analyzing their similarities. By comparing with HPLC fingerprints of reference substance ，the common peaks were identified. SPSS 25.0 and SIMCA 13.0 software were used for cluster analysis and principal component analysis ；the above HPLC method was used for the content determination of 4 index components in L. japonicus granules such as leonurine hydrochloride ，ferulic acid ，rutin，hyperoside. RESULTS HPLC fingerprints of 10 batches of L. japonicus granules were established ，and 16 common peaks were matched ，and 4 peaks identified were leonurine hydrochloride （peak 6），ferulic acid （peak 13），rutin（peak 14），hyperoside（peak 16）；the similarities of 10 batches of samples were all higher than 0.970. The 10 batches of samples could be divided into four categories by cluster analysis and principal component analysis；the classification results were consistent. The contents of leonurine hydrochloride ，ferulic acid ，rutin and hyperoside were 122.10-138.82 μ g/g，9.33-10.45 μ g/g，14.12-18.95 μ g/g，5.87-8.06 μ g/g，respectively. CONCLUSIONS Established HPLC fingerprint of L. japonicus granules and the method for the content determination of 4 index components are simple and easy to operate，and have high precision and good repeatability ，which provide reference for the quality evaluation of L. japonicus granules.

Study on network pharmacology mechanism of Leonurus japonicus in treating dysmenorrhea caused by cold coagulation and blood stasis / 中草药

Objective: To establish a chemical constitution-disease target-metabolic signaling pathway network of Leonurus japonicus, and explore the mechanism of multi-component, multi-target and multi-pathway of L. japonicus for the treatment of dysmenorrhea caused by cold coagulation and blood stasis. Methods: TCMSP database and Swiss Target Prediction server were used to obtain the chemical components and action targets of L. japonicus. Combined with DrugBank, DisGeNET, TTD and other databases, the action targets of L. japonicus for treating dysmenorrhea symptoms wtih cold coagulation and blood stasis were obtained. Through DAVID's website, GO function enrichment analysis and KEGG pathway analysis were conducted on the targets, and cytoscape 3.6.0 was used to construct the network diagram of the active component-dysmenorrhea target-metabolic signaling pathway of L. japonicus, to explore the mechanism of action of L. japonicus in treating dysmenorrhea with cold coagulation and blood stasis. Furthermore, Western blotting experiments were conducted to verify the effect of L. japonicus on the expression of PTGS1 and PTGS2 proteins in the uterine tissues of the model rats with cold coagulation and blood stasis dysmenorrhea. Results: Eight potential active ingredients of L. japonicus were obtained, including 22 dysmenorrhea related disease targets, main targets PTGS1, PTGS2, ALOX5, PLAG2A, AKR1C3, etc. A total of 71 GO items were obtained by GO functional enrichment analysis (P < 0.05), including 46 biological process (BP) items, four cell component (CC) items, and 21 molecular function (MF) items. There were 22 possible targets for the treatment of dysmenorrhea, and seven signaling pathways were obtained through KEGG pathway enrichment and screening (P < 0.05), involving arachidonic acid metabolism, linoleic acid metabolism, steroid hormone biosynthesis, etc. L. japonicus significantly increased the protein expression levels of PTGS1 and PTGS2 in the uterus of the model rats (P < 0.05), which confirmed some of the predicted results of network pharmacology. Conclusion: L. japonicus may treat dysmenorrhea with cold coagulation and blood stasis by acting on arachidonic acid metabolism pathway.

Evaluation on content difference of multi-index components between Yao medicine Young Leonurus heterophyllus and Leonurus japonicus / 中草药

Objective: To study the content difference of multi-index components between Yao medicine Young Leonurus heterophyllus (YLH) and Leonurus japonicus, and evaluate the quality with the content. Methods: A high performance liquid chromatography (HPLC) method was established for the simultaneous content determination of five chemical constituents of chlorogenic acid, leonurine hydrochloride, rutin, hyperin and isoquercitrin in Yao medicine YLH and Leonurus japonicus. SPSS 25.0 statistical software was used to conduct paired samples t-test and one-way ANOVA to infer the content differences among the samples. Principal component analysis (PCA) was used to evaluate the quality of medicinal materials. Results: T-test results of paired samples of Yao medicine YLH and Leonurus japonicus showed that there was significant difference in rutin content among the five chemical constituents, with no significant difference in other constituents. The results of one-way ANOVA analysis showed that there were significant differences in five chemical constituents of Yao medicine YLH and Leonurus japonicus from different habitats (P < 0.01). The results of principal component analysis showed that the higher scores of Leonurus japonicus from different habitats were from Nanning and Yulin, with the lowest in Shangsi County. Conclusion: There is a significant difference between the content of Yao medicine YLH and Leonurus japonicus. The quality of medicinal materials from Nanning and Yulin is better. The results provide data support for the comparison of the content between two kinds of Leonurus heterophyllus and Leonurus japonicus from different habitats.

Pharmacological effects of the active ingredient genkwanin in Leonurus on coagulation and anti-inflammation in mice / 西安交通大学学报(医学版)

Objective: To investigate the pharmacological effects of genkwanin, the active ingredient in Leonurus on coagulation and anti-inflammation in mice. Methods: The body torsion pain caused by acetic acid model, auricle swelling induced by xylene, and the blood capillary permeability model were used to investigate the analgesic and anti-inflammatory effects of genkwanin in mice. Results: The clotting time was significantly reduced in medium- and high-dose genkwanin groups compared with the control group (P0.05) in the low-dose genkwanin group, a significant reduce of A value (P<0.05) in the medium-dose group, and an extremely significant decrease of A value (P<0.01) in the high-dose group. Conclusion: Genkwanin can promote blood coagulation function of mice, and reduce the times of their body torsion pain caused by acetic acid, showing obvious analgesic effects. Furthermore, genkwanin can inhibit auricle swelling of mice induced by xylene and reduce the blood capillary permeability of their abdominal cavity, suggesting its mild anti-inflammatory effects. The findings can provide clinical evidence for treating dysmenorrheal and endometritis.

Mechanism of Tripterygium hypoglaucum Radix-Leonurus japonicus Herba for Treating Rheumatoid Arthritis Based on Network Pharmacology / 中国实验方剂学杂志

Objective:Computer network pharmacology technology was used to screen the main active ingredients of Tripterygium hypoglaucum radix-Leonurus japonicus herba for the treatment of rheumatoid arthritis(RA), predict the targets of the active ingredients, establish a pharmaceutical ingredient-active ingredient-target network, and further explore the potential mechanism of Tripterygium hypoglaucum radix-Leonurus japonicus herba for the treatment of RA. Method:RA disease targets were collected through DisGeNET, TTD, and Drugbank databases, the potential active components of Tripterygium hypoglaucum radix and Leonurus japonicus herba and their corresponding targets were obtained from the Chinese Medicine System Pharmacology Analysis Platform (TCMSP); common targets for drugs and diseases were screened by using the ImageGP platform; a common target interaction (PPI) network model was constructed by using the String database, a "drug-active ingredient-key target" network was constructed by using Cytoscape software, a protein interaction network was constructed by using the String database, gene function (GO) analysis and pathway enrichment analysis based on the Kyoto Gene and Genomic Encyclopedia (KEGG) were performed by using the ClueGO plug-in. Result:Through screening, 9 active pharmaceutical ingredients were obtained, involving a total of 235 targets, and 7 active ingredients were related to the disease targets. 24 common targets for Tripterygium hypoglaucum radix Leonurus japonicus herba-disease were obtained. The common targets were mainly enriched in 278 biological processes and 141 signaling pathways to play a role in the treatment of RA. Conclusion:The therapeutic effect of Tripterygium hypoglaucum radix Leonurus japonicus herba on RA reflects the characteristics of multi-component-multi-target-multi-channel of traditional Chinese medicine, and provides a scientific basis for explaining its mechanism and clinical application of RA.

Multi-center clinical study of motherwort injection for retained fetal membrane after vaginal delivery / 中国实用妇科与产科杂志

OBJECTIVE: To evaluate the efficacy and safety of motherwort(herba leonuri)injection in the treatment of fetal membrane retention after vaginal delivery.METHODS: The prospective study was designed as a multicenter,open,randomized,controlled research from December 2017 to October 2018.A total of 244 women who achieved fullterm vaginal delivery were enrolled from 7 tertiary hospitals in China.Sixteen people were lost to follow-up(7 in the experimental group and 9 in the control group).All cases were randomly divided into group of motherwort(experimental group)and group of basic treatment(control group).Full Analysis Set(FAS)and Per ProtocolSet(PPS)were used for statistical analysis.The results of main validity indicators were the same.Therefore,only the results of PPS set analysis were reported in detail.PPS set included 109 cases in control group and 114 cases in experimental group.Control group were administered by oxytocin 20 U and cephalosporinⅡintravenous injection daily for3 days after birth;experimental group were administered by motherwort 20 mg intramuscular injection per 12 hours for 5 consecutive days on the basis of basic treatment.Both groups of patients were given oral herb medicine Chan-fu-kang or Chan-fu-an Granules after discharge for 7 consecutive days.The following clinical parameters were collected and analyzed for evaluation of the efficacy and safety of motherwort injection in the treatment of retained fetal membrane after vaginal delivery.The main effectiveness indicators were maternal lochia,uterine volume change,and discharge of retained fetal membrane;the secondary effectiveness indicators were the maternal infection-related factors and infections,the incidence of secondary postpartum hemorrhage,postpartum body temperature changes,and the use of other hemostatic drugs.Safety indicators were laboratory tests(blood routine,electrocardiogram),adverse reactions/events,which were used to evaluate the safety and efficacy of motherwort injection in the treatment of retained fetal membrane after vaginal delivery.RESULTS:(1)Lochia:the duration of bloody lochia was significantly shorter in the experiment group than in the control group([(5.12±1.83)d]vs.(6.27±2.07)d,P=0.000);rate of termination of bloody lochia within 5 days was significantly higher in the experiment group than in the control group(64.91% vs. 35.78%,P=0.000).(2)Comparison of uterine volume:the reduction of uterus volume in the experiment group was significantly greater than that in the control group(Z=-2.27,P8.0 mg/L or PCT>0.5 ng/L was defined as infection,the infection rate of the experiment group after 5 days of treatment was significantly lower than that of the control group(P0.05).No other hemostatic drugs were used in the two groups,and no secondary postpartum hemorrhage occurred.(6)There were no adverse reactions reported in both groups,and no abnormal blood routine indicators or electrocardiogram appeared.CONCLUSION: The application of motherwort injection combined with the basic treatment after the vaginal delivery can significantly shorten the duration of bloody lochia,promote uterine involution,increase the discharge rate of retained fetal membrane,and reduce the rate of uterine curettage.

Fingerprint analysis and multi-component determination of Leonurus japonicus by high performance liquid chromatography / 药学学报

An HPLC fingerprint and multi-component determination method of Leonurus japonicus was established for comprehensive evaluation and quality control of Leonurus japonicus. The sample was incubated in 70% ethanol in a water bath for 2 h, and the extract was analyzed by HPLC using Kromasil C18 column (250 mm×4.6 mm, 5 μm). The mobile phase consisted of acetonitrile-0.1% formic acid with gradient elution. The flow rate was 1.0 mL·min-1. The temperature of column was 30 ℃. The detection wavelength was 280 nm. HPLC fingerprint of characteristic components of Leonurus japonicus was established. There were 12 common peaks among 25 batches of samples, and 5 of them were identified and determined. Syringic acid, leonurine hydrochloride, rutin, hyperoside or isoquercitrin showed a good linearity in the ranges of 0.426 1-85.22 ng (r = 0.999 9), 7.948-1 590 ng (r = 0.999 3), 10.20-2 040 ng (r = 1.000 0), 2.018-403.6 ng (r = 0.999 9), or 8.704-1 741 ng (r = 0.999 9), respectively. The average recoveries were 99.0%, 97.6%, 97.4%, 96.9% and 98.5% with RSD of 1.1%, 1.8%, 1.4%, 1.5% and 1.3%, respectively. The HPLC characteristic fingerprint of Leonurus japonicus was specific, and this method can simultaneously determine the content of 5 components.

Quality assessment of crude and processed Leonuri Fructus by chemical and color analysis combined with chemometric method / 中草药·英文版

Objective: Crude Leonuri Fructus (CLF), the fruits of the Leonurus japonicus Houtt, and processed Leonuri Fructus (PLF) by stir-baking as the important Chinese herbal medicines, have been used in China and other Asian countries for thousands of years. The objective of this research is to reveal the difference between CLF and PLF. Methods: The sensory technologies of the colorimetry, sensitive and validated HPLC-ELSD and GC combined with flame ionization detector (GC-FID) were employed to discriminate CLF and its processed product PLF. The color parameters of the samples were determined by colorimetric instrument CR-410. Moreover, the content of stachydrine and six fatty acids were determined by HPLC and GC. Subsequently, analysis of variance (ANOVA), principal components analysis (PCA), hierarchical cluster analysis (HCA), and Kendall's correlation test were performed for data analysis. Results: The CLF and PLF were divided into two categories by PCA and HCA in terms of their component content and color. The results distinctly demonstrated significant changes in color and the content of indicative components between CLF and PLF. Conclusion: The study revealed that HPLC, GC, and colorimetric method in combination with chemometric method could be used as comprehensive quality evaluation for CLF and PLF.

Clinical Observation of Leonurus artemisia Injection Combined with Carboprost Tromethamine for Prevent-ing Postpartum Hemorrhage after Cesarean Section / 中国药房

OBJECTIVE:To observe therapeutic efficacy and safety of Leonurus artemisia injection combined with carboprost tromethamine for preventing postpartum hemorrhage (PPH) of pregnant women after cesarean section. METHODS:177 pregnant women undergoing cesarean section were randomly divided into control group(87 cases)and observation group(90 cases). Preg-nant women of both groups received cesarean section. Control group was given intramuscular injection of oxytocin 20 U in uterine muscle wall above the incision after the foetus parturition,and given intravenous dripping of oxytocin 20 U added into 0.9% sodi-um chloride 250 mL;4 h after the operation,the pregnant women received intramuscular injection of oxytocin 10 U,every 12 hours,for 3 days. Observation group was given intramuscular injection of L. artemisia injection 2 mL and Carboprost tromethamine injection 1 mL in uterine incision after the foetus parturition;4 h after the operation,the pregnant women received intramuscular in-jection of L. artemisia injection 2 mL and Carboprost tromethamine injection 1 mL,and then give L. artemisia injectien 2 mL,ev-ery 12 hours,for 3 days. Clinical efficacies of 2 groups were observed as well as blood loss during operation,2 h after operation and 24 h after operation,the amount of hemoglobin(Hb)before operation and 24 h after operation,height of uterine fundus 3,7 d after operation,the occurrence of ADR. RESULTS:The total response rate of observation group was significantly higher than that of control group;blood loss during operation,2 h after operation and 24 h after operation,height of uterine fundus 3,7 d af-ter operation were also significantly than control group,with statistical significance(P0.05). 24 h after operation,Hb of pregnant women in control group was significantly lower than before operation and observation group,with statistical significance(P0.05). There was no statisti-cal significance in the incidence of ADR between 2 groups(P>0.05). CONCLUSIONS:L. artemisia injection combined with car-boprost tromethamine shows significant therapeutic efficacy for PPH of pregnant women underwent cesarean section,can signifi-cantly reduce intraoperative and postoperative blood loss,accelerates the recovery of uterus without increasing the rate of ADR.

Effects of Compound Leonurus artemisia Ointment Combined with Drospirenone and Ethinylestradiol Tablets on Serum Progesterone and Th1/Th2 Cytokine after Medical Abortion / 中国药房

OBJECTIVE:To investigate the effects of Compound Leonurus artemisia ointment combined with Drospirenone and ethinylestradiol tablets on serum progesterone and T helper (Th) 1/Th2 cytokine after medical abortion.METHODS:A total of 228 patients underwent medical abortion selected from obstetrical outpatient of our hospital during our hospital during Mar.2013 to Jul.2015 as research object were divided into control group (109 cases) and observation group (119 cases) according to random number table.Control group was given Cefuroxime axetil tablets 0.25 g,po,bid,for consecutive 6 d for anti-infective treatment+ Drospirenone and ethinylestradiol tablets one tablet,po,qd,21 d as a treatment course,8 d later receiving second course,3 courses in total after fetal sac exclusion.Observation group was additionally given Compound L.artemisia ointment 10 g,po,bid,7 d as a treatment course,2 courses in total on the basis of control group.The levels of serum progesterone and Th1 (TNF-α,IFN-γ,IL-2)/Th2 cytokine (IL-4,IL-6,IL-10) were observed in 2 groups,and the occurrence of ADR was recorded.RESULTS:Before treatment,there was no statistical significance in serum progesterone or Th1/Th2 cytokine levels between 2 groups (P＞0.05).After treatment,serum progesterone,TNF-α,IL-2 and IL-6 levels of 2 groups were decreased significantly,and above indexes of observation group were significantly lower than those of control group.The levels of IL-4 and IL-10 in 2 groups were increased significantly,and above indexes of observation group were significantly higher than control group,with statistical significance (P＜0.05).After treatment,IFN-γ levels of 2 groups were decreased significantly,but there was no statistical significance between 2 groups (P＞0.05).No obvious ADR was found in 2 groups during treatment.CONCLUSIONS:Compound L.artemisia ointment combined with Drospirenone and ethinylestradiol tablets can regulate immune function of patients after medical abortion,and promote dynamic balance of Th1/Th2 cytokines with good safety.

Anti-acetylcholinesterase activity of the aglycones of phenolic glycosides isolated from Leonurus japonicus

Objective: To find the genuine structure with anti-acetylcholinesterase(anti-AChE)from the phenolic glycosides abundant in Leonurus japonicus(Lamiaceae).The assay for anti-AChE activity is often used to lead anti-Alzheimer's drugs. Methods: The five phenolic glycosides, tiliroside, leonurusoside C, 2'''-syringoylrutin, rutin, and lavanduliofolioside were isolated from L. japonicus. The activities of the glycosides were relatively low. Seven compounds including p-coumaric acid, caffeic acid, hydroxytyrosol, salidroside, syringic acid, kaempferol, and quercetin, which are produced by the hydrolysis of the five glycosides, were also assayed for anti-AChE activity. Results: Of those seven compounds, the five compounds other than salidroside and syringic acid exhibited potent anti-AChE activities.In particular,the IC50s of caffeic acid and quercetin were (1.05 ± 0.19)and (3.58 ± 0.02)μg/mL, respectively. Rutin was the most abundant flavonoid in the extract(9.18 mg/g as measured by HPLC). Conclusion: The substances with potent anti-AChE were caffeic acid, quercetin, p-coumaric acid, kaempferol, and hydroxytyrosol that can be produced from their glycosides.

New diterpenoids isolated from Leonurus japonicus and their acetylcholinesterase inhibitory activity / 中国天然药物

Three new labdane diterpenoids, leojaponicone A (1), isoleojaponicone A (2) and methylisoleojaponicone A (3), were isolated from the herb of Leonurus japonicus. The chemical structures of these secondary metabolites were elucidated on the basis of 1D and 2D NMR, including HMQC, and HMBC spectroscopic techniques. All the new compounds were tested in vitro for their acetylcholinesterase and α-glucosidase inhibitory activity. Compounds 1-3 exhibited low inhibitory effects on α-glucosidase with respect to acarbose and exhibited high inhibitory effects on acetylcholinesterase with respect to huperzine A.

Chemical constituents from aerial parts of Leonurus macranthus / 中草药

Objective: To investigate the chemical constituents from the aerial parts of Leonurus macranthus. Methods: The chemical constituents were separated and purified by silica gel, Sephadex LH-20, ODS column chromatographies, and semi-preparative HPLC. Their structures were determined by physicochemical properties and spectroscopic data. Results: Nineteen compounds were isolated from the CH2Cl2 layer of 70% aqueous acetone extract in the aerial parts of L. macranthus, and identified as (+)-syringaresinol (1), (+)-1-hydroxysyringaresinol (2), rayalinol (3), erythro-guaiacylglycerol-β-O-4'-coniferyl ether (4), (7R, 7'R, 7″S, 8S, 8'S, 8″S)-3', 4″- dihydroxy-3, 5, 4', 5″-tetramethoxy-7, 9': 7', 9-diepoxy-4, 8″-oxy-8, 8'-sesquineo-lignan-7″, 9″-diol (5), (7R, 7'R, 7″S, 8S, 8'S, 8″S)-4', 5″- dihydroxy-3, 5, 3', 4″-tetramethoxy-7, 9': 7', 9-diepoxy-4, 8″-oxy-8, 8'-sesquineo-lignan-7″, 9″-diol (6), genkwanin (7), 3'-hydroxy- genkwanin (8), eriodictyol (9), isoscopoletin (10), p-coumaric acid (11), caffeic acid methyl ester (12), trans-ferulic acid (13), syringic aldehyde (14), vanillic acid (15), oct-1-en-3-yl β-glucopyranoside (16), 5-hydroxy-2-pyrrolidone (17), pterolactam (18), and nicotinamide (19), respectively. Conclusion: Compounds 1-6 and 9-19 are isolated from the plants of genus Leonurus Linn. for the first time, and compounds 7 and 8 are found from L. macranthus for the first time.

Isolation and preparation of leonurine from Leonurus japonicus by high speed countercurrent chromatography / 中草药

Objective: To establish a simple and effective method for the isolation of leonurine from Leonurus japonicus by high speed countercurrent chromatography (HSCCC). Methods: The extraction conditions of leonurine were optimized by one-factor experimental design. After comparing several different solvent systems, the two phase system of ethyl acetate-n-butanol-water (3∶2∶5) was finally chosen as operating solvent of HSCCC for the separation of leonurine, in which the lower phase was determined as the mobile phase and the upper phase as stationary. The detection of eluates was performed with an ultraviolet detector at 277 nm. The rotation speed was adjusted at 850 r/min, and the flow rate was 2.2 mL/min. Results: Leonurine was successively isolated from n-butanol fraction by HSCCC, and the above established method was also successively applied to the crude extact of L. japonicus. Finally, 68 mg of leonurine with purity about 96.2% could be obtained from 2.48 g crude extract of L. japonicus in a single injection. Conclusion: The described approaches actively promote efficient preparation strategy to obtain high purity of leonurine.

Anti-acetylcholinesterase activity of the aglycones of phenolic glycosides isolated from Leonurus japonicus

Objective To find the genuine structure with anti-acetylcholinesterase (anti-AChE) from the phenolic glycosides abundant in Leonurus japonicus (Lamiaceae). The assay for anti-AChE activity is often used to lead anti-Alzheimer's drugs. Methods The five phenolic glycosides, tiliroside, leonurusoside C, 2‴-syringoylrutin, rutin, and lavanduliofolioside were isolated from L. japonicus. The activities of the glycosides were relatively low. Seven compounds including p-coumaric acid, caffeic acid, hydroxytyrosol, salidroside, syringic acid, kaempferol, and quercetin, which are produced by the hydrolysis of the five glycosides, were also assayed for anti-AChE activity. Results Of those seven compounds, the five compounds other than salidroside and syringic acid exhibited potent anti-AChE activities. In particular, the IC

Optimize concentrate process of alkaloid from Leonurus japonicus by ultrafultration-nanofiltration coupling technology / 中国中药杂志

To optimize the concentrate process of alkaloid from Leonurus japonicus by nanofiltration-ultrafiltration coupling technology with response surface methodology. The experiment showed that after ultrafiltration pre-treatment, the total protein removal rate was 94.38% in aqueous extract from L. japonicus, and the nanofiltration technology had obvious advantages over the conventional concentrate process. The optimal concentrate conditions were as follows：molecular weight cut-off 450, pH 3.07, concentration of stachydrine hydrochloride 80.15 mg•L⁻¹, and concentration of the total alkaloid 285.73 mg•L⁻¹. The cut-off rate was 93.37% and 95.85% respectively for stachydrine hydrochloride and the total alkaloid under the optimum conditions, with a relative error of 0.79% and 1.16% respectively. The combination of Box-Behnken design and response surface analysis can well optimize the concentrate process of L. japonicus by nanofiltration, and the results provide the basis for nanofiltration concentrate for heat-sensitive traditional Chinese medicine.

Effect of fluidized bed technology on micromeritics properties of Leonurus Herba extract / 中国中药杂志

Based on different binders, the Leonurus Herba extract powders were fluidized and modified. The physical properties such as hygroscopicity, flowability, filling property and compression property were studied by various micromeritics methods before and after modification. The results showed that the physical properties of Leonurus Herba extract were close to those of microcrystalline cellulose, and its comprehensive flow index was between 61-75. Fluidization process can improve hygroscopicity, so the moisture absorption indexes of the samples were significantly lower than those of the original Leonurus Herba extract samples. With the plastic constant, compression ratio and yield stress, Heckel equation and Kawakita equation as the the investigation indicators, results showed that fluidization process based on binder water was superior to other methods in increasing the compressibility of the extracts. In low and medium pressure, the fluidized and modified extract can form the tablets with a certain strength. Fluidized transformation had a greater influence on the properties of original Leonurus Herba extracts, which was instructive to guide significance for the surface modification of pharmaceutical powders and provide the basis for the development of extract tablet.

Research on Evaluation of Different Germplasm ofLeonurus japonicus / 中国中医药信息杂志

Objective To study the difference ofLeonurus japonicus germplasm resources and provide good materials for breeding.Methods Totally 20 wildLeonurus japonicus germplasm resources from different places of China were collected. Experiment was conducted in homogeneous garden in Quzhou City of Zhejiang Province. Phenological phase, cold endurance and habitat adaptability were observed; the plant height, fresh weight and dry weight in early flowering were measured; the contents of stachydrine hydrochloride and leonurine hydrochloride were determined in early flowering and out-of-season cultivation.Results Considering the habitat adaptability, dry plant weight in early flowering, the contents of stachydrine hydrochloride and leonurine hydrochloride separately in early flowering and out-of-season cultivation, it was believed that the germplasms from Linbao County, Sheqi County in Henan Province and Guidong County in Hunan Province were better, in which Linbao germplasm was the best: the dry plant weight was 30.6 g, the content of stachydrine hydrochloride and leonurine hydrochloride were 1.31% and 0.19% respectively in early flowering, and were 3.44% and 0.37% respectively under anti-season cultivation, and it can be well adapted in Zhejiang Province.Conclusion The germplasm ofLeonurus japonicas from Lingbao can be the best materials for breeding.

Clinical Observation of the Leonurus artemisia Cream versus Dan’e Fukang Cream in the Treatment of Pri-mary Dysmenorrhea / 中国药房

OBJECTIVE:To compare the efficacy and safety of Leonurus artemisia cream and Dan’e fukang cream in the treat-ment of primary dysmenorrhea. METHODS:80 patients with primary dysmenorrheal were randomly divided into L. artemisia cream group (40 cases) and Dan’e fukang cream group (40 cases). L. artemisia cream group received L. artemisia cream 10 g, orally,twice a day. Dan’e fukang cream group received Dan’e fukang cream 10 g,orally,twice a day. The treatment was stated before 10 days of menstruation. 10 days was regarded as 1 treatment course,and it lasted for 6 courses. Cold drink and food were forbid during medication,washing face and feet with warm water,soaking feet with hot water if they can,paying attention to keep the lower abdomen and legs warm. If patients felt unbearable pain in menstruation,0.3 g Ibuprofen sustained release capsule was given,orally twice a day. Clinical efficacy,symptom score(dysmenorrhea degree,abdominal pain,lumbosacral pain)before and af-ter treatment,dysmenorrhea duration,frequency of taking painkillers and the incidence of adverse reactions in 2 groups were ob-served. RESULTS:There were no significant differences in the total effective rate and the incidence of adverse reactions in 2 groups (P>0.05). Before treatment,there were no significant differences in dysmenorrhea degree,abdominal pain,lumbosacral pain score,dysmenorrheal duration and frequency of taking painkillers in 2 groups (P>0.05). After treatment,the dysmenorrhea degree,abdominal pain,lumbosacral pain score in 2 groups were significantly lower than before,and Dan’e fukang cream group was lower than L. artemisia cream group with statistical sighificance(P0.05). CONCLUSIONS:Both L. artemisia cream and Dan’e fukang cream have good efficacy and safety in the treat-ment of primary dysmenorrhea,while Dan’e fukang cream is superior to L. artemisia cream in terms of improving clinical symp-toms.