Herbal Textual Research on Forsythiae Fructus in Famous Classical Formulas / 中国实验方剂学杂志

In this paper， the name， origin， medicinal properties， specifications， clinical efficacy， producing area， quality evaluation and processing methods of Forsythiae Fructus in the famous classical formulas are researched by consulting related herbal literature， medical books and prescription books. The results showed that Forsythiae Fructus was sourced from Hypericum ascyron and its genus plants before Song dynasty， and it is used as medicine in many parts. After Song dynasty， Forsythiae Fructus is sourced from the fruit of Forsythia suspensa. Since the Ming dynasty， Forsythiae Fructus is divided into Qingqiao and Laoqiao according to different harvesting time. According to the research results， it is suggested to refer to the following suggestions for the application of Forsythiae Fructus in the development of famous classical formulas：①F. suspensa should be chosen as the origin since the Ming and Qing dynasties. ②If there is no special requirement for the source of prescriptions， it is recommended that Laoqiao be used in famous classical formulas since the Ming and Qing dynasties. ③The harvest time of Qingqiao should be from July 15th to August 15th， and Laoqiao should be in September， and it should be the husk after the seeds have been removed.

Study on residues of heavy metals and harmful elements in Qingqiao and Laoqiao based on chemometrics / 中国中药杂志

Forsythiae Fructus is divided into Qingqiao and Laoqiao due to different harvesting periods. So far, the accumulation of heavy metals in the two types of Forsythiae Fructus has not been reported. In this study, the residual levels of copper(Cu), lead(Pb), chromium(Cr), arsenic(As), cadmium(Cd) and mercury(Hg) in 29 batches of Laoqiao and 60 batches of Qingqiao were determined by inductively coupled plasma mass spectrometry(ICP-MS). The samples were collected from Shanxi, Shaanxi, Henan, and Hebei Provinces. In addition, the diversity and correlation of harmful elements in Qingqiao and Laoqiao were analyzed by multivariate statistical method. Furthermore, principal component analysis(PCA) was used to analyze the harmful elements concentrations of Qingqiao and Laoqiao. The results showed that there was a significant difference on the residual levels of heavy metals and harmful elements between Qingqiao and Laoqiao. Among them, the content of Pb in Laoqiao is significantly higher than that in Qingqiao(P<0.01), while the content of Cu is significantly lower than that in Qingqiao. However, the difference in harmful elements among different producing areas of Forsythiae Fructus is not significant. PCA analysis showed that Qingqiao and Laoqiao were successfully grouped into two categories. This study suggests significant difference in the residual levels of heavy metals and harmful elements between Qingqiao and Laoqiao. Besides, Forsythiae Fructus has a certain enrichment of Pb in the fruit ripening stage(Laoqiao). This study provides a reference for the quality classification and safety of Forsythiae Fructus.

Phenolic constituents from Wikstroemia chamaedaphne / 中国中药杂志

The phenolic constituents of Wikstroemia chamaedaphne were investigated by various column chromatographic methods including silica gel,Sephadex LH-20,ODS and preparative HPLC,and their chemical structures were identified by physico-chemical properties and spectral analyses. Thirteen phenolic compounds were isolated and elucidated,including five flavonoids: luteolin 7-O-β-D-glucopyranoside(1),luteolin 4'-O-β-D-glucopyranoside(2),kaempferol 3-O-β-D-glucopyranoside(3),chrysoeriol 4'-O-β-D-glucopyranoside(4),chrysoeriol(5); and eight lignans:(-)-secoisolariciresinol(6),acanthosessilin A(7),(-)-nortrachelogenin(8),(+)-isolariciresinol(9),sesamin(10),syringaresinol(11),(+)-epipinoresinol(12),and [3,3',4,4'-tetrahydro-6,6'-dimethoxy-3,3'-bi-2 H-benzopyran]-4,4'-diol(13). Compounds 1, 3, 5-8, 10, 11 and 13 were obtained from the plants of W. chamaedaphne for the first time,and compounds 1,5,7,10 and 13 were obtained from the Wikstroemia genus for the first time.

Biological activity and hydroxy safflor yellow A content of intermediates in preparation of Safflower Injection / 中国中药杂志

In order to investigate the effect of various production processes on the quality of Safflower Injection, the biological activities of the intermediates were evaluated by measuring activated partial thromboplastin time (APTT) and adenosine diphosphate (ADP) induced platelet aggregation in vitro. Intermediates were produced by key processes, such as extraction, concentration, twice alcohol precipitation, water sedimentation and two sterilizations during the production of Safflower Injection. The content of main chemical components in intermediates was determined by HPLC. The results showed that with the advance of the preparation process of Safflower Injection, the inhibition of ADP-induced platelet aggregation rate of each intermediate decreased gradually, and the trend of extending APTT activity decreased first and then increased. Meanwhile, the content of hydroxy safflor yellow A (HSYA) was gradually lowered, the content of p-hydroxy-cinnamic acid was increased, and new chemical component p-hydroxybenzaldehyde was produced. In conclusion, sterilization played a key role in the biological activity and HSYA content of Safflower injection.

Optimization of method for determination of Forsythia Fructus and discussion on the establishment of quality control standard for green (old) Forsythia Fructus / 中国中药杂志

In order to obtain the optimum method for content determination of Forsythia Fructus (FF), a variety methods for the sample preparation of FF were evaluated by the content determination methods of Chinese Pharmacopoeia. And an optimum method was screened and as follows: 30 times with 70% ethanol solution in ultrasonic extractor for half an hour. The method can achieve the best effect of simultaneously extracting forsythoside A and forsythin. Then, a HPLC method for simultaneous determination of forsythoside A and forsythin was established by methodology. The HPLC chromatographic conditions: the mobile phase consisted of acetonitrile (A)-0.4% acetic acid solution (B) with gradient elution [0-33 min，15%A，33-43 min，15%-25%A，43-60 min，25% A] was at the flow rate of 1 mL·min⁻¹, the column temperature was 25 °C, and the detection wavelength was 330 and 277 nm. Moreover, the contents of forsythoside A and forsythin for 10 Green Forsythia Fructus (GF) and 5 Old Forsythia Fructus (OF) were determined by this method and Chinese Pharmacopoeia. The result not only displayed that the established method is effective, rapid, and simple, but also showed that the contents of forsythoside A and forsythin for GF and OF were significantly different. Which implied that the forsythoside A and forsythin limit standard for GF and OF should be controled by different values. This studies provide an important basis for the establishment of the content determination of FF and the quality control standard for GF and OF.

Effects of sclerostin-single chain antibody fragment on the proliferation and osteogenic differentiation of bone marrow mesenchymal stem cells / 中国组织工程研究

BACKGROUND: Antagonism of bone sclerosis protein can stimulate osteogenesis and increase bone synthesis and metabolism through the Wnt/β-catenin signaling pathway. OBJECTIVE: To investigate the effects of sclerostin-single chain antibody fragment (Scl-scFv) on the proliferation and osteogenic differentiation of C57BL/6 mouse bone marrow mesenchymal stem cells (BMSCs). METHODS: BMSCs were isolated from C57BL/6 mice using whole bone marrow adherence method. Alizarin red staining was performed at the 14thday of osteogenic induction, and oil red O staining performed at the 7thday of adipogenic induction. Passage 3 BMSCs were cultured with α-MEM complete medium with (experimental) or without (control) 50 μg/L Scl-scFv aScl-scFv. Real-time PCR was used to detect type 1 collagen, alkaline phosphatase, RUNX2, osteopontin, osteocalcin at the 7thday of culture and meanwhile, alkaline phosphatase staining was done; western blot assay was used to detect expression of type 1 collagen and osteopontin proteins, and ELISA was used to detect the level of osteocalcin in the cell supernatant at 4, 7, 10 days of culture. RESULTS AND CONCLUSION: Formation of calcium nodules and orangered oil droplets was obviously visible in the BMSCs after osteogenic and adipogenic induction, respectively. Over time, the absorbance value showed no difference between the experimental and control group. Compared with the control group, the experimental group showed significant increases in mRNA and protein expression of type 1 collagen and osteopontin as well as in protein expression of alkaline phosphatase, RUNX2 and osteocalcin (P < 0.05). Moreover, stronger alkaline phosphatase staining was found in the experimental group relative to the control group. These findings indicate that Scl-scFv has no effect on BMSCs proliferation,but can promote the osteogenic capacity of BMSCs in vitro.

Sclerostin: a new hope for the treatment of osteoporosis / 中国组织工程研究

BACKGROUND:Sclerostin has been shown to promote bone formation and decrease bone resorption,which provides a new idea for the treatment of osteoporosis.OBJECTIVE:To review the literatures related to sclerostin and osteoporosis,thereby providing theoretical basis for sclerostin applied in the treatment and prevention of osteoporosis,so as to improve the diagnosis and curative efficacy of osteoporosis.METHODS:PubMed database was searched using the keywords of "osteoporosis,sclerostin,sclerosteosis,Wnt/β-catenin,LRP5/6,sclerostin antibody,sclerostin and expertise,romosozumab,blosozumab".Finally,58 pertinent articles were enrolled for analysis.RESULTS AND CONCLUSION:Sclerostin inhibits bone formation,so anti-sclerostin antibody is utilized,and animal experiments and clinical trials have shown that it can promote bone formation and inhibit bone reaorption.Phase Ⅲ trial results potentially signify a significant step in achieving market approval,which support the preclinical and clinical emergence of sclerostin antibody therapies for both osteoporosis and alternative applications.The serum level of sclerostin is found to be closely related to lifestyle,but still need to be studied in depth.Increasing trial results show that sclerostin is the promising therapeutic candidate,which provides a new direction in the prevention and treatment of osteoporosis.

Cycloartane triterpenoid and its glucoside isolated from Cassia occidentalis / 中国天然药物

In the present study, one new cycloartane triterpenoid, named cycloccidentalic acid C (1) and its glucoside, cycloccidentaliside VI (2) were isolated from the whole plant of Cassia occidentalis. Their structures were elucidated by a combinational analyses of 1D and 2D NMR data and HRMS. Compound 2 showed modest anti-HIV-1 activity with EC value of 1.44 μmol·L and TI (Therapeutic Index) value of 15.59.

Simultaneous determination of four coumaroylspermidine constituents in Carthamus tinctorius by HPLC-DAD / 中国中药杂志

The HPLC-DAD method was established to simultaneously determine the contents of four coumaroylspermidine[ N1, N5, N10-(Z)-tri-p-coumaroylspermidine (1), N1, N5-(Z)-N10-(E)-tri-p-coumaroylspermidine (2), N1(E)-N5-(Z)-N10-(E)-tri-p-coumaroylspermidine (3), and N1, N5, N10-(E)-tri-p-coumaroyl-spermidine (4) ] in Carthamus tinctorius. The method was performed on an Eclipse XDB-C18 column (4.6 mm×250 mm, 5 μm) eluted with 47% methanol in an isocratic program. The flow rate was 1 mL•min⁻¹; the injection volume was 10 μL, and the column temperature was 30 ℃. The detective wavelength was 270, 280, 290, and 300 nm, respectively. Four coumaroylspermidine constituents showed a good linearity in the range of 0.002 1-0.041 6 (r=0.999 5), 0.002 6-0.051 2 (r=0.999 7), 0.002 7-0.054 0 (r=0.999 8) g•L⁻¹, and 0.005 0-0.100 4 (r=0.999 8) g•L⁻¹, respectively. The average recoveries of these four coumaroylspermidine constituents were in the range of 98.61%-100.9% (RSD 2.3%-3.0%). In conclusion, the method is simple, rapid, and sensitive, which could be used as a quantitative determination method for the four coumaroylspermidine components in C.tinctorius.

A new Amaryllidaceae alkaloid from the bulbs of Lycoris radiata / 中国天然药物

AIM@#To study the Amaryllidaceae alkaloids of the bulbs of Lycoris radiata.@*METHODS@#The chemical constituents were isolated and purified by various chromatographic techniques, and the chemical structures were elucidated on the basis of spectroscopic methods. In addition, the antiviral activities of alkaloids 1-10 were evaluated using flu virus A.@*RESULTS@#One new homolycorine-type alkaloid 2α-methoxy-6-O-ethyloduline (1), together with nine known alkaloids 2α-methoxy-6-O-methyloduline (2), trispherine (3), 8-O-demethylhomolycorine (4), homolycorine (5), 9-O-demethylhomolycorine (6), oduline (7), lycorenine (8), 6α-O-methyllycorenine (9) and O-ethyllycorenine (10) were obtained.@*CONCLUSION@#Alkaloid 1 is a new compound, and 1-3 were major alkaloids in this plant. Alkaloids 1-3 showed weak antiviral activities against flu virus A with IC50 values of 2.06, 0.69, and 2.71 μg·mL-1 and CC50 values of 14.37, 4.79, and 80.12 μg·mL-1, respectively.