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Objective: To screen inhibitors targeting SARS-CoV-2 S protein-ACE2 interaction by molecular docking. Methods: Candidate natural products were collected from Selleck China natural product library (Catalog No. L1400, 2 054 natural products). The structure of SARS-CoV-2 S protein-ACE2 had been determined by Qiang Zhou team (PDB: 6M17). The molecular docking was performed by Discovery Studio. Results: Based on the virtual amino acid mutation experiment which determined the key amino acids, the binding cavity was created. Then, 11 compounds were screened out from the natural compound library: digitonin, Lonicera grisea saponin A, forsythiaside B, L. grisea saponin B, Dipsacus asperges saponin B, hederacoside D, platycodon D, echinacoside, ginsenoside Rb2, ginsenoside Rc, and chlorogenic acid C. Conclusion: The 11 potential inhibitors targeting SARS-CoV-2 S protein-ACE2 interaction were screened out from natural products library, which provides a reference for the research of new anti SARS-CoV-2 drugs.
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Objective: To compare the antidiarrheal effects of Mongolian medicine, Holarrhena antidysenterica, Forsythia suspensa and Cynanchum thesioides on diarrhea model rats and investigate its effects on serum DAO (diamine oxidase), cAMP (cyclic adenosine phosphate), TNF-α (tumor necrosis factor-α), ATPase and calcium ions. Methods: The normal control group, model group, H. antidysenterica low-dose and high-dose groups, F. suspensa low dose and high-dose groups, C. thesioides low dose and high dose groups were set. Except the normal control group, the other groups were ig administrated water decoction of Cassia angustifolia to establish diarrhea model; After the success of the model, the rats in treatment groups were administrated by gastric drug for 7 d, the type mental state, diarrhea and body weight changes were observed. the abdominal aortic blood was obtained at the last day of fasting 12 h after the administration. DAO, cAMP, TNF-α, ATP enzyme, OD value of the calcium ions in serum were determined by using ELISA (enzyme-linked immune detection reagent) kits. Results: General status: except for the normal group, the mental state of the rats in the other groups was depressed after modeling, the fur color of them was significantly decreased and the body weight was decreased. The diarrhea rate was 100% on the 4th day after modeling. Compared with the model group, there were significant differences in the number of loose stools, grade of loose stools and diarrhea index (P < 0.05, 0.01) in each administration group. The serum DAO, TNF-α, ATPase, cAMP and calcium ion OD values were compared: the serum concentrations of DAO in H. antidysenterica low dose group, C. thesioides low dose group and F. suspensa high and low dose groups of rats were significantly lower than model group with significant differences (P < 0.05), and were significantly higher than normal group. The serum concentration of TNF-α in C. thesioides high and low dose groups were lower compared with model group (P < 0.05). The serum ATPase in C. thesioides high and low dose groups had significant difference (P < 0.05) compared with model group. The serum concentration of cAMP in H. antidysenterica high-dose group and F. suspensa low-dose group was significantly lower compared with model group with significant differences (P < 0.05). Serum Ca2+ concentration in the drug administration groups was significantly different from that in the model group (P < 0.05). Conclusion: The antidiarrheal effect of C. thesioides is better than that of H. antidysenterica and F. suspensa.
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Objective: To investigate the genetic diversity of Forsythia suspensa from different populations. Methods: ISSR markers were used to analyze the genetic diversity of 25 populations of F. suspensa. Percentage of species level polymorphic bands (P), Nei’s genetic diversity index (H), and Shannon’s information index (I) of genetic information were calculated by POPGEN 32. UPGMA relationship dendrogram was clustered by NTSYS. Results: Thirteen primers produced 353 bands and P was 100%. H and I were 0.252 3 and 0.394 0, and genetic differentiation coefficient (Gst) and gene flow (Nm) were 0.331 8 and 1.007 0 within the population levels. The genetic distance varied from 0.031 0 to 0.155 5. NTSYSpc software was used to cluster the system. A total of 25 clusters were divided into two categories and seven groups. Cluster analysis was conducted among Forsythia individuals. A total of 195 samples were divided into two categories and five groups. Conclusion: The genetic diversity among the populations of F. suspensa is at higher level. However, the genetic distance among the Forsythia population is not related to the geographical distance, which is mainly dependent on the ecological factors and the growth environment.
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Objective To study the chemical constituents from the fruits of Forsythia suspensa. Methods Compounds were isolated by a combination of various chromatographic techniques including column chromatography over macroporous resin, Sephadex LH-20 and reversed-phase HPLC. Their structures were elucidated by physiochemical properties and spectral analysis. Results Two new compounds from the 50% ethanol extract of F. suspensa were isolated and identified as (2R,3S)-3-(4-hydroxy-3-methoxyphenyl) - 3-methoxypropane-1,2-diol (1) and 2-methylhexane-1,2,3,6-tetraol (2). Conclusion Compound 1 is a new epimer of a known phenylpropanoid named (2R,3S)-forsythiayanoside D, and compound 2 is a new compound named rengyquaol.
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Objective: To study the chemical constituents from the fruits of Forsythia suspensa. Methods: Compounds were isolated by a combination of various chromatographic techniques including column chromatography over macroporous resin, Sephadex LH-20, and reversed-phase HPLC. Their structures were elucidated by physiochemical property and spectral analysis. Results: Thirteen compounds were isolated and identified as salidroside (1), forsythoside E (2), quinolacetic acid (3), rengyolone (4), senecio lactone (5), cleroindicin C (6), 4-hydroxy-4-isopropylcyclohex-1-enecarboxylic acid (7), oleuropeic acid (8), rel-(1S,2S,4S)-trihydroxy-p-menthane (9), azelaic acid (10), 2-hydroxy-succinic acid 4-methylester (11), glochidioboside (12), and (+)-isolariciresino-9-O-β-D-glucopyranoside (13). Conclusion: Compounds 5-13 are isolated from genus Forsythia Vahl. for the first time.
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OBJECTIVE: To study the chemical constituents from the fruits of Forsythia suspensa (Thunb.) Vahl.. METHODS: Compounds were isolated by a combination of various chromatographic techniques including column chromatography over macroporous resin, Sephadex LH-20 and reversed-phase HPLC. Their structures were elucidated by physiochemical properties and spectral analysis. RESULTS: Sixteen compounds were isolated and identified as 3, 4, α-trihydroxy-methyl phenylpropionate (1), protocatechaldehyde (2), vanillic acid (3), p-hydroxybenzoic acid (4), p-hydroxylbenzylalcohol (5), p-hydroxyphenylethyl alcohol (6), 2-(4-methoxyphenyl) acetaldehyde (7), 2-(4-hydroxyphenyl) acetic acid (8), 4-hydroxyphenethyl 2-(4-hydroxyphenyl) acetate (9), p-coumatic acid (10), methyl 2-(4-hydroxyphenyl) acetate (11), 3, 4-dihydroxyphenylethanol (12), 1, 2, 4-benzentriol (13), 1-(4- hydroxyphenyl)-2, 3 -dihydroxypropan-1-one(14), 4-hydroxybenzaldehyde (15), and isovanillic acid (16). CONCLUSION: Compounds 1-3, 5, 7, 9, 11, and 14 are isolated from this plant for the first time.
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Objective: RAPD technique has been used to construct DNA fingerprints and analyze the genetic diversity in 14 batches of Forsythia suspensa from different origins. Methods: Primers with good polymorphism were screened from 45 RAPD primers combinations by PCR, and the DNA fingerprints for 14 batches of F. suspensa were constructed by RAPD technique. Results: Eleven RAPD primers with good polymorphism were screened from 45 RAPD primers by PCR amplification, and 80 bands were amplified by the 11 RAPD primers with average 7.27 bands for each primer, of which 67 were polymorphic and PPB was 83.8%. The genetic similarity (GS) ranged from 0.4875 to 0.9625 in 14 batches of F. suspensa from different origins, which showed they had rich genetic diversity. The result of cluster analysis showed that F. suspensa was correlated with sample origin and was consistent with species distribution. Conclusion: The DNA fingerprints for 14 batches of F. suspensa are established based on the RAPD amplified bands.
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Objective: To establish an HPLC method for the simultaneous determination of cafferic acid, forsythoside A, forsythoside B, rutin, hyperoside, forsythin, and arctigenin in Forsythia suspensa. Methods: The analysis was carried out on an Inertsil ODS-3 C18 column (250 mm × 4.6 mm, 5 μm). The mobile phase was composed of acetonitrile and 0.2% phosphorie acid aqueous with gradient elution. The detection wavelength was set at 275 nm. The flow rate was 1.0 mL/min at column temperature of 30 °C. Results: Cafferic acid, forsythoside A, forsythoside B, rutin, hyperoside, forsythin, and arctigenin were well separated by this method, and showed a good linearity in the ranges of 18.24-91.20, 5.88-29.40, 132.60-663.00, 8.34-41.70, 1.96-9.80, 7.60-38.00, and 11.34-56.70 μg/mL, respectively. The average recoveries of the seven components were 97.7%, 96.7%, 102.6%, 101.3%, 93.2%, 91.8%, and 96.7% and the RSD values were 2.3%, 1.4%, 2.4%, 2.2%, 1.0%, 1.0%, and 1.3%, respectively. Conclusion: The established method is accurate, reliable, and could be used for the simultaneous determination of the seven components in F. suspense, which provides a scientific basis for the quality evaluation of F. suspense.
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Objective To study the regulation of dry substance and active components accumulation in the fruit of Forsythia suspensa. Methods The dry substance of the fruit was analyzed by the method of hundred grain mass. The contents of the active components in leaves, shucks, and seeds were analyzed by HPLC. Results The period for F. suspensa to accumulate the dry substance was mainly May and July. During the whole growth phase, the active components, such as forsythiaside, forsythin, and rutin in different parts, were decreasing. From the last ten-day of August to the first ten-day of September, the accumulation of the dry substance came to stability and the contents of active components in shucks and seed were stable. The contents of active components in shucks decreased rapidly from September to October, and then came to stability and the contents in shucks is the least during the last ten-day of October. So the contents of active components in younger F. suspensa are higher than that in elder one, and the proportion among forsythiaside, forsythins, and lution is also significantly different from elder seeds. Conclusion It is more preferable to pick younger F. suspensa from the last ten-day of August to the first ten-day of September and to pick elder F. suspensa during last ten-day of October.