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ObjectiveBy observing the effect of Xiaoluowan on phosphatidylinositol 3-kinase （PI3K）/protein kinase B （Akt）/mammalian target of rapamycin complex 1 （mTORC1） pathway in experimental goiter rats， this study aims to explore its therapeutic effect on experimental goiter rats. MethodSixty 5-month-old SD rats of SPF grade were purchased， half males and half females， of which 10 were used as a normal group， and the remaining rats were administrated with propylthiouracil （PTU） solution to induce nodular goiter. After successful modeling， rats were randomly divided into a model group， levothyroxine sodium tablets group， Xiaoluowan low-dose group， medium-dose group， and high-dose group， ten rats each. The levothyroxine sodium tablets group was given 15 μg·kg-1 levothyroxine sodium tablets by gavage. The Xiaoluowan low-， medium-， and high-dose groups were given （ig） Xiaoluowan low-dose （10 g·kg-1）， medium-dose （20 g·kg-1）， and high-dose （30 g·kg-1） Xiaoluowan， and the normal group and model group were administered （ig） with the same volume of 0.9% sodium chloride solution. Four weeks after the intervention， rats were sacrificed by routine intraperitoneal anesthesia using 5% phenobarbital. Subsequently， the histopathology was observed under a microscope， and serum thyroid hormone levels were measured using a Roche electrochemiluminescence immunoassay analyzer. Serum cytokines were detected by enzyme-linked immunosorbent assay （ELISA）， and neurotransmitters were measured using a high-performance liquid chromatograph. The protein level of PI3K/Akt/mTORC1 pathway was determined by Western blot. ResultAs compared with the normal group， the levels of basic fibroblast growth factor （bFGF）， vascular endothelial growth factor （VEGF）， insulin-like growth factor （IGF-1）， 5-hydroxytryptamine （5-HT）， and thyroid stimulating hormone （TSH） were increased， and PI3K， Akt， and mTORC1 protein levels were up-regulated in the model group， while the levels of norepinephrine （NE）， triiodothyronine （T3）， tetraiodothyronine （T4）， free triiodothyronine （FT3）， and free thyroid hormone （FT4） were decreased （P<0.05）. Compared with the model group， the levothyroxine sodium tablets group， and Xiaoluowan low-， medium-， and high-dose groups exhibited reduced levels of bFGF， VEGF， IGF-1， 5-HT， and TSH， and down-regulated PI3K， Akt， and mTORC1 protein levels， and increased NE， T3， T4， FT3， and FT4 levels （P<0.05）. ConclusionXiaoluowan may act on the PI3K/Akt/mTORC1 signaling pathway to play its role in the treatment of nodular goiter， and it is dose-dependent.
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By consulting ancient herbal medicines， medical and prescription books， combined with modern documents， the textual research of Morindae Officinalis Radix has been conducted to verify the name， origin， changes in production areas， quality evaluation， harvesting， and processing methods， so as to provide reference and basis for the development and utilization of the famous classical formulas. After textual research， the production areas of Morindae Officinalis Radix has experienced great changes from north to south in history. The original plants involve 11 families， 14 genera and 21 species， and the mainstream varieties in ancient times were Damnacanthus officinarum and D. indicus， and the basis of Morindae Officinalis Radix in modern times has changed into the dry roots of Morinda officinalis produced in Guangdong province and other places. The medicinal parts of Morindae Officinalis Radix in ancient and modern times are all roots， and the quality is better if it has many beads， thick flesh， and purple color. Ancient medical books recorded that it was usually harvested in February and August， dried in the shade， and used to remove the wood core. And the modern harvesting and processing method is to dig throughout the year， first remove the fibrous roots， dry in the sun until 60%-70% dry， gently beat flatten and dry in the sun. The processing methods of the past dynasties are mainly salt-， vinegar-， wine-processed， etc. Based on the systematic research of Morindae Officinalis Radix， from the perspective of clinical experience and safety and effectiveness， it is recommended that the famous classical formulas should be developed from the mainstream variety since modern times， namely Morindae Officinalis Radix.
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In this paper， the name， origin， changes of producing area， medicinal parts， quality evaluation and processing methods of Arecae Semen in the famous classical formulas by consulting related herbal medicines， medical books and prescription books. The results showed that the names of Arecae Semen in the past dynasties were mostly derived from its shape， efficacy and producing area. The main base of the past generations was Areca catechu， the medicinal parts were its seeds （Arecae Semen） and pericarps （Arecae Pericarpium）. Arecae Semen is produced in Hainan province of China. Since modern times， it has been concluded that the best quality is large， heavy， firm， and unbreakable. The main processing methods of Arecae Semen in the past dynasties were netting， cutting and frying. Therefore， it is suggested that Arecae Semen should be used in Dayuanyin. If the processing requirements of Arecae Semen are not clearly indicated， it can be processed according to raw products in the 2020 edition of Chinese Pharmacopoeia.
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The direct acting substances of Cuscuta chinensis in vivo were preliminarily identified through the correlation analysis of "metabolites-effect identification" model. The ovariectomized female rats were i.g administered with 95% ethanol extract part, 40% ethanol elution part and n-butanol extract part of Cuscuta chinensis. The serum fingerprints of different parts and times of administration were established by UPLC/Q-TOF-MS. At the same time, serum estradiol (E2), follicle-stimulating hormone (FSH) and luteinizing hormone (LH) levels were detected. Bivariate correlation analysis and grey correlation analysis were used to screen estrogenic components. The results showed that nine direct acting substances in vivo highly related to estrogen effect were found in the drug containing serum, which were hyperoside, astragalin, methyl quercetin glucuronide, quercetin-diglucuronide, quercetin, apigenin, isoquercitrin, kaempferol glucuronide and kaempferol. We can preliminarily screen out the direct acting substance of estrogen effect of Cuscuta chinensis in vivo based on the research idea of serum spectrum effect correlation. It provides a reliable basis for revealing the estrogeneffective substances of Cuscuta chinensis and confirming the quality markers. This experiment was approved by Harbin University of Commerce Ethics Committees (Approval No. HSDU2020-065).
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Coptidis Rhizoma-Evodia Fructus is a classic herb pair in traditional Chinese medicine prescriptions, the famous prescription is called Zuojinwan, which comes from Danxi Xinfa, is composed of Coptidis Rhizoma-Evodia Fructus (6∶1). In this formula, Coptidis Rhizoma has the effect of clearing heat and drying diuresis, purging fire to remove toxin and clearing heart. Evodia Fructus has the effects of expelling cold and alleviating pain, checking upward adverse flow of Qi tostop vomiting, and assisting yang to stop diarrhea. Coptidis Rhizoma has the properties of bitter and cold, and Evodia Fructus has the properties of pungent and calidus. Pungent drugs have divergent effects, and bitter drugs have sedimentation effect, when used in combination, they can clear the liver and purge fire, calm the adverse-rising energy and stop vomiting. On the basis of Zuojinwan, Coptidis Rhizoma-Evodia Fructus medicine has derived different compatibility ratios. Different ratios are different in terms of efficacy, usage, clinical application. Although with the application of modern analytical instruments and the development of molecular pharmacology theory, the chemical constituents and Pharmacological effects of Coptidis Rhizoma and Evodia Fructus have been fully studied, as to the principle of compatibility, and the study of pharmacological effects and chemical constituents after the compatibility of the two drugs in different proportions, there is still no comprehensive system summary. This article makes a systematic and comprehensive explanation of Coptidis Rhizoma-Evodia Fructus from the aspects of famous literature, chemical composition, pharmacological effects and clinical applicationthrough querying literature and ancient books. In order to make this herb pair more standardized, and provide reference materials for further research and development for this herb pair.
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The qualitative analysis method of ultra performance liquid chromatography tandem quadrupole time of flight mass spectrometry (UPLC-Q-TOF-MS/MS) was established for the chemical constituents in Sanhuang tablets. Waters ACQUITY BEH C₁₈ (2.1 mm×100 mm, 1.7 μm) column was used with 0.1% formic acid solution (A)-0.1% formic acid acetonitrile (B) as the mobile phase for gradient elution. The flow rate was 0.2 mL•min⁻¹; the sample volume was 1 μL and the column temperature was 30 ℃. The high-resolution quadrupole time-flight mass spectrometry was used as detector with electrospray ion source in both positive and negative models, and the dry gas temperature was 325 ℃. Based on the analysis of mass spectrometry and literature reports, 38 compounds were confirmed, including 1 alkaloid, 1 dianthrone compound, 6 tannins, 7 anthraquinone glycosides, 6 anthraquinones and 17 flavonoids. Liquid chromatography-mass spectrometry method is simple, reliable and rapid to identify the chemical compositions of Sanhuang tablets, and it is helpful to reveal its chemical constituents and pharmacodynamic substances.
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OBJECTIVE: To establish a high-performance liquid chromatography-quadrupole time of flight tandem mass spectrom¬etry (HPLC-Q TOF-MS/MS) method for analysis of estrogen-like active ingredients in Cuscuta chinensis.
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Objective: To screen the phytoestrogenic effective extracts and dose of Cistanche deserticola including estrogenic and anti-estrogenic activities. Methods: The effect of phytoestrogen was determined through uterus growth test in low and high estrogen female model mice. Then MTT assay of the estrogen-dependent breast cancer cells MCF-7 was conducted with the medicated serum of mice. Results: After ig administration with 95% ethanol extract of C. deserticola [EECD, 30 g/(kg·d)], the uterus coefficient of low estrogen model mice increased. The medicated serum of 30 g/(kg·d) EECD significantly promoted the proliferation of MCF-7 cells. 40 g/(kg·d) EECD + diethylstilbestrol significantly inhibited the growth of the uterus in high estrogen model mice and the proliferation of MCF-7 cells as well. Conclusion: With the dose of 30 g/(kg·d), EECD could exert quasi estrogen effect, and with the dose of 40 g/(kg·d), EECD could exert the estrogen antagonistic action. The method established is accurate and reliable, which could be used for the follow-up studies on the phytoestrogen material basis of C. deserticola. © 2013 Tianjin Press of Chinese Herbal Medicines.
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<p><b>OBJECTIVE</b>The study aimed to clone the open reading frame of chalcone synthase (CHS) from Aquilaria sinensis and analyze the bioinformatics and expression of the gene.</p><p><b>METHOD</b>One unique sequence containing CHS domain was discovered in our previous reported wound transcriptome dataset of A. sinensis. The open reading frame of CHS was cloned by RT-PCR strategy with the template of mixed RNA extracted from A. sinensis stem which treated by different wound time. The bioinformatic analysis of this gene and its corresponding protein was performed. The AsCHS1 expression in calli was analyzed with histone gene as an internal control gene under wound condition by qRT-PCR technique.</p><p><b>RESULT</b>One unique sequence of CHS, named as AsCHS1, was cloned from A. sinensis. The full length of AsCHS1 cDNA was containing a 1 192 bp ORF that encoded 397 amino acids. The result of qRT-PCR displayed that the highest expression level was at 12 h, which indicated that it was possibly involved in early-stage response to wound.</p><p><b>CONCLUSION</b>Cloning and analyzing AsCHS1 gene from A. sinensis provided basic information for study the function and expression regulation of AsCHS1 in the flavonoids biosynthesis.</p>
Subject(s)
Acyltransferases , Genetics , Base Sequence , Cloning, Molecular , Computational Biology , DNA, Complementary , Chemistry , Genetics , DNA, Plant , Chemistry , Genetics , Drugs, Chinese Herbal , Flavonoids , Metabolism , Gene Expression Regulation, Enzymologic , Gene Expression Regulation, Plant , Models, Molecular , Molecular Sequence Data , Phylogeny , Plant Proteins , Genetics , Plant Stems , Chemistry , Genetics , Plants, Medicinal , Protein Structure, Tertiary , RNA, Messenger , Genetics , RNA, Plant , Genetics , Reverse Transcriptase Polymerase Chain Reaction , Sequence Analysis, DNA , Thymelaeaceae , Chemistry , GeneticsABSTRACT
<p><b>OBJECTIVE</b>To investigate the absorption mechanism of loganin at different intestine segments of rats and the influence of the drug solution concentration, pH, P-gp inductor.</p><p><b>METHOD</b>Rats were randomly divided into 10 groups, high, middle and low concentration groups (0.1, 0.025, 0.012 5 mg x mL(-1)), duodenum, jejunum and ileum groups (0.013 mg x mL(-1)), high, middle and low pH groups (0.013 mg x mL(-1)), inducer group (0.013 mg x mL(-1)). The intestine cannulation was performed for in situ recirculation. Loganin concentration in the flux was measured by the reversed phase HPLC.</p><p><b>RESULT</b>When the concentration was raised from 0.012 5 to 0.1 mg x mL(-1), the uptake of loganin was linearly increased, and no change of Ka is not found. The pH of flux has no effect on drug absorption. The absorbed dose and Ka sequence (from high to low) of loganin at different intestine segments is ileum, duodenum, jejunum. Furthermore, P-gp inductor RFP has effect on the intestinal absorption.</p><p><b>CONCLUSION</b>The absorption of loganin in intestine of rat is a first-order kinetics, the absorption mechanism is probably the passive diffusion. It has specific absorption locus and access to locating administration, meanwhile it's the P-gp substrate, and could increase its fraction of bioavailability by corporation with P-gp inhibitor.</p>
Subject(s)
Animals , Male , Rats , Drugs, Chinese Herbal , Pharmacokinetics , Duodenum , Metabolism , Hydrogen-Ion Concentration , Ileum , Metabolism , In Vitro Techniques , Intestines , Metabolism , Iridoids , Pharmacokinetics , Jejunum , Metabolism , Kinetics , Rats, WistarABSTRACT
<p><b>OBJECTIVE</b>To study relatively pharmacological activities of cinnamon acid in blood serum of rabbit administered cinnamon acid, cinnamon and Jingui Shenqi pills.</p><p><b>METHOD</b>RP-HPLC determine and analysis blood serum sample from rabbits administered cinnamon acid, cinnamon and Jingui Shenqi pills. Condition of colour spectrum was Symmetry C18 (3.9 mm x 150 mm, 5 microm) chromato bar, mobile phase was methanol-1% glacial acetic acid water-solution (45:55), flow rate was 0.8 mL x min(-1), temperature of bar was 35 degrees C, detection wave length was 285 nm. The serum pharmacokinetic parameters were calculated with 3p87.</p><p><b>RESULT</b>Linear range of cinnamon acid is from 0.06-15 microg x mL(-1) (r = 0.9997), the lowest detectability is 0.054 microg x mL(-1). Pharmacokinetic process of cinnamon acid in rabbit could be all fitted to two-compartment model.</p><p><b>CONCLUSION</b>Sensitive and exclusive HPLC that adopt can exactly detect serum concentration in rabbits administerd cinnamon acid. Pharmacokinetic parameters of three conditions can reveal pharmacokinetics regularity of cinnamon acid in rabbit.</p>
Subject(s)
Animals , Male , Rabbits , Cinnamomum zeylanicum , Chemistry , Drugs, Chinese Herbal , Pharmacokinetics , Serum , ChemistryABSTRACT
<p><b>OBJECTIVE</b>To study systematically the factors which affect separation and purification of the total alkaloids and mesaconitine with X -5 macroporous resin.</p><p><b>METHOD</b>With the content of the total alkaloids and mesaconitine as parameters, the optimum condition of absorption and elution were studied in the process of the purification with X -5 macroporous resin.</p><p><b>RESULT</b>The X - 5 macroporous resin yielded the best separating efficiency when the concentration of the extracted solution was 1 g raw material per 1 mL, pH 12.0, the absorptive time of 6 hour and the volume of 95% ethanol (7BV pH 8) as the eluant; X -5 macroporous resins was used five times in a reproducible way. The rate of extraction and content of the total alkaloid were 80% and 30% respectively after purification with X - 5 macroprous resin.</p><p><b>CONCLUSION</b>The method can increase the purity of mesaconitine and total alkaloids.</p>
Subject(s)
Aconitine , Aconitum , Chemistry , Alkaloids , Ethanol , Chemistry , Hydrogen-Ion Concentration , Plant Roots , Chemistry , Plants, Medicinal , Chemistry , Resins, Synthetic , ChemistryABSTRACT
<p><b>OBJECTIVE</b>To establish a method for fingerprinting of Fuzhisan (FZS, a traditional Chinese medicinal preparation) using high-performance liquid chromatography with ultraviolet and evaporative light scattering detector (HPLC-UV/ELSD) to allow simultaneous determination of 5 major constituents in the preparation.</p><p><b>METHODS</b>HPLC-UV/ELSD analysis was performed on water AlltechC18 column (5 microm, 4.6 mm x 250 mm) with a mixture of acetonitrile (A) and 0.1% acetice acid water (B) as the mobile phase. The solvent A gradient for elution was 0, 12%; 25, 20%; 30, 20%; 75, 30%; 105, 40%; 120, 80%; 130, 12%, with the flow rate of 1.0 ml/min; and the column temperature at 30 degrees . The detective wavelength was 335 nm, drift tube temperature was 80 degrees , pressure of nebulizer gas was 25 psi. The similarities between the HPLC-UV/ELSD fingerprints of the 12 extracts were calculated using similarity evaluation software.</p><p><b>RESULTS</b>The fingerprint of FZS was established and the 5 major constituents were identified. The complementarity between the fingerprints of UV and ELSD was analyzed, showing good correlation between 12 batches of FZS.</p><p><b>CONCLUSION</b>The method for fingerprinting can simultaneously characterize the main chemical constituents in FZS and allows stable, effective and comprehensive quality control and evaluation of FZS for a single sample.</p>