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1.
Acta Pharmaceutica Sinica ; (12): 3313-3324, 2021.
Article in Chinese | WPRIM | ID: wpr-906824

ABSTRACT

italic>Crataegus pinnatifida is a traditional Chinese medicine, which contains organic acids, triterpenoid acids and other active components, has important medicinal and edible value. In order to study the difference of gene expression level in different developmental stages of hawthorn and explore the genes of active ingredient biosynthesis in Crataegus pinnatifida, high-throughput Illumina HiSeq 2000 technology were used to conduct transcriptome sequencing and bioinformatics analysis on Crataegus pinnatifida fruits from the same origin at different developmental stages. 78 496 Unigenes with an average length of 941 nt were obtained by Trinity software. Among them, 58 395 Unigenes can be annotated by NR, NT, Swiss prot, KEGG, COG, GO and other public databases. KEGG pathway analysis showed that 52 Unigenes encoding 15 key enzymes involved in the citric acid cycle. There are 62 Unigenes were involved in the triterpene biosynthesis pathway of Crataegus pinnatifida. Two key enzymes SQE of triterpenoid metabolism pathway in Crataegus pinnatifida were cloned and performed bioinformatic analysis. The results showed that ORF of CpSQE1 and CpSQE2 were 1 594 bp and 1 597 bp, respectively, encoding 530 and 531 amino acids. The molecular weight of proteins was 57.6 kDa and 57.5 kDa. Bioinformatics analysis showed that both CpSQE1 and CpSQE2 proteins have a PLN02985 superfamily conserved domain, belonging to the squalene monooxygenase superfamily. The phylogenetic tree shows that CpSQE1 and CpSQE2 are clustered together with SQE with squalene epoxidase function in other plants. This study provides a research basis for further exploring the key genes in the biosynthesis process of hawthorn active ingredients and analyzing the regulation pathway of its active ingredient biosynthesis.

2.
Acta Pharmaceutica Sinica ; (12): 2059-2069, 2021.
Article in Chinese | WPRIM | ID: wpr-887060

ABSTRACT

The active ingredients in traditional Chinese medicine have been reported to possess significant pharmacological activity and played an important role in clinical treatments. However, lots of the active ingredients in traditional Chinese medicine suffer from disadvantages such as low solubility, high melting point and low stability that results in low bioavailability and limit its clinical application. Crystal structure plays an important role in improving physicochemical properties and efficacy of the active ingredients in traditional Chinese medicine. This review concludes the research advances of several crystal forms used in the active ingredients in traditional Chinese medicine in terms of polymorph, cocrystal, amorphous/coamorphous and nanocrystal. And the effects of crystal forms on the physicochemical properties and efficacy of the active ingredients in traditional Chinese medicine were reviewed. This research may be useful for the formulation preparation and development of the active ingredients in traditional Chinese medicine.

3.
Article in Chinese | WPRIM | ID: wpr-886563

ABSTRACT

Objective@#To explore the potential mechanism of the main active component Tripterygium wilfordii in the treatment of oral lichen planus based on network pharmacology.@*Methods@#The components of Tripterygium wilfordii and targets were searched through the Traditional Chinese Medicine system pharmacology database and analysis platform (TCMSP) and the Traditional Chinese Medicine integrated database (TCMID) databases. The related targets of oral lichen planus (OLP) were obtained through databases such as Gene Cards. The OLP targets were mapped by Venn analysis to the targets of Tripterygium wilfordii to screen out the common targets as the treatment of OLP targets of Tripterygium wilfordii. The Cytoscape software and STRING were used to construct a chemical component-target network and protein-protein interaction network, a network analyzer was used to compute the network topology properties, a cluster profiler software was used to analyze the GO classification enrichment analysis and KEGG signal path analysis, and a Tripterygium wilfordii chemical components-targets-pathway network diagram was constructed. @*Results@#Twenty-three components and 44 OLP treatmenttargets of Tripterygium wilfordii were obtained. The key active ingredients of Tripterygium wilfordii in the treatment of OLP are triptolide, kaempferol, and tangerine peel. The key targets include TNF and AKT1. The GO classification enrichment analysis obtained 63 GO terms, which are mainly involved in the leukocyte differentiation and reaction to lipopolysaccharides. The KEGG analysis identified 111 signaling pathways, which are mainly related to the TNF signaling pathway and IL17 signaling pathway. @*Conclusion@#Tripterygium wilfordii in the treatment of OLP. This study can provide a theoretical basis for further research to explore drugs with high activity and low toxicity to treat OLP from Tripterygium wilfordii.

4.
Article in Chinese | WPRIM | ID: wpr-846431

ABSTRACT

Objective: To screen the potential type II 5α-reductase inhibitors from active ingredients of traditional Chinese medicine (TCM) based on molecular docking and molecular dynamics (MD) simulation technology. Methods: The molecular docking was used to screen 26 monomer compositions from TCM. Based on the docking results, MD was performed to evaluate the binding strength of compounds with protein. The binding free energy of the system was calculated using the MM/PBSA method. The in vitro micro-reaction system was used to investigate biological activity. Results: The binding energies of 26 monomer compositions from TCM to type II 5-alpha Reductase were different. Among them, ligustroflavone, safflower yellow and hinokiflavone have low binding energies to type II 5-alpha reductase, and their binding abilities were strong. The molecular dynamics simulation results are consistent with the docking results (binding capacity: ligustroflavone-protein > safflower yellow-protein > hinokiflavone-protein). The three components ligustroflavone, safflower yellow and hinokiflavone have a certain inhibitory activity on type II 5α-reductase with the IC50 value of (42.12 ± 3.83), (69.06 ± 6.35), and (191.28 ± 5.90) μmol/L, respectively. Conclusion: Among the screened 26 monomer compositions, ligustroflavone, safflower yellow and hinokiflavone have the potential to be used in the study of treatment and prevention of androgen-dependent diseases, which provides a reference for further exploration and discovery of type II 5α-reductase inhibitors.

5.
Chinese Pharmacological Bulletin ; (12): 127-134, 2020.
Article in Chinese | WPRIM | ID: wpr-857057

ABSTRACT

Aim To explore the mechanism of Mongolian medicine Zhonglun-5 in the treatment of rheumatoid arthritis via carrying out the network pharmacologyre-search. Methods Through various databases,we obtained the composition information and targets of Mongolian medicine Zhonglun-5, and perform multiple ana-lyses on these targets. Then, combined with theabove results,we concluded the significance of targets in anti-rheumatoid arthritis. Results Ninety targets for the treatment of rheumatoid arthritis with Mongolian medicine Zhonglun-5 were screened. The network analysis showed that Zhonglun-5 participated in 126 biological processes andgets 43 pathways for regulating RAS, FPAR,autopagy,JAK-STAT,tumor necrosis factor,etc. which were closely related with rheumatoid arthritis. It-was confirmed that the key targets of anti-rheumatoid arthritis were MAPK9, MAPK8, Aktl, MAPK14, STAT1, STAT3 and Bcl-2. Conclusions The therapeutic target of Mongolian medicine Zhonglun-5 is predicted by network pharmacology, which also reflected its multi-target and multi-channel characteristics, and provided a theoretical clue for the follow-up research anddevelopment of Zhonglun-5.

6.
Article in Chinese | WPRIM | ID: wpr-828409

ABSTRACT

Gastric cancer is a disease with high mortality, which threatens the health of people for a long time. At present, the main treatment methods are surgery and chemotherapy, but these methods have great harm to the human body. However, it is found that the active ingredients of traditional Chinese medicine have an obvious therapeutic effect in the adjuvant treatment of the tumor. Therefore, the active ingredients of traditional Chinese medicine have become a research hotspot in the anti-tumor field. In recent years, many related researchers have been particularly active in studying the in vitro activity and mechanism of active ingredients of traditional Chinese medicine on human gastric cancer cells. In this paper, the Chinese herbal medicine extracts, polysaccharides, alkaloids, saponins, flavones, terpenes, quinones, volatile oils, esters, phenols, protein components and other active ingredients of Chinese medicine were used as the starting points to investigate the anti-gastric cancer mechanism, such as inhibiting cell proliferation and inducing apoptosis of cancer cells, inhibiting cell invasion and migration; inhibiting over-expression of vascular endothelial growth factor(VEGF); interfering with cell mitosis; and regulating cell signaling pathways. Their in vitro inhibitory activity and mechanism for gastric cancer cells were described in this study, providing a theoretical reference for the development and application of anti-gastric cancer drugs.


Subject(s)
Drugs, Chinese Herbal , Humans , Medicine, Chinese Traditional , Saponins , Stomach Neoplasms , Vascular Endothelial Growth Factor A
7.
Article in English | WPRIM | ID: wpr-777107

ABSTRACT

Recently, studying myocardial energy metabolism pathways or improving myocardial metabolism through drugs is another effective strategy for treating ischemic heart disease. Many active components of Chinese herbal medicines (CHMs) have been found to modulate energy metabolism in myocardial cells, cerebral vascular cells, endothelial cells and tumour cells. This paper reviews the advances in studies on the active components of CHMs that modulating energy metabolism in treating cardiovascular diseases over the past five years.

8.
Acta Pharmaceutica Sinica ; (12): 258-268, 2019.
Article in Chinese | WPRIM | ID: wpr-780100

ABSTRACT

Anti-tumor intervention using a combination of drugs shows unique advantages in research and clinical practice. Active ingredients of Chinese herbal medicines can offer many advantages, such as high efficiency, low toxicity, wide effect and multiple targets. At present, the combination active ingredients of Chinese herbal and chemotherapy drugs have attracted increased attention. Nano-drug delivery system provides a good carrier platform for anti-tumor drugs. Nano-carrier-mediated drug combination is a promising strategy. In this paper, we review the mechanisms of the anti-tumor effects of active ingredients of traditional Chinese medicine combined with chemotherapeutic drugs and consider the advantages of drug-loaded nanoparticles, the types and characteristics of carriers. The aim is to provide a reference for the research of effective regimen for anti-tumor therapy.

9.
Article in Chinese | WPRIM | ID: wpr-777508

ABSTRACT

Cervical cancer is the second cancer that threatens women' s health,and has attracted the attention of researchers at home and abroad because of its extremely high mortality rate. At present,most of the radiotherapy methods and chemical drugs for cancer treatment have serious side effects,and the active ingredients of traditional Chinese medicine have become the key research and development targets of anti-cancer drugs due to many advantages,such as multi-channel,multi-link,multi-target,and less toxicity. In recent years,researchers have been particularly active in researching the inhibitory activity and mechanism of active ingredients of traditional Chinese medicine for human cervical cancer cells. In this paper,the inhibitory activity and mechanism of traditional Chinese medicine against human cervical cancer cells were investigated from crude extract of traditional Chinese medicine,polysaccharides,alkaloids,saponins,flavonoids,terpenoids,quinones,volatile oils,esters,phenols,arsenical,protein components as the starting point; anti-cervical cancer mechanism was investigated,such as inhibiting cell proliferation inducing apoptosis of cancer cells,inhibiting cell invasion,migration and focal adhesion kinase( FAK) phosphorylation,inhibiting vascular endothelial growth factor( VEGF)over-expression interfering with cell mitosis,inhibiting Granzyme activity,regulating cellular signaling pathway,down-regulating HPV E6 gene expression,and regulating immune function. Its in vitro inhibitory activity and mechanism of action on cervical cancer cells were reviewed,in order to provide a theoretical basis for the development and utilization of anti-cervical cancer drugs.


Subject(s)
Drugs, Chinese Herbal , Female , Humans , Medicine, Chinese Traditional , Saponins , Uterine Cervical Neoplasms , Drug Therapy , Vascular Endothelial Growth Factor A
10.
Article in Chinese | WPRIM | ID: wpr-802155

ABSTRACT

Sepsis is a kind of systemic inflammatroy response syndrome (SIRS) induced by severe infection,operation,and trauma,with high mortality rate,treatment cost,and high consumption of medical resources.It has caused a great burden to the medical industry and even the national economy.Therefore,it is urgent to find effective treatment methods for sepsis.At present,the sepsis has been treated with certain drugs pointing at its pathogenesis,such as antibiotics,glucocorticoids,and vasoactive drugs.,but the therapeutic effect is not ideal,with many side effects,poor prognosis,and high clinical mortality.Based on the overall macro-dialectical thinking mode,and with the unique effect and low side effect,traditional Chinese medicine (TCM) has attracted the attention from researchers and clinicians around the world for treatment of sepsis.In recent years,some traditional Chinese medicine prescriptions,Chinese patent medicines,single Chinese medicines and active ingredients are increasingly used as new drugs to prevent and treat sepsis.Such treatment methods have been widely recognized and have reduced the mortality and inflammatory indexes of patients to a certain extent,playing an important role in the prevention and treatment of sepsis.In this paper,the actions of nuclear factor kappa B (NF-κB) signal pathway in sepsis as well as the advances in research of NF-κB signal pathway-related proteins in Chinese medicine for sepsis were reviewed.

11.
Article in Chinese | WPRIM | ID: wpr-801549

ABSTRACT

This article reviews the basic research on the treatment of pancreatic cancer from the aspects of Chinese medicine monomer and active ingredients, in order to provide a useful reference for the in-depth study of traditional Chinese medicine for pancreatic cancer. Chinese medicine has achieved remarkable effects in the treatment of pancreatic cancer, which can enhance the efficacy of chemotherapy drugs, alleviate clinical symptoms, reduce adverse reactions, and improve quality of life. The mechanism needs further study.

12.
Chinese Pharmacological Bulletin ; (12): 701-706, 2019.
Article in Chinese | WPRIM | ID: wpr-857266

ABSTRACT

Aim To study the active ingredients of essential oil in Xinjiang Ocimum basilicum L. based on system network pharmacology. Methods Information on the active ingredients of essential oil in Ocimum basilicum L. was collected from different open source databases. The functional targets together with their signaling pathway were predicted and screened. The ingredients, target proteins and their signaling pathways were established to illustrate the functional mechanism of active ingredients of essential oil in Ocimum basilicum L. against the diseases. Results Six active com-ponents of basil volatile oil were identified by analyzing the network of ingredient, target and pathway. Twenty-five main functional targets with five major pathways were also recognized. Conclusions The active components of basil essential oil mainly exert their effects on skin diseases, cancer and cardiovascular and cerebrovascular diseases through five signaling pathways.

13.
Article in Chinese | WPRIM | ID: wpr-851375

ABSTRACT

Objective: To construct the “active components-inflammatory target-anti-inflammatory pathway” network of Zanthoxylum nitidum intervened in inflammation, and predict the target of Z. nitidum intervened in inflammation and its anti-inflammatory mechanism. Methods: Using domestic and foreign literatures, TCMSP database, Pharmmapper server, oral availability (OB), and pharmacodynamics (DL) as the limiting conditions, the components of Z. nitidum were screened and the relative targets were predicted and collected. OMIM database was used to screen inflammation-related genes and protein targets; The STRING database was used to construct the interactive network between inflammatory targets; The network file of “active ingredient-predictive target-inflammatory target” was obtained by PPI analysis and imported into Cytoscape 3.5.1 software to construct the network of “active ingredient- inflammatory target”, so as to obtain the targets directly related to the anti-inflammatory effects of Z. nitidum. DAVID database was used to enrich the KEGG pathway of the selected targets, and then ClueGO plug-in was used to analyze the biological function of the target involved. Finally, the “active component-inflammatory target-anti-inflammatory pathway” network was constructed by combining the above relationships. Results: Twenty-three active ingredients were screened, and nine core anti-inflammatory targets were identified as COX-2, iNOS, PPARG, COX1, MAPK-14, JUN, NR3C1 and so on; The most critical pathways included TNF TRLs signaling pathways. Conclusion: It is preliminarily revealed that the anti-inflammatory effect of Z. nitidum is achieved through the interaction of multiple components and multiple targets, regulating the joint intervention of multiple pathways. However, the key targets and specific regulatory mechanisms need to be explored and verified by further experimental studies.

14.
Article in Chinese | WPRIM | ID: wpr-851089

ABSTRACT

Objective: To screen the anti-depressant active ingredients in Acori Tatarinowii Rhizoma by molecular docking technique. Methods: All the chemical constituents of Acori Tatarinowii Rhizoma were obtained by Traditional Chinese Medicine Pharmacology Database (TCMSP). Combined with oral bioavailability, 65 candidate compounds were obtained. The studied anti-depressant targets included monoamine oxidase A, dopamine transporter, serotonin transporter, and histamine H1 receptor. AutoDock Vina was used to explore the affinity and binding modes of the candidate compounds with the above targets. Results: There were 18 compounds from Acori Tatarinowii Rhizoma that could bind to the above four targets. Among them, four compounds could bind to four targets, three compounds could bind to two targets, and the other 11 compounds could interact with one target. Conclusion: Molecular docking technology can be used to investigate the molecular mechanism of Acori Tatarinowii Rhizoma and determine the active ingredients, which provides an alternative method for the discovery of novel anti-depressants and lead compounds from Chinese herbal medicines.

15.
Article in Chinese | WPRIM | ID: wpr-850967

ABSTRACT

According to the literatures at home and abroad, this paper comprehensively summarized and analyzed the research progress of regulation ways and means of various active ingredients of Chinese materia medica (CMM) on G2/M phase of tumor cells in recent years. Most of the active ingredients of CMM cause mitotic disaster of tumor cells by affecting Cyclin-CDK complex or inducing mitotic catastrophe in tumor cells, inducing DNA damage, mitotic defects and cytokinesis failure, thereby blocking tumor cells in G2/M phase, thus inhibiting tumor cell proliferation and finally inducing apoptosis. The active constituents of CMM can inhibit tumor growth and induce apoptosis by up-regulating or inhibiting key genes at the G2/M detection site, arresting tumor cells in G2/M phase, thereby exerting antitumor effects.

16.
Article in Chinese | WPRIM | ID: wpr-752192

ABSTRACT

Objective: To analyze the chemical constituents of Morchella esculenta, and to determine the main activeingredient of it, so as to better control the quality of Morchella esculenta and promote the development and utilization of Morchella. Methods: The compounds were extracted and percolated by ethanol. The samples were separated using silicagel and identified by13C-NMR data. HPLC was used to assay the contents of 4-Hydroxybenzyl alcohol. Results: A totalof 5 compounds were isolated and their structures were identified as 11, 15, 19-trimethyl-5, 9-eicosadienoic acid, cis-13-Docosenoic acid&Erucic acid, 4-Hydroxybenzyl alcohol, Ergosta-5, 7, 22-triene-3β-ol and Mannitol. Conclusion: 4-Hydroxybenzyl alcohol was first isolated from the Morchella esculenta fruiting body, and HPLC method for thedetermination of 4-Hydroxybenzyl alcohol was established. The content of 4-Hydroxybenzyl alcohol were no less than0.40%. The determination method can be used for quality control of Morchella esculenta.

17.
Article in Chinese | WPRIM | ID: wpr-687403

ABSTRACT

The study is aimed to explore the effect of combination use of nitrogen(N) and zinc(Zn) fertilizers on the growth, yield and the effective components of Agastache rugosa. A. rugosa was grown under two N application rate (120, 300 kg·hm⁻²) and five Zn levels (0, 20, 50, 100,150 kg·hm⁻²) under field condition. The effect of the treatments on the physiological indicators, distribution of nitrogen and zinc and volatile oil components of A. rugosa were studied. The results showed that the combination use of N and Zn could significantly affect the growth and development, yield and volatile oil components of A. rugosa. Under the test conditions, the highest yield of Agastaches Herba was obtained when 50 kg·hm⁻² of Zn fertilizer was applied with high N application rate of 300 kg·hm⁻². Under the same N application rate, the increase of Zn production was positively correlated with the amount of Zn application in a certain concentration range, but excessive Zn application led to the decrease of yield. With the increase of N application level, the content of Zn also significantly increased. The combination use of N and Zn increased the yield of Agastaches Herba. High level of N application was beneficial to the absorption and accumulation of N and Zn of A. rugosa. Zn fertilizer could also promote the absorption and accumulation of N of A. rugosa. The interaction between N and Zn had significant influence on the main chemical constituents of the volatile oil of A. rugosa. Among the volatile oil chemical constituents of A. rugosa the content of pulegone (34.56%-53.91%) and piperonyl methyl ether (18.86%-42.27%) were much higher. Under the same N application rate, different Zn application rates also had significant effects on the main chemical components of volatile oil.

18.
Article in Chinese | WPRIM | ID: wpr-687329

ABSTRACT

The human health is seriously affected by central nervous system(CNS) diseases, but the pathogenesis of CNS diseases is still not completely clear. Currently, the drugs used to treat CNS diseases are mainly receptor modulators and neurotransmitter inhibitors, which have serious side effects; and there are short of drugs for treating CNS diseases clinically. Studies suggest that animal medicines mainly include protein, polypeptide and small-molecule compounds, and have such pharmacological effects in calming, resisting convulsions and improving brain tissues. Plenty of studies suggest that animal medicines usually have a strong activity and good curative effect on these diseases, with a promising prospect in research and development of drugs treating CNS diseases. Based on systematic reviews of literatures, this paper summarizes active ingredients and main pharmacological effects of animal medicines in "extinguishing wind to arrest convulsions" for the CNS diseases, epilepsy and cerebral ischemia, and discusses their study value and application prospects. The results showed that the studies of protein and peptides were relatively simple, and some animal medicines were still blank. The authors believed that amino acids and small molecular compounds should be transferred to oligopeptide, advanced protein extraction and separation techniques shall be adopted for identifying the protein polypeptide composition structure and studying the efficacy, and the methods of biological technology were used to develop peptide biological products for the treatment of CNS diseases. This paper could provide ideas and reference for developing animal medicine products for the treatment of CNS diseases.

19.
Article in Chinese | WPRIM | ID: wpr-705364

ABSTRACT

OBJECTIVE Our group mainly focuses on the target identification and pharmacological mechanism study of TCM.We deeply identified the direct targets of the active ingredients in TCM using molecule probe-'Target Fishing' technology in chemical biology, and explored the related signaling pathways to explain the traditional efficiency of TCM. METHODS We synthesized biotin-tagged mole-cule probe by connecting biotin tag to TCM active molecule using PGE as a linker. Then, the biotin-tagged molecule probe was bound to the surface of solid beads by strong biotin-avidin interaction. Thus, the molecule probe-bound beads were mixed with cell lysates to capture the potential targets and identified by MS.RESULTS Our study found that SA which was an anti-inflammatory compound-could selectively bind to IMPDH2 in microglial cells,and SA showed weaker anti-inflammatory effect on IMPDH2-knock down microglial cells,suggesting IMPDH2 as a key anti-inflammatory target for SA.Ad-ditionally,handelin was a key anti-inflammatory compound.We identified the target protein of handelin as Hsp70 from microglial cells using target pull-down technology. Moreover, handelin showed weaker anti-inflammatory effect on Hsp70-knock down microglial cells,revealing that Hsp70 was the direct anti-inflammatory target of handelin. CONCLUSION Our study provided methodology references for TCM target identification in the future, and also showed a new insight for exploring the pharmacological mechanism of TCM active ingredients.More importantly,we can perform scientific annotation for TCM efficiency by clarifying the biological functions of each target protein,showing important significance on modernization and internationalization of TCM.

20.
Article in Chinese | WPRIM | ID: wpr-838245

ABSTRACT

Objective To explore the effect of antiosteoporotic active fraction from Er-Xian Decoction (EXD) on retinoic acid-induced osteoporosis in rats. Methods Sixty female SD rats were randomly divided into normal control group, model group, estradiol valerate (0.2 mg/kg) group and antiosteoporotic active fraction from EXD low-, middle- and high-dose groups (50, 100, 200 mg/kg). Except for the rats of normal group, the others were intragastrically treated with 70 mg/(kg • d) of retinoic acid for 14 days to induce osteoporosis. Then the rats were treated with estradiol valeratse or antiosteoporotic active fraction from EXD (10 mL/kg) for 28 days. The biochemical parameters in serum and urine of rats were detected by ELISA. The bone mineral density and trabecular bone microstructure of distal femur were analyzed with micro-CT. Results The antiosteoporotic active fraction from EXD significantly decreased calcium content in urine and activities of alkaline phosphatase and tartratse-resistant acid phosphatase in the sera of retinoic acid-induced osteoporotic rats (P0.05, P0.01). High-dose of antiosteoporotic active fraction from EXD significantly increased bone mineral density of distal femur (P0.05). And the antiosteoporotic active fraction from EXD improved the trabecular bone microstructure of distal femur in retinoic acid-induced osteoporotic rats. Conclusion Antiosteoporotic active fraction from EXD can reduce bone loss and deterioration of bone microstructure in retinoic acid-induced osteoporotic rats.

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