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ObjectiveTo reveal the medication rules of the clinical prescriptions containing Citri Sarcodactylis Fructus， and to provide a basis for the modern clinical application of Citri Sarcodactylis Fructus， the development of health products and the research and development of new drugs. MethodThe clinical prescriptions containing Citri Sarcodactylis Fructus were retrieved from CNKI， Wanfang Data， and VIP， and then a basic database of prescriptions was established via the traditional Chinese medicine inheritance auxiliary platform （V2.5）， IBM SPSS V20， and Excel （Microsoft Office 2016）. The frequency and association rules of the medicines in prescriptions （compatible medicines） and the corresponding syndromes were then mined. ResultThe prescriptions were screened according to the inclusion and exclusion criteria. A total of 458 clinical prescriptions containing Citri Sarcodactylis Fructus were collected， involving 388 Chinese medicines， and the total frequency of medicines reached 6 199. The core compatible medicines （frequency > 130） of Citri Sarcodactylis Fructus included Poria （frequency of 222）， Atractylodis Macrocephalae Rhizoma （217）， Paeoniae Radix Alba （196）， Bupleuri Radix （159）， and Citri Reticulatae Pericarpium （142）. The Citri Sarcodactylis Fructus-compatible medicines with frequency > 49 were selected for further analysis， which included 34 medicines with the cumulative frequency of 3 131 （50.51% of the total frequency）. These medicines mainly have the functions of tonifying Qi， invigorating Qi， tonifying blood， alleviating edema and promoting urination， promoting digestion， and activating blood and relieving pain. They are mainly warm， cold， or mild-natured， taste bitter， sweet， or acrid， and have the tropism in the spleen， liver， stomach， or lung meridians. The association rule analysis demonstrated that 14 medicine combinations were commonly used， and the core combinations were Poria-Citri Sarcodactylis Fructus， Atractylodis Macrocephalae Rhizoma-Citri Sarcodactylis Fructus， Paeoniae Radix Alba-Citri Sarcodactylis Fructus， Bupleuri Radix-Citri Sarcodactylis Fructus， Atractylodis Macrocephalae Rhizoma-Poria-Citri Sarcodactylis Fructus， and Citri Reticulatae Pericarpium-Citri Sarcodactylis Fructus. The clinical prescriptions containing Citri Sarcodactylis Fructus were mainly used to treat 52 diseases corresponding to 11 types of traditional Chinese medicine （TCM） syndromes. Three representative syndrome types， including spleen and stomach syndromes， Qi-blood-body fluid syndromes， and gynecological syndromes were selected for further association rule analysis. In the treatment of spleen and stomach syndromes， the core compatible drugs were Atractylodis Macrocephalae Rhizoma， Poria， Paeoniae Radix Alba， Bupleuri Radix， Citri Reticulatae Pericarpium， and Pinelliae Ehizoma， which， together with Citri Sarcodactylis Fructus， formed 25 commonly used medicine combinations （16 combinations composed of 2 medicines and 9 combinations composed of 3 medicines）. In the treatment of Qi-blood-body fluid syndromes， the core compatible drugs were Poria， Paeoniae Radix Alba， Atractylodis Macrocephalae Rhizoma， Astragali Radix， Hordei Fructus Germinatus， and Bupleuri Radix， which， together with Citri Sarcodactylis Fructus， formed 23 common medicine combinations （17 combinations composed of 2 medicines， 5 combinations composed of 3 medicines， and 1 combination composed of 4 medicines）. In the treatment of gynecological syndromes， the core compatible medicines were Atractylodis Macrocephalae Rhizoma， Paeoniae Radix Alba， Angelicae Sinensis Radix， Astragali Radix， Cyperi Rhizoma， and Poria， which constituted 25 common medicine combinations （15 combinations composed of 2 medicines and 10 combinations composed of 3 medicines）. ConclusionWe employed the traditional Chinese medicine（TCM） inheritance auxiliary platform to explore the compatibility of Citri Sarcodactylis Fructus-containing clinical prescriptions and the corresponding TCM syndromes， which intuitively showcased the medication rules of Citri Sarcodactylis Fructus. Specifically， Citri Sarcodactylis Fructus was mainly combined with the medicines for tonifying Qi， invigorating Qi， tonifying blood， alleviating edema and promoting urination， promoting digestion， and activating blood and relieving pain to treat different TCM syndromes. While soothing liver， regulating Qi， harmonizing stomach， and relieving pain， the combinations tonify and activate blood， invigorate spleen， and resolve dampness. The findings are of great significance to the rational application of Citri Sarcodactylis Fructus， the development of health food， and the research of new drugs and will bolster the development of Chinese medicine industry.
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Curcuma kwangsiensis root tuber is a widely used genuine medicinal material in Guangxi, with the main active components of terpenoids and curcumins. It has the effects of promoting blood circulation to relieve pain, moving Qi to relieve depression, clearing heart and cooling blood, promoting gallbladder function and anti-icterus. Modern research has proved its functions in liver protection, anti-tumor, anti-oxidation, blood lipid reduction and immunosuppression. Considering the research progress of C. kwangsiensis root tubers and the core concept of quality marker(Q-marker), we predicted the Q-markers of C. kwangsiensis root tubers from plant phylogeny, chemical component specificity, traditional pharmacodynamic properties, new pharmacodynamic uses, chemical component measurability, processing methods, compatibility, and components migrating to blood. Curcumin, curcumol, curcumadiol, curcumenol, curdione, germacrone, and β-elemene may be the possible Q-markers. Based on the predicted Q-markers, the mechanisms of the liver-protecting and anti-tumor activities of C. kwangsiensis root tubers were analyzed. AKT1, IL6, EGFR, and STAT3 were identified as the key targets, and neuroactive ligand-receptor interaction signaling pathway, nitrogen metabolism pathway, cancer pathway, and hepatitis B pathway were the major involved pathways. This review provides a basis for the quality evaluation and product development of C. kwangsiensis root tubers and gives insights into the research on Chinese medicinal materials.
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Humans , China , Curcuma/chemistry , Liver , Neoplasms , Terpenes/pharmacologyABSTRACT
Objective: To analyze the medication rules of traditional Chinese medicine (TCM) preventive oral prescriptions for COVID-19. Methods: The preventive oral prescriptions for COVID-19 published by national and provincial health and wellness committees, administrations of TCM, medical institutions at all levels, medical masters and Chinese medicine experts were collected to establish a database, manual screening was carried out according to the inclusion and exclusion criteria, and frequency statistics, association rule analysis. The mutual information method, entropy hierarchical clustering and other methods were improved through Excel and the TCM inheritance auxiliary platform V2.5 to mine the rules and characteristics of medication. Results: The selected 157 prescriptions contained a total of 130 TCMs. The top five TCMs with the highest use frequency were Glycyrrhizae Radix et Rhizoma (86), Astragali Radix (80), Lonicerea Japonicae Flos (70), Atractylodis Macrocephalae Rhizoma (62), Saposhnikoviae Radix (60). In accordance with TCM efficacy classification, most of them were medicines for qi-tonifying (279), followed by medicines for clearing heat and drying dampness (163), dispelling pathogenic wind-cold (126), resolving dampness (111), as well as dispelling pathogenic wind-heat (99). The characteristics of four-natures of the selected medicines are as follows: most of them were cold (59), followed by warm (38) and mild (21). In terms of five-taste, most of them were sweet (26) and acrid-and-bitter (24), followed by sweet-and-bitter (20), bitter (20) and acrid (15). For the meridian attribution, the five-zang organs and six-fu organs were all involved, most of them attributed to lung meridian (80), followed by stomach meridian (57) and spleen meridian (40). Based on association rule analysis, 12 commonly used medicine combinations with two or three TCMs were found. The commonly used medicinal pairs included Astragali Radix and Saposhnikoviae Radix (51), Astragali Radix and Atractylodis Macrocephalae Rhizoma (46), Atractylodis Macrocephalae Rhizoma and Saposhnikoviae Radix (43), Astragali Radix and Atractylodis Macrocephalae Rhizoma and Saposhnikoviae Radix (38), Forsythiae Fructus and Astragali Radix (37), and so on. In addition, 14 core combinations of medicines were obtained by complex system entropy cluster analysis, on this basis, six new prescriptions were screened out based on unsupervised entropy hierarchical clustering analysis. According to The Catalogue of Edible Traditional Chinese Medicinal Materials, Traditional Chinese Medicinal Materials for Health Food, and New Resources of Food published by National Health Commission of the People's Republic of China, there are 35 species belonging to the group of edible traditional Chinese medicinal materials, 20 species belonging to the group of new resources of food, 31 species belonging to the group of traditional Chinese medicinal materials for health food, 19.11% of the preventive oral prescriptions for COVID-19 were composed of the medicines belonging to the above three groups. Besides, there are 11 toxic species, and 24.84% of the preventive oral prescriptions for COVID-19 contained toxic TCMs. Conclusion: We found that invigorating qi and resolving dampness were the main treatment used to prevent for COVID-19, combined with the methods for strengthening vital energy and eliminating pathogenic factors. Most of the preventive oral prescriptions for COVID-19 were treated in lung, spleen and stomach meridians. In the process of selecting prescriptions and using TCMs to prevent for COVID-19, the safety of preventive medicines was also emphasized. And the theory of “Preventive Treatment of Disease” was embodied in these preventive oral prescriptions for COVID-19. For the prescriptions containing toxic TCMs, special attention should be paid to their safety in clinical application.
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Objective: Coronavirus Disease 2019 (COVID-19) has been diagnosed as an epidemic disease characterized by cold and dampness pathogens in TCM clinic. Due to many Chinese medicines with different functions were used in the treatment of COVID-19, it is very important to find the law of application of damp-removing traditional Chinese medicine with high frequency application, with view to providing a reference for the use and research of Chinese medicine to further control the pandemic. Methods: The publicly released diagnosis and treatment programs issued by the National Health Commission and Health Commission of provinces, autonomous regions and municipalities, and Chinese herbs prescription information in these were collected, a database was established, and Excel and Graphpad 8.0 software were used to analyze the frequency of use of various Chinese medicines, the frequency and property characters including five flavors (bitter, pungent, sweet, sour, and salty) and four natures (warm, hot, cool, and cold) and channel tropisms of Chinese medicine for removing dampness. Results: A total of 137 prescriptions of Chinese medicine for treating COVID-19 were collected, including 178 TCMs showing functions of resolving phlegm, relieving cough and asthma, resolving dampness, clearing damp and inducing dieresis, clearing heat, tonifying deficiency, and relieving exterior syndrome, in which the TCMs with the first four functions that we called the dampness-removing TCMs, accounted for 35.78%. Also a number of TCMs in the rest functions showed removing-dampness. The first four functions were divided into subfunctions including aromatic resolving dampness, clearing heat and drying dampness, drying dampness and tonifying spleen qi, drying dampness and removing phlegm, inducing diuresis and relieving swelling, inducing diuresis and relieving exterior syndrome. Among them, the most frequently used TCMs was Ephedrae Herba, followed by Citri Reticulatae Pericarpium, Pogostemonis Herba, Pinelliae Rhizoma, Poria, Scutellariae Radix, and Atractylodis Rhizoma. The property character analysis in the dampness-removing TCMs showed that bitter and pungent were largely present and sour and astringent were absent, warm and hot were dominant; And the lung, spleen, stomach, large intestine, bladder were main channel tropisms. Conclusion: Dampness-removing TCMs are the first important type of traditional Chinese medicine to be considered in the treatment of COVID-19 in Chinese medicine. The application of dampness-removing TCMs in the treatment of COVID-19 needs to be combined with its application law. This study may provide meaningful and useful information on further research to investigate the effective compounds from the dampness-removing Chinese medicine with high frequency application, and also provide a reference for the clinical treatment of COVID-19 accurately against dampness evil with dampness-removing traditional Chinese medicines.
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Durio zibethnus is mainly distributed in Southeast Asia. Traditional Chinese medicine believes that durian shells have the effects of clearing heat and purging fire, nourishing yin and moisturizing dryness. Therefore, it is often used as a pharmaceutic food in the Chinese folk to assist treating diseases. At present, the chemical constituents isolated from durian shell include phenolic acids, phenolic glycosides, flavonoids, coumarins, triterpenes, simple glycosides and other compounds. Modern pharmacological studies show that durian shell has many pharmacological activities, such as antioxidant, anti-inflammatory, regulation of glucose and lipid metabolism. The chemical composition and pharmacological effects of durian shells are summarized in order to provide references for the further research and application of durian shell.
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Arthropod-borne diseases, such as malaria and dengue fever, have frequently beset five countries(Cambodia, Vietnam, Laos, Myanmar, and Thailand) in the tropical rainy Lancang-Mekong region, which pose a huge threat to social production and daily life. As a resort to such diseases, chemical drugs risk the resistance in plasmodium, non-availability for dengue virus, and pollution to the environment. Traditional medicinal plants have the multi-component, multi-target, and multi-pathway characteristics, which are of great potential in drug development. Exploring potential medicinals for arthropod-borne diseases from traditional medicinal plants has become a hot spot. This study summarized the epidemiological background of arthropod-borne diseases in the Lancang-Mekong region and screened effective herbs from the 350 medicinal plants recorded in CHINA-ASEAN Traditional Medicine. Based on CNKI, VIP, and PubMed, the plants for malaria and dengue fever and those for killing and repelling mosquitoes were respectively sorted out. Their pharmacological effects and mechanisms were reviewed and the material basis was analyzed. The result is expected to serve as a reference for efficient utilization of medicinal resources, development of effective and safe drugs for malaria and dengue fever, and the further cooperation between China and the other five countries in the Lancang-Mekong region.
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Animals , Culicidae , Malaria , Plants, Medicinal , Plasmodium , ThailandABSTRACT
Cinnamomi Ramulus is a dry tender branch of <italic>Cinnamomum cassia</italic> Presl, which is a multifunctional traditional Chinese medicine(TCM). Cinnamomi Ramulus has different efficacy under different compatibility environment. Complet medicine is a commonly used and relatively fixed compatibility form of two drugs, and it is the smallest unit in the compatibility of TCM. The four kinds of complet medicine commonly used in Cinnamomi Ramulus were as follows: the diaphoretics pungent in flavour and warm in property pairs include Cinnamomi Ramulus Ephedrae Herba and Cinnamomi Ramulus Bupleuri Radix complet medicine. The stasis dredge collaterals pairs involve Cinnamomi Ramulus Poria and Cinnamomi Ramulus Persicae Semen complet medicine. The regulation Qi and Blood Cinnamomi Ramulus Paeoniae Radix Alba complet medicine. Wenda Tongyang pairs consist of Cinnamomi Ramulus Aconiti Lateralis Radix Praeparaia, Cinnamomi Ramulus Astragali Radix, and Cinnamomi Ramulus Glycyrrhizae Radix et Rhizoma complet medicine. After compatibility, some changes have taken place in the chemical composition of complet medicines. For example, after compatibility of Cinnamomi Ramulus and Ephedrae Herba, the content of effective components of both herbs decreases, and the chemical constituents that are not found in single herbs are produced. After compatibility of Cinnamomi Ramulus and Bupleuri Radix, the dissolution of active ingredients is related to compatibility ratio. The active ingredients of Cinnamomi Ramulus Poria, Cinnamomi Ramulus Paeoniae Radix Alba pair and Cinnamomi Ramulus Aconiti Lateralis Radix Praeparaia have also changed to some extent.The content of active ingredients in Astragali Radix and Glycyrrhizae Radix et Rhizoma both increase after compatibility with Cinnamomi Ramulus. Different complet medicine have different pharmacological effects, Cinnamomi Ramulus Ephedrae Herba complet medicine have the effect of transpiration and antipyretic, Cinnamomi Ramulus Bupleuri Radix complet medicine can analgesia. Cinnamomi Ramulus Poria complet medicine have the effect of diuretic, improve myocardial ischemia and so on. Cinnamomi Ramulus Persicae Semen complet medicine have the anti-coagulation action.Cinnamomi Ramulus Paeoniae Radix Alba complet medicine have the anti-inflammatory and analgesic activities. Cinnamomi Ramulus Aconiti Lateralis Radix Praeparaia complet medicine have the effect of dispelling cold to relieve pain. Cinnamomi Ramulus Astragali Radix complet medicine have the many effects in relieving anti-coagulation, antioxidation and anti-myocardial ischemia. Cinnamomi Ramulus Glycyrrhizae Radix et Rhizoma complet medicine displays diverse activities, including antiarrhythmic, antithrombosis. In this paper, the chemical constituents and pharmacology of four kinds of complet medicine of Cinnamomi Ramulus were reviewed, which provided a reference for the better open utilization of Cinnamomi Ramulus complet medicine.
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Momordicae Semen a traditional toxic Chinese medicine, which was first recorded in Kaibao Bencao of the Northern Song Dynasty. It has the effects in reducing swelling, dispersing knot, and attacking sores. It is mainly distributed in South China, such as Guangxi and Guangdong. It is also distributed in Southeast Asian countries, such as Thailand and Vietnam. The present study showed abundant chemical components extracted from Momordicae Semen, including steroids, sterols, volatile oils and fatty acids. Among them, 30 terpenoids, 102 compounds in volatile oil, 6 sterols and 19 fatty acids have been identified. Aqueous extracts and alcohol extracts of Momordicae Semen have the toxicity, and the toxicity decreases with the increase of oil content. The main toxic components reported in the literatures are cochinchinin and saponins. Pharmacological studies have shown that in addition to its traditional anti-cancer, anti-inflammatory, antibacterial and other pharmacological effects, Momordicae Semen also exhibited many pharmacological effects, such as anti-ulcer, anti-oxidation and immune regulation. In recent years, there have been increasingly more research reports on Momordicae Semen. By studying relevant domestic and foreign literatures from 1964 to 2019 in China National Knowledge Infrastructure, Wanfang, PubMed and Web of Science, chemical constituents, pharmacological effects and toxicological research of Momordicae Semen were summarized, which will provide reference for further research and application of Momordicae Semen in the future.
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Objective:To take zebrafish embryo as the research object, in order to investigate the development toxicity, cardiotoxicity, liver toxicity and kidney toxicity of water extract of Jiaotaiwan (JTW) on zebrafish embryo. Method:Zebrafish embryos with normal development at 12 h (hpf) after fertilization were selected as model animals for the growth and cardiotoxicity experiments. The embryos were treated with 125, 250, 500 mg·L-1 of JTW water extracts, and the effects of the drugs on the heart rate and morphology of the embryos and LD50 were observed at 72 h (hpf) after fertilization. Zebrafish embryos with normal development at 72 h (hpf) after fertilization were used as model animals for the liver and kidney toxicity experiments. The embryos were treated with 125，250，500 mg·L-1 of JTW water extracts, and the effect of the drugs on morphological changes, Alanine aminotransferase(ALT), Aspartate aminotransferase (AST) activity, and creatinine content of the larvae and LD50 were observed at 72 d (dpf) after fertilization. Result:The zebrafish embryos in control group developed normally, the heart was well developed, and the heartbeat was even and powerful. The LD50 of JTW water extract on zebrafish embryos for 72 h was 1 023 mg·L-1. Compared with the embryos in the control group, 250，500 mg·L-1 treatment groups in the development toxicity had a smaller head, shorter body lengths (P<0.05), and decreased eye size (P<0.05). Compared with the control group embryos, the pericardial edema was observed in the 500 mg·L-1 group, the heart rate was significantly decreased in the 250，500 mg·L-1 JTW water extract groups (P<0.01), the atrial and ventricular areas were significantly reduced (P<0.05), the distance of SV-BA became significantly larger (P<0.05), the distance of AV channel became significantly larger (P<0.01), and the in-flow distance was significantly shorter (P<0.01). In the acute toxicity experiment, the LD50 of JTW water extract for zebrafish larvae for 72 h was 1 067 mg·L-1. Compared with control group, JTW water extract significantly reduced ALT activity in zebrafish larvae (P<0.05). Conclusion:This experiment found that JTW has an obvious toxicity in embryonic development, which is mainly manifested as delayed growth and severe cardiotoxicity. Great attention shall be paid to clinical administration to pregnant women, lactating women and patients with heart disease.
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Objective: To optimize the extraction technology of Guizhi Zhumian Capsules (GZC). Methods: Based on the analysis of the single factor experiment Results:, the orthogonal test method was adopted to study the three factors including the amount of water added, extraction time, and extraction frequency by taking the dry extract yield of the medicinal materials and transfer rate of geniposide as indicators to optimize the water extraction process of GZC. To optimize the alcohol precipitation process of GSC, these factors including the concentration of the medicinal materials, alcohol content, and time of alcohol precipitation were investigated. The extracts before and after alcohol precipitation were compared by improving sleep pharmacodynamics. Results: The best water extraction technology of GZC was decocted three times with 10 times of water, 0.5 h each time. The optimal alcohol precipitation process was to concentrate the filtrate of water extraction to 1 mL, which was equivalent to 1 g of the original medicinal materials, with 80% alcohol content and 12 h alcohol precipitation time. Compared with the negative control group, the water extract group of GZC could prolong the sleep time of pentobarbital sodium mice and increase the sleep rate of mice under the lower dose of pentobarbital sodium valve (P 0.05). Conclusion: The pharmaceutical efficacy of the extract before and after alcohol precipitation was different. In order not to affect the drug effect, the water extraction process was finally selected as the best extraction process.
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Objective: To establish the determination and fingerprint of Gesang Jiangtang Capsules (GJC) for its quality control. Methods: UV spectrophotometric method was used for determining polysaccharides, total saponins, and total flavonoids of GJC. Ten batches of GJC were detected and recorded by UPLC. Similarity evaluation was performed by using Similarity Evaluation System for Fingerprint Chromatogram of TCM (2012) to confirm the common peaks. Results: In three batches of GJC, average polysaccharides content, average total saponins content, and average total flavonoids content were 4.56%, 2.97%, and 2.61%, respectively. UPLC fingerprints of 10 batches of GJC were established and 15 common peaks were confirmed. Puerarin, rutin, notoginsenoside R1, ginsenoside Rg1, ombuoside, ginsenoside Rb1, and ombuin were identified by chemical identification of the reference substance, corresponding to peaks 1, 5, 8, 10, 12, 14, and 15. Conclusion: The methods can be used for the quality control of GJC with good precision, accuracy, and reproducibility.
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Gramineous crops occupy a remarkable proportion of grain crops in the word,and wheat,rice and corn account for more than 80%of the world's food crops. Agricultural residues bring tremendous pressure on the environment,and inefficient development of resources has caused huge waste of resources. At present,the research on agricultural residues mainly focuses on energy,fertilizer,feed and materialization. However, there are still a lot of resources that have not been rationally utilized. The author has found that in recent years,the medicinal research on gramineous crop waste has focused on four varieties-rice,corn,wheat and sugar cane,and their waste rice bran,rice husk,rice straw,corn stigma,corn bract,wheat bran,sugar cane leaf,sugar cane skin. The compounds isolated and identified from agricultural residues include phenylpropanoids,flavonoids,steroids and their glycosides,organic acids and their esters,volatile oil and saccharides. Studies have shown that agricultural residues from gramineous crops have pharmacological activities, such as anti-oxidation,hypolipidemia,hypoglycemia,anti-inflammation,anti-tumor,anti-cardiovascular disease,anti-liver and kidney damage. This paper is a systematic review of the chemical composition and pharmacological effects of agricultural residues from the major gramineous crops,so as to provide useful information for further research and development of agricultural residues.
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The quality definition of traditional Chinese medicine (TCM) is a hot area in modern research of TCM. In recent years, the characteristics of one herb with multiple effects have been widely accepted and studied. The typical opposite-effect of herbs is considered as a special part of one herb with multiple effects, and was summarized in this paper. Sanqi was used as an example of opposite-effect herbs for developing the strategies and approaches on the Q-markers. The traditional opposite-effect should be studied by modern pharmacological research methods. The correlation of the chemical components with the opposite effects should be established in order to verify the material basis and evaluate the mechanism including targets and pathways. The unique characteristics of chemical components should be analyzed and defined. Finally, the Q-markers of the opposite effect herb will be confirmed. This paper provides a useful reference for the precise quality control of herbal opposite-effects.
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AIM@#To synthesize three novel esterified-derivatives of mangiferin and evaluate their hypoglycemic activities.@*METHODS@#Acetic, propionic, and butyric anhydride were reacted with mangiferin, respectively. The hypoglycemic activity of the derivatives was evaluated using a hyperglycemic mouse model induced by streptozotocin (STZ), and the islet cells were checked by biopsy inspection.@*RESULTS@#7, 2', 3', 4', 6'-penta-acetyl-mangiferin (PAM), 3, 6, 7, 2', 3', 4', 6'-hepta-propionyl-mangiferin (HPM) and 3, 6, 7, 2', 3', 4'-hexa-butyryl-mangiferin (HBM) were synthesized and their structures were identified by MS,(1)H, (13)C NMR, and 2D NMR. These three compounds were reported for the first time. PAM group (0.5, 0.25 mmol·kg(-1)), HPM group (0.5, 0.25 mmol·kg(-1)), and HBM group (0.5, 0.25, 0.125 mmol·kg(-1)) mice showed strong hypoglycemic activity (P < 0.01); mangiferin group (1, 0.5 mmol·kg(-1)), PAM group (0.125 mmol·kg(-1)) and HPM group (0.125 mmol·kg(-1)) showed marginal hypoglycemic activity (P < 0.05); mangiferin group (0.25 mmol·kg(-1)) had the potential for a hypoglycemic effect, although it did not demonstrate that statistically. In histological examination, the islet cells of the PAM, HPM, and HBM groups could recover from the STZ damage; islet cells of the mangiferin group could recover also, but less than the esterified-derivative groups.@*CONCLUSION@#Derivatives could repair the damaged islet cells, and had higher lipid-solubility and stronger hypoglycemic activity than mangiferin itself. There existed a structure activity effect, and a solubility effect relationship: the larger esterification moieties, or the higher lipid-solubility, the stronger the hypoglycemic activity (no ester → acetyl → propionyl → butyryl). Esterified derivatives of mangiferin are potential compounds for new anti-diabetes drugs.
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Animals , Humans , Male , Mice , Diabetes Mellitus, Experimental , Drug Therapy , Esterification , Hypoglycemic Agents , Chemistry , Islets of Langerhans , Molecular Structure , Xanthones , ChemistryABSTRACT
<p><b>OBJECTIVE</b>To further study the characteristics of drugs with neutral property in two-way application and conditioned dominance by observing the action characteristic of 10 traditional Chinese medicines with neutral property in hemorheological indicators of heat stagnation and blood stasis syndrome and cold stagnation and blood stasis syndrome rats.</p><p><b>METHOD</b>The model of heat stagnation and blood stasis syndrome rats was established by injecting carrageenan and dry yeast, while the model of cold stagnation and blood stasis syndrome rats was established by body freezing. Subsequently, 10 traditional Chinese medicines with neutral property, 5 traditional Chinese medicines with heat property and 5 traditional Chinese medicines with cold property were selected for intervention to observe the changes in such indicators as whole blood viscosity, plasma viscosity and hematocrit and analyze the action characteristics of drugs with neutral property.</p><p><b>RESULT</b>ANOVA showed that among six of the 10 traditional Chinese medicines with neutral property, including Typhae Pollen, Sarcandrae Herba and Sappan lignum, could obviously increase the hemorheological indicators of both heat stagnation and blood stasis syndrome and cold stagnation and blood stasis syndrome rats; five traditional Chinese medicines with cold property, such as Salviae Miltiorrhizae Radix et Rhizoma, Leonuri Herba, Rhei Radix et Rhizoma, could significantly ameliorate the hemorheological indicators of heat stagnation and blood stasis syndrome rats (P < 0.01 or P < 0.05), and Salvia Miltiorrhiza Radix et Rhizoma alone could ameliorate the hemorheological indicators of cold stagnation and blood stasis syndrome rats (P < 0.05); all of the five traditional Chinese medicines with heat property could significantly ameliorate the hemorheological indicators of cold stagnation and blood stasis syndrome rats (P < 0.01), among which Carthami Flos and Notoginseng Radix et Rhizoma could significantly ameliorate the hemorheological indicators of cold stagnation and blood stasis syndrome rats. According to the average high-shear blood viscosity analysis, drugs with neutral property showed similar action characteristics to those with cold property in ameliorating hemorheology indicators of heat stagnation and blood stasis syndrome rat and better effect than those with heat property in reducing whole blood viscosity; and traditional Chinese medicines with neutral property have the similar action characteristics to those with heat property in improving the hemorheology indicators of cold stagnation and blood stasis syndrome rat and better effect than those with heat property in reducing whole blood viscosity.</p><p><b>CONCLUSION</b>Under the condition of heat stagnation and blood stasis syndrome, traditional Chinese medicines with neutral property show the similar action characteristics to those with cold property; but under the condition of cold stagnation and blood stasis syndrome, traditional Chinese medicines with neutral property show the similar action characteristics to those with heat property. This indicates that traditional Chinese medicines with neutral property show both heat and cold properties under he conditions of heat stagnation and blood stasis syndrome and cold stagnation and blood stasis syndrome.</p>
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Animals , Male , Rats , Analysis of Variance , Blood Circulation , Physiology , Drugs, Chinese Herbal , Pharmacology , Therapeutic Uses , Hemorheology , Homeostasis , Medicine, Chinese Traditional , Methods , Rats, Sprague-Dawley , Thrombosis , Drug TherapyABSTRACT
<p><b>OBJECTIVE</b>To establish a rat model of blood stasis and heat accumulation syndrome in accordance with the Chinese medicine (CM) theoretic features.</p><p><b>METHODS</b>Thirty male SD rats were randomly divided into the normal group, the model group, and the danshen root group, 10 in each. Rats in the danshen root group were given danshen decoction at 13.5 g/kg by gastrogavage, with the volume of 20 mL/kg, twice daily for 7 successive days. As for rats in the normal group and the model group, equal volume of pure water was given to them by gastrogavage, twice daily for 7 successive days. On the 4th day of medication, carrageen at 50 mg/kg was peritoneally injected to rats in the model group and the danshen root group, once daily for 3 successive days. Twenty-four h after the last injection, 20% dry yeast suspension (10 mL/kg) was given to the rats by subcutaneous injection. The indictors such as body temperature, tongue figure, tail ecchymosis, skin color of the ears and four limbs, microcirculation indicators, and hemorheological indicators were observed 6 h later.</p><p><b>RESULTS</b>Compared with the normal group, red and purple tongue, longer and thicker arteries and veins under the tongue, red and purple claw color, red ear flap edge, obvious ecchymosis of the tail occurred in rats of the model group (P<0.01), with obviously increased body temperature (P<0.01). The blood velocity of the microcirculation in the ear flap obviously decreased. The hemorheology tests showed that the whole blood viscosity (high, middle, and low), hematocrit, and erythrocyte electrophoretic time obviously increased, red blood cell deformation index obviously deceased, showing statistical difference (P<0.01, P<0.05). Compared with the model group, the length of ecchymosis in the tail obviously decreased in rats of the danshen root group. The blood velocity score of the microcirculation obviously increased. The hemorheology tests showed that the whole blood viscosity (high, middle, and low), hematocrit, and erythrocyte electrophoretic time obviously decreased, red blood cell deformation index obviously increased, showing statistical difference (P<0.05, P<0.01).</p><p><b>CONCLUSION</b>The rat model of blood stasis and heat accumulation syndrome established with carrageen and dry yeast suspension injection had obvious features, with good reproducibility and stability. It could be used in the study of CM basic theories, screening of Chinese herbs, and the theories of Chinese-drug properties.</p>
Subject(s)
Animals , Male , Rats , Disease Models, Animal , Hemorheology , Medicine, Chinese Traditional , Microcirculation , Rats, Sprague-DawleyABSTRACT
<p><b>OBJECTIVE</b>To study the action characteristics of "two-way application and conditioned dominance" of traditional Chinese medicines with neutral property by observing the action characteristic of 10 traditional Chinese medicines capable of promoting blood circulation and removing blood stasis with neutral property in the microcirculation in rats with heat stagnation and blood stasis syndrome.</p><p><b>METHOD</b>The rat model with heat stagnation and blood stasis syndrome was established by injecting carrageenan and dry yeast, and the rat model with cold stagnation and blood stasis syndrome was built by the body freezing method. Ten traditional Chinese medicines with neutral property, including 5 with hot property and 5 with cold property, were selected for intervention to observe blood flow rate and flow state indicators in rat auricles and make a comparative analysis on action characteristics of traditional Chinese medicines with neutral property.</p><p><b>RESULT</b>ANOVA showed that among the 10 traditional Chinese medicines with neutral property, 6 such as Typhae Pollen, Sappan Lignum and Vaccariae Semen can obviously increase the blood flow rate (P < 0.01 or P < 0.05) in the above two models; all of the 5 traditional Chinese medicines with cold property can increase the blood flow rate (P < 0.01 or P < 0.05) in the rat model with heat stagnation and blood stasis syndrome, but only Salvia miltiorrhiza can increase the blood flow rate (P < 0.01 or P < 0.05) in the rat models with cold stagnation and blood stasis syndrome, while other medicines showed no notable effect; among the 5 traditional Chinese medicines with hot property, Carthamus tinctorius and Ligusticum chuanxiong can increase the blood flow rate (P < 0.01 or P < 0.05) in the rat models with cold stagnation and blood stasis syndrome, but had no obvious effect to the blood flow rate in the rat models with heat stagnation and blood stasis syndrome. According to the analysis on average blood flow rate, traditional Chinese medicines with natural and cold properties showed similar effect on heat stagnation and blood stasis syndrome and better effect in increasing blood flow rate than those with hot property; those with natural and hot properties showed similar effect and better effect in increasing blood flow rate than those with cold property.</p><p><b>CONCLUSION</b>Under the condition of heat stagnation and blood stasis syndrome, traditional Chinese medicines with neutral property have the similar action characteristics with those with cold property; wile under the condition of cold stagnation and blood stasis syndrome, traditional Chinese medicines with neutral property have the similar action characteristics with the Chinese medicinal herbs with hot property. This indicates the action characteristics of "two-way application and conditioned dominance" of traditional Chinese medicines with neutral property to some extent.</p>