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OBJECTIVE To study the quality difference of different specifications of Citri Grandis Exocarpium from different origins，and to provide reference for the orderly development of Citri Grandis Exocarpium industry. METHODS Different specifications [ Citrus grandis ‘Tomentos’young fruit ，Citrus grandis （L.）Osbeck young fruits ，exocarp] of 93 batches of Citri Grandis Exocarpium medicinal materials （decoction pieces ）from different origins [ Citrus grandis ‘Tomentosa’or Citrus grandis （L.）Osbeck] were taken as samples. The contents of naringin and rhoifolin in samples were determined by HPLC. Through pheatmap parameters of R language ，heatmap was drawn for the contents of naringin and rhoifolin according to origins and specifications （young fruit and exocarp ）. RESULTS Of 93 batches of samples ，the contents of naringin and rhoifolin were 16.52-214.64 and 1.03-10.96 mg/g，respectively. Among different specifications ，the contents of naringin and rhoifolin in the young fruit were the highest （their average contents were 108.96 and 6.30 mg/g respectively ）. Heatmap analysis of R language content showed that the contents of naringin and rhoifolin in Citri Grandis Exocarpium from origin of C. grandis ‘Tomentosa’were generally higher than those from origin of C. grandis （L.）Osbeck. Of different specifications of Citri Grandis Exocarpium from origins，the contents of naringin and rhoifolin were higher in KTP young fruit relatively. CONCLUSIONS The quality of Citri Grandis Exocarpium from origin of C. grandis ‘Tomentosa’with the young fruit as specification is the best.
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ObjectiveTo explore the pharmacodynamic effect of the water extract of Citri Grandis exocarpium （WEC） on mice with alcohol-induced acute liver injury and provide data support for the development of this medicinal for anti-alcoholism and liver protection. MethodThe main components of WEC were determined by high performance liquid chromatography （HPLC）. Sixty Balb/c mice were randomized into 6 groups： control group （equal volume of 0.5% carboxymethyl cellulose sodium solution）， model group （equal volume of 0.5% carboxymethyl cellulose sodium solution）， low-， medium-， and high-dose WEC groups （0.5， 1.0， 2.0 g·kg-1）， and Haiwang Jinzun tablet positive control group （2.0 g·kg-1）. The administration lasted 14 days. One day before the end of the administration， mice were fasted for 12 h with free access to water. The mice， except the control group， were given 56° Chinese liquor （13 mL·kg-1）. After 2 h， blood was taken from eyeballs and the liver was dissected and weighed. Automatic biochemical analyzer was employed to detect the expression of alanine aminotransferase （ALT）， aspartate aminotransferase （AST）， and alcohol dehydrogenase （ADH）. The pathological changes of liver tissues were observed based on hematoxylin-eosin （HE） staining， and apoptosis of hepatocytes based on TUNEL/DAB staining. The expression of proteins related to apoptosis was detected by Western blot. ResultAccording to the HPLC fingerprint， the main components of WEC were rhoifolin and naringin. Compared with the control group， the model group showed increase in liver/body weight ratio （P<0.01） and the expression of ALT and AST （P<0.05， P<0.01）， decrease in the expression of ADH （P<0.05）， blurred structure of hepatic lobules， pathological changes of liver tissue， loose cytoplasm with edema， severe steatosis， rise of the TUNEL-positive rate （P<0.01）， reduction in expression of Bcl-2 （P<0.01）， and increase in Bax and Caspase-3 （P<0.01）. Compared with the model group， medium-dose WEC lowered liver/body weight ratio （P<0.05）. All doses of WEC depressed the activity of ALT and AST （P<0.05， P<0.01）， up-regulated the expression of ADH （P<0.05）， significantly improved the pathological features of alcohol-induced cytoplasmic porosity， edema， and steatosis， down-regulated the TUNEL-positive rate （P<0.05， P<0.01）， enhanced the expression of Bcl-2 （P<0.05）， and decreased Bax and Caspase-3 （P<0.01）. ConclusionWEC regulates the expression of ALT， AST， and ADH and improves hepatic steatosis and hepatocyte apoptosis to fight against acute liver injury.
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ObjectiveTo explore the pharmacodynamic effect of the water extract of Citri Grandis exocarpium （WEC） on mice with alcohol-induced acute liver injury and provide data support for the development of this medicinal for anti-alcoholism and liver protection. MethodThe main components of WEC were determined by high performance liquid chromatography （HPLC）. Sixty Balb/c mice were randomized into 6 groups： control group （equal volume of 0.5% carboxymethyl cellulose sodium solution）， model group （equal volume of 0.5% carboxymethyl cellulose sodium solution）， low-， medium-， and high-dose WEC groups （0.5， 1.0， 2.0 g·kg-1）， and Haiwang Jinzun tablet positive control group （2.0 g·kg-1）. The administration lasted 14 days. One day before the end of the administration， mice were fasted for 12 h with free access to water. The mice， except the control group， were given 56° Chinese liquor （13 mL·kg-1）. After 2 h， blood was taken from eyeballs and the liver was dissected and weighed. Automatic biochemical analyzer was employed to detect the expression of alanine aminotransferase （ALT）， aspartate aminotransferase （AST）， and alcohol dehydrogenase （ADH）. The pathological changes of liver tissues were observed based on hematoxylin-eosin （HE） staining， and apoptosis of hepatocytes based on TUNEL/DAB staining. The expression of proteins related to apoptosis was detected by Western blot. ResultAccording to the HPLC fingerprint， the main components of WEC were rhoifolin and naringin. Compared with the control group， the model group showed increase in liver/body weight ratio （P<0.01） and the expression of ALT and AST （P<0.05， P<0.01）， decrease in the expression of ADH （P<0.05）， blurred structure of hepatic lobules， pathological changes of liver tissue， loose cytoplasm with edema， severe steatosis， rise of the TUNEL-positive rate （P<0.01）， reduction in expression of Bcl-2 （P<0.01）， and increase in Bax and Caspase-3 （P<0.01）. Compared with the model group， medium-dose WEC lowered liver/body weight ratio （P<0.05）. All doses of WEC depressed the activity of ALT and AST （P<0.05， P<0.01）， up-regulated the expression of ADH （P<0.05）， significantly improved the pathological features of alcohol-induced cytoplasmic porosity， edema， and steatosis， down-regulated the TUNEL-positive rate （P<0.05， P<0.01）， enhanced the expression of Bcl-2 （P<0.05）， and decreased Bax and Caspase-3 （P<0.01）. ConclusionWEC regulates the expression of ALT， AST， and ADH and improves hepatic steatosis and hepatocyte apoptosis to fight against acute liver injury.
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In ancient times, the original plants of Citri Exocarpium Rubrum and Citri Grandis Exocarpium had experienced succession and change, including tangerine(Citrus reticulata), pomelo(C. grandis), and Huazhou pomelo(C. grandis 'Tomentosa'), a specific cultivar of C. grandis produced in Huazhou, Guangdong. Before the Qing Dynasty, tangerine was the main original plant, while Huazhou pomelo came to the fore in the Qing Dynasty. In the 1950 s and 1960 s, the producing area of Huazhou pomelo was destroyed, and thus it had to be supplemented with pomelo. From then on, C. grandis 'Tomentosa' and C. grandis were both listed as the original plants of Citri Grandis Exocarpium in the Chinese Pharmacopoeia. This paper reviewed the historical evolution of the collection, processing, and efficacy of Citri Exocarpium Rubrum and Citri Grandis Exocarpium. The research showed that:(1)The harvest time of the original plants of Citri Grandis Exocarpium and Citri Grandis Exocarpium had changed from maturity to immaturity. The collection and processing of Citri Exocarpium Rubrum was first recorded in the Illustrated Classics of Materia Medica in the Song Dynasty. During the Ming and Qing Dynasties, the mesocarp of Citri Exocarpium Rubrum needed to be removed completely, and Citri Grandis Exocarpium from C. grandis 'Tomentosa' was processed into different specifications such as seven-piece, five-piece, and single piece. Furthermore, processed young fruits of Huazhou pomelo appeared.(2)Citri Exocarpium Rubrum and Citri Grandis Exocarpium were processed with carp skin for the first time in the Master Lei's Discourse on Medicinal Processing. It was suggested that carp skin might be helpful for eliminating bones stuck in throat. During the Song, Jin, and Yuan Dynasties, some other processing methods such as ba-king, stir-frying, and salt-processing appeared. Honey, soil, ginger juice, and alum were firstly used as adjuvants for the processing in the Ming and Qing Dynasties. Citri Exocarpium Rubrum was mainly prepared with salt in order to improve the effect of lowering Qi, while it was unnecessary for Citri Grandis Exocarpium from C. grandis 'Tomentosa' because of its obvious effect of lowering Qi and eliminating phlegm. The stir-frying and honey-frying methods helped reduce the strong effect of Citri Grandis Exocarpium from C. grandis 'Tomentosa'.(3)According to the application of Citri Exocarpium Rubrum and Citri Grandis Exocarpium in history, their medicinal use began in Han and Tang Dynasties, developed in Song, Jin, and Yuan Dynasties, and matured in Ming and Qing Dynasties. Citri Grandis Exocarpium from C. grandis 'Tomentosa' was originally applied in Ming and Qing Dynasties, and it still plays an important in role treating COVID-19 nowadays. Moreover, Citri Grandis Exocarpium from C. grandis had cold medicinal property, while Citri Grandis Exocarpium from C. grandis 'Tomentosa' had warm medicinal property, and thus they should not be treated the same. At present, Huazhou pomelo has a certain production scale. Therefore, it is recommended that in the next edition of Chinese Pharmacopoeia, only C. grandis 'Tomentosa' should be included as the original plant of Citri Grandis Exocarpium, and C. grandis should be deleted. The results are conducive to the further development and utilization of Citri Exocarpium Rubrum and Citri Grandis Exocarpium, and support the rational use of Citri Grandis Exocarpium and its processed products.
Subject(s)
Humans , COVID-19 , Citrus , Drugs, Chinese Herbal , Materia Medica , SARS-CoV-2ABSTRACT
Objective: The present study aims to explore the application prospects of Citri Grandis Exocarpium for protecting against novel coronavirus pneumonia (COVID-19). Methods: The pharmacological effects, including expectorant, anti-acute lung injury, anti-inflammatory, anti-pulmonary fibrosis, relieving cough, anti-oxidation, anti-liver injury, anti-kidney injury effects and etc, of both Citri Grandis Exocarpium and its main chemical constituents were analyzed through literature review. The constituents of Citri Grandis Exocarpium were collected by using traditional Chinese medicine systems pharmacology (TCMSP) database and literature searching. The molecular docking study was performed to evaluate the binding ability between the chemical constituents and angiotensin converting enzyme 2 (ACE2), 3C-like main protease (Mpro), papain-like protease (PLP), and dendritic cell-specific ICAM-3-grabbing nonintegrin (DC-SIGN) to predict its potential activity in inhibiting the infection and replication of SARS-CoV-2 virus. Results: The literature review indicated that Citri Grandis Exocarpium possesses expectorant, anti-acute lung injury, anti-inflammatory, anti-pulmonary fibrosis, relieving cough, anti-oxidation, anti-liver injury, anti-kidney injury effects, and so on. Molecular docking results indicated that naringin, neohesperdin, rhoifolin, poncirin, and sitogluside were the main active flavonoids due to showing strong interactions with ACE2, MPro, PLP and DC-SIGN with potential activity in inhibiting the infection and replication of SARS-CoV-2 virus. Conclusion: Citri Grandis Exocarpium may probably delay the progression of COVID-19 through a variety of pharmacological activities and the inhibition of the infection and replication of SARS-CoV-2 due to targeting ACE2, MPro, PLP, and DC-SIGN, reminding that Citri Grandis Exocarpium may possess a potential capacity to protect against COVID-19.
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Recent advances in studies on Citri Grandis Exocarpium of both at home and abroad were reviewed,to fully dig its medicinal value,so as to provide reference for better utilization and development of Citri Grandis Exocarpium.Literatures were retrieved from the China National Knowledge Infrastructure (CNKI),Wanfang database,VIP database,PubMed and etc.Study progress was summarized and concluded from aspects of herbal medicine research,chemical constituents,pharmacological effects and clinical research.Clinical studies on Citri Grandis Exocarpium as the monarch drug in a prescription of recent years were collected and summarized,which provided further reference in the development and utilization of clinical application and its related products.The results showed that both CitriExocarpium Rubrum and Citri Grandis Exocarpium were herbal medicine recorded in the Pharmacopoeia of the People's Republic of China.In Qianlong 30 years,A Supplement to the Compendium of Materia Medica written by Zhao Xuemin,Citri Grandis Exocarpium has been officially made separately and then many later herbal works was based on this.Thus,Citri Grandis Exocarpium was distinguished from Citri Exocarpium Rubrum which was throughout recorded history.Citri Grandis Exocarpium contained polysaccharides,flavonoids,coumarins,volatile oil,and etc.The animal experiments showed that it had significant effects on expectorant and antitussive,anti-inflammatory,antioxidation,immune regulation,prevention and treatment of diabetic myocardial injury.Clinical observations of the past also showed that Citri Grandis Exocarpium had antitussive,expectorant and antiasthmatic effect.It was concluded that Citri Grandis Exocarpium was rich in polysaccharides,flavonoids,coumarin,volatile oil and other active ingredients.It has good effect to treat cough,expectorant and asthma.Its medicinal value is high.It is worth of further development and utilization.
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Objective To optimize the processes of extraction and inclusion of volatile oil from Citri Grandis Exocarpium. Methods With yield ratio of volatile oil as evaluation index, single factor experiments were used to study the extraction process of volatile oil. With the inclusion rate of the volatile oil and the yield of inclusion as evaluation indexes, saturated aqueous solution was used to the L9(34) orthogonal experiments to reach the best inclusion process optimization. And the microscopic imaging analysis and X-ray scattering technology were adopted to character the inclusion compound. Results The optimum extraction process of volatile oil was extracted for 10 hours with 10 folds the amount of water, and without soaking. The optimum conditions of inclusion process were as follows: volatile oil (mL): β-CD (g): water (mL) ratio was 1:8:80; inclusion temperature was 50 ℃; inclusion time was 3 hour. The validation experiments of the inclusion rate of the volatile oil and the yield of inclusion were 91.50% and 88.36%. Microscopic imaging analysis and X-ray scattering technology proved the inclusion compound had been formed. Conclusion Optimal extraction and inclusion process are feasible and stable, which can provide certain supporting data for preparation and production.
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Objective To optimize the processes of extraction and inclusion of volatile oil from Citri Grandis Exocarpium. Methods With yield ratio of volatile oil as evaluation index, single factor experiments were used to study the extraction process of volatile oil. With the inclusion rate of the volatile oil and the yield of inclusion as evaluation indexes, saturated aqueous solution was used to the L9(34) orthogonal experiments to reach the best inclusion process optimization. And the microscopic imaging analysis and X-ray scattering technology were adopted to character the inclusion compound. Results The optimum extraction process of volatile oil was extracted for 10 hours with 10 folds the amount of water, and without soaking. The optimum conditions of inclusion process were as follows: volatile oil (mL): β-CD (g): water (mL) ratio was 1:8:80; inclusion temperature was 50 ℃; inclusion time was 3 hour. The validation experiments of the inclusion rate of the volatile oil and the yield of inclusion were 91.50% and 88.36%. Microscopic imaging analysis and X-ray scattering technology proved the inclusion compound had been formed. Conclusion Optimal extraction and inclusion process are feasible and stable, which can provide certain supporting data for preparation and production.
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To understand the history development and changes of Citri Grandis Exocarpium and initially establish its standard system after exploring the historical origins and modern development of Citri Grandis Exocarpium. In CNKI, Wanfang database and other academic search platforms were searched for literature on Citri Grandis Exocarpium and Chinese medicine standard system； the books related to its modern cultivation techniques and processing technology were also accessed, and after combining with the actual situation analysis, the prospective design of the standard system of Citri Grandis Exocarpium was finally established with research conclusion. The earliest records of the Citri Grandis Exocarpium were documented in the Northern and Southern Dynasties, but its medicinal value was discovered in the Song Dynasty. Its drug use was developed on the basis of Jupi（orange peel） and Citri Exocarpium Rubrum. In 21st century, a number of large-scale, intensive Citri Grandis Exocarpium bases have been formed due to high price, good planting efficiency, and rapid growth of cultivation areas. The standard system includes the technical specifications of seed selection and seedling cultivation of Citri Grandis Exocarpium, technical norms of cultivation, technical specifications of fertilizing and weeding, technical specifications of irrigation and drainage, technical standard of pest and disease control, standard of medicinal materials grade, standard of processing technology of sliced pieces and the quality standard of slices, etc.
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Objective: To compare the UPLC and HPLC fingerprints of flavonoids in Citri Grandis Exocarpium (CGE). Methods: The HPLC and UPLC methods for analyzing the fingerprint of 17 samples were established respectively. Results: There were 21 mutual peaks selected from UPLC chromatography and 17 mutual peaks selected from HPLC chromatography. The similarity of 17 samples was over 0.9. Conclusion: Both the UPLC and HPLC methods could be used for the quality control of CGE. Compared to HPLC, the UPLC method is efficient, quickly, and sensitive.