Volume 16,Issue 3,2024 Table of Contents

1 Herb induced liver injury by Xianling Gubao Tablets: A case assessed for causality using updated RUCAM and integrated evidence chain

Guohui Li a , , Xiaohe Xiao b ,

2024, 16(3):301-309. DOI: https://doi.org/10.1016/j.chmed.2023.10.005

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Objective: A typical case of Xianling Gubao (XLGB) Tablets-induced liver injury was systematically studied in the clinic and the laboratory. Methods: A patient with herb-induced liver injury (HILI) and a history of taking XLGB Tablets before disease onset was engaged as the study subject, and the case was diagnosed according to the updated Roussel Uclaf Causality Assessment Method (RUCAM) and the integrated evidence chain (iEC) method recommended by the Guidelines for Diagnosis and Treatment of Herb-induced Liver Injury (HILI Guidelines). Results: Clinical history, biochemical indexes and imaging tests were used to exclude the influence of fundamental diseases and confusing liver diseases such as viral, alcoholic and autoimmune liver diseases on the diagnosis. Based on an investigation of the patient’s medication history, she was suspected to have HILI caused by XLGB Tablets, as the patient was only taking an oral preparation of XLGB Tablets, and the influence of other drugs on the diagnosis was excluded. This patient with alanine aminotransferase (ALT)≥ 3× upper limit of normal (ULN) and a calculated R of 6 was diagnosed with possible acute drug-induced hepatocellular injury. The relationship was considered ‘‘highly probable” (score of 9) using the updated RUCAM of 2016. Moreover, the fingerprint similarity between the preparation taken by the patient and a commercially available preparation was 0.99, suggesting that the patient was consuming XLGB Tablets rather than another drug. LC-MS technology and the Agilent Fake TCM-Drugs database were used to investigate the drug, and no chemical additions were found. Examination of the drug for pesticide residues, heavy metals, aflatoxins and other exogenous substances indicated compliance with the content limits of the Chinese Pharmacopoeia. Conclusion: In summary, the final diagnosis of XLGB-induced liver injury reached the clinical diagnosis of HILI and was acute severe hepatocellular injury type by the updated RUCAM and iEC. Therefore, this study provides scientific evidence regarding the causality evaluation of compound preparations of traditional Chinese medicines-induced liver injury.

2 Comprehensive summary of material basis - Laying a foundation for substances of medicine food homology development

Wenyuan Gao

2024, 16(3):311-312. DOI: https://doi.org/10.1016/j.chmed.2024.05.001

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3 Chemical composition, pharmacological activity and development strategies of Rubus chingii: A review

Xiangmei Xiong a , Zheng Liu b , Xiance Che a , Xuemin Zhang c , Xia Li b , , Wenyuan Gao a , b ,

2024, 16(3):313-326. DOI: https://doi.org/10.1016/j.chmed.2024.01.007

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Raspberries are used for both food and medicine, but it has not yet attracted widespread attention. In this paper, the chemical constituen of the original plant raspberry. R. chingii is one of the new "Zhe Bawei" medicinal materials selected in 2017. ‘‘Zhe Bawei” refers to eight kinds of genuine medicinal materials in Zhejiang Province. The chemical constituents, pharmacological effects, processing, and application of Rubus chingii Hu were reviewed to provide a reference for its further development. Relevant literature in recent years was collected in databases such as China Knowledge Network, Web of Science, Elsevier, PubMed, and X-Mol, using ‘‘raspberry”, ‘‘Rubus chingii”, ‘‘traditional use”, ‘‘chemical composition”, ‘‘pharmacology”, etc. as keywords individually or in combination. The summary of pharmacological activities shows that the relationship between the pharmacological activities of raspberry is still not deep enough. More in-depth research should be carried out in this direction to explore the mechanism of action of its active ingredients and provide effective reference for the further development of the raspberry industry. In the future, with the participation of more researchers, it is expected to develop innovative drugs based on raspberry for the treatment of diseases.

4 Ethnopharmacology, phytochemistry, pharmacology and product application of Platycodon grandiflorum: A review

Lanying Zhang a , c , Xinrui Wanga , c , Jingze Zhang c , Dailin Liu a , c , , Gang Bai b ,

2024, 16(3):327-343. DOI: https://doi.org/10.1016/j.chmed.2024.01.005

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Platycodonis Radix (Jiegeng in Chinese) is a well-known traditional Chinese medicine used for both medicinal and culinary purposes. Its historical use as an antitussive and expectorant has been extensively documented. Researchers, to date, have identified 219 chemical constituents in Platycodon grandiflorum (Jacq.) A. DC, encompassing 89 saponins, 11 flavonoids, 21 polysaccharides, 14 phenolic acids, six polyacetylenes, five sterols, 34 fatty acids, 17 amino acids, and 22 trace elements. Jiegeng exhibits diverse pharmacological effects, including antitussive and anti-phlegm properties, anti-cancer activity, antiinflammatory effects, immune regulation, antioxidant properties, anti-obesity, and antidiabetic effects. Additionally, Jiegeng shows potential in protecting the heart and liver. Beyond its medicinal benefits, Jiegeng is highly esteemed in culinary applications, and its global demand is on the rise. Its utilization has expanded beyond medicine and food to encompass daily necessities, cosmetics, agricultural supplies, and other fields. Currently, there are 18 272 patents related to P. grandiflorum. This comprehensive review summarizes the latest research published over the past 20 years, providing a robust foundation for further exploration of the medicinal and health benefits of P. grandiflorum.

5 Chemical constituents, pharmacological activities and quality evaluation methods of genus Hippocampus: A comprehensive review

Zhiyong Zhang a , b , Xiaoyang Zhang a , b , Xi Wang a , b , Xuting Guo a , Xinhao Yan a , Zheng Li a , b , c , , Wenlong Li a , b , c ,

2024, 16(3):344-357. DOI: https://doi.org/10.1016/j.chmed.2023.04.001

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The genus Hippocampus is a multi-origin animal species with high medicinal and healthcare values. About 57 species of Hippocampus spread worldwide, of which about 14 species can be used as medicine, showing anti-oxidation, anti-inflammation, anti-depressant, anti-hypertension, anti-prostatic hyperplasia, antivirus, anti-apoptotic, antifatigue, and so on. And those pharmacological effects are mainly related to their active ingredients, including amino acids, abundant proteins (peptides and oligopeptides), fatty acids, nucleosides, steroids, and other small molecular compounds. The main means of authentication of Hippocampus species are morphological identification, microscopic identification, thin layer chromatography method, fingerprint method and genomics method. This review will provide useful insight for exploration, further study and precise medication of Hippocampus in the future.

6 Ethnopharmacology, chemical composition and functions of Cymbopogon citratus

Xiqin Dua , b , Meng Zhang a , b , Shuping Wang c , Jingyang Li d , Jingze Zhang a , b , , Dailin Liu a , b ,

2024, 16(3):358-374. DOI: https://doi.org/10.1016/j.chmed.2023.07.002

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Cymbopogon citratus in the gramineous family, also known as lemongrass (LG), is a perennial herb. LG, a drug and food homologous medicine, has a widely recorded medicinal value and food applications. To date, 158 LG compounds have been reported, including terpenoids, flavonoids, phenolic acids. Pharmacological and clinical studies have indicated that LG has antibacterial, neuroprotective, hypoglycemic, hypotensive, anti-inflammatory, and anti-tumor effects. This article reviews LG in ethnopharmacology, chemical composition, pharmacology, food, medicine, and daily chemical applications to provide a basis for the subsequent development of food and medicine.

7 Bioactive components, pharmacological properties and underlying mechanism of Ganoderma lucidum spore oil: A review

Jianying Liu a , Binzhi Zhang a , Leqi Wang a , b , Shasha Li b , c , Qinqiang Long a , , Xue Xiao a , c ,

2024, 16(3):375-391. DOI: https://doi.org/10.1016/j.chmed.2023.09.007

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Ganoderma lucidum is a Chinese medicinal fungus with a long history of use in healthcare and disease treatment. G. lucidum spores (GLS) are tiny germ cells released from the mushroom cap during the mature stage of growth. They contain all the genetic active substances of G. lucidum. G. lucidum spore oil (GLSO) is a lipid component extracted from broken-walled Ganoderma spores using supercritical CO2 extraction technology. GLSO contains fatty acids, Ganoderma triterpenes, sterols and other bioactive compounds. Previous studies have demonstrated that GLSO has a wide range of pharmacological properties, including anti-tumor, anti-aging, neuroprotection, immunomodulation, hepatoprotection and modulation of metabolic diseases. This review summarizes the research progress of GLSO over the past two decades in terms of its bioactive components, extraction and processing techniques, pharmacological effects and safety evaluation. This provides a solid foundation for further research and application of GLSO.

8 Biotransformation and pharmacological activities of platycosides from Platycodon grandiflorum roots

Lin Shi a , Tong Cui a , Xinyue Wang a , Rina Wu a , , Junrui Wua , Yanqun Wang a , Weiming Wang b ,

2024, 16(3):392-400. DOI: https://doi.org/10.1016/j.chmed.2024.01.004

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In Northeast China, Goubao pickle is a popular food fermented from the roots of Platycodon grandiflorum as the main material, offering a unique flavor and rich nutritional value. Platycosides in roots of P. grandiflorum may play a crucial role in determining the quality of Goubao pickle through microorganism fermentation. However, biotransfermation of platycosides has not been reviewed during fermentation. In this study, we reviewed platycosides in chemical diversity, metabolic processes in vivo, biotransformation of platycosides in vitro, and pharmacological effects. Finally, we also discussed how to improve the bioactive secondary platycosides we desire by regulating enzymes from microorganisms in the future.

9 Genetic diversity of food-medicinal Lycium spp. in China: Insights from chloroplast genome

Ruyu Yao a , d , Bin Wang a , b , Michael Heinrich c , Qiuling Wang a , , Peigen Xiao a ,

2024, 16(3):401-411. DOI: https://doi.org/10.1016/j.chmed.2024.02.003

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Objective: Goji (fruits of Lycium spp.) is commonly consumed as food and medicine. The increasing market demand for goji has led to its wide cultivation and broad breeding, which might cause loss of genetic diversity. This study aims to uncover the genetic diversity of the cultivated and wild Lycium. Methods: The chloroplast genome (CPG) of 34 accessions of Chinese food-medicinal Lycium spp., including the popular cultivars and their wild relatives, was re-sequenced and assembled, based on which the genetic diversity was evaluated. Results: Sequence structural comparison shows that CPG is comparatively conserved within species. Phylogenetic analysis indicates that CPG is sufficient for the discrimination of Lycium species; combined with nuclear ribosomal internal transcribed spacer (Nr ITS) sequences, materials with mixed genetic backgrounds can be identified. Nucleotide diversity analysis reveals that the modern cultivars are probably with a common maternal parent, while the wild accessions are with higher level of genetic diversity. Conclusion: For the first time this study reveals the intraspecies genetic diversity of Lycium spp. using CPG, highlighting the urgent conservation demand of wild genetic resources of Lycium. Our study also demonstrates that CPG provides crucial evidence for identification of Lycium species with mixed genetic backgrounds and highlights the importance of the wild relatives in genetic diversity conservation. This CPG-based technology will contribute to the sustainable development of medicinal plants broadly.

10 Analysis on patents of health care products with substances of medicine food homology in China

Haibo Liu a , b , Yanfeng Wang b , c , Jiali Huang a , b , Zhengqi Dong a , , Peigen Xiao a ,

2024, 16(3):412-421. DOI: https://doi.org/10.1016/j.chmed.2024.03.005

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Objective: The concept of substances of medicine food homology (SMFH) has garnered significant attention in recent years. This study conducts a systematic analysis of patent literature related to SMFH, and elucidates the development trends, technical hotspots, and the overall patent protection landscape of SMFH in China over the past two decades. Methods: The patent search focused on the SMFH varieties as the objects of inquiry, with retrieval conducted in patent databases. Subsequently, the acquired data underwent processing, analysis, and visualization. Results: While the technical threshold for pharmaceutical applications surpasses that of the food service sector, the former may assume a prominent role in the future. Research and development (R&D) activities in the southeast of China demonstrate robust activity than other regions. Colleges and scientific research institutions exhibit substantial advantages in patent applications compared with individuals and hold greater potential for future development. Conclusion: The findings of this patent analysis indicate that China’s SMFH industry are presently undergoing a transition from an extensive model to a high-quality model. The quality and technical standards of SMFH products are consistently improving. Consequently, there is a need for more stringent patent application requirements to align with the evolving development needs.

11 Amplifying protection against acute lung injury: Targeting both inflammasome and cGAS-STING pathway by Lonicerae Japonicae Flos-Forsythiae Fructus drug pair

Junjie Li a , b , c , d , Ming Dong b , c , e , Qing Yao b , c , f , Xu Dong b , c , Yuanyuan Chen b , c , Jincai Wen b , c , Yingjie Xu b , c , Zhixin Wu b , c , Xiaomei Zhao b , c , Ye Xiu b , c , Xiaoyan Zhan b , c , d , Zhaofang Bai b , c , d , , Xiaohe Xiao a , b , c , d ,

2024, 16(3):422-434. DOI: https://doi.org/10.1016/j.chmed.2024.04.001

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Objective: Acute lung injury (ALI) is characterized by inflammation and currently lacks an efficacious pharmacological intervention. The medicine combination of Lonicerae Japonicae Flos (LJF) and Forsythiae Fructus (FF) demonstrates combined properties in its anti infective, anti-inflammatory, and therapeutic effects, particularly in alleviating respiratory symptoms. In previous studies, Chinese medicine has shown promising efficacy in lipopolysaccharides (LPS)-induced ALI. However, there have been no reports of LJF and FF pairing for lung injury. The aim of this study is to compare the efficacy of herb pair Lonicerae Japonicae Flos-Forsythiae Fructus (LF) with LJF or FF alone in the treatment of ALI, and to explore whether LJF and FF have a combined effect in the treatment of lung injury, along with the underlying mechanism involved. Methods: A total of 36 mice were divided into six groups (control, model, LJF, FF, LF, dexamethasone) based on the treatments they received after undergoing sham-operation/LPS tracheal instillation. H&E staining and pulmonary edema indexes were used to evaluate lung injury severity. Alveolar exudate cells (AECs) were counted based on cell count in bronchoalveolar lavage fluid (BALF), and neutrophil percentage in BALF was measured using flow cytometry. Myeloperoxidase (MPO) activity in BALF was measured using enzyme-linked immunosorbent assay (ELISA), while the production of IL-1b, TNF-a, and IL-6 in the lung and secretion level of them in BALF were detected by quantitative polymerase chain reaction (qPCR) and ELISA. The effect of LJF, FF, and LF on the expression of caspase-1 and IL-1b proteins in bone marrow derived macrophages (BMDMs) supernatant was assessed using Western blot method under various inflammasome activation conditions. In addition, the concentration of IL-1b and changes in lactatedehydrogenase (LDH) release levels in BMDMs supernatant after LJF, FF, and LF administration, respectively, were measured using ELISA. Furthermore, the effects of LJF, FF and LF on STING and IRF3 phosphorylation in BMDMs were detected by Western blot, and the mRNA changes of IFN-b, TNF-a, IL-6 and CXCL10 in BMDMs were detected by qPCR. Results: LF significantly attenuated the damage to alveolar structures, pulmonary hemorrhage, and infiltration of inflammatory cells induced by LPS. This was evidenced by a decrease in lung index score and wet/dry weight ratio. Treatment with LF significantly reduced the total number of neutrophil infiltration by 75 % as well as MPO activity by 88 %. The efficacy of LF in reducing inflammatory factors IL-1b, TNF-a, and IL-6 in the lungs surpasses that of LJF or FF, approaching the effectiveness of dexamethasone. In BMDMs, the co-administration of 0.2 mg/mL of LJF and FF demonstrated superior inhibitory effects on the expression of nigericin-stimulated caspase-1 and IL-1b, as well as the release levels of LDH, compared to individual treatments. Similarly, the combination of 0.5 mg/mL LJF and FF could better inhibit the phosphorylation levels of STING and IRF3 and the production of IFN-b, TNF-a, IL-6, and CXCL10 in response to ISD stimulation. Conclusion: The combination of LJF and FF increases the therapeutic effect on LPS-induced ALI, which may be mechanistically related to the combined effect inhibition of cyclic-GMP-AMP synthase (cGAS)-stimulator of interferon genes (STING) and NOD-like receptor family protein 3 (NLRP3) inflammasomes pathways by LJF and FF. Our study provides new medicine candidates for the clinical treatment of ALI.

12 Integrative analysis of metabolome and transcriptome provides new insights into functional components of Lilii Bulbus

Wenjun Wei a , b , Tao Guo a , b , , Wenguang Fan c , Mengshan Ji a , b , Yu Fu a , b , Conglong Lian a , b , Suiqing Chen a , b , Wenjing M a c , Wenfang Ma d , Shuying Feng e ,

2024, 16(3):435-448. DOI: https://doi.org/10.1016/j.chmed.2023.10.004

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Objective: Lilium brownii var. viridulum (LB) and L. lancifolium (LL) are the main sources of medicinal lily (Lilii Bulbus, Baihe in Chinese) in China. However, the functional components of these two species responsible for the treatment efficacy are yet not clear. In order to explore the therapeutic material basis of Lilii Bulbus, we selected L. davidii var. willmottiae (LD) only used for food as the control group to analyze the differences between LD and the other two (LB and LL). Methods: Metabolome and transcriptome were carried out to investigate the differences of active components in LD vs LB and LD vs LL. Data of metabolome and transcriptome was analysed using various analysis methods, such as principal component analysis (PCA), hierarchical cluster analysis (HCA), and so on. Differentially expressed genes (DEGs) were enriched through KEGG and GO enrichment analysis. Results: The PCA and HCA of the metabolome indicated the metabolites were clearly separated and varied greatly in LL and LB contrasted with LD. There were 318 significantly differential metabolites (SDMs) in LD vs LB group and 298 SDMs in LD vs LL group. Compared with LD group, the significant upregulation of steroidal saponins and steroidal alkaloids were detected both in LB and LL groups, especially in LB group. The HCA of transcriptome indicated that there was significant difference in LB vs LD group, while the difference between LL and LD varied slightly. Additionally, 47 540 DEGs in LD vs LB group and 18 958 DEGs in LD vs LL group were identified. Notably, CYP450s involving in the biosynthesis of steroidal saponins and steroidal alkaloids were detected, and comparing with LD, CYP724, CYP710A, and CYP734A1 in LB and CYP90B in LL were all up-regulated. Conclusion: This study suggested that steroidal saponins and steroidal alkaloids maybe the representative functional components of Lilii Bulbus, which can provide new insights for Lilii Bulbus used in the research and development of classic famous formula.

13 HPLC combined with chemometrics for quality control of Huamoyan Granules or Capsules

Minhang Dou a , Jiayi Huang a , Mimi Yu b , Huahua Li a , Yang Song a , Ziwei Peng a , Shouying Du a , , Jie Bai a ,

2024, 16(3):449-456. DOI: https://doi.org/10.1016/j.chmed.2023.03.005

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Objective: Huamaoyan Granules (HMYG) and Huamaoyan Capsules (HMYC) are Chinese patent medicines with different dosage forms of the same prescription. Due to the different preparation process, the chemical composition of these Chinese patent medicines varies greatly among different forms, but there were few studies on the difference comparison and quality control of them. In order to improve the effectiveness and safety in its clinical application, an idea combining high performance liquid chromatography (HPLC) and chemometrics was put forward to study the quality control of Chinese patent medicines in different dosage forms of the same prescription. Methods: The differential markers of HMYG and HMYC were explored based on HPLC fingerprint and chemometrics including orthogonal projections to latent structures-discriminant analysis (OPLS-DA), principal component analysis (PCA), and hierarchical cluster analysis (HCA). Finally, the quantitative analysis method of related components was established by HPLC. Results: A quality control method for HMYG and HMYC was established. Firstly, the chemical components of HMYG and HMYC were systematically analyzed by HPLC fingerprinting. Further exploration showed that there were 20 characteristic peaks and 57 common peaks. Then, the potential differential markers between HMYG and HMYC were explored by chemometrics, and the differential markers were screened after intersection with the 20 characteristic peaks. Finally, HPLC quantitative analysis methods for nine components were established, including seven differential markers (neochlorogenic acid, protocatechualdehyde, chlorogenic acid, cryptochlorogenic acid, caffeic acid, rosmarinic acid and salvianolic acid A). The results of HPLC quantitative analysis showed that the contents of eight components in HMYG and HMYC samples were significantly different. According to the above results, the differential markers between HMYG and HMYC screened based on HPLC fingerprint and chemometrics can effectively characterize the differences between the two dosage forms. Conclusion: The present work provides a rapid and effective method for routine quality evaluation and control of HMYG and HMYC. This work also provides feasible methods for the quality evaluation and control of Chinese patent medicines with different dosage forms of the same prescription.

14 Comparative pharmacokinetics of six components in normal and rheumatoid arthritis rats after intragastrical administration of Qianghuo Shengshi Decoction granules by LC-MS/MS

Xin Li a , b , c , Min Wang a , b , c , Yuhong Zhong a , b , c , Qianqian Yin a , b , c , Zheming Hu a , b , c , Wenli Tian a , b , c , Zhongyan Liu a , b , c , Zhidong Liu a , b , c ,

2024, 16(3):457-465. DOI: https://doi.org/10.1016/j.chmed.2023.07.005

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Objective: To investigate the plasma pharmacokinetics of six representative components (nodakenin, osthole, 5-O-methylvisammioside, ferulic acid, liquiritigenin, and liquiritin), which were the ingredients of Qianghuo Shengshi Decoction (QSD) granules, in normal and rheumatoid arthritis (RA) rats administrated QSD granules intragastrically. Methods: A rapid and accurate ultra-high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed for the simultaneous determination of six components in plasma, and it showed a good specificity, linearity, intra-day and inter-day precision, intra-day and inter-day accuracy, extraction recovery, stability, and the less matrix effect. Results: The validated LC-MS/MS method was successfully used to compare the plasma pharmacokinetics of six ingredients between normal and RA rats after intragastrical administration of QSD granules and differences in the pharmacokinetics were found in two types of rats. The absorption rate in the RA rats was lower for nodakenin, osthole, 5-O-methylvisammioside, liquiritigenin and liquiritin than in the normal group, while the absorption rate of ferulic acid remained constant in two groups. In comparison with the normal rats, the exposure concentration of nodakenin was higher and that of other five components except for nodakenin was lower under pathological conditions. Additionally, the absorptive amount of nodakenin, osthole, 5-O-methylvisammioside and liquiritin was increased and that of ferulic acid and liquiritigenin was reduced in the RA rats than in the normal rats. Compared with the normal rats, the retention time of nodakenin, ferulic acid and liquiritin was reduced in vivo, whereas the retention time of osthole, 5-O methylvisammioside and liquiritigenin was raised in the body for the RA rats. In contrast to the normal rats, the data demonstrated an increase in the elimination velocity of nodakenin and a decrease in the elimination velocity of the other five components except for nodakenin in the pathological state. Conclusion: This study showed that the pharmacokinetic behavior of the six components, nodakenin, osthole, 5-O-methylvisammioside, ferulic acid, liquiritigenin, and liquiritin, is different in vivo between normal and pathological states of rats, and this research provided the necessary experimental data to explain the pharmacokinetics of QSD granules in both normal and pathological states and provide some references for its clinical application at some level.

15 Identification and characterization of chemical constituents in Mahuang Guizhi Decoction and their metabolites in rat plasma and brain by UPLC-Q-TOF/MS

Ping Wei a , Shiying Huang b , Juan Yang a , Mo Zhao a , Qiugu Chen b , Xiaoyu Deng a , Jianping Chen b , , Yisheng Li c ,

2024, 16(3):466-480. DOI: https://doi.org/10.1016/j.chmed.2024.01.006

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Objective: Mahuang Guizhi Decoction (MGD), an essential herbal pair in traditional Chinese medicine, is able to release cold, fever and asthma, mainly containing alkaloids, flavonoids, phenylpropanoids and amino acids. However, the absorption and distribution of these four category compounds in vivo still remained unclearly. Methods: In our research, we utilized UPLC-Q-TOF-MS technique to identify the constituents within MGD, as well as the prototypes of MGD and their metabolites absorbed in plasma and brain. We further profiled the drug-time curve of prototypes and metabolites of MGD both in plasma and brain. Results: Our results showed that 105 constituents were characterized in MGD. Thirty of them could be absorbed into blood, and ten of them could be distributed into brain. We also discovered eight new bio-transformed metabolites in blood, and a half of which could pass through the blood–brain barrier. In addition, all components detected in vivo could be absorbed and distributed immediately. Conclusion: These findings provide an approachable method to analyze the potential bio-active compounds in MGD and their in vivo behaviors, which could promote the efficacious material basis study of MGD and the security of clinical utilization.

16 Constituents from leaves of Macaranga hemsleyana

Joseph Sakah Kaunda a , Jia Liu b , Yaojun Xu a , Yuansi Chen a , Chenfang Yue a , Xingjie Zhang a , Ruihan Zhang a , Muhammad Amin a , Weilie Xiao a , Hongliang Li a , , Xiaoli Li a ,

2024, 16(3):481-486. DOI: https://doi.org/10.1016/j.chmed.2023.03.006

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Objective: To study constituents of the leaves of Macaranga hemsleyana, and evaluate their inhibitory effects against NOD-like receptor thermal protein domain associated protein 3 (NLRP3) inflammasome activation, and antiproliferative activity. Methods: The constituents were isolated and purified by column chromatography on MCI gel CHP20P/P120, silica gel, Sephadex LH-20, and HPLC. The structures of compounds were determined by 1D, 2D NMR, and HR-ESI-MS data. The inhibitory effect of compounds on inflammasome activation was determined by lactate dehydrogenase (LDH) procedure. The antiproliferative activity was evaluated using MTT assay. Results: The study led to the isolation of 23 compounds, including one new compound, identified as (2Z)-3-[4-(b-D-glucopyranosyloxy)-20-hydroxy-50-methoxyphenyl]-2-propenoic acid (1), together with 22 known compounds recognized as 1,4-dihydro-4-oxo-3 pyridinecarbonitrile (2), methyl 4-methoxynicotinate (3), 4-methoxynicotinonitrile (4), 1-(3-O-b-D-glucopyranosyl-4,5-dihydroxyphenyl)-ethanone (5), neoisoastilbin (6), isoastilbin (7), aromadendrin (8), neoastilbin (9), astilbin (10), quercitrin (11), neoschaftoside= (12), apigenin 6,8-bis-C-a-L-arabinoside (13), vitexin (14), bergenin (15), scopoletin (16), glucopyranoside salicyl (17), koaburside (18), benzyl b-D-glucoside (19), icariside B5 (20), roseoside (21), loliolide (22), and adenosine (23). The tested compounds did not show LDH inhibition nor antiproliferative activity. Conclusion: Compound 1 was a new glycoside. Compounds 2 and 3 were obtained for the first time from natural source. The 22 known compounds constituted of alkaloids (2–4, 23), phenolics (5, 15, 17, 18), flavonoids (6–14), coumarin (16), benzyl glycoside (19), and norsesquiterpenes (20–22). All the compounds, 1–23, were revealed from M. hemsleyana for the first time. This is the initial uncovering of molecules 1–10, 12, 13, 17–19, and 23 from the genus Macaranga. The isolated compounds, 11, 14–16, and 20–22 established taxonomic classification of M. hemsleyana in Euphorbiaceae family. Flavonoids were outstanding as chemosystematic markers of Macaranga genus.

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