Research status of Bovis Calculus and relevant Chinese patent medicines based on bibliometric analysis / 中国中药杂志

With scarce resources, natural Bovis Calculus is expensive and hard to meet clinical demand. At the moment, four kinds of Bovis Calculus are available on the market: the natural product, in vitro cultured product, synthesized product, and the product formed in cow after manual intervention. In this study, papers on the four kinds of Bovis Calculus products and relevant Chinese patent medicines were searched from Web of Science, PubMed, and China National Knowledge Infrastructure(CNKI). CiteSpace, citexs AI, and CNKI were employed for bibliometric analysis and knowledge map analysis. On this basis, the status, trend, and focuses of research on Bovis Calculus and relevant Chinese patent medicines were summarized. The results suggested overall slow development in the research on Bovis Calculus and relevant Chinese patent medicines with three typical growth stages. It is consistent with the development of Bovis Calculus substitutes and the national policy for the development of traditional Chinese medicine. At the moment, the research on Bovis Calculus and relevant Chinese patent medicines has been on the rise. In recent years, there has been an explosion of research on them, particularly the quality control of Bovis Calculus and the Chinese patent medicines, the pharmacological efficacy of Chinese patent medicines, such as Angong Niuhuang Pills, and the comparison of the quality of various Bovis Calculus products. However, there is a paucity of research on the pharmacological efficacy and the mechanism of Bovis Calculus. This medicinal and the relevant Chinese patent medicines have been studied from diverse perspectives and China becomes outstanding in this research field. However, it is still necessary to reveal the chemical composition, pharmacological efficacy, and mechanism through multi-dimensional deep research.

Research and development practice of traditional Chinese medicine based on network target theory and technology / 中国中药杂志

Network targets theory and technology have transcended the limitations of the "single gene, single target" model, aiming to decipher the mechanisms of traditional Chinese medicine(TCM) based on biological network from the perspective of informatics and system. As the core of TCM network pharmacology, with the development of computer science and high-throughput experimental techniques, the network target theory and technology are beginning to exhibit a trend of organic integration with artificial intelligence technology and high-throughput multi-modal multi-omics experimental techniques. Taking the network target analysis of TCM like Yinqiao Qingre Tablets as a typical case, network target theory and technology have achieved the systematic construction, in-depth analysis, and high-throughput multi-modal multi-omics validation of multi-level biological networks spanning from traditional Chinese and Western phenotypes to tissues, cells, molecules, and traditional Chinese and Western medicines. This development helps to address critical issues in the analysis of mechanisms of TCM, including the discovery of key targets, identification of functional components, discovery of synergistic effects among compound ingredients, and elucidation of the regulatory mechanisms of formulae. It provides powerful theoretical and technological support for advancing clinical precision diagnosis and treatment, precise positioning of TCM, and precise research and development of TCM. Thus, a new paradigm of TCM research gradually emerges, combining big data and artificial intelligence(AI) with the integration of human experience and scientific evidence.

Global progress in peptide radiopharmaceutical research and China's opportunities / 药学学报

Radiopharmaceutical is an essential component of nuclear medicine and molecular imaging, as well as a key component of precision medicine. The United States Food and Drug Administration (FDA) has recently approved the marketing of several peptide-based radiopharmaceuticals, sparking a global trend of research in this area and propelling nuclear medicine into the precision theranostic era. This has created a new wave of technological competition in the field of nuclear medicine. It is the responsibility of Chinese scientists in the radiopharmaceutical field to capitalize on this opportunity, leverage the momentum, and strengthen their independent innovation capability in order to stay ahead in the future global nuclear science and technology competition. This review provides an overview of the remarkable progress made in the research, development, and translation of global peptide-based radiopharmaceuticals. It examines the advantages of peptide-based radiopharmaceuticals and outlines the current hot targets and progress in drug development in this field. Additionally, it proposes six opportunities for China to overtake others in the field of peptide-based radiopharmaceuticals and achieve technological self-reliance, based on interdisciplinary collaboration and independent innovation. Lastly, the future prospect of peptide-based radiopharmaceuticals is discussed.

Anti-inflammatory effects of Abelmoschus manihot (L.) Medik. on LPS-induced cystitis in mice: potential candidate for cystitis treatment based on classic use / 中国天然药物

Abelmoschus manihot (L.) Medik. (A. manihot) is a traditional Chinese herbal medicine with a variety of pharmacological properties. It was first recorded in Jiayou Materia Medica dating back to the Song dynasty to eliminate urinary tract irritation by clearing away heat and diuretic effect. However, its pharmacological action on urinary tract infections has not been investigated. The present study aims to evaluate the anti-inflammatory activity of A. manihot on a mouse model of lipopolysaccharide (LPS)-induced cystitis. The results showed that A. manihot decreased white blood cell (WBC) count in urine sediments of the cystitis mice, alleviated bladder congestion, edema, as well as histopathological damage, reduced the expression levels of tumor necrosis factor-α, interleukin-6, and interleukin-1β simultaneously. Moreover, A. manihot administration significantly downregulated the expression levels of TLR4, MYD88, IκBα, p-IκBα, NF-κB p65, and p-NF-κB p65 in LPS-induced cystitis mice. These findings demonstrated the protective effect of A. manihot against LPS-induced cystitis, which is attributed to its anti-inflammatory profile by suppressing TLR4/MYD88/NF-κB pathways. Our results suggest that A. manihot could be a potential candidate for cystitis treatment.

Protective Effect of Ginsenosides Rg1 and Rb1 Against Intestinal Epithelial Barrier Injury Induced by Lipopolysaccharide in Vitro / 中国实验方剂学杂志

ObjectiveTo investigate the effects of ginsenoside Rg1 and ginsenoside Rb1 on the release of inflammatory factors of human myeloid leukemia monocytes （THP-1） induced by lipopolysaccharide （LPS） and their protective effects on the inflammatory injury of intestinal epithelial cells （Caco-2） induced by THP-1 cell activation based on the co-culture system of THP-1 and Caco-2. MethodFirstly，the microfluidic chip of co-culture of THP-1 and Caco-2 cells was prepared. In the experiment， a blank group， an LPS group， and drug intervention groups were set up.The cells in the blank group were cultured conventionally. In the LPS group，LPS （1 mg·L-1） was added to the lower THP-1 cells after the upper Caco-2 cells formed a monolayer barrier. On the basis of the LPS group， 33 mg·L-1 ginsenoside Rg1 and 33 mg·L-1 ginsenoside Rb1 were added to THP-1 cells respectively. After the co-culture of THP-1 cells and Caco-2 cells for 24 hours， the fluorescein isothiocyanate （FITC）-Dextran fluorescence value in the lower chip channel was detected by FITC-Dextran tracer method. A blank group， an LPS group，and drug intervention groups were set up in the THP-1 cell experiment. THP-1 cells in the blank group were cultured conventionally. In the LPS group， LPS （1 mg·L-1） was added to THP-1 cells.Ginsenoside Rg1 and ginsenoside Rb1 of the corresponding doses （11，33，100 mg·L-1） were added to the drug intervention groups respectively on the basis of the LSP group. After 24 hours of cell culture， the activity of THP-1 cells was detected by cell counting kit-8 （CCK-8）. Real-time quantitative polymerase chain reaction （Real-time PCR） was used to detect the expression of inflammatory cytokines such as interleukin-6 （IL-6）， interleukin-1β （IL-1β）， and tumor necrosis factor （TNF）-α of THP-1 cells. A blank group， an LPS group， and drug intervention groups were set up in the Caco-2 cell experiment. Caco-2 cells in the blank group were cultured conventionally， and in other groups， the corresponding cell supernatant in the second part of the THP-1 cell experiment was employed in Caco-2 cells. After 24 hours of cell culture，the activity of Caco-2 cells was detected by CCK-8. Real-time PCR was used to detect the expression of IL-6，interleukin-8 （IL-8）， TNF-α， and Occludin of Caco-2 cells. The expression of tight junction protein Occludin in Caco-2 cells was detected by Western blot. ResultBoth ginsenoside Rg1 and ginsenoside Rb1 could effectively protect LPS-induced intestinal epithelial barrier permeability in the co-culture system of THP-1 and Caco-2 cells （P<0.01）. Ginsenosides Rg1 and Rb1 antagonized LPS-induced increased expression of IL-6，IL-1β， and TNF-α in THP-1 cells （P<0.05）. When the supernatant of THP-1 cells treated with ginsenosides Rg1 and Rb1 was co-cultured with Caco-2 cells， the expression of IL-6，IL-8， and TNF-α in Caco-2 cells was significantly reduced （P<0.01）， and the expression of tight junction protein Occludin was up-regulated. ConclusionIn the co-culture system of THP-1 and Caco-2 cells simulating the intestinal epithelial barrier function in vitro，ginsenosides Rg1 and Rb1 play a protective role against LPS-induced intestinal epithelial barrier injury by regulating the release of inflammatory cytokines by THP-1 cells， thereby regulating the inflammatory response and cell barrier integrity of Caco-2 cells.

Cdkn2a Tracer Mice: A Novel Model to Study Cellular Senescence in Post-traumatic Osteoarthritis / 中国生物化学与分子生物学报

Osteoarthritis (OA) is one of the most common geriatric motor system diseases in the clinical practice. Aging, whose hallmark is cellular senescence, is an important factor leading to the occurrence and development of OA, but its exact role in the pathological development of OA is not completely clear. Studies have proved that targeting senescence can effectively treat aging-related diseases. In this study, the heterozygous mouse model of Cdkn2a-e (Luc-2A-tdTomato-2a-CreerT2-Wpre-PA)1 was established by the CRISPR/ Cas9 technique. The expression of Cdkn2a (p16, p16INK4a), a classical marker of senescence, can be traced in vivo in mice. We then utilized anterior cruciate ligament transection (ACLT) to induce OA in Cdkn2a mice, and we hope to verify the relationship between aging and the occurrence and development of OA and visualize aging changes during OA development through the mice model. In this study, 10-12 weeks old Cdkn2a mice were randomly divided into no surgery control group, sham operation group and ACLT group. OA model was constructed in mice by ACLT operation. After surgery for 4 weeks, animals were collected for fluorescence imaging detection in vivo, which showed that local fluorescence expression of Cdkn2a increased in knee joints of mice in the ACLT group four weeks after surgery (P < 0. 05) . The Safranin O-Fast Green Staining of mouse knee tissue sections showed degeneration of the knee cartilage in the ACLT group at 4 weeks after surgery (P < 0. 05) . Immunohistochemical staining of Cdkn2a was performed on the knee tissue of mice. Compared with the other two groups, Cdkn2a staining on the cartilage surface of the knee tissue of mice in the ACLT group was deeper. The results showed that the OA model induced by surgery showed local aging, which further verified the relationship between aging and OA. At the same time, the Cdkn2a tracer mouse model can reflect the aging progress of mice in vivo, with combination of imaging examinations, so that the occurrence and progress of the relationship between aging and OA can be observed in real time. This heterozygous mouse model of Cdkn2a-e(Luc-2A-tdTomato-2a-CreerT2-Wpre-PA) 1 is not only useful for mechanism research of aging and OA diseases, but also beneficial for finding more potential therapy targets to OA and aging.

Forensic Progress on Death Following Carotid Sinus Inhibition / 法医学杂志

Death after carotid sinus trauma is usually attributed to death from inhibition, a type of sudden death. Currently, the number of incidents is scarce, and related studies are few. Therefore, how to determine the involvement of carotid sinus and determine the role of diseases in the cause of death has always been a difficult point in forensic investigation. This article sorts out the research literature on carotid sinus related death at home and abroad in recent years, systematically reviews the anatomic structure of the carotid sinus nerve, the clinical epidemiology of carotid sinus syndrome, and the research on the death mechanism of carotid sinus injury at home and abroad in recent years, in order to provide references for forensic pathology research and prosecution.

Role of Puerariae Lobatae Radix in Gegen Decoction for treatment of primary dysmenorrhea / 中国中药杂志

This study aimed to explore the characteristic role of Puerariae Lobatae Radix(PLR) in Gegen Decoction for the treatment of primary dysmenorrhea(PD). Estrogen(E_2) was combined with oxytocin to establish a mouse model of PD. The mice were randomly divided into a normal group, a model group, a Gegen Decoction group, a PLR-free Gegen Decoction group, a PLR group, and a positive drug group(ibuprofen). Writhing response times and writhing incubation of mice in each group were tested by behavio-ral assessment, and the serum levels of prostaglandin F_(2α)(PGF_(2α)), prostaglandin E_2(PGE_2), E_2, and progesterone(PROG) were detected by ELISA kits. Western blot method was adopted to detect cyclooxygenase-2(COX-2) and estrogen receptor alpha(ER_α) expression levels in uterine tissues. Doppler ultrasound was employed to detect changes in uterine artery blood flow in mice, including peak systolic blood flow velocity(maximum velocity), end-diastolic velocity(minimum velocity), peak systolic blood flow velocity/end-diastolic velocity(S/D), pulsatility index(PI), and resistive index(RI). Histopathological changes in the uterus were detected by HE staining. Based on the oxytocin-induced isolated uterine contraction model, the effects of Gegen Decoction, PLR-free Gegen Decoction, and PLR on the amplitude, frequency, and activity of isolated uterine contraction were compared to investigate the role of PLR in Gegen Decoction for the treatment of PD. The results showed that compared with the Gegen Decoction group, the PLR-free Gegen Decoction improved the indicators of PD except for E_2 content, ER_α expression, and uterine artery blood flow. PLR could significantly down-regulate the serum content of E_2 and the protein expression of uterine ER_α, and improve the uterine artery blood flow. The data suggested that PLR, as the sovereign drug of Gegen Decoction, might function in Gegen Decoction for the treatment of PD by mediating E_(2 )and improving the uterine artery blood flow.

Analysis on ingredients and metabolites of Gegen Decoction absorbed into blood based on UHPLC-Q-TOF-MS / 中国中药杂志

This study analyzed the plasma components of Gegen Decoction(GGD) by ultra-high-performance liquid chromatography-quadrupole-time of flight mass spectrometry(UHPLC-Q-TOF-MS), which is expected to serve as a reference for exploring the pharmacodynamic substances of GGD. Female Wistar rats were given(ig) GGD and then plasma samples were collected and analyzed by UHPLC-Q-TOF-MS. The results showed that 42 chemical components were identified: 25 prototypes(14 from Puerariae Lobatae Radix, 6 from Glycyrrhizae Radix et Rhizoma, 3 from Paeoniae Radix Alba, and 2 from Ephedrae Herba) and 17 metabolites(from isoflavonoids in Puerariae Lobatae Radix and Glycyrrhizae Radix et Rhizoma). UHPLC-Q-TOF-MS was employed to achieve rapid analysis of plasma components of GGD, laying a basis for elucidating the therapeutic material basis and mechanism of GGD.

Analysis on new research and development ideas and technical points of traditional Chinese medicine for prevention and treatment of chronic heart failure / 中国中药杂志

Chronic heart failure(CHF), a serious and end stage of various heart diseases, is a common chronic cardiovascular disease in the 21 st century. Literature data show that the 5-year mortality rate of hospitalized patients with heart failure is as high as 50%. Nowadays, the development of drugs treating heart failure has become a hot spot, meanwhile, traditional Chinese medicine(TCM) has shown the advantages in the treatment of chronic heart failure. In this article, four stages to develop traditional Chinese medicine for chronic heart failure were proposed. Firstly, discuss and screen ideas and methods with regard to the development of TCM and its prescriptions based on clinical needs. Secondly, study the preparation process and quality control method by referring to the existing clinical background of TCM prescriptions and analyzing the chemical compositions and pharmacological action characteristics of each herb in the prescription. Then, design non-clinical evaluation programs and carry out researches on pharmacodynamics and toxicology by combining the experience of clinical use of TCM prescriptions and future clinical positioning, and gradually adjust and improve the programs during implementation. Finally, conduct clinical trial application(IND) by submitting registration application data which are base on the clinical drug experience, preclinical research pharmacy, main pharmacodynamics, safety test results of the prescription, clinical positioning, and reasonable clinical trial plan designed by the theory of TCM. After passing the IND technical review, the clinical trial study shall be officially launched to achieve the desired results and obtain effective Chinese patent medicines for heart failure treatment.

Analysis of Chemical Variability on Different Processed Products of Glycyrrhiza uralensis Dry Roots and Rhizomes Based on UPLC-Q-TOF-MSE and Plant Metabolomics / 中国实验方剂学杂志

Objective:To identify the quality differential markers of different processed products of Glycyrrhiza uralensis dry roots and rhizomes. Method:Ultra-high performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MSE) was used to collect high-precision mass-charge ratio and ion response strength information of the components in G. uralensis dry roots and rhizomes before and after processing by negative ion mode. The data set collected after pretreatment was analyzed with principal component analysis (PCA) and orthogonal partial least squares-discriminant analysis (OPLS-DA) to quickly search the differential components in different processed products of G. uralensis dry roots and rhizomes. Differential components were identified according to the relative molecular weight, fragment ion, mass spectrum database and related literature information, then the migration of components before and after processing was studied. Result:A total of 10 quality differential markers were searched from raw products, roasted products and honey-roasted products of G. uralensis dry roots and rhizomes, mainly derivatives of liquiritin and glycyrrhizic acid. Among them, the contents of 6''-O-acetylliquiritin apioside, 6''-O-acetylliquiritin apioside isomer, 6''-O-acetylliquiritin, formononetin and 11-deoxo-18β-glycyrrhetic acid were the highest in the raw products, the contents of 6''-O-acetylisoliquiritin apioside, 6''-O-acetylisoliquiritin, isoliquiritin and glycyrrhetic acid 3-O-glucuronide were the highest in the roasted products, the content of liquiritin was the lowest in the honey-roasted products. Conclusion:There are some chemical differences among the three products. This study can provide material basis for the quality control and pharmacodynamic research of processed products of G. uralensis dry roots and rhizomes.

Study on protective effect of vanillic acid from Astragalus membranaceus on hypertensive cardiac remodeling based on network pharmacology screen / 中国中药杂志

To identify and verify the active ingredients from Astragalus membranaceus on hypertensive cardiac remodeling based on network pharmacology and heart RNA-sequencing data. The monomers of A. membranaceus and their intervention target database were established by using network pharmacology. The genes associated to cardiac remodeling were then screened by analyzing cardiac RNA-sequencing data. An overlap between genes related to cardiac remodeling and targets of ingredients form A. membranaceus was collected to obtain monomers with protective effect on hypertensive cardiac remodeling. Angiotensin Ⅱ(AngⅡ)-induced mouse cardiac remodeling model was used to validate the protective effect of active ingredients from A. membranaceus on hypertensive cardiac remodeling. Finally, a total of 81 monomers and 1 197 targets were enrolled in our database. Mouse RNA-sequencing data showed that 983 genes were significantly up-regulated and 465 genes were down-regulation in myocardial tissues of the cardiac remodeling mice as compared with blank group mice, respectively. Ninety-two genes were found via overlapping between genes related to cardiac remodeling and targets, involving 59 monomers from A. membranaceus. Further research found that vanillic acid(VA) could intervene 27 genes associated with hypertensive cardiac remodeling, ranking top 1. Meanwhile, VA could significantly inhibit AngⅡ-induced increase in ratio of heart weight to body weight and heart weight to tibial length, ANP and BNP mRNA levels in myocardial tissues, myocardial tissue damage, cardiac fibrosis level and cardiac hypertrophy level in vivo. Those results showed that network pharmacology screen-based VA has protective effect on AngⅡ-induced cardiac remodeling.

Discussion on Research and Development of Following Original Methods of Famous Classical Formulas——Taking Xiebaisan as an Example / 中国实验方剂学杂志

The National Medical Products Administration intends to simplify the registration and approval process of the classic Chinese herbal compound preparations that meet the requirements, but it is a prerequisite for obtaining preferential policies that the preparation method and the route of administration are consistent with the records of ancient medical books. As most of the famous classical formulas are recorded in the medical books of the Qing dynasty and before the Qing dynasty, during the use of medicinal materials in various dynasties, the processing of herbs, dose of medicinal herbs, and the method of decocting may have changed. If researchers simply adopt modern methods to study the formula, it is easy to deviate from policy requirements. The strengthening of preliminary data survey and definition of prescription component and the medication situation of the dynasties can provide strong theoretical support for the study of famous classical formulas. Based on this, the authors take Xiebaisan as an example, which being collected in the First Batch of Catalogue of Ancient Classical Formulas. By following the principles of ancient methods, the research and development ideas of the classic Chinese herbal compound preparations were expounded from the aspects of origin of medicinal materials, processing of medicinal materials, preparation of standard decoction and quality standard of Xiebaisan granules, so as to provide a referential method for the development and research of the famous classical formulas.

Novel analgesic targets and corresponding analgesic leading compounds / 中国药理学与毒理学杂志

Opioid medications have been used for pain management, but there are negative side effects, including a potential delay in recovery and increased risk of permanent disability. In this paper, analgesic targets including N-methyl-D-aspartate receptors, cannabinoid receptors, prostaglandin E2 receptor 4 receptors, matrix metalloproteinase receptors, and some new targets for blocking pain signaling pathways associated with these receptors are reviewed. In addition, some novel agonists, antagonists, and leading compounds with agonistic (antagonistic) activities interacting with the target are also described. These novel compounds usually have better analgesic activity and lower side effects than traditional opioids. They are expected to be developed into new analgesics and benefit clin?ical patients who need pain treatment.

Exploration on method and strategy of Gegen decoction from its novel application in primary dysmenorrhea / 中国中药杂志

Many classical prescriptions still have superior clinical values nowadays, and their modern studies also have far-reaching scientific research demonstration values. Gegen decoction, a representative prescription for common cold due to wind-cold, can treat primary dysmenorrhea due to cold and dampness, characterized by continuous administration without recurrence. It is not only in accordance with the principle of homotherapy for heteropathy, but also demonstrates the unique feature of traditional Chinese medicine of relieving the primary and secondary symptoms simultaneously. This article aimed to discuss the method and strategy of Gegen decoction study based on the discovery of its novel application in treatment of primary dysmenorrhea and previous research progress of our group. It was assumed that modern medicine and biology studies, as well as chemical research based on biological activity should be used for reference. Principal active ingredients (groups) in Gegen decoction could be accurately and effectively identified, and its possible mechanism in treatment of primary dysmenorrhea could be eventually elucidated as well. Simultaneously, the theoretical and clinical advantages of traditional Chinese medicine were explored in this paper, focusing on the compatibility characteristics of Gegen decoction. The research hypothesis showed the necessity of following the characteristics and advantages of traditional Chinese medicine in the modern research and reflected the importance of basic research based on the clinical efficacy, expecting to provide some ideas and methods for reference for further modern studies of classical prescriptions.

Morphological and chemical studies of artificial Andrographis paniculata polyploids / 中国天然药物

Andrographis paniculata (Burm. f.) Nees (AP) is commonly used for the treatment of many infectious diseases and has been cultivated widely in Asian countries, and has been included in United States Pharmacopoeia as a dietary supplement, but the cultivars of A. paniculata are not abundant due to its self-pollinated. With the aims to enrich AP resources and provide materials for after breeding we explored the polyploidy induction. Different explants, colchicine concentration, and treatment time were tested. After identification by flow cytometry, eleven polyploid plants with different morphologic traits were obtained. The agronomic traits and andrographolide concentration of the polyploids were improved greatly. One of the polyploids (serial 3-7) was chosen for further study. The traits of the second and third generation polyploids (serial 3-7) were stable. Compared with the normal plants, the seeds (2nd generation) weight increased by 31%, and the andrographolide concentration of the leaves increased by 14% (2nd) and 28% (3rd). In conclusion, AP autopolyploids with different morphologic traits were established successfully for the first time, and the polyploids induction might be effective for crop improvement of AP.

Identification of active compound combination contributing to anti-inflammatory activity of Xiao-Cheng-Qi Decoction via human intestinal bacterial metabolism / 中国天然药物

Human intestinal bacteria play an important role in the metabolism of herbal medicines, leading to the variations in their pharmacological profile. The present study aimed to investigate the metabolism of Xiao-Cheng-Qi decoction (XCQD) by human intestinal bacteria and to discover active component combination (ACC) contributing to the anti-inflammatory activity of XCQD. The water extract of XCQD was anaerobically incubated with human intestinal bacteria suspensions for 48 h at 37 °C. A liquid chromatography-hybrid quadrupole time-of-flight mass spectrometry (LC-Q-TOF/MS) method was performed for identification of the metabolites. In addition, the anti-inflammatory effects of XCQD and biotransformed XCQD (XCQD-BT) were evaluated in vitro with cytokines in RAW264.7 cells induced by lipopolysaccharide (LPS). A total of 51 compounds were identified in XCQD and XCQD-BT. Among them, 20 metabolites were proven to be transformed by human intestinal bacteria. Significantly, a combination of 14 compounds was identified as ACC from XCQD-BT, which was as effective as XCQD in cell models of inflammation. In conclusion, this study provided an applicable method, based on intestinal bacterial metabolism, for identifying combinatory compounds responsible for a certain pharmacological activity of herbal medicines.

Advances in the antitumor activities and mechanisms of action of steroidal saponins / 中国天然药物

The steroidal saponins are one of the saponin types that exist in an unbound state and have various pharmacological activities, such as anticancer, anti-inflammatory, antiviral, antibacterial and nerves-calming properties. Cancer is a growing health problem worldwide. Significant progress has been made to understand the antitumor effects of steroidal saponins in recent years. According to reported findings, steroidal saponins exert various antitumor activities, such as inhibiting proliferation, inducing apoptosis and autophagy, and regulating the tumor microenvironment, through multiple related signaling pathways. This article focuses on the advances in domestic and foreign studies on the antitumor activity and mechanism of actions of steroidal saponins in the last five years to provide a scientific basis and research ideas for further development and clinical application of steroidal saponins.

Morphological and chemical studies of artificial Andrographis paniculata polyploids / 中国天然药物

Andrographis paniculata (Burm. f.) Nees (AP) is commonly used for the treatment of many infectious diseases and has been cultivated widely in Asian countries, and has been included in United States Pharmacopoeia as a dietary supplement, but the cultivars of A. paniculata are not abundant due to its self-pollinated. With the aims to enrich AP resources and provide materials for after breeding we explored the polyploidy induction. Different explants, colchicine concentration, and treatment time were tested. After identification by flow cytometry, eleven polyploid plants with different morphologic traits were obtained. The agronomic traits and andrographolide concentration of the polyploids were improved greatly. One of the polyploids (serial 3-7) was chosen for further study. The traits of the second and third generation polyploids (serial 3-7) were stable. Compared with the normal plants, the seeds (2nd generation) weight increased by 31%, and the andrographolide concentration of the leaves increased by 14% (2nd) and 28% (3rd). In conclusion, AP autopolyploids with different morphologic traits were established successfully for the first time, and the polyploids induction might be effective for crop improvement of AP.

Identification of active compound combination contributing to anti-inflammatory activity of Xiao-Cheng-Qi Decoction via human intestinal bacterial metabolism / 中国天然药物

Human intestinal bacteria play an important role in the metabolism of herbal medicines, leading to the variations in their pharmacological profile. The present study aimed to investigate the metabolism of Xiao-Cheng-Qi decoction (XCQD) by human intestinal bacteria and to discover active component combination (ACC) contributing to the anti-inflammatory activity of XCQD. The water extract of XCQD was anaerobically incubated with human intestinal bacteria suspensions for 48 h at 37 °C. A liquid chromatography-hybrid quadrupole time-of-flight mass spectrometry (LC-Q-TOF/MS) method was performed for identification of the metabolites. In addition, the anti-inflammatory effects of XCQD and biotransformed XCQD (XCQD-BT) were evaluated in vitro with cytokines in RAW264.7 cells induced by lipopolysaccharide (LPS). A total of 51 compounds were identified in XCQD and XCQD-BT. Among them, 20 metabolites were proven to be transformed by human intestinal bacteria. Significantly, a combination of 14 compounds was identified as ACC from XCQD-BT, which was as effective as XCQD in cell models of inflammation. In conclusion, this study provided an applicable method, based on intestinal bacterial metabolism, for identifying combinatory compounds responsible for a certain pharmacological activity of herbal medicines.