Properties Of Traditional Chinese Medicine Research Articles

Database-aided ultrahigh-performance liquid chromatography Q-Exactive-Orbitrap tandem mass spectrometry putatively identifies 16 unexpected compounds and three anticounterfeiting pharmacopoeia quality markers for Perillae Fructus.

Perillae Fructus (PF) is a common traditional Chinese medicine (TCM) for the treatment of asthma. It has not been effectively characterized by rosmarinic acid (RosA), which is currently designed as the sole quality indicator in the Chinese Pharmacopoeia. This study introduced a database-aided ultrahigh-performance liquid chromatography equipped with quadrupole-Exactive-Orbitrap mass spectrometry (UHPLC/Q-Exactive-Orbitrap MS/MS) technology to putatively identify the compounds in PF, followed by literature research, quantum chemical calculation, and molecular docking to screen potential quality markers (Q-markers) of PF. A total of 27 compounds were putatively identified, 16 of which had not been previously found from PF. In particular, matrine, scopolamine, and RosA showed relatively high levels of content, stability, and drug-likeness. They exhibited interactions with the asthma-related target and demonstrated the TCM properties of PF. The database-aided UHPLC/Q-Exactive-Orbitrap MS/MS can identify at least 27 compounds in PF. Of these, 16 compounds are unexpected, and three compounds (matrine, scopolamine, and RosA) should be considered anticounterfeiting pharmacopoeia Q-markers of PF.

Impact of Preparative Isolation of C-Glycosylflavones Derived from Dianthus superbus on In Vitro Glucose Metabolism.

Dianthus superbus L. has been extensively studied for its potential medicinal properties in traditional Chinese medicine and is often consumed as a tea by traditional folk. It has the potential to be exploited in the treatment of inflammation, immunological disorders, and diabetic nephropathy. Based on previous studies, this study continued the separation of another subfraction of Dianthus superbus and established reversed-phase/reversed-phase and reversed-phase/hydrophilic (RPLC) two-dimensional (2D) high-performance liquid chromatography (HPLC) modes, quickly separating two C-glycosylflavones, among which 2″-O-rhamnosyllutonarin was a new compound and isomer with 6‴-O-rhamnosyllutonarin. This is the first study to investigate the effects of 2″-O-rhamnosyllutonarin and 6‴-O-rhamnosyllutonarin on cellular glucose metabolism in vitro. First, molecular docking was used to examine the effects of 2″-O-rhamnosyllutonarin and 6″-O-rhamnosyllutonarin on AKT and AMPK; these two compounds exhibited relatively high activity. Following this, based on the HepG2 cell model of insulin resistance, it was proved that both of the 2″-O-rhamnosyllutonarin and 6‴-O-rhamnosyllutonarin demonstrated substantial efficacy in ameliorating insulin resistance and were found to be non-toxic. Simultaneously, it is expected that the methods developed in this study will provide a basis for future studies concerning the separation and pharmacological effects of C-glycosyl flavonoids.

The Classification Study and Categorization of Medicinal Properties in Traditional Chinese Medicine

The Classification Study and Categorization of Medicinal Properties in Traditional Chinese Medicine

L-Borneol promotes skin flap survival by regulating HIF-1α/NF-κB pathway

Ethnopharmacological relevanceThe clinical application of skin flaps in surgical reconstruction is frequently impeded by the occurrence of distant necrosis. L-Borneol exhibits myogenic properties in traditional Chinese medicine and is used in clinical settings to promote wound healing and conditions such as stroke. Nevertheless, the precise mechanism by which borneol exerts its protective effects on skin flap survival remains unclear. Aim of the studyTo explore the potential of L-borneol to promote skin flap survival and elucidate the underlying mechanisms. Materials and methodsThirty-six male Sprague–Dawley rats were randomly divided into three groups: a high-dose (200 mg/kg L-borneol per day), a low-dose (50 mg/kg/day), and control group (same volume of solvent). In each rat, a modified rectangular McFarlane flap model measuring 3 × 9 cm was constructed. Daily intragastric administration of L-borneol or solvent was performed. The flap was divided into three square sections of equal size, namely Zone I (the proximal zone), Zone II (the intermediate zone), and Zone III (the distal zone). The survival rate was quantified, and the histological state of each flap was evaluated on the seventh day following the surgical procedure. The assessment of angiogenesis was conducted using lead oxide/gelatin angiography, whereas the evaluation of blood flow in the free flap was performed using laser Doppler flow imaging. Superoxide dismutase activity was detected using the water-soluble tetrazolium salt-8 method. The quantities of vascular endothelial growth factor, interleukin (IL)-1β, IL-6, and tumour necrosis factor-α were determined using immunohistochemistry. The levels of nuclear transcription factor-κB, hypoxia-inducible factor-1, B-cell lymphoma-2 (BCL-2), and BCL-2-associated X (BAX) were determined by Western blotting technique. ResultsFlap survival rate significantly improved and neutrophil recruitment and release were enhanced after treatment with the compound. Angiogenesis was promoted. L-borneol protected against oxidative stress by increasing superoxide dismutase activity and decreasing malondialdehyde content. It downregulated the hypoxia-inducible factor nuclear transcription factor-κB pathway, leading to the inhibition of several inflammatory factors. Simultaneously, it facilitated the expression of vascular endothelial growth factor and BCL-2. ConclusionThe study shows that L-borneol may promote skin flap survival by inhibiting HIF-1α/NF-κB pathway.

Perspective on the Modern Interpretation of the Property Theory of Mild-natured and Sweet-flavored Traditional Chinese Medicine via Gut Microbiota Modulation

ABSTRACT The property theory of traditional Chinese medicine (TCM) has guided its clinical application for thousands of years. Although the TCM modernization project has made significant progress, several challenges, such as identifying modern biological indicators, remain. Recent investigations have demonstrated that the gut microbiota contributes to the metabolism and efficacy of TCMs, providing a potential indicator of TCM properties. To investigate whether the gut microbiota can partially interpret the property theory of TCM, we searched the “PubMed” and “China National Knowledge Infrastructure” databases using “gut microbiota” and “traditional Chinese medicine” as keywords. This review mainly focused on the relationship between mild-natured and sweet-flavored TCMs (MS-TCMs) and the gut microbiota. We discovered that MS-TCMs can recalibrate the gut microbiota to alleviate various diseases. At the family level, MS-TCMs upregulated Erysipelotrichaceae, Verrucomicrobiaceae, Bacteroidaceae, Christensenellaceae, Lactobacillaceae, and Prevotellaceae, while downregulating Enterobacteriaceae, Rikenellaceae4, and S24-7. At the genus level, MS-TCMs increased the abundance of Ruminococcus, Turicibacter, Parabacteroides, Dubosiella, Bifidobacterium, Bacteroides, Lactobacillus, Oscillospira, and Prevotella, and decreased the abundance of Parasutterella, Mucispirillum, Lachnoclostridium, Escherichia, Enterococcus, Butyricicoccus, Clostridiales, Blautia, Desulfovibrio, and Oscillibacter. Mechanistically, changes in gut bacteria can influence the levels of metabolites such as short-chain fatty acids, lipopolyaccharides, and neurotransmitters, which further regulate a series of physiological signaling pathways within the host. Overall, analyzing the TCM–microbiota interaction is an effective means to reveal the mechanisms of TCM, suggesting that the gut microbiota can be developed into a modern indicator of TCM properties.

Fermentation of Ganoderma lucidum and Raphani Semen with a probiotic mixture attenuates cyclophosphamide-induced immunosuppression through microbiota-dependent or -independent regulation of intestinal mucosal barrier and immune responses

BackgroundProbiotic fermentation is a promising strategy for improving the nutritional and functional properties of traditional Chinese medicines (TCMs). Ganoderma lucidum and Raphani Semen are famous TCMs that have been shown to help alleviate immune system disorders. However, few studies have experimentally investigated the effects of probiotic-fermented G.lucidum and Raphani Semen on the immune system. PurposeWe established the in vitro fermentation of G. lucidum and Raphani Semen with a probiotic mixture (Bifidobacterium longum, Lactobacillus acidophilus, and l. fermentum) (GRFB), investigated its ameliorating effect against cyclophosphamide (CTX)-induced immunosuppression, and explored its possible mechanisms. MethodsFirst, the different components in GRFB were identified by high-performance liquid chromatography. Second, its immune-stimulatory activities were evaluated in CTX-treated mice. Lastly, its possible in vitro and in vivo mechanisms were studied. ResultsProbiotic fermentation of G. lucidum and Raphani Semen altered some of its chemical constituents, potentially helping improve the ability of GRFB to alleviate immunosuppression. As expected, GRFB effectively ameliorated CTX-induced immunosuppression by increasing the number of splenic lymphocytes and regulating the secretion of serum and ileum cytokines. GRFB supplementation also effectively improved intestinal integrity in CTX-treated mice by upregulating tight junction proteins. It also protects against CTX-induced intestinal dysbiosis by increasing the abundance of beneficial bacteria and reducing the abundance of harmful bacteria. GRFB could directly promote intestinal immunity but not systemic immunity in vitro, suggesting a microbiota-dependent regulation of GRFB. Interestingly, cohousing CTX-induced immunosuppressed mice with GRFB-treated mice promoted their symptoms recovery. Enhanced CTX-induced immunosuppression by GRFB in vitro depended on the gut microbiota. Remarkably, a Kyoto Encyclopedia of Genes and Genomes analysis showed that the GRFB-reprogrammed microbiota was significantly enriched in DNA damage repair pathways, which contribute to repairing the intestinal mucosal barrier. ConclusionThis is the first study to suggest that compare with unfermented G. lucidum and Raphani Semen, GRFB can more effectively promote intestinal immunity and manipulate the gut microbiota to promote immunostimulatory activity and repair immunosuppression-induced intestinal barrier damage by biotransforming G.lucidum and Raphani Semen components.

First Report of Penicillium subrubescens Causing Root Rot of Knoxia roxburghii in China.

Knoxia roxburghii (syn. Knoxia valerianoides), locally known as 'Zi Daji', is a perennial herb that belongs to the Rubiaceae family, cultivated in different areas of China and recognized for its medicinal properties in traditional Chinese medicine (Chen et al. 2022). In 2021, root rot was observed during summer on K. roxburghii in Xiangyun and Dali, Yunnan Province (25°25'N, 100°40'E), China. Root rots were characterized by dark brown tissue from stem base to root, loss of vitality in tender leaves and wither. Three symptomatic root samples of K. roxburghii collected from different fields were rinsed with running water, and 0.5-1 cm2 fragments of diseased tissues were cut and surface-disinfested with 75% ethanol for 30 s, and 1% NaClO for 180 s. The fragments were then washed with sterile water, transferred to potato dextrose agar (PDA, 4.6%) and incubated at 28℃ in the dark for 3 days. A total of 13 isolates with consistent appearances were obtained by single spore isolation. These colonies on PDA showed gray and light brown obverse, and light green reverse after 10 days. The average growth rate was 3 mm per day. Conidia were nearly spherical or broadly elliptic, greyish-green, and 1.4-2.4×1.3-2.2 μm in size (n=50). The conidiophore has symmetrical or asymmetrical broom branches from the tip, with 2-4 small stems. The conidiophore branching patterns were predominantly biverticillate; stipes coarsely roughened, 80-210×2.6-3.0 μm; metulae were usually appressed verticils of 3-6, 6.4-12.5×1.6-3.0 μm; phialides were short and wide neck, 3.8-4.8×1.1-1.8 μm (n=30). The morphological characteristics of the fungus were identical to Penicillium (Mansouri et al. 2013). To further identify the isolate, one isolate (ByF10) was randomly selected for identification. DNA was extracted from mycelia using a simplified CTAB method. Primer pairs, ITS1/ITS4 and Bt2a/Bt2b were used to amplify the partial regions of rDNA internal transcribed spacer (ITS) and β-tubulin (TUB), respectively (White et al. 1990; Glass and Donaldson 1999). Blast searches showed that the sequences of ITS (OQ954757) and TUB (OQ970059) of isolate ByF10 were 99% (MH865456) and 100% (KC797611) identical with P. subrubescens CBS 130205 and CBS 129617, respectively. A concatenated phylogenetic tree (ITS+TUB) constructed using the maximum likelihood method showed that ByF10 was closely grouped next to isolates of P. subrubescens. Pathogenicity test was carried out using 1-year-old healthy seedlings of K. roxburghii cv. Yunji-1 growing on autoclaved soil (n=10). Ten plants were inoculated with mycelial blocks (5 mm2), which were taken from the colony margins of a 10-day-old culture (PDA) colony, and placed on the roots near the soil. Five control plants were inoculated with non-colonized PDA plugs. The pathogenicity test was repeated three times. All plants were kept at 25℃, 70% relative air humidity, and 12 h light/12 h regime dark for 35 days. After that period 95% of inoculated plants showed typical symptoms of root browning. P. subrubescens was only re-isolated from the inoculated plants, and identified based on morphological and molecular characteristics. No symptoms were observed in the controls. To the best of our knowledge, this is the first report of P. subrubescens causing root rot on K. roxburghii in China and the world.

Antidepressant effect of Perilla frutescens essential oil through monoamine neurotransmitters and BDNF/TrkB signal pathway

Ethnopharmacological relevanceTraditional Chinese medicine posits that affect-mind ill-being is the primary cause of depression, with Qi movement stagnation as its pathogenesis. As such, clinical treatment for depression should prioritize regulating Qi and relieving depressive symptoms. The pharmacological properties of traditional Chinese medicine indicate that Perilla frutescens may have potential therapeutic effects on depression and other neuropsychiatric diseases due to its ability to regulate Qi and alleviate depressive symptoms. Although previous studies have reported the antidepressant effects of Perilla frutescens, the mechanism underlying PFEO inhalation-mediated antidepressant effect remains unclear. Aim of the studyThe aim of this investigation is to elucidate the antidepressant mechanisms of PFEO by examining its effects on monoamine neurotransmitters and the BDNF/TrkB signaling pathway. Materials and methodsThe CUMS rat model of depression was established, and the depressive state of the animals was assessed through sucrose preference and forced swim tests. ELISA assays were conducted to determine monoamine neurotransmitter levels in the hippocampus and cerebral cortex of rats. Immunohistochemistry, western blotting, and RT-PCR experiments were employed to investigate the BDNF/TrkB signaling pathway's regulation of depression via PFEO inhalation. ResultsIt has been observed that inhalation administration of PFEO can significantly enhance the preference for sugar water in CUMS rats and reduce their immobility time during forced swimming. Additionally, there was an increase in the levels of monoamine transmitters in both the hippocampus and cerebral cortex of these rats. Furthermore, there was an upregulation in the expression levels of BDNF and TrkB positive cells as well as BDNF and TrkB proteins within both regions, along with increased BDNF mRNA and TrkB mRNA expression levels. ConclusionThe antidepressant effect of PFEO via inhalation administration is speculated to be mediated through the monoamine neurotransmitters and BDNF/TrkB signaling pathway.

The linkage of gut microbiota and the property theory of traditional Chinese medicine (TCM): Cold-natured and sweet-flavored TCMs as an example.

The property theory of traditional Chinese medicine (TCM) is a unique medical theory based on an extensive clinical practice for thousands of years, which guides TCM doctors choosing proper medicines to treat specific diseases. The nature and flavor of TCM are a high generalization of drug's characteristics according to the property theory. Despite intensive investigations, the modern interpretation of TCM property theory still confronts several challenges, which greatly hampers the elucidation of TCM's mechanisms as well as its application. Compelling evidence has proved that gut microbiota may be a potential indicator for TCM's efficacy and mechanism. Nevertheless, at present, the relationship between the gut microbiota and the nature and flavor of TCM has not been fully elucidated. To fill the gap in this field, we developed a comprehensive study to investigate the relationship between gut microbial community and TCM's property. We searched "PubMed" and "China National Knowledge Infrastructure (CNKI)" with the key word "gut microbiota", and screened the published articles related to TCM. In this review, we mainly applied cold-natured and sweet-flavored TCMs as an example to explore the modulation of cold-natured and sweet-flavored TCMs on gut microbiota, and identify the potential relationship between the alterations of gut microbiota and TCM's efficacy. We found cold-natured and sweet-flavored TCMs possess several pharmacological activities and generally enrich beneficial bacteria like Akkermansia, Bacteroides, Lactobacillus and Bifidobacterium, which is in good accordance with their pharmacological effects. Simultaneously, these TCMs reduce the relative abundance of some harmful bacteria belonging to Firmicutes (Streptpcoccus, Enterococcus, Turicibacter, Anaerostipes and Oscillibacter) and Proteobacteria (Helicobacter, Enterobacter, Sutterella, Klebsiella, Desulfovibrio, Escherichia coli and Campylobacter jejuni). These results indicate that there are some intrinsic correlations between gut microbiota and the property of TCM, and gut microbiota may serve as a potential indicator to reflect the property of TCM. This pilot but comprehensive review provides an interesting proposal that the ancient theory of TCM property may be interpreted by the modern biological findings in gut microbiome.

[Classification optimization of traditional Chinese medicine materials based on additive physical properties of powder].

According to the method of predicting the physical properties of oily powder based on the additive physical properties of Chinese medicinal powder, Dioscoreae Rhizoma and calcined Ostreae Concha with high sieve rate and good fluidity were mixed and crushed with Persicae Semen, Platycladi Semen, Raphani Semen, Ziziphi Spinosae Semen, and other typical oily materials with high fatty oil content in proportion to obtain 23 mixed powders. Fifteen physical properties such as bulk density, water absorption, and maximum torque force were measured, and the physical properties of typical oily powders were predicted. When the mixing and grinding ratio was in the range of 5∶1-1∶1, the r value in the correlation equation between the weighted average score of the mixed powder and the powder proportion ranged from 0.801 to 0.986, and the linearity was good, indicating that the method of predicting the physical properties of oily powder based on the additive physical properties of traditional Chinese medicine(TCM)powder was feasible. The results of cluster analysis showed that the classification boundaries of the five kinds of TCM materials were clear, and the similarity of the physical fingerprints of powdery and oily materials decreased from 80.6% to 37.2%, which solved the problem of fuzzy classification boundaries of powdery and oily materials due to the lack of representativeness of oily material model drugs. The classification of TCM materials was optimized, laying a foundation for optimizing the prediction model of the prescription of personalized water-paste pills.

[Properties of new exotic traditional Chinese medicinal Vernonia amygdalina leaves:a literature research].

The leaves of Vernonia amygdalina Delile of the family Asteraceae(also known as "bitter leaf"), rich in biological activities, are used as both medicine and food for a long time in West tropical Africa. They have been introduced into Southeast Asia and Fujian and Guangdong provinces of China in recent years. However, little is known about the properties of the plant in traditional Chinese medicine(TCM), which limits its combination with other Chinese medicinal herbs. In this study, 473 articles on V. amygdalina leaves were selected from PubMed, Web of Science, CNKI, Wanfang Data and VIP to summarize their components, pharmacological effects and clinical research. V. amygdalina leaves presented anti-microbial, hypoglycemic, anti-hypertensive, lipid-lowering, anti-tumor, anti-inflammatory, antioxidant, and other pharmacological effects. On the basis of the theory of TCM properties, the leaves were inferred to be cold in property and bitter and sweet in flavor, acting on spleen, liver, stomach and large intestine and with the functions of clearing heat, drying dampness, purging fire, removing toxin, killing insects and preventing attack of malaria. They can be used to treat dampness-heat diarrhea, interior heat and diabetes, malaria, insect accumulation and eczema(5-10 g dry leaves by decoction per day and an appropriate amount of crushed fresh leaves applying to the affected area for external use). Due to the lack of TCM properties, V. amygdalina leaves are rarely used medicinally in China. The determination of medicinal properties of the leaves is conducive to the introduction of new exotic medicinal herbs and the development of new TCM resources, which facilitated further clinical application and research and development of Chinese medicinal herbs.

Investigation on property differences of ginseng and American ginseng by spatial metabolomics of neurochemicals with desorption electrospray ionization mass spectrometry imaging

Ethnopharmacological relevanceThe properties are the body's response to traditional Chinese medicine (TCM). The essence of traditional Chinese medicine properties are cold, hot, warm, and cool. In the theory of traditional Chinese medicine, ginseng is warm and American ginseng is cool, they present two opposite properties. The material basis of property differences and effect mechanism of property degree need further investigation. Aim of the studyThe aim of this work was to screen out the neurochemicals related to warm and cool properties of ginseng and American ginseng, and investigate the distributions of identified neurochemicals in rat brain and the metabolic mechanism. Materials and methodsSpatial metabolomics was applied to study the effects of ginseng and American ginseng on the distributions of neurochemicals in rat brain by desorption electrospray ionization mass spectrometry imaging (DESI-MSI). Based on discriminant coefficients in partial least square discriminant analysis (PLS-DA) processing, neurochemicals related to warm and cool properties were classified. In addition, the score contributions of the neurochemicals markers could be used to evaluate the warm and cool property degrees. ResultsA total of 25 neurochemicals were imaged and identified in brain section. The distribution regions of main neurochemicals were consistent with in sagittal and coronal sections of brain reported in literature. 17 neurochemicals were classified as warm markers. Meanwhile, 8 neurochemicals were identified as cool markers, correlated with the cool properties of American ginseng. It demonstrated that the score contributions of the 25 neurochemicals markers could be used to evaluate the warm and cool property degrees. Based on the regulatory effects of neurochemicals, the warm markers could promote the body's energy metabolism, improve the function of endocrine system, and enhance the excitability of central nervous system. The cool property markers have reduced excitability of central nervous system, weakened metabolism and stress response ability, thus presented the biological activity of cool and cold. ConclusionsOur findings provided a rapid and effective visualization method for the spatial distribution and metabolism of small molecular neurochemicals in rat brain. DESI-MSI was a reference methodology for evaluating the properties of TCM.

UPLC-Q-Exactive-based rats serum metabolomics for characterization of traditional Chinese medicine Natures and Flavors

Ethnopharmacology relevant“Four Natures and five “Flavors” comes from the high generalization of medicine pharmacological rules from clinical practice by ancients. “Flavor” and “Natures”are both descriptions of the effect properties of traditional Chinese medicine. At present, researchers have realized that the “Flavors” (Pungent, Sour, Sweet, Bitter and Salty) are related to the different pharmacological effects of treatment. The “Natures” (Warm, Hot, Cold and Cool) are closely related to energy and substance metabolism and contribute to the effect of the “Flavors”. Since “Four Natures and five Flavors” are the rules derived from clinical practice, how to describe and characterize “Natures” and “Flavors” scientifically is still a problem that needs to be solved. Aim of the studythe aim is to objectively further understand the scientific connotations of properties (“Flavors”and “Natures”) from the perspective of metabolomics and characterize them by metabolites. Materials and method“Pungent-Neutral”, “Sweet-Neutral and “Bitter-Neutral” TCMs were selected to characterize the “Flavors” (Pungent, Sweet and Bitter). “Pungent-Warm” and “Bitter-Cold” were selected to characterize the “Natures” (Warm and Cold). The rat serum metabolomics was performed on UHPLC-Q-Exactive. Metabolites were identified through the metabolites databases and related literature. ResultsThe “Flavors” and “Natures” metabolites were identified, respectively, including four “Pungent”, four “Sweet” and thirteen “Bitter” characterized metabolites and thirteen “Cold” and sixteen “Warm”related metabolites. ConclusionsThe “Natures” characterized metabolites show the “Natures” are closely related to lipid and energy metabolism. The “Warm” may promote lipid metabolism to produce ATP to generate energy through bile acid metabolism and purine metabolism. The “Cold” may inhibit lipid metabolism to generate ATP to decrease energy through the way of tryptophan metabolism and purine metabolism. The “Flavors” characteristic metabolites can provide a theoretical basis for the rules of the “Flavors”. These metabolites can also be used to characterize TCM's “Natures” and “Flavors” in the development of traditional Chinese medicine resources and quality control.

Antimicrobial mechanisms of traditional Chinese medicine and reversal of drug resistance: a narrative review.

In recent years, the extensive use of antibiotics worldwide has led to an increase in the number of drug-resistant bacterial strains, thus resulting in an increasingly severe degree of bacterial resistance. For thousands of years, traditional Chinese medicine (TCM) has provided natural and unique advantages in the treatment of infectious diseases. Therefore, it is important to develop further and use TCM to treat clinical infections caused by drug-resistant bacteria. A literature search was performed using PubMed, Web of Science, Google Scholar, and the China National Knowledge Infrastructure databases. The articles were analyzed to extract information on the antimicrobial effects of Chinese herbal medicines, compounded Chinese medicines, monomeric compounds of herbal origin, and the combined use of Chinese medicine and antimicrobial drugs and to determine the synergistic effect of the combination of Chinese medicine and antibiotics, as well as investigate the possibility of restoring the antibiotic sensitivity of drug-resistant strains. The mechanisms underlying the antibacterial properties of TCM involve altering membrane permeability, inhibiting protein and nucleic acid synthesis, inhibiting enzyme activity in vivo, and controlling the ability of pathogenic bacteria. In addition, the mechanism underlying TCM-induced reversal of bacterial drug resistance is discussed, particularly in terms of the elimination of resistant (R) plasmids and the inhibition of extended-spectrum β-lactamases, bacterial biofilm formation, and bacterial efflux pump activity. This paper reviewed the recent relevant literature on antimicrobial action and its mechanisms, as well as the mechanisms of drug resistance reversal by TCM to provide a reference for clinical drug use, prevention and control of bacterial infection, and research and development of new drugs.

Definition of the molecular bases of cold and hot properties of traditional Chinese medicine through machine learning

The purpose of this study is to confirm whether the 'cold-hot properties' of traditional Chinese medicine (TCM) have modern scientific connotations on the molecular level of compounds using machine learning (ML).In this study, 393 Chinese herbs were selected, modeling was based on three ML algorithms, and the voting fusion algorithm was used to construct the fusion model. According to the ROC area under the curve (AUC), the cold-hot herb property classification model was screened. The a priori and K-means algorithms were used to mine key molecules related to cold-hot properties.The AUC of the ML models and fusion models under the ROC curve after 10 rounds of folding cross-verification was above 0.75. Mining obtained 15 cold key compounds (CKCs), 26 hot key compounds (HKCs), a CKC structure similarity of 0.75 on average, and an HKC structure similarity of 0.69 on average. The average similarity between the molecular structures of CKCs compounds and HKCs compounds was 0.18, lower than 0.5. Twelve physical and chemical indices, such as molecular weight (MW) and molecular hydrophobicity (Alogp), had a statistically significant difference in molecular characteristics (P<0.05).In this study, the classification model and algorithm (RF&GNB Ensemble Classifier) of TCM cold-hot properties constructed from the molecular level of compounds are robust. At the same time, it was found that Chinese herbs with the same medicinal properties had a common molecular structure, while Chinese herbs with different medicinal properties had different molecular structures. In terms of physicochemical characteristics, compounds have statistically significant differences.

K Value: An Indicator that can Characterize the Cold and Hot Properties of Traditional Chinese Medicines.

Aims: The cold and hot properties of Chinese medicines are an important concept to represent the function of drugs, and are also a unique classification method of traditional Chinese medicine (TCM). The method reflects an herb’s therapeutic properties and guides reasonable clinical prescription. However, the present key problem is the lack of an objective and quantitative evaluation index for the cold and hot properties of Chinese herbs. Delayed luminescence (DL) is the long-term afterglow of biological systems after illumination with light, which can reflect differences in herbal materials prepared under different conditions. We aim to use S. obliquus as an indicator organism to characterize the differences between the cold and hot properties of Chinese herbs. Methods: Scenedesmus obliquus (S. obliquus) was used as an indicator organism to characterize the differences between the cold and hot properties of Chinese herbs. The decoction solution of different properties of Chinese herbs was added to S. obliquus culture medium; then, the delayed luminescence (DL) of S. obliquus after the addition of decoctions of different properties of Chinese herbs was measured to obtain information on the effect of different properties of Chinese herbs on S. obliquus. Many DL parameters were calculated, and ROC curve analysis was applied with the aim of finding a suitable parameter that can characterize the differences in cold and hot properties of Chinese herbs. Results: Our results show that the K value is a sensitive parameter that can reflect the differences of cold and hot properties of Chinese herbs, thus providing new insights into the cold and hot properties of Chinese herbs. Conclusions: DL measurement of S. obliquus after addition of different properties of Chinese herbs could be a novel and promising method to study the cold and hot properties of Chinese herbs.

Effect of Traditional Chinese Medicine on the Cardiovascular Diseases.

Background: Traditional Chinese medicine (TCM) is the health care system developed with the help of clinical trials that are based ideally on the scientific model of regulation. Objective: This systematic health care system relies on some specific unique theories and practical experiences to treat and cure diseases, thus enhancing the public’s health. Review Methodology: The current review covers the available literature from 2000 to 2021. The data was collected from journals research articles, published books, thesis, and electronic databases, search engines such as Google Scholar, Elsevier, EBSCO, PMC, PubMed, ScienceDirect, Willey Online Library, Springer Link, and CNKI) searching key terms, cardiovascular disease, traditional Chinese medicines, natural products, and bioactive compounds. Full-length articles and abstracts were screened for the collection of information included in the paper. Results: Clinical trials on the TCM and basic research carried out on its mechanism and nature have led to the application and development of the perfect design of the research techniques, for example, twofold striking in acupuncture that aid in overcoming the limitations and resistances in integrating and applicability of these experiences and trials into the pre-existing biomedical models. Furthermore, TCM has also been utilized from ancient times to treat heart diseases in Asia, particularly in China, and is now used by people in many other areas. Cardiovascular disease (CVD) is mainly developed by oxidative stress. Hence antioxidants can be beneficial in treating this particular disease. TCM has a wide variety of antioxidant components. Conclusion: The current review article summarizes the underlying therapeutic property of TCM and its mechanism. It also overviews the evidence of the mechanism of TCM action in CVD prevention by controlling oxidative stress and its signaling pathway.

Quantification of "Cold-Hot" Medicinal Properties of Chinese Medicines Based on Primary Metabolites and Fisher's Analysis.

Background Chinese medicinal properties (CMP) are an important part of the basic theory of traditional Chinese medicines (TCMs). Quantitative research on the properties of TCMs is of great significance to deepen the understanding and application of the theory of drug properties and promoting the modernization of TCMs. However, these studies are limited to strong subjectivity or distinguish different drug properties based on certain indicators since CMP studies are diverse. Objective To realize quantitative comparison of same medicinal properties of different Chinese medicines. Method To solve the above problem, we proposed and explored quantification of Chinese medicinal properties (QMP) and the quantification value of medicinal properties “R”. The correlation between primary metabolites and “cold-hot” medicinal properties was explored on the premise of material basis of Chinese herbal medicines and Fisher's analysis. Based on indicators related to “cold-hot” medicinal properties, we utilized quantitative values “R” to characterize the strength or weakness of “cold-hot” medicinal properties. Results According to QMP, the same medicinal properties were quantified and compared by quantification value of medicinal properties that expressed by alphabet “R”. The general theoretical formula of “R” deduced is R = (‖l‖ × cos θ)/‖L‖ = ∑i=1njipi/∑i=1npi2, in which n ≥ 1. In the light of formula of “R” and indicators related to “cold-hot” medicinal properties, we got “R” value of “cold-cool” and “warm-hot” medicinal properties. “R” values of “cold-cool” medicinal properties of Phellodendri chinensis cortex, Coptidis rhizoma, and Menthae haplocalycis herba were 0.63, 1.00, and 0.49, respectively. The result showed that Coptidis rhizoma is the most “cold-cool”, followed by Phellodendri chinensis cortex, with Menthae haplocalycis herba is the weakest in the three Chinese medicines, consistent with cognition of TCM theory. Conclusion QMP has certain guiding significance for the quantification of “cold and hot” drug properties. “R” is feasible to realize the quantitative comparison of the same drug properties of different traditional Chinese medicine, which is helpful to promote process of modern Chinese medicine construction.

Research on Cold and Hot Properties of Traditional Chinese Medicine at the Molecular Level Based on Machine Learning

Research on Cold and Hot Properties of Traditional Chinese Medicine at the Molecular Level Based on Machine Learning

Design, synthesis and bioactivity evaluation of novel N-phenyl-substituted evodiamine derivatives as potent anti-tumor agents

Natural products are important sources for the development of therapeutic medicine, among which evodia fruit has a wide range of medicinal properties in traditional Chinese medicine. Evodiamine, the main active component of evodia fruit, has various anti-cancer effects and has been proved to be a Topo inhibitor. From our previous attempts of modifying evodiamine, we found that the N14 phenyl substituted derivatives had showed great anti-tumor activity, which prompted us to further explore the novel structures and activities of these compounds. Compound 6f, as a N14 3-fluorinated phenyl substituted evodiamine derivative, showed a certain inhibitory activity against Topo I at 200 μM. By studying its anti-tumor effects in vitro, compound 6f could inhibit proliferation and induce apoptosis, as well as arrest the cell cycle of HGC-27 and HT-29 cell lines at G2/M phase in a concentration-dependent manner. Moreover, compound 6f could inhibit the migration and invasion of HGC-27 cell lines. Meanwhile, compound 6f could induce apoptosis of HGC-27 cells by inhibiting PI3K/AKT pathway. Overall, this work demonstrated that the N14 phenyl-substituted evodiamine derivatives had a good inhibitory effect on tumor cells in vitro, providing a promising strategy for developing potential anticancer agents for the treatment of gastrointestinal tumors.