Traditional Medicine Compound Research Articles

Therapeutic potential of Bergenin in the management of neurological-based diseases and disorders.

Originally sourced from plants, Bergenin has been used as a medicinal compound in traditional medicine for centuries, and anecdotal reports suggest a wide range of therapeutic uses. Naturally-occurring and lab-synthesized Bergenin, as well as some of its related compounds, have been shown in in vivo and in vitro studies to alter activity of several enzymes and proteins critical in cellular functioning, including reelin, GSK-3β, Lingo-1, Ten-4, GP-43, Aβ 1-42, P-tau, SOD1,2, GPx, Glx1, NQO1, HO1, PPAR-ɣ, BDNF, VEGF, and STAT6. Additionally, Bergenin alters levels of several cytokines, such as IL-6, IL-1β, TNF-α, and TGF-β. Behavioral and cellular effects of Bergenin have been shown to involve PI3K/Akt, NF-κB, PKC, Nrf2, and Sirt1/FOXO3a pathways. These pathways, enzymes, and proteins have been shown to be important in normal neurological functioning, and/or dysfunctions in these pathways and proteins have been shown to be important in several neuro-based disorders or diseases, which suggests that Bergenin could be therapeutic in management of neuropsychiatric conditions or neurological disorders. In preclinical studies, Bergenin has been shown to be useful for the management of Alzheimer's disease, Parkinson's disease, anxiety, depression, addiction, epilepsy, insomnia, stroke, and potentially, state control. Our review aims to summarize current evidence supporting the conclusion that Bergenin could play a role in treating various neuro-based disorders and that future studies should be conducted to evaluate the mechanisms by which Bergenin could exert its therapeutic effects.

Nrf2 Activation in Keratinocytes: A Central Role in Diabetes-Associated Wound Healing.

Wound healing is a complex biological process crucial for tissue repair, wherein keratinocytes play a pivotal role in initiating, sustaining and completing the cascade. Various local and systemic factors, such as lifestyle, age metabolic disorders and vascular insufficiency, can influence this process, and in the context of diabetic wounds, disrupted biological mechanisms, including inflammation, tissue hypoxia, decrease in collagen production along with increased oxidative stress and keratinocyte dysfunction, contribute to delayed healing. During re-epithelialisation, keratinocytes undergo rapid multiplication and migration, forming a dense hyperproliferative epithelial layer that restores the epidermal barrier. Nuclear factor-erythroid 2-related factor (Nrf2), a vital transcription factor, emerges as a central regulator in managing antioxidant proteins and detoxifying enzymes, serving as a guardian against elevated reactive oxygen species (ROS) levels during stress. Nrf2 also orchestrates angiogenesis and anti-inflammatory responses crucial for wound repair. Studies demonstrate that under high-glucose conditions, Nrf2 activation promotes wound healing by enhancing cell proliferation and migration while reducing apoptosis. Nrf2 activators stimulate endogenous antioxidant production, thereby mitigating oxidative stress. Furthermore, Nrf2 upregulation is associated with decreased expression of cytokines such as TNF-α and IL- 6. Recent research underscores the potential of bioactive molecules, including dietary polyphenols, traditional medicinal compounds and pharmacological agents, in activating Nrf2 and preventing diseases such as diabetes due to their robust antioxidative properties. This review aims to investigate the activation of Nrf2 by these bioactive molecules in cultured keratinocytes and animal models, elucidating the key molecular regulatory mechanisms involved in alleviating oxidative stress and facilitating the diabetic wound healing process. Understanding these complex pathways may offer insights into novel therapeutic strategies for enhanced wound healing in diabetes-associated complications.

Pharmacological targeting of adaptor proteins in chronic inflammation.

Inflammation, a biological response of the immune system, can be triggered by various factors such as pathogens, damaged cells, and toxic compounds. These factors can lead to chronic inflammatory responses, potentially causing tissue damage or disease. Both infectious and non-infectious agents, as well as cell damage, activate inflammatory cells and trigger common inflammatory signalling pathways, including NF-κB, MAPK, and JAK-STAT pathways. These pathways are activated through adaptor proteins, which possess distinct protein binding domains that connect corresponding interacting molecules to facilitate downstream signalling. Adaptor molecules have gained widespread attention in recent years due to their key role in chronic inflammatory diseases. In this review, we explore potential pharmacological agents that can be used to target adaptor molecules in chronic inflammatory responses. A comprehensive analysis of published studies was performed to obtain information on pharmacological agents. This review highlights thetherapeutic strategies involving small molecule inhibitors, antisense oligonucleotide therapy, and traditional medicinal compounds thathave been found to inhibit the inflammatory response and pro-inflammatory cytokine production. These strategies primarily block the protein-protein interactions in the inflammatory signaling cascade.Nevertheless, extensive preclinical studies and risk assessment methodologies are necessary to ensure their safety.

Molecular Docking and Dynamic Simulation Studies of Bioactive Compounds from Traditional Medicinal Compounds Against Exfoliative Toxin B from Staphylococcus aureus

Background Staphylococcal scalded skin syndrome (SSSS) is a dermatological condition caused by Staphylococcus aureus, characterized by exfoliative toxin B, and its increasing resistance to conventional antibiotics necessitates the search for new therapeutic options. Aim The study aimed to investigate the potential of traditional medicinal compounds (TMCs) as potential pharmaceuticals against SSSS using molecular-level research. Introduction Staphylococcus aureus, commonly known as S. aureus, is the main cause of SSSS. These infections are a major concern for public health because they are becoming resistant to antibiotics. There is an urgent need for new medications to effectively fight against this infection. The main objective of this study was to assess the interaction between TMC compounds and S. aureus exfoliative toxins ETA and ETB utilizing computational approaches. Materials and Methods The investigation selected TMC compounds based on their potential to combat S. aureus infections. To predict binding affinities with the ETB toxin, molecular docking simulations were performed using AutoDock and AutoDock Vina. In order to evaluate the stability and interaction dynamics with the toxins, the most promising compound was subjected to a 100 ns molecular dynamics simulation. Stability was evaluated through various methods. Results Liquiritin showed the highest binding affinity, with a docking score of −7.6 kcal/mol. MD simulation confirmed the complex’s stability, and the binding free energy of −17.76 kcal/mol indicated potent inhibitory activity against S. aureus ETB. Conclusion Liquiritin, a TMC, effectively inhibits S. aureus toxins ETB, with promising potential for treating SSSS and antibiotic-resistant infections, requiring further research.

Research on the Medicinal Chemistry and Pharmacology of Taxus × media.

Taxus × media, belonging to the genus Taxus of the Taxaceae family, is a unique hybrid plant derived from a natural crossbreeding between Taxus cuspidata and Taxus baccata. This distinctive hybrid variety inherits the superior traits of its parental species, exhibiting significant biological and medicinal values. This paper comprehensively analyzes Taxus × media from multiple dimensions, including its cultivation overview, chemical composition, and multifaceted applications in the medical field. In terms of chemical constituents, this study delves into the bioactive components abundant in Taxus × media and their pharmacological activities, highlighting the importance and value of these components, including paclitaxel, as the lead compounds in traditional medicine and modern drug development. Regarding its medicinal value, the article primarily discusses the potential applications of Taxus × media in combating tumors, antibacterial, anti-inflammatory, and antioxidant activities, and treating diabetes. By synthesizing clinical research and experimental data, the paper elucidates the potential and mechanisms of its primary active components in preventing and treating these diseases. In conclusion, Taxus × media demonstrates its unique value in biological research and tremendous potential in drug development.

Machine-learning-based virtual screening and ligand docking identify potent HIV-1 protease inhibitors

The human immunodeficiency virus type 1 (HIV-1) is a retrovirus that can cause acquired immunodeficiency syndrome (AIDS), severely weakening the immune system. The United Nations estimates that there are 37.7 million people with HIV worldwide. HIV-1 protease (PR) cleaves polyproteins to create the individual proteins that comprise an HIV virion. Inhibiting PR prevents the creation of new virions, rendering PR an attractive antiviral target. In the present study, a machine-learning regression model was constructed to predict pIC50 bioactivity concentrations using data from 2547 experimentally characterized PR inhibitors. The model achieved Pearson correlation coefficient of 0.88, R-squared of 0.78, and a RMSE of 0.717 in pIC50 units on unseen data using 199 high-variance PubChem substructure fingerprints. The SWEETLEAD database of approximately 4300 traditional medicine compounds and drugs from around the world was screened using the model. Fifty molecules were identified as highly potent, with pIC50 of at least 7.301 (IC50 <= 50 nM). Nine of these molecules, such as lopinavir and ritonavir, are known antiviral drugs. The highly potent molecules were ligand-docked to the 3D structure of HIV protease at the active site. Dihydroergotamine mesylate (daechu alkaloids) had a very strong binding affinity of −13.2, outperforming all known antiviral drugs that were tested. It was also predicted by the model to have an IC50 of 9.16 nM, which is considered very low and desirable. Overall, this study demonstrates the use of machine-learning regression models for virtual screening and highlights several drugs with significant promise for repurposing against HIV-1. Future steps include testing dihydroergotamine mesylate and other candidates in vitro.

Simultaneous Analysis of 12 Aphrodisiacs in Traditional Medicine using Liquid Chromatography-Tandem Mass Spectrometry

People tend to consume traditional medicines compared to synthetic drugs due to their safety and low side effects. The high demand of traditional medicine consumption in public stimulates some traditional medicine industries illegally add medicinal chemicals into their products to elevate the therapeutic effect. In order to accelerate the monitoring program of product quality and safety, the availability of a rapid and reliable analytical method becomes a necessity. The research aims to determine the validity of the liquid chromatography-tandem mass spectrometry (LC-MS) and its application to simultaneously identify 12 aphrodisiac compounds in male sexual enhancer traditional medicine. The chromatography system used an ion modifier of 0.1% formic acid. The mass spectrometer was equipped with a triple quadrupole (TQD) as a mass analyzer in a positive mode of ESI. The analysis was conducted in multiple reaction monitoring (MRM) transition. Qualitative analysis was performed using retention time (Rt) of peaks in each compound, within their value of m/z quantifier and qualifier ions. Method validation was performed by evaluating the profile of selectivity, precision, matrix effect, and limit of detection (LOD). A qualitative analysis of the selectivity test was carried out by comparing the retention times between the blank sample added with the reference standards (spiked sample) and those in reference standards, with a difference of ±1minute shifts. Precision analysis on intra-day precision gives results in the range of 2.0–8.6%. The method showed that there was no matrix effect with the extraction efficiency values ranging from 86.2 to 110.9%. The LOD values for the 12 compounds were in the range of 1.6 ± 0.58 to 18.2 ± 6.14 µg/g. The method can be applied to test 49 samples of male sexual enhancer traditional medicines consisting of powder, capsules, solutions, soft capsules, and caplets dosage forms. The tested samples contained 8 (eight) types of aphrodisiac compounds. This study shows that LC-MS can be used to confirm the content of aphrodisiac compounds in traditional medicinal samples.

Therapeutic target mapping from the genome of Kingella negevensis and biophysical inhibition assessment through PNP synthase binding with traditional medicinal compounds.

Kingella negevensisbelongs to the Neisseriaceae family. It is implied that it has significant virulence potential due to RTX toxin production, which can cause hemolysis. It usually colonizes the orophayrynx of pediatric population, along with Kingella kingae but has also been isolated from vagina. Todate no report on its drug targets is present, therefore putative therapeutic targets were identified from its genomic sequence data. Traditional Chinese (n > 36,000) and Indian medicinal compounds (n > 2000) were then screened against its pyridoxine 5'-phosphate synthase, a vital therapeutic target. Prioritized TCM compounds included ZINC02525131, ZINC33833737 and ZINC85486932, and Cadiyenol, 9,11,13-Octadecatrienoic acid and 6-Gingerol from Indian medicinal library. Molecular dynamics simulation of top compounds revealed ZINC02525131 as having best stability for 100ns, compared to Cadiyenol. ADMET profiling was then done, along with physiologically based pharmacokinetic simulation of these compounds in a population of 200 individuals, for 12h to see fate of the ingested compound. Additionally, the impact of these compounds in a population with cirrhosis and renal impairment was also simulated. We imply in light of all the studied parameters of safety and bioavailability, etc., that 6-Gingerol from Zingiber officinalis rhizome must be proceeded further for in vitro and in vivo testing for inhibition of K. negevensis.

Discovery of the directionally detoxification effect and chemical mechanism of Ginseng-Fuzi co-decoction based on real-time online filtration electrospray ionization mass spectrometry

BackgroundThe synergic action of compound prescriptions is an important feature and core advantage of traditional medicine. Ginseng-Fuzi decoction is a classic compatible phytomedicine in China, of which Ginseng can effectively reduce the toxicity of Fuzi in clinical, but the detoxification chemical mechanism is still unclear. PurposeDevelop a novel method for real-time tracking and monitoring of complex substances in the decoction system of traditional Chinese medicine to uncover the detoxification effect Ginseng on Fuzi and explore the possible chemical reaction mechanism of Ginseng-Fuzi co-decoction. MethodsA novel real-time monitoring system, online filtration electrospray ionization mass spectrometry, was developed for extremely complex substances analysis in the decoction of traditional medicine compounds to uncover the directionally detoxification effect and the mechanism of compatibility interaction. ResultsNine key alkaloids and 7 ginsenosides in Ginseng-Fuzi decoction were simultaneously in-situ monitoring in positive ion mode or negative ion mode respectively. Both types of targeted analytes had satisfactory MS signal response for real-time qualitative and quantitative analysis with high precision (RSD < 14.04%) and low LLODs (0.002 ng/ml-10 ng/ml). Through long-term tracking analysis, the exact detoxification and synergistic effect of Ginseng-Fuzi decoction were confirmed as the concentration of main toxic alkaloids decreased (e.g. the content of mesaconitine has been reduced by about 38%) and the main active monoester alkaloids increased obviously. More importantly, the possible molecular mechanism of the detoxification effect of Ginseng compatibility was revealed for the first time, which was the nucleophilic substitution reaction of diester alkaloids catalyzed by fatty acids. ConclusionThis study revealed the exact effect of co-decoction of Ginseng and Fuzi at the molecular level and the chemical reaction mechanism of fatty acid-catalyzed degradation of toxic diester-type alkaloids. The comprehensive multi-component real-time monitoring strategy for complex traditional medicine compounds developed and implemented here has important demonstration significance for revealing the scientific connotation of the compatibility of compound traditional medicine.

Chemical composition of Gastrocotyle hispida (Forssk.) bunge and Heliotropium crispum Desf. and evaluation of their multiple in vitro biological potentials.

Medicinal plants largely serve as a source of bioactive compounds in traditional medicines to cure various diseases. The present study was aimed at chemical composition, antioxidant, antimicrobial, cytotoxic and antihemolytic potential of five different extracts of G. hispida and H. crispum (Boraginaceae). G. hispida methanolic extract displayed highest number (eleven) of polyphenolic compounds by using high performance liquid chromatography (HPLC). Functional groups were identified by Fourier-transformed infrared spectroscopy (FTIR) and elements (Si, Fe, Ba, Mg, Ti, Ca, Mg and Cr) were observed by using laser-induced breakdown spectroscopy (LIBS) which were also highly expressed in G. hispida as compared to H. crispum. Antioxidant activity was determined via six assays and antibacterial activity was observed in decreasing order of methanol > ethanol > chloroform > ethyl acetate > n-Hexane in both species. Cytotoxic potential was investigated against brine shrimps and then liver (HepG2) and skin (HT144) cancer cell lines which was detected highest in the G. hispida ethanolic extract (50.76 % and 72.95 %). However, H. crispum chloroform extract revealed highest (31.869 μg/mL) antihemolytic activity and its methanolic extract indicated highest (13.5 %) alpha-amylase inhibitory potential. Altogether, results suggested that both species could be used effectively in food and drug industries owing to the presence of vital bioactive compounds and elements. In future, we recommend to isolate active compounds and to perform in vivo biological assays to further validate their potential biological applications.

Construction of "2R network pharmacology" research method for effective components of traditional Chinese medicine based on "prediction of dominant components-screening of potential targets"

Chinese traditional medicine compound is the main form of Chinese medicine clinical application. The elucidation of the effective components of traditional Chinese medicine is one of the key scientific issues to promote the modernization of traditional Chinese medicine. At present, there are many research ideas on the effective components of traditional Chinese medicine compounds. By analyzing the current status and existing problems of existing research ideas, the author proposes a &quot;double reduction network pharmacology&quot;(2 R network pharmacology) research method based on &quot;prediction of dominant components-potential target selection&quot;. Chemical components with good properties were selected by ADMET property prediction technology, and compared with the blood components and target organ components to determine the dominant components with potential therapeutic effect, that is &quot;reducing constituents&quot;; the potential core regulatory pathway of traditional Chinese medicine compound was enriched by RNA-Seq technology combined with network database, and then the target of traditional Chinese medicine compound was mined based on the signal pathway, that is &quot;reducing targets&quot;. To improve the efficiency and accuracy of effective component screening, the network relationship of &quot;component target&quot; was established by the related technology of network pharmacology. The purpose of this study is to provide practical research ideas and methods for clarifying the effective components of traditional Chinese medicine, revealing the law of compatibility of traditional Chinese medicine and clarifying the target of drug action.

Hypoxia enhances the cytotoxic effect of As4S4 on rat ventricular H9c2 cells through activation of ubiquitin–proteasome system

BackgroundAs4S4 is widely used in Chinese traditional medicine compound. However, based on some recent studies, we found that the cardiotoxicity risk of using As4S4 in ischemic heart disease patients may be increased. To study this potential risk, we compared the effects of As4S4 on rat ventricular H9c2 cell line with or without hypoxic pretreatment, and to elucidate mechanisms of c-Cbl mediated ubiquitination/degradation of integrin β1. MethodsThe present study was conducted on rat ventricular H9c2 cell line in the absence or presence of hypoxic pretreatment for 6 h followed by As4S4 treatment for 24 h. Following As4S4 treatment, cell viability assay, flow cytometric quantification of apoptotic cells, caspase-3 activity assay and DAPI staining were conducted. Western blotting was carried out to detect expressions of ubiquitination related proteins. In addition, the ubiquitination/degradation of integrin β1 and the role of c-Cbl in it was evaluated by immunoprecipitation and immunoblot assay. ResultsThe viability of cells with hypoxic pretreatment followed by As4S4 treatment was decreased significantly, apoptosis rate and the activity of caspase-3 were increased than As4S4 treatment alone. The ubiquitin-proteasome degradation pathway induced by As4S4 was further enhanced by hypoxic pretreatment. The results of IP and immunoblot assay showed hypoxic enhanced down-regulation effect of As4S4 on integrin β1 probably through c-Cbl activation. ConclusionsThis study demonstrated that the hypoxia enhanced cytotoxicity of As4S4 on H9c2 cells may through increasing the ubiquitin-proteasome degradation of integrin β1 mediated by the E3 ligase c-Cbl. The results provide an important clue that, in patients with ischemic heart disease, use of As4S4 may be associated with increased cardiotoxicity. We believe that the results worth to be further illuminated by in vivo and clinical research.

Health Beneficial Effects of Moomiaii in Traditional Medicine.

Traditional medicine (TM) that developed over the years within various societies consists of medical experimental knowledge and practices, which apply natural methods and compounds for general wellness and healing. Moomiaii as a pale-brown to blackish-brown natural exudate is one of the natural compounds in traditional medicine that has been used over 3000 years in many countries of the world especially in India, China, Russia, Iran, Mongolia, Kazakhstan and Kirgizstan. We reviewed all English-language studies about Moomiaii that we accessed them. In traditional medicine, many beneficial activities have been attributed to Moomiaii and to its main constituents, Humic acid and Fulvic acid, which are widely used to prevent and treatment of different diseases. Some modern scientific investigations showed that Moomiaii as a safe dietary supplement can be beneficial in various health complications. Even though the beneficial effects of Moomiaii have been confirmed in traditional and modern medicine, it seems that additional in-vitro/in-vivo studies and comprehensive clinical trials are necessary to explain the whole mechanisms of action and to determine the effective doses in various diseases. We discuss and clarify the claimed health beneficial effects of Moomiaii in some wide-spread diseases regarding its anti-ulcerogenic, immunomodulatory, antidiabetic, antioxidative and anticancer properties.

Health Beneficial Effects of Moomiaii in Traditional Medicine

raditional medicine (TM) that developed over the years within various societies consists of medical experimental knowledge and practices, which apply natural methods and compounds for general wellness and healing. Moomiaii as a pale-brown to blackish-brown natural exudate is one of the natural compounds in traditional medicine that has been used over 3000 years in many countries of the world especially in India, China, Russia, Iran, Mongolia, Kazakhstan and Kirgizstan. We reviewed all English-language studies about Moomiaii that we accessed them. In traditional medicine, many beneficial activities have been attributed to Moomiaii and to its main constituents, Humic acid and Fulvic acid, which are widely used to prevent and treatment of different diseases. Some modern scientific investigations showed that Moomiaii as a safe dietary supplement can be beneficial in various health complications. Even though the beneficial effects of Moomiaii have been confirmed in traditional and modern medicine, it seems that additional in-vitro/in-vivo studies and comprehensive clinical trials are necessary to explain the whole mechanisms of action and to determine the effective doses in various diseases. We discuss and clarify the claimed health beneficial effects of Moomiaii in some wide-spread diseases regarding its anti-ulcerogenic, immunomodulatory, antidiabetic, antioxidative and anticancer properties. [GMJ.2020;9:e1743]

Network Pharmacology-Based Prediction and Verification of Qingluo Tongbi Formula to Reduce Liver Toxicity of Tripterygium wilfordii via UGT2B7 in Endoplasmic Reticulum.

BackgroundThe hepatotoxicity of Tripterygium wilfordii Hook. f. (TWHF) limits its clinic utilization. Qingluo Tongbi formula (QTF) was formulated based on a basic Chinese medicine theory. Previous studies have confirmed the safety and efficacy of QTF in treating rheumatoid arthritis. Therefore, we considered that TWHF could be detoxified based on its reasonable compatibility with QTF. We investigated the detoxicity mechanism of QTF in reducing the liver toxicity of TWHF.Material/MethodsWe used network pharmacology to determine the relevant metabolism targets of TWHF, focusing on the phase II metabolic enzymes uridine diphosphate-glucuronosyltransferase 1A1 (UGT1A1), UGT1A6, and UGT2B7. Based on the molecular mechanisms of these predictions and the results of the network analysis, we designed experiments to verify our hypothesis in vivo. We used western blotting, real-time quantitative polymerase chain reaction (RT-qPCR), double immunofluorescence, and laser confocal microscopy to detect the expression of UGTs. Finally, we used transmission electron microscopy to observe the endoplasmic reticulum structure.ResultsThe results confirmed that QTF reversed the TWHF-induced reduction of UGT content in liver microsomes, upregulated UGT1A1 and UGT1A6 but not UGT2B7 in the liver tissue. UGT2B7 expression in the liver and liver microsomes was inconsistent. QTF upregulated the expression of UGT2B7 in the endoplasmic reticulum, and QTF upregulated UGT2B7 expression levels in the endoplasmic reticulum compared with TWHF, which reduced liver toxicity. Structural changes were observed in the endoplasmic reticulum.ConclusionsThe Chinese traditional medicine compound QTF can achieve the effect of detoxification by upregulating the expression of UGT2B7 in the endoplasmic reticulum.

Anticancer effect of the traditional Chinese medicine herb Maytenus compound via the EGFR/PI3K/AKT/GSK3β pathway

Background: Cancer is a leading cause of death worldwide; folk anticancer medicinal plants have applied for cancer treatment. The Maytenus compound tablet as traditional Chinese compound medicine has been approved for alleviating hyperplasia of mammary glands, whether it can inhibit cancer still unknown. The study was to evaluate the anticancer activity of the Maytenus compound tablet. Methods: MTS assay evaluated the anti-proliferation effect of the Maytenus compound on H226, A2058, 786O and HeLa cancer cells and two normal epithelial cell lines, namely, 16HBE and Hecate. Nude mouse xenograft tumor model using H226 and HeLa cells examined the drug’s anticancer effect in vivo. Western blot assay studied the possible mechanism. Results: The Maytenus compound indicated obvious ability to against proliferation in four strains of cancer cells, particularly against H226 cells by an IC50 of 85.47±10.06 µg/mL and against HeLa cells by an IC50 of 128.74±17.46 µg/mL. However, it had a low cytotoxicity in human normal epithelial cell lines 16HBE with an IC50 of 4,555.86±25.21 µg/mL and Hecate with an IC50 of 833.56±181.88 µg/mL. The Maytenus compound at the 2.45 g/kg oral dosages inhibited the proliferation of H226 cells and HeLa cells in nude mouse with inhibitory rates of 36.06% and 26.45%, respectively, and no organ toxicity. The Maytenus compound could significantly downregulate the expression of pEGFR, pPI3K, pAKT, pGSK3β, β-catenin, and c-MYC and upregulate the protein expression of GSK3β. Conclusions: The Maytenus compound has significant anticancer activities against human cancer H226 and HeLa cells both in vitro and in vivo, highlighting it may be an anticancer medicine.

You-Gui-Yin improved the reproductive dysfunction of male rats with chronic kidney disease via regulating the HIF1α-STAT5 pathway.

You-Gui-Yin (YGY) is a famous Chinese traditional medicine compound that has been used to treat renal function diseases for more than 300 years. It is recorded in Jing Yue Quanshu, which was written by a famous medical scientist named Jiebing Zhang in the Ming Dynasty. Reproductive dysfunction is one of the most serious complications of chronic kidney disease (CKD). The aim of this study was to observe the effect of You-Gui-Yin (YGY) on reproductive dysfunction of male rats with adenine-induced CKD and to determine if any effects occurred via regulation of the HIF1α-STAT5 pathway. UPLC-Q-TOF-MS was used to detect the main medicinal components and conduct quality control of YGY. A total of 60 rats were randomly divided into 2 groups: the NC group (10 rats) and the CKD model group (50 rats). The CKD model rats was established by administration of adenine 150 mg kg-1 orally for 14 days. After that, the CKD rats were randomly divided into 5 groups: the CKD group, YGY (10 g kg-1 group, 20 g kg-1 group, 40 g kg-1 group) and the GUI-LU-ER-XIAN-JIAO (GL) 10 g kg-1 group with 10 rats in each group. From the 15th day to the 45th day rats were given 150 mg kg-1 adenine orally every other day to maintain the model (except in the NC group). The YGY groups and the GL group were orally administered the relevant drug once per day for 30 days. The NC group and the CKD group were orally administered an equal volume of normal saline for 30 days. On the 45th day, the rats' sexual behavior index was tested. On the 46th day, the rats were sacrificed. Biochemical indexes, histopathological changes of the kidneys and testes, sperm morphology, sperm abnormality rate, and key proteins in the HIF1α-STAT5 pathway in the kidney and testis were detected. Thirteen components in the YGY extract were identified by UPLC-Q-TOF-MS for quality control of the YGY extract. The results of the biochemical and physiological tests validated the success of inducing CKD accompanied by reproductive dysfunction in rats. YGY significantly retarded the CKD progression and improved the hormone levels of male CKD rats. Sexual behavior tests showed YGY can significantly improve CKD rats' sexual function. In addition, the pathological changes of the kidney and testis, sperm abnormality rate and sperm morphological abnormalities of the CKD rats were reduced by YGY. Furthermore, decreased expression of HIF1α and EPO, and increased expression of p-EPOR (Tyr368), p-JAK2 (Tyr570) and p-STAT5 (Ser725) were observed in the kidney and the testis of the CKD rats. The YGY extract dramatically increased the expression of HIF1α and EPO, and decreased the expression of p-EPOR (Tyr368), p-JAK2 (Tyr570) and p-STAT5 (Ser725) to regulate key proteins in the HIF1α-STAT5 pathway of the kidney and testis. YGY has obvious reversal effects on the abnormal symptoms of adenine-induced CKD and the abnormal symptoms of rats with hypothyroidism and male reproductive hypotension. Its mechanism is related to its ability to regulate the HIF1α-STAT5 pathway.

Ononin, sec-O-β-d-glucosylhamaudol and astragaloside I: antiviral lead compounds identified via high throughput screening and biological validation from traditional Chinese medicine Zhongjing formulary

Traditional medicine (TM) is a valuable source for drug discovery. The knowledge in healing traditions has led to the success of some of the best-known drugs. However, the concept of ancient medical knowledge, such as herbal remedies and their therapeutic experience is rarely used in the current methodologies for developing therapeutics from TM. As a result, the screening procedure of TM compounds remains tough and labor-intensive. This study aimed to develop a new strategy that is capable of efficiently identifying antiviral leads from complex traditional Chinese medicine (TCM) by integrating knowledge from ancient healing practices with luciferase-based high-throughput screening (HTS). ‘Shanghan Zabing Lun’, an ancient TCM treatise which contains over 200 formulae was selected for knowledge mining based on its antiviral activity. Thirty formulae were rationally selected and utilized for the preparation of a 1306-fraction herbal formulae extract library by standardized chromatographic fractionation. The antiviral activity of the library was screened on a HEK293T cell model carrying a luciferase-driven interferon stimulated response element (ISRE). Hit compounds were further identified using liquid chromatography mass spectrometry analysis, and the mechanism of action of which were preliminarily explored through western blotting and immunofluorescence. A total of 18 fractions and 3 compounds were found activating ISRE. The three compounds, namely ononin, sec-O-β-d-glucosylhamaudol and astragaloside I could activate p65 phosphorylation and nuclear translocation. By doing so, a new strategy termed Knowledge-Based High Throughput Screening (KB-HTS) has been established, which provides an alternative approach to unearth antiviral lead compounds from TM. This new discovery pipeline can expedite the discovery process by improving dereplication and lead prioritization strategies, which is valuable for novel lead discovery from traditional medicine.

The Anti-Hyperplasia of Mammary Gland Effect of Chinese Traditional Medicine compound RPXT in Rats

The Anti-Hyperplasia of Mammary Gland Effect of Chinese Traditional Medicine compound RPXT in Rats

Blue Nile Flower Rituals from the Perspective of Transpersonal Psychology - The Role of Nuciferine and its Putative Value as an Antipsychotic Drug

Pharmaco- or psycho-active compounds in traditional medicines or in plants used during neoshamanic rituals can sometimes lead to the (re-) discovery of new drugs for chronic pain, anxiety, depression or schizophrenia. Neoshamanic rituals fulfill the needs for healing and transformation of a number of people, who are partly dissatisfied with the absence of certain healing aspects in western medicine. A recent neoshamanic ritual is based on the administration of a resin from the Blue Nile Flower (Nymphaea caerulea), also referred to as Blue Lotus or Sacred Blue Lily of the Nile). This extract contains a number of alkaloids such as aporphine and nuciferine, although the quality of commercial available extracts is highly variable. We will discuss the biological effects of nuciferine, a compound which may be of value for the treatment of psychiatric disorders, and discuss the use of Blue Nile Flower in rituals from a transpersonal psychological perspective. Nuciferine has an enriched pharmacological profile, with affinities for a number of serotonergic and dopaminergic receptors. Nuciferine and its derivatives might lead to a new family of atypical antipsychotic compounds. Furthermore, a recent identified mechanism of action related to its anti-inflammatory activity, suggest this molecule might also play a role in the treatment of depression and posttraumatic stress disorder.