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Background Epilepsy is a typical nervous system disorders identified by the spontaneous recurrence of seizures which injure periods of electroencephalographic activity and behavior. Traditional Chinese Medicine (TCM) herb pairs Polygala tenuifolia and Zizyphus jujuba have been used in treatment of epilepsy in China, while the mechanism of action still remains unclear. This article aims to disclose the substances and potential mechanisms of the anti-epilepsy activity of P. tenuifolia and Z. jujuba extract (PZE) using LC-MS/MS, network pharmacology, ethology and molecular biology methods.Methods With the help of the self-built components database, identification of the chemical parameters of PZE was possessed through LC-MS/MS method, and the “ingredient-target-pathway” network of PZE was established through online databeses. Molecular docking was performed using Discovery Studio Visualizer. In the setting of the epilepsy model, pentylenetetrazol (PTZ, 10 mg/kg) was administered intraperitoneally injected for a period of 21 days. Mice were assessed for anxiety-like behavior by Elevated plus maze test, open field test, forced swimming test and tail suspension test. HE staining, western blotting, and immunofluorescence staining were used to detect morphological changes and signal pathway.Results Through network analysis, 37 active ingredients were obtained from PZE, SLC6A4, CHRNA4 and MAOA and were found to play a major role in the PPI network. GO and KEGG analyses that display their anti-epilepsy activity. The"Ingredient-target-pathway"network diagram consists of 99 targets, 24 kinds of constituents, and 20 signaling pathways. The values of M15 and M17 show the largest degree. Molecular docking analysis shows the key components screened by network pharmacology have a good interaction with the predicted targets. Animal experiments results showed that: 1) PZE effectively lengthened the latent time of PTZ-induced epilepsy in mice model. 2) PTZ-induced depression-like behavior was strikingly ameliorated by PZE. 3) Hippocampal neurons are significantly shielded by PZE. 4) PZE was shown to play a key role in modulating the CHRNA4/CaMK II signaling pathway in to show anti-epilepsy potency.Conclusion This study has successfully identified constituents of PZE through LC-MS/MS methods and predicted the potential targets and CHRNA4/CaMK II as potential signaling pathways of anti-epilepsy effects for PZE, which was proved by animal experiments. The results of this paper are conducive to the systematic elucidating of its mechanism of action and the development of TCM-based anti-epilepsy agents.

A quantitative analysis method and a chemical pattern recognition method were developed to evaluate raw Ligustri Lucidi Fructus (LLF) from different regions and different processed products. In this study, a comprehensive strategy using ultra-high-performance liquid chromatography-mass spectrometry quantitative analysis method was established for the simultaneous determination of 16 components in 47 batches of LLF covering 19 regions belonging to 8 provinces and 24 batches of different processed products (steamed LLF without auxiliary material, wine-steamed LLF, salt-steamed LLF, and vinegar-steamed LLF). The results of this study indicated that the proposed method was reliable and accurate for the rapid analysis proved by detection limit, quantification limit, precision, and accuracy. Furthermore, principal component analysis and hierarchical cluster analysis were employed to analyze the experimental data, showing that the best-quality samples of 47 batches of raw LLF were S47 (Lantian, Shaanxi), S39 (Pingyang-2, Shandong), S38 (Pingyang-1, Shandong), and S45 (Lingbao, Henan), whereas the worst-quality samples were S7-S16 (Huzhou, Zhejiang). In 24 batches of processed products, the best-quality samples were S48 (salt steamed 2 h), S60 (wine steamed 2 h), and S61 (wine steamed 4 h). Meanwhile, the heat map showed that the contents of triterpenoid saponins, including C16 (ursolic acid), C15 (oleanic acid), and C14 (maslinic acid), were higher than those of other compounds in 71 batches of samples. These results suggested that the quality of raw LLF in the central and northern regions was better than that in the southern regions, and regarding the processed products, different auxiliary materials had little effect on the quality of LLF, but steaming time of 2 h was appropriate. Briefly, this study proposed a multiparameter quantitative analysis method for the overall quality control of raw LLF samples covering different regions in China and different processed LLF.

In this paper, a combined cooling, heating and power system based on diesel-fueled chemical looping hydrogen generation and solid oxide fuel cell, and with CO2 capture was established. The system can achieve efficient power generation while separating CO2 without energy consumption, and effectively avoid the carbon deposition problem. Aspen software is used to simulate the process of the system, and FORTRAN program is used to calculate, through the thermodynamic analysis model, the unique performance change law of the new system using diesel is obtained, and thermodynamic analysis is performed on the system at last. The results show that the power efficiency of the new system is 54.1%, while the exergy efficiency and fuel energy saving ratio can reach 53%. At the same time, the influence of fuel flow and fuel utilization factor on the system performance does not continue to increase or decrease, and the system performance parameters will have a peak value with the change of pressure. The results not only provide a theoretical basis for the future construction of new diesel-fueled energy supply system, but also provide a new idea for the optimization scheme of energy-saving system and carbon recovery.

Osteoporosis is a common metabolic bone disease, and treatment is required for the prevention of low bone mass, deterioration of microstructural bone tissue, and fragility fractures. Osteoporosis therapy includes calcium, vitamin D, and drugs with antiresorptive or anabolic action on the bone. Therapy for osteoporosis does not include taking non-steroidal anti-inflammatory drugs (NSAID), but pain associated with osteoporotic fractures can be treated by taking non-steroidal anti-inflammatory drugs (NSAID). Recently, polysaccharides extracted from medicinal herbs and edible substances (PsMHES) have attracted attention on account of their safety and promising anti-osteoporosis effects, whereas a systematic review about their potential in anti-osteoporosis is vacant to date. Herein, we reviewed the recent progress of PsMHES with anti-osteoporosis activities, looking to introduce the advances in the various pharmacological mechanisms and targets involved in the anti-osteoporosis effects, extraction methods, main mechanism involved in Wnt/[Formula: see text]-catenin pathways and RANKL (Receptor Activator for NF[Formula: see text]B ligand or TNFSF25) pathways, and Structure-Activity Relationships (SAR) analysis of PsMHES. Typical herbs likeAchyranthes bidentate and Morinda officinalis used for the treatment of osteoporosis are introduced; their traditional uses in traditional Chinese medicine (TCM) are discussed in this paper as well. This review will help to the recognition of the value of PsMHES in anti-osteoporosis and provide guidance for the research and development of new anti-osteoporosis agents in clinic.

Baicalein (5,6,7-trihydroxyflavone) and wogonin (5,7-dihydroxy-8-methoxyflavone), as typical flavonoids isolated from Scutellaria baicalensis, are well important precursors in drug discovery which produce diverse therapeutically related applications in pharmacological practices. Researches in medicinal chemistry field have synthesized baicalein and wogonin derivatives with multiple medicinal properties including antitumor, central nervous system (CNS), anti-inflammatory, antiviral, antimicrobial and hypoglycemic activities. Simultaneously, SAR (Structure-Activity Relationship) analysis has been gradually possessed, along with a great deal of derivatives have been derived for potential targets. In this article, we comprehensively summarize the biological activities and SAR for baicalein and wogonin derivatives, along with the featuring bioactive molecules reported in patents, wishing to provide an overall retrospect and prospect on baicalein and wogonin analogues.

CXCL8 (also known as IL-8) can produce different biological effects by binding to its receptors: CXCR1, CXCR2, and the Duffy antigen receptor for chemokines (DARC). CXCL8 and its receptors are associated with the development of various tumor types, especially colorectal cancer and its liver metastases. In addition to promoting angiogenesis, proliferation, invasion, migration, and the survival of colorectal cancer (CRC) cells, CXCL8 and its receptors have also been known to induce the epithelial-mesenchymal transition (EMT) of CRC cells, to help them to escape host immunosurveillance as well as to enhance resistance to anoikis, which promotes the formation of circulating tumor cells (CTCs) and their colonization of distant organs. In this paper, we will review the established roles of CXCL8 signaling in CRC and discuss the possible strategies of targeting CXCL8 signaling for overcoming CRC drug resistance and cancer progression, including direct targeting of CXCL8/CXCR1/2 or indirect targeting through the inhibition of CXCL8-CXCR1/2 signaling.

Huazhong University of Science and Technology has been developing a proton therapy facility based on a superconducting cyclotron. As an important section of the facility, the gantry beamline has been designed using TRANSPORT code with simplified fringing field model and linear transfer matrix. However, realistic magnetic fringing field and second-order terms of particle motion cannot be precisely described in this approach, which may deviate the actual result from the design value and thereby increase uncertainties for radiation therapy during beam delivery. For this consideration, the specific effects of fringing field and second-order aberrations have been investigated using OPERA code and ODE solvers. For the potential problems of the designed gantry beamline, COSY INFINITY code, which can calculate transfer matrix of any order under the realistic fringing field represented by Enge function, was used to optimize the optics of present gantry beamline. The final results suggest the beam analysis and optimization methods mentioned in this paper are effective and valuable for relevant applications.

TMCA (3,4,5-trimethoxycinnamic acid) ester and amide are privileged structural scaffolds in drug discovery which are widely distributed in natural products and consequently produced diverse therapeutically relevant pharmacological functions. Owing to the potential of TMCA ester and amide analogues as therapeutic agents, researches on chemical syntheses and modifications have been carried out to drug-like candidates with broad range of medicinal properties such as antitumor, antiviral, CNS (central nervous system) agents, antimicrobial, anti-inflammatory and hematologic agents for a long time. At the same time, SAR (structure-activity relationship) studies have draw greater attention among medicinal chemists, and many of the lead compounds were derived for various disease targets. However, there is an urgent need for the medicinal chemists to further exploit the precursor in developing chemical entities with promising bioactivity and druggability. This review concisely summarizes the synthesis and biological activity for TMCA ester and amide analogues. It also comprehensively reveals the relationship of significant biological activities along with SAR studies., Graphical abstract Image 1, Highlights • 3,4,5-Trimethoxycinnamic acid (TMCA) derivatives show applications in different pathophysiological conditions due to its privileged structural scaffolds. • Natural derived TMCA analogues and chemically modified TMCA ester and amide analogues and their bioactivities are focused in this review. Additionally, it also comprehensively summarized the relationship of significant biological activities along with SAR studies of synthetic TMCA derivatives.

Isochromans are well recognized heterocyclic compounds in drug discovery which produce diverse therapeutically related applications in pharmacological practices. Medicinal chemistry investigators have synthesized drug-like isochroman candidates with multiple medicinal features including central nervous system (CNS), antioxidant, antimicrobial, antihypertensive, antitumor and anti-inflammatory agents. Simultaneously, SAR (Structure-Activity Relationship) analysis has drawn attentions among medicinal chemists, along with a great deal of derivatives have been derived for potential targets. In this article, we thoroughly summarize the biological activities and part of typical SAR for isochroman derivatives reported on existing literatures and patents, wishing to provide an overall retrospect and prospect on the isochroman analogues.

Passiflora edulis, also known as passion fruit, is widely distributed in tropical and subtropical areas of the world and becomes popular because of balanced nutrition and health benefits. Currently, more than 110 phytochemical constituents have been found and identified from the different plant parts of P. edulis in which flavonoids and triterpenoids held the biggest share. Various extracts, fruit juice and isolated compounds showed a wide range of health effects and biological activities such as antioxidant, anti-hypertensive, anti-tumor, antidiabetic, hypolipidemic activities, and so forth. Daily consumption of passion fruit at common doses is non-toxic and safe. P. edulis has great potential development and the vast future application for this economically important crop worldwide, and it is in great demand as a fresh product or a formula for food, health care products or medicines. This mini-review aims to provide systematically reorganized information on physiochemical features, nutritional benefits, biological activities, toxicity, and potential applications of leaves, stems, fruits, and peels of P. edulis.

International audience; Rhodomyrtus tomentosa (Aiton) is a flowering plant native to southern and southeastern Asia. Up to date, 106 chemical constituents have been isolated and identified from R. tomentosa. Among these compounds, triterpenoids, flavonoids, phenols and meroterpenoids are the major constituents. Investigations of pharmacological activities of R. tomentosa revealed that this edible medicinal herb exhibits a wide range of therapeutic potential including antibacterial, antitumor, anti-inflammatory and antioxidant activities both in vivo and in vitro. The purpose of this review is to provide an overview of R. tomentosa studies until 2019. This article also intends to review advances in the botanical, phytochemical, pharmacological studies and industrial applications of R. tomentosa, which will provide a useful bibliography for further investigations and applications of R. tomentosa in medicines and foods.

The genus Saururus, belonging to Saururaceae, contains two species, S. cernuus L. and S. chinensis (Lour) Baill. with common utilization in traditional medicine from Asia to North America for the treatment of edema, beriberi, jaundice, leucorrhea, urinary tract infections, hypertension, hepatitis diseases, and tumors. An extensive review of literature was made on traditional uses, phytochemistry, and ethnopharmacology of Saururus using ethno-botanical books, published articles, and electronic databases. The 147 of chemical constituents have been isolated and identified from S. cernuus and S. chinensis, and lignans, flavonoids, alkaloids, anthraquinones, saponins, and phenols are the major constituents. Various pharmacological investigations in many in vitro and in vivo models have revealed the potential of the genus Saururus with anti-inflammatory, antitumor, anti-oxidant, hepatoprotective, antimelanogenic, lipid-lowering, and bone protective activities, supporting the rationale behind numerous of its traditional uses. Due to the noteworthy pharmacological properties, Saururus can be a better option for new drug discovery. Data regarding many aspects of this plant such as toxicology, pharmacokinetics, quality-control measures, and the clinical value of the active compounds is still limited which call for additional studies.

The pyrazolone structural motif is a critical element of drugs aimed at different biological end-points. Medicinal chemistry researches have synthesized drug-like pyrazolone candidates with several medicinal features including antimicrobial, antitumor, CNS (central nervous system) effect, anti-inflammatory activities and so on. Meanwhile, SAR (Structure-Activity Relationship) investigations have drawn attentions among medicinal chemists, along with a plenty of analogues have been derived for multiple targets. In this review, we comprehensively summarize the biological activity and SAR for pyrazolone analogues, wishing to give an overall retrospect and prospect on the pyrazolone derivatives., Graphical abstract Image 1, Highlights • The pyrazolone structural motif is a critical element of drugs aimed at different biological end-points. • The pyrazolone analogues have been carried out to drug-like candidates with broad range of medicinal properties. • This review wishes to give an overall retrospect and prospect on the pyrazolone derivatives.

In this article, a novel series of (E)-3-(3,4,5-trimethoxyphenyl)acrylic acid (TMCA) amide derivatives 1-18 were designed and synthesized by a facile and one-pot step, which were achieved with good yields using 1-hydroxybenzotriazole (HOBT) and 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDCI) as activation system. All the synthesized derivatives were biologically evaluated for their anticonvulsant, sedative activity and neurotoxicity using the maximal electroshock (MES) model, sc-pentylenetetrazol (PTZ) model, pentobarbital sodium-induced sleeping model, and locomotor activity tests, respectively. Among them, compounds 4, 9 and 16 exhibited good anticonvulsant activity in primary evaluation. Furthermore, compound 4 is the most effective anticonvulsant and sedative agent in subsequent tests, while the low threshold of toxicity of compound 4 is vigilant. Compounds 9 and 16 also performed significantly anticonvulsant activity in subsequent tests with weak toxicity. The molecular modeling experiments also predicted good binding interactions of the obtained active molecules with the GABA transferas. Therefore, it could be concluded that the synthesized derivatives 4, 9 and 16 would represent useful lead compounds for further investigation in the development of anticonvulsant and sedative agents.

A proton therapy facility with two 360° gantry treatment rooms and one fixed beamline is under development in the Huazhong University of Science and Technology, which is based on the isochronous superconducting cyclotron scheme. This paper presents the beam optics and main magnetic elements including dipoles, quadrupoles, and fast scanning magnets of the gantry beamline. In addition, the energy selection system will be introduced, which enables fast energy modulation of proton beam between 70 and 240 MeV.

Background Epilepsy is one of chronic neurological disorders that affects 0.5–1.0% of the world’s population during their lifetime. There is a still significant need to develop novel anticonvulsant drugs that possess superior efficacy, broad spectrum of activities and good safety profile. Methods α-Asaronol and two current antiseizure drugs (α-asarone and carbamazepine (CBZ)) were assessed by in vivo anticonvulsant screening with the three most employed standard animal seizure models, including maximal electroshock seizure (MES), subcutaneous injection-pentylenetetrazole (PTZ)-induced seizures and 3-mercaptopropionic acid (3-MP)-induced seizures in mice. Considering drug safety evaluation, acute neurotoxicity was assessed with minimal motor impairment screening determined in the rotarod test, and acute toxicity was also detected in mice. Results In our results, α-asaronol displayed a broad spectrum of anticonvulsant activity (ACA) and showed better protective indexes (PI = 11.11 in MES, PI = 8.68 in PTZ) and lower acute toxicity (LD50 = 2940 mg/kg) than its metabolic parent compound (α-asarone). Additionally, α-asaronol displayed a prominent anticonvulsant profile with ED50 values of 62.02 mg/kg in the MES and 79.45 mg/kg in the sc-PTZ screen as compared with stiripentol of ED50 of 240 mg/kg and 115 mg/kg in the relevant test, respectively. Conclusion The results of the present study revealed α-asaronol can be developed as a novel molecular in the search for safer and efficient anticonvulsants having neuroprotective effects as well as low toxicity. Meanwhile, the results also suggested that α-asaronol has great potential to develop into another new aromatic allylic alcohols type anticonvulsant drug for add-on therapy of Dravet’s syndrome.

Traditional Chinese medicine (TCM) has a long history and been widely used in prevention and treatment of epilepsy in China. This paper is intended to review the advances in the active anticonvulsant compounds isolated from herbs in the prescription of TCM in the treatment of epilepsy. These compounds were introduced with the details including classification, CAS number specific structure and druggability data. Meanwhile, much of the research in these compounds in the last two decades has shown that they exhibited favorable pharmacological properties in treatment of epilepsy both in in vivo and in vitro models. In addition, in this present review, the evaluation of the effects of the anticonvulsant classical TCM prescriptions is discussed. According to these rewarding pharmacological effects and chemical substances, the prescription of TCM herbs could be an effective therapeutic strategy for epilepsy patients, and also could be a promising source for the development of new drugs.

This paper is intended to review advances in the botanical, traditional uses, phytochemical and pharmacological studies of the Pulsatilla chinensis. Up to date, 68 kinds of chemical constituents have been isolated and identified from P. chinensis. Among these compounds, triterpenoids, flavonoids, lignans and coumarins are the major constituents. Researches about the pharmacological properties of P. chinensis revealed that this plant exhibited therapeutic potential both in vivo and in vitro, including antitumor, anti-inflammatory, anti-microbial and antiviral activities. Further attention should be paid to gathering information about their toxicology data, quality-control measures, and the clinical value of the active compounds from P. chinensis.

Lasing emission is a good way to exhibit the excellent optical properties of quantum dots (QDs). In this paper, we synthesize the Tin disulfide (SnS2) QDs by a facile method of sonication. In a Fabry–Perot laser cavity, the lasing emission at ~500 nm is realized by the SnS2 QDs with an excitation threshold value of 19.3 kW/cm2. The results show that the SnS2 QDs have a promising application as laser gain medium.

Grifola frondosa (Dicks.) Gray is a widely consumed edible and medicinal fungus, Ancient books record that it can boost qi and fortify the spleen, moisten the lung and protect the liver. Modern people mainly use it to assist in the treatment of diabetes mellitus and various cancers. Over the past three decades, G. frondosa polysaccharides were shown to possess various promising bioactivities, mainly including antitumor and immunomodulation, anti-oxidation, anti-hyperglycemia, and meanwhile can effectively act on the skin and hematopoietic stem cells. The purpose of the present review is to provide systematically reorganized information on structural characteristics, biological activities, and structure-activity relationship of G. frondosa polysaccharides to support their further therapeutic potentials and sanitarian functions.

Ethnopharmacological relevance Bletilla striata (Thunb.) Reichb. f. (Orchidaceae), also known as Hyacinth Orchid and Baiji (Simplified Chinese: 白及), not only has been widely used for the treatment of hematemesis, hemoptysis, and traumatic bleeding due to the efficacy of arresting bleeding with astringent action, but also has been applied topically to overcome ulcers, sores, swellings, and chapped skin due to the efficacy of dispersing swelling and promoting tissue regeneration. Additional medical applications include the treatment of tuberculosis, malignant ulcers, hemorrhoids, anthrax, eye diseases, and silicosis. Aim of this review This review aims to provide up-to-date information on the botanical characterization, medicinal uses, chemical constituents, pharmacological activities, and toxicity of B. striata. In addition, this paper also focuses on the possible exploitation of this plant for the treatment of different diseases, and uncovers opportunities for future research. Materials and methods The relevant information on B. striata was gathered from worldwide accepted scientific databases via an electronic search (Google Scholar, Web of Science, ScienceDirect, ACS Publications, PubMed, Wiley Online Library, SciFinder, CNKI). Information was also obtained from The Plant List, Chinese pharmacopoeia, Chinese herbal classics books, PhD and MSc dissertations, etc. Results A comprehensive analysis of the literature obtained through the above-mentioned sources confirmed that the ethnomedical usages of B. striata have been recorded in Mongolia, Korea, Japan, and China. Phytochemical investigations revealed that the major chemical constituents of B. striata are polysaccharides, bibenzyls, phenanthrenes, triterpenoids and its saponins, steroids and its saponins, which also have been proven to be the main bioactive substances capable of exhibiting numerous pharmacological activities including wound healing, antiulcer, hemostasis, cytotoxicity, antimicrobial, anti-inflammation, anti-oxidation, immunomodulation, anti-fibrosis, antiaging, anti-allergy, and anti-itch. Conclusions Preliminary investigations on pharmacological properties of B. striata have shown that B. striata is an outstanding astringent hemostatic medicinal, B. striata polysaccharides (BSP) as the major bioactive components not only capable of promoting wound healing, but also show good performance as a kind of promising natural biomaterial. More importantly, BSP are also reported to be excellent embolic material. However, further investigations need to be carried out to fully clarify its efficacy of dispersing swelling and promoting tissue regeneration. Moreover, this plant also needs a lot more investigations to clarify the pathways of absorption, distribution, metabolism and excretion, and to evaluate its long-term in vivo chronic toxicity before proceeding to the development of pharmaceutical formulation.

The aim of the present review is to comprehensively outline the botanical description, traditional uses, phytochemistry, pharmacology and toxicology of Patrinia, and to discuss possible trends for the further study of medicinal plants from the genus Patrinia. The genus Patrinia plays an important role in Asian medicine for the treatment of erysipelas, conjunctival congestion with swelling and pain, peri-appendicular abscesses, lung carbuncle, dysentery, leucorrhea, and postpartum disease. More than 210 chemical constituents have been isolated and identified from Patrinia plants, especially P. scabiosaefolia Fisch., P. scabra Bunge, P. villosa Juss., P. heterophylla Bunge and P. rupestris(Pall.) Juss[Formula: see text] Of these compounds, triterpenoids and saponins, iridoids, flavonoids, and lignans are the major or active constituents. Both in vitro and in vivo studies have indicated that some monomer compounds and crude extracts from the genus Patrinia possess wide pharmacological activities, including antitumor, anti-inflammatory, antibacterial, and antiviral effects. In addition, they have been shown to have valuable and positive effects on the immune and nervous system in experimental animals. There are also some reports on the clinical uses and toxicity of these species. However, few reports have been published concerning the material identification or quality control of Patrinia species, and the clinical uses and toxic effects of these plants are relatively sparse. More attention must be given to these issues.

Actinidia chinensis Planch. (A. chinensis), commonly known as Chinese kiwifruit, is a China native fruit, which becomes increasingly popular due to attractive economic, nutritional, and health benefits properties. The whole plant including fruits, leaves, vines, and roots of A. chinensis are used mainly as food or additive in food products and as folk medicine in China. It is a good source of triterpenoids, polyphenols, vitamin C, carbohydrate, amino acid, and minerals. These constituents render the A. chinensis with a wide range of pharmacological properties including antitumor, antioxidant, anti-inflammatory, immunoregulatory, hypolipemic, antidiabetic, and cardiovascular protective activities, suggesting that it may possibly be value in the prevention and treatment of pathologies associated to cancer, oxidative stress, and aging. This minireview provides a brief knowledge about the recent advances in chemistry, biological activities, utilization, and storage of Chinese kiwifruit. Future research directions on how to better use of this crop are suggested.

Inspired by the traditional Chinese herbal pair of Polygala tenuifolia-Acori Tatarinowii for treating epilepsy, 33 novel substituted cinnamic α-asaronol esters and analogues were designed by Combination of Traditional Chinese Medicine Molecular Chemistry (CTCMMC) strategy, synthesized and tested systematically not only for anticonvulsant activity in three mouse models but also for LDH inhibitory activity. Thereinto, 68–70 and 75 displayed excellent and broad spectra of anticonvulsant activities with modest ability in preventing neuropathic pain, as well as low neurotoxicity. The protective indices of these four compounds compared favorably with stiripentol, lacosamide, carbamazepine and valproic acid. 68–70 exhibited good LDH1 and LDH5 inhibitory activities with noncompetitive inhibition type, and were more potent than stiripentol. Notably, 70, as a representative agent, was also shown as a moderately positive allosteric modulator at human α1β2γ2 GABAA receptors (EC50 46.3 ± 7.3 μM). Thus, 68–70 were promising candidates for developing into anti-epileptic drugs, especially for treatment of refractory epilepsies such as Dravet syndrome.

This study aimed to synthesize and screen tyrosinase inhibitors for delay fruit browning. A series of vanillyl cinnamate analogues were designed and synthesized by simple processes, and the inhibitory effects of all the synthesized derivatives on mushroom tyrosinase were evaluated. In the enzymatic activity test, compounds 21, 22, and 26 had significant (P 0.05) effect on mushroom tyrosinase at a preliminary screening dose (1 mg/mL in vitro). IC

Succinimides are well recognized heterocyclic compounds in drug discovery which produce diverse therapeutically related applications in pharmacological practices. Researches in medicinal chemistry field have isolated and synthesized succinimide derivatives with multiple medicinal properties including anticonvulsant, anti-inflammatory, antitumor and antimicrobial agents, 5-HT receptor ligands and enzyme inhibitors. Simultaneously, SAR (Structure-Activity Relationship) analysis has been gradually possessed, along with a great deal of derivatives have been derived for potential targets. In this article, we comprehensively summarize the biological activities and SAR for succinimide derivatives, along with the featuring bioactive molecules reported in patents, wishing to provide an overall retrospect and prospect on the succinimide analogues.

Ethnopharmacological relevance Sophora japonica (Fabaceae), also known as Huai (Chinese: 槐), is a medium-sized deciduous tree commonly found in China, Japan, Korea, Vietnam, and other countries. The use of this plant has been recorded in classical medicinal treatises of ancient China, and it is currently recorded in both the Chinese Pharmacopoeia and European Pharmacopoeia. The flower buds and fruits of S. japonica , also known as Flos Sophorae Immaturus and Fructus Sophorae in China, are most commonly used in Asia (especially in China) to treat hemorrhoids, hematochezia, hematuria, hematemesis, hemorrhinia, uterine or intestinal hemorrhage, arteriosclerosis, headache, hypertension, dysentery, dizziness, and pyoderma. To discuss feasible trends for further research on S. japonica , this review highlights the botany, ethnopharmacology, phytochemistry, biological activities, and toxicology of S. japonica based on studies published in the last six decades. Materials and methods Information on the S. japonica was collected from major scientific databases (SciFinder, PubMed, Elsevier, SpringerLink, Web of Science, Google Scholar, Medline Plus, China Knowledge Resource Integrated (CNKI), and “ Da Yi Yi Xue Sou Suo ( http://www.dayi100.com/login.jsp )” for publications between 1957 and 2015 on S. japonica . Information was also obtained from local classic herbal literature, government reports, conference papers, as well as PhD and MSc dissertations. Results Approximately 153 chemical compounds, including flavonoids, isoflavonoids, triterpenes, alkaloids, polysaccharides, amino acids, and other compounds, have been isolated from the leaves, branches, flowers, buds, pericarps, and/or fruits of S. japonica . Among these compounds, several flavonoids and isoflavonoids comprise the active constituents of S. japonica , which exhibit a wide range of biological activities in vitro and in vivo such as anti-inflammatory, antibacterial, antiviral, anti-osteoporotic, antioxidant, radical scavenging, antihyperglycemic, antiobesity, antitumor, and hemostatic effects. Furthermore, flavonoids and isoflavonoids can be used as quality control markers for quality identification and evaluation of medicinal materials and their preparations. Information on evaluating the safety of S. japonica is very limited, so further study is required. To enable safer, more effective, and controllable therapeutic preparations, more in-depth information is urgently needed on the quality control, toxicology data, and clinical value of crude extract and active compounds of S. japonica . Conclusions S. japonica has long been used in traditional Chinese medicine (TCM) due to its wide range of biological activities, and is administered orally. Phytochemical and pharmacological studies of S. japonica have increased in the past few years, and the extract and active components of this plant can be used to develop new drugs based on their traditional application as well as their biological activities. Therefore, this review on the ethnopharmacology, phytochemistry, biological activities, and toxicity of S. japonica offers promising data for further studies as well as the commercial exploitation of this traditional medicine.

In this paper, the chemical looping hydrogen generation (CLHG) and solid oxide fuel cell (SOFC) are combined to achieve efficient power generation and CO2 separation and capture without energy consumption. The system can realize the utilization of H2 produced by CLHG in SOFC to avoid carbon deposition in it. The anode of the SOFC is completely refluxed into the steam reactor (SR) of CLHG without the need to install an afterburner, which avoids the direct combustion of fuel and greatly reduces the generation of NOx. High temperature air at SOFC cathode outlet and high temperature gas at fuel reactor (FR) outlet enter GT to do work. The transcritical carbon dioxide cycle (TRCC) is used to recover waste heat, making the system compact and efficient. The new CLHG/SOFC combined cycle system proposed in this paper has high performance, which can recover CO2 and prevent NOx generation, and also prevent carbon deposition in SOFC. In addition, the anode of SOFC is completely refluxed to SR to further improve the system performance. This paper discusses the effects of fuel flow, fuel utilization, SOFC operating temperature, system operating pressure, and CO2 turbine inlet pressure on system performance. The calculation results show that the total efficiency of the system can reach more than 80%, the power generation efficiency can reach more than 65%, and the exergy efficiency is more than 60%.

Ethnopharmacological relevance The dried fruit of Tetradium ruticarpum is frequently utilized as a common traditional medicine in China, Japan and Korea. It has been widely used for the treatment of various diseases such as headache, menorrhalgia, dermatophytosis, celialgia, emesis and aphtha and so on. Aim of this review Despite the wide biological activities of Tetradium plants, there is no current review summarizing medicinal properties of the genus of plants; thus, this review aims to systematically summarize studies on botanical characteristics, traditional uses, phytochemical ingredients, quality control, pharmacokinetics, pharmacological activities and toxicity of Tetradium species to demonstrate their therapeutic capacity. Materials and methods Information and materials related to Tetradium species were obtained from scientific databases such as Google Scholar, Wikipedia, Web of Science, PubMed, ScienceDirect, ACS Publications, SciFinder. Information was also gathered from International Plant Names Index, Global Biodiversity Information Facility, Chinese Pharmacopoeia and Traditional Chinese Medicine classics, etc. All studies of this genus were included in this review until July 2018. Results Tetradium is widely assessed regarding its phytochemistry and biological activities. Approximately 131 chemical compounds, including alkaloids, saponins, phenols and other compounds, have been isolated from Tetradium plants. Among these components, alkaloid evodiamine is the most representative active ingredients of Tetradium plants. These compounds isolated from Tetradium plants exhibit a wide range of biological activities in vitro and in vivo including antitumor, antibacterial, anti-inflammatory, insecticide, cardioprotective and lipid-lowering, treating CNS disorders, digestive system regulation and endocrine system improving activities. Furthermore, alkaloids could be used as markers for quality identification and evaluation of medicinal materials and their preparations. Information on evaluating the safety and pharmacokinetics of Tetradium often focuses on the alkaloids, thus further study and clinical data are required to enable the drug safety of the utilization of Tetradium plants. Conclusions Phytochemical and pharmacological studies of Tetradium plants have proved Tetradium plants are important medicinal herb resource. However, well-designed randomized clinical trials are necessary to confirm the therapeutic benefits of this genus in clinical settings.

Epilepsy is a common chronic neurological disorder disease, and there is an urgent need for the development of novel anticonvulsant drugs. In this study, the anticonvulsant activities and neurotoxicity of 12 cinnamic acid derivatives substituted by fluorine, chlorine, bromine, and trifluoromethyl groups were screened by the maximal electroshock seizure (MES) and rotarod tests (Tox). Three of the tested compounds (compounds 3, 6 and 12) showed better anticonvulsant effects and lower neurotoxicity. They showed respective median effective dose (ED50) of 47.36, 75.72 and 70.65 mg/kg, and median toxic dose (TD50) of them was greater than 500 mg/kg, providing better protective indices. Meanwhile, they showed a pentylenetetrazol (PTZ) ED50 value of 245.2, >300 and 285.2 mg/kg in mice, respectively. Especially, the most active compound 3 displayed a prominent anticonvulsant profile and had lower toxicity. Therefore, the antiepileptic mechanism of 3 on glycosylation changes in chronic epilepsy in mice was further investigated by using glycomics techniques. Lectin microarrays results showed that epilepsy was closely related to abnormal glycosylation, and 3 could reverse the abnormal glycosylation in scPTZ-induced epilepsy in mice. This work can provide new ideas for future discovery of potential biomarkers for evaluation of antiepileptic drugs based on the precise alterations of glycopatterns in epilepsy.

Morus alba L. (family Moreaceae), also known as white mulberry, is distinguished as a source of highly promising traditional medicines (including Mori Folium, Mori Fructus, Mori Ramulus and Mori Cortex) and also functional foods. Over the past two decades, the vast majority of the studies with regard to the isolation and bioactivities of M. alba polysaccharides have mainly focused on its leaves and fruits, which are both medicinal and edible. The tender M. alba leaf is edible and can be used to make tea, the mature M. alba fruit is sweet and juicy. M. alba fruits and leaves contain rich bioactive polysaccharides, which are shown to possess various promising bioactivities, mainly including antidiabetic, immunomodulation, anti-inflammation, antioxidation, anti-obesity, hepatoprotection and renoprotection. The main purpose of this review is to provide systematically reorganized information on structural characteristics and bioactivities of M. alba polysaccharides to support their further therapeutic potentials and sanitarian functions.

Plants from the genus Sanguisorba have been treated as medicinal ingredients for over 2000 years. This paper reviews advances in the botanical, phytochemical and pharmacological studies of the genus. To date, more than 120 chemical constituents have been isolated and identified from these plants, especially from S. officinalis and S. minor. Among these compounds, triterpenoids, phenols and flavonoids are the primary biologically active constituents. Triterpenoids can be used as quality control markers to determine the quality of medicinal materials and their preparations. In vivo and in vitro studies have shown that plants from the genus Sanguisorba exhibit a wide range of pharmacological properties, including hemostatic, antibacterial, antitumor, neuroprotective and hypoglycemic activities. In Chinese medical practice, many drugs (e.g., tablets and powders) that contain S. officinalis roots have been used to treat leukopenia, hemorrhaging and burns. However, there is still a multitude of Sanguisorba species that have garnered little or no attention. Indeed, there are few reports concerning the clinical use and toxic effects of these plants. Further attention should be focused on the study of these species in order to gather information on their respective toxicology data, any relevant quality-control measures, and the clinical value of the crude extracts, active compounds, and bioactive metabolites from Genus Sanguisorba.

International audience; The voltage-gated potassium channel Kv1.5, which mediates the cardiac ultra-rapid delayed-rectifier (IKur) current in human cells, has a crucial role in atrial fibrillation. Therefore, the design of selective Kv1.5 modulators is essential for the treatment of pathophysiological conditions involving Kv1.5 activity. This review summarizes the progress of molecular structures and the functionality of different types of Kv1.5 modulators, with a focus on clinical cardiovascular drugs and a number of active natural products, through a summarization of 96 compounds currently widely used. Furthermore, we also discuss the contributions of Kv1.5 and the regulation of the structure-activity relationship (SAR) of synthetic Kv1.5 inhibitors in human pathophysiology. SAR analysis is regarded as a useful strategy in structural elucidation, as it relates to the characteristics that improve compounds targeting Kv1.5. Herein, we present previous studies regarding the structural, pharmacological, and SAR information of the Kv1.5 modulator, through which we can assist in identifying and designing potent and specific Kv1.5 inhibitors in the treatment of diseases involving Kv1.5 activity.