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Alzheimer's disease （AD） is a neurodegenerative disease often characterized by cognitive impairment in clinical practice. The main pathogenesis includes β amyloid protein （Aβ） excessive deposition， neuroinflammatory response， Tau protein hyperphosphorylation， and other factors， and currently only a few chemical drugs have been approved for clinical treatment of AD. The mechanism of action is relatively single， so it is imperative to find new treatment strategies. Traditional Chinese medicine theory believes that the loss of nourishment in the brain and marrow， as well as the loss of vital energy， is the internal mechanisms underlying the occurrence and development of AD， which runs through the entire treatment process. The pathogenesis of AD is closely related to the inflammasome signaling pathway of nucleotide binding oligomerization domain-like receptor protein 3 （NLRP3）. Activating the NLRP3 signaling pathway increases neuroinflammatory response， intervenes in microglial polarization， and regulates Aβ sedimentation， cellular autophagy， brain homeostasis， etc. This article takes the NLRP3 signaling pathway as the starting point to sort out and summarize the upstream and downstream targets under the AD mechanism in the past five years， as well as the research on the NLRP3 signal pathway targets with the participation of the relevant traditional Chinese medicine compounds， such as Danggui Shaoyaosan， modified Shuyu Wan， Qingxin Kaiqiao prescription， Kaixin San， Jiedu Yizhi prescription， and modified Buwang San， traditional Chinese medicine monomer extracts， such as silibinin， Lycium barbarum polysaccharides， liquiritigenin， salidroside， baicalin， cinnamaldehyde， betaine， acacetin， and Hericium erinaceus， and acupuncture and moxibustion. It also reviews the latest achievements in the prevention and treatment of AD. This study provides ideas and directions for in-depth research on the prevention and treatment of cognitive dysfunction related diseases with traditional Chinese medicine.
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Diabetes retinopathy （DR） is an important cause that threatens the visual health of adults. There are some treatment methods of western medicine with definite efficacy， such as anti-vascular endothelial growth factor and laser photocoagulation， but they have many adverse reactions such as intraocular infection and visual field damage. Traditional Chinese medicine （TCM） therapies are safe and effective， which can complement western medicine. Phosphatidylinositol3-kinase （PI3K）/protein kinase B （Akt） signaling pathway regulates a range of processes including glucose metabolism， cell proliferation， and cell transcription and apoptosis， which is closely related to the occurrence and development of DR. Numerous studies have shown that TCM monomers can participate in maintaining the integrity of blood-retinal barrier and inhibiting retinal neovascularization and neurodegeneration in many aspects such as inhibiting oxidative stress and alleviating inflammatory reaction by regulating the PI3K/Akt pathway， so as to delay the progress of DR. Therefore， this study reviewed PI3K/Akt pathway and its relationship with DR， as well as the TCM monomers in interfering with DR based on PI3K/Akt pathway to provide some ideas for the prevention and treatment of DR in integrated TCM and western medicine.
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OBJECTIVE To analyze the risks of prescription drugs sold online by drug retail enterprises， and to provide countermeasures and suggestions for risk prevention and control of prescription drugs sold online. METHODS The risk hierarchy structure model of prescription drugs sold online by drug retail enterprises was constructed by using analytic hierarchy process. Multiple rounds of risk research and judgment were carried out on 123 pairs of evaluation indicators by using Delphi expert survey method. The normalized weight calculation and consistency test of risk judgment matrix were carried out to perform fuzzy quantitative research. RESULTS The risk of prescription dispensing and review （6.48%）， the risk of drug first and prescription later （5.48%）， the risk of rational drug use guidance （4.99%）， the risk of buying drugs by abnormal channel （4.97%）， the risk of “first diagnosis， non-chronic disease and non-common disease” （4.43%）， and the quality and safety risk of returned drugs （4.34%） and the application risk of regulatory technology （4.06%） were high risks； the overall risk of drug retail enterprises （chain） selling prescription drugs online was 38.67%， and the overall risk of drug retail enterprises （individual） selling prescription drugs online was 61.33%， with a difference of 22.66% between them. CONCLUSIONS There were 7 high-risk indicators for prescription drugs sold online by drug retail enterprises. Among them， the risk of prescription dispensing and review， the risk of drug first and prescription later， and the risk of rational drug use guidance are the top three high-risk points. The risk of prescription drugs sold online by drug retail enterprises （individual） is higher than that of drug retail enterprises （chain）. It is recommended that regulatory authorities focus on and regulate the prescription drugs sold online by drug retail enterprises （individual）， and encourage drug retail enterprises （chain） to establish a systematic online sales process for prescription drugs； for high-risk points of prescription drugs sold online， it is recommended that regulatory authorities and drug retail enterprises focus on it and take effective risk prevention and control measures to ensure the safe use of prescription drugs by the general public.
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Autoimmune diseases（ADs） are diseases in which the body’s immune tolerance is impaired， causing damage to its tissues. The pro-inflammatory helper T cell 17 （Th17） and anti-inflammatory regulatory T cell （Treg） are functionally antagonistic to each other， and the immune imbalance between them and the imbalance of related inflammatory factors are closely related to the occurrence of a variety of ADs. Plenty of evidence has shown that gut microbiota can regulate Th17/Treg differentiation， rebuild immune tolerance and delay the ADs process through regulating cytokine production， transcription factor expression and energy metabolism. This paper reviews the intervention effects of traditional Chinese medicine（TCM） monomers on the common ADs by regulating Th17/Treg differentiation balance based on intestinal flora： ulcerative colitis，rheumatoid arthritis and diabetes mellitus type 1. It is found that its mechanism of action may be to restore the balance of pro-inflammatory factors and anti-inflammatory factors to alleviate intestinal mucosal barrier damage， reduce synovial angiogenesis and improve pancreatic β cell destruction， which provides some ideas for the prevention and treatment of ADs with integrated traditional Chinese and western medicine.
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Embryo implantation is one of the most critical steps in the reproductive process. The failure of embryo implantation to continue development is one of the important reasons leading to infertility. The success of embryo implantation depends on the high receptivity of endometrium and the embryo with implantation ability. Autophagy is a process in which cytoplasm， organelles， and inclusions are absorbed by double-membrane vesicles and transported to lysosomes for degradation and recycling， which is a way to maintain the homeostasis. A large amount of evidence have shown that autophagy plays an important role in all aspects of embryo implantation. Based on this， this paper explored the relationship between autophagy and endometrial receptivity and embryo implantation ability. According to the latest research progress， this paper combed 5 mechanisms （promotion of decidualization of endometrial stromal cells， promotion of apoptosis， regulation of hormone levels， coordination of inflammation， and promotion of ovulation） of 14 kinds of Chinese medicine monomers， including emodin， catalpol， paeoniflorin， resveratrol， folic acid， zearalenone， curcumin， wogonin， quercetin， chrysin， berberine， apigenin， phisetine， and kaempferol， in regulating different links of autophagy intervention in embryo implantation. This paper is expected to provide references and ideas for future Chinese medicine monomers to improve the success rate of embryo implantation.
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Bombesin receptor subtype-3(BRS-3) is an orphan receptor in the bombesin receptor family. Its signal transduction mechanism and biological function have attracted much attention. Seeking the ligand for BRS-3 is of great significance for exploring its function. Considering the fact that the activation of BRS-3 receptor can induce the change in intracellular Ca~(2+) concentration, the fluo-rometric imaging plate reader(FLIPR) was utilized for ligand screening at the cellular level. Among more than 400 monomeric compounds isolated from Chinese herbs, yuanhunine from Corydalis Rhizoma and sophoraisoflavanone A and licoriphenone from Glycyrrhizae Radix et Rhizoma antagonized BRS-3 to varying degrees. It was confirmed in HEK293 cells expressing BRS-3 that yuanhunine, sophoraisoflavanone A, and licoriphenone inhibited the calcium current response after the activation of BRS-3 by [D-Phe~6,β-Ala~(11),Phe~(13),Nle~(14)]bombesin-(6-14) in a dose-dependent manner with the IC_(50) values being 8.58, 4.10, and 2.04 μmol·L~(-1), respectively. Further study indicated that yuanhunine and sophoraisoflavanone A exhibited good selectivity for BRS-3. In this study, it was found for the first time that monomers derived from Chinese herbs had antagonistic activity against orphan receptor BRS-3, which has provided a tool for further study of BRS-3 and also the potential lead compounds for new drug discovery. At the same time, it provides reference for the research and development of innovative drugs based on the active ingredients of Chinese herbs.
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Humans , Drugs, Chinese Herbal/chemistry , HEK293 Cells , Ligands , Receptors, BombesinABSTRACT
Paclitaxel is the first-line chemotherapy drug for a variety of cancers. However， the paclitaxel resistance greatly reduced the efficacy in the later treatment stage， which seriously increased the mortality and recurrence rate of cancer and limited the clinical application of paclitaxel. At present， Chinese medicine compound prescription， proprietary Chinese medicine， and Chinese medicine injection are widely used as the adjuvant chemotherapy drugs for the treatment of cancer in clinic. Chinese medicine has shown unique advantages in improving the efficacy of chemotherapy drugs and the prognosis of chemotherapy， and reducing the toxic and side effects. However， the specific mechanism and effective monomer composition of Chinese medicine for reversing the resistance of chemotherapy drugs are unclear， and the application of Chinese medicine in different types of cancer is also limited， which are worthy of further exploration. This review summarized the composition of Chinese medicine monomer with synergistic antitumor effect combined with paclitaxel in recent years. The specific mechanism and pharmacological activities of Chinese medicine monomer reversing paclitaxel resistance were classified. This review found that through acting on the membrane transport protein， Chinese medicine monomer promoted the accumulation of paclitaxel in tumor cells， inhibited the expressions of protein and metabolic enzyme related to multidrug resistance and the metabolism of paclitaxel， and regulated the levels of apoptosis genes and factors and apoptosis-related pathways to promote the inhibitory effect of paclitaxel on cell proliferation. Chinese medicine monomer also significantly improved paclitaxel chemotherapy sensitivity by regulating the expression levels of micro ribonucleic acid （microRNA） and long non-coding ribonucleic acid RNA （lncRNA）， inhibiting the characteristics of tumor stem cells and tumor metabolic reprogramming， improving tumor microenvironment， and triggering tumor cell death autophagy and oxidative stress response. This review provides a theoretical basis for clarifying the specific anti-tumor mechanism of Chinese medicine monomer combined with paclitaxel， which is of great significance for the development of new Chinese medicine and the clinical research of the drugs combined with paclitaxel， and has certain value for the application of Chinese medicine combined with other chemotherapy drugs.
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Because the early symptoms of ovarian cancer are not typical and there is a lack of effective screening methods， most patients are diagnosed at an advanced stage， which seriously endangers the health of modern women. Platinum-based chemotherapy after tumor reduction is the first choice for patients with advanced and recurrent ovarian cancer， but almost all patients with recurrent ovarian cancer will eventually develop platinum resistance. Therefore， the search for natural， safe， and effective chemotherapeutic sensitizers has become an urgent and important topic in the study of ovarian cancer. With the increasingly extensive application of traditional Chinese medicine （TCM） in the treatment of cancer， the research on Chinese herbal monomers is also deepening， and the mechanisms of Chinese herbal monomers in intervening in cisplatin （DDP）-induced resistance of ovarian cancer is becoming increasingly clearer. Based on the research status of Chinese herbal monomers available in many Chinese and English databases， it was found that Chinese herbal monomers were involved in the reversal of DDP-induced resistance of ovarian cancer via many routes， mainly through increasing the intracellular drug concentration， reversing the blocked apoptosis， correcting the abnormal intracellular signaling pathway， enhancing DNA damage and inhibiting DNA repair， regulating intracellular autophagy， and suppressing epithelial mesenchymal transition （EMT）. Chinese herbal monomers weaken the resistance of ovarian cancer to DDP from multiple targets and enhance the toxicity of DDP to ovarian cancer cells in vitro and transplanted tumors in vivo. Therefore， Chinese herbal monomers are expected to become natural sensitizers for ovarian cancer chemotherapy with DDP. However， the current studies on Chinese herbal monomers are still confined to the single experimental type， and their action mechanisms and toxic and side effects remain to be further clarified. The application of Chinese herbal monomers for sensitizing DDP chemotherapy still needs to be verified by multi-target， multi-level experimental studies and large-scale clinical studies in the future.
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Autophagy is a lysosome-mediated catabolic process that captures and degrades dysfunctional organelles and useless proteins during cellular stress process， which plays a dual role in cervical cancer. In the early stage of cervical cancer， autophagy inhibits the occurrence and development of cervical cancer by prohibiting the accumulation of oncogenic p62 protein. In the advanced stage of cervical cancer， inhibition of autophagy of cancer cells enhances the sensitivity of cancer cells to chemotherapeutic drugs， thus inhibiting their proliferation. In recent years， the research on Chinese medicine monomers regulating autophagy in the treatment of cervical cancer has attracted extensive attention from scholars at home and abroad. Chinese medicine monomers regulate the autophagy of cervical cancer cells through multiple pathways and multiple targets， so as to increase the apoptosis rate and reduce the resistance of cancer cells to chemotherapeutic drugs. Therefore， this paper reviewed the mechanism of Chinese medicine monomers in inhibiting cervical cancer through autophagy， expecting to find new breakthroughs in the discovery and development of preventive and therapeutic drugs for cervical cancer. By reviewing the literature， it was found that in the early stage of cervical cancer， Chinese medicine monomers activated autophagy to promote apoptosis of cancer cells， and the main mechanism was to increase lysosomal membrane permeability and chemotherapeutic sensitivity and activate intact autophagy flow. In the advanced stage of cervical cancer， inhibition of autophagy reduced the sensitivity of cancer cells to chemotherapy drugs by inhibiting the formation of autophagosomes and autolysosomes. The treatment of cervical cancer by Chinese medicine monomers regulating autophagy has achieved certain effect， but there are few clinical experimental studies and lack of reliable clinical theoretical basis. Therefore， it is essential to carry out more clinical experimental studies on Chinese medicine monomers regulating autophagy to treat cervical cancer， thus finding more reliable theoretical basis for the treatment of tumors.
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Ovarian cancer is a malignant tumor of female reproductive system with high morbidity and mortality. Currently， ovarian cancer patients are mainly treated by primary debulking surgery combined with taxotere/cyclophosphamide （TC） chemotherapy， with the five-year survival rate of 36%-46%. Chinese medicinal materials play a positive role in preventing the occurrence and development of ovarian cancer via multiple targets. The flavonoid monomers in representative Chinese herbal medicines， such as Epimedii Folium， Scutellariae Radix， Curcumae Longae Rhizoma， Ginkgo Folium， Bupleuri Radix， and Longicerae Japonicae Flos， have been proved to have significant anti-tumor activity and been widely used in the treatment of malignant tumors. We reviewed the relevant literature and summarized that flavonoid monomers can regulate multiple signaling pathways to inhibit cell proliferation， block tumor cell cycle， induce apoptosis and autophagy， reduce the ability of cell invasion and migration， inhibit tumor angiogenesis， and reverse platinum resistance， thereby inhibiting the occurrence and development of ovarian cancer. Such pathways include phosphatidylinositol 3- kinase （PI3K）/protein kinase B （Akt）/mammalian target of rapamycin （mTOR） signaling pathway， Janus kinase （JAK）/signal transducer and activator of transcription 3 （STAT3） signaling pathway， mitogen-activated protein kinase （MAPK） signaling pathway， secreted glycoprotein （Wnt）/β-catenin signaling pathway， Notch signaling pathway， and nuclear factor kappaB （NF-κB） signaling pathway. By reviewing the regulatory effect of flavonoid monomers on the signaling pathways of ovarian cancer， we aim to provide a theoretical basis for the research on the roles of flavonoid monomers in inhibiting the occurrence and development of ovarian cancer.
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Ovarian cancer is a malignant tumor of female reproductive system with high morbidity and mortality. Currently， ovarian cancer patients are mainly treated by primary debulking surgery combined with taxotere/cyclophosphamide （TC） chemotherapy， with the five-year survival rate of 36%-46%. Chinese medicinal materials play a positive role in preventing the occurrence and development of ovarian cancer via multiple targets. The flavonoid monomers in representative Chinese herbal medicines， such as Epimedii Folium， Scutellariae Radix， Curcumae Longae Rhizoma， Ginkgo Folium， Bupleuri Radix， and Longicerae Japonicae Flos， have been proved to have significant anti-tumor activity and been widely used in the treatment of malignant tumors. We reviewed the relevant literature and summarized that flavonoid monomers can regulate multiple signaling pathways to inhibit cell proliferation， block tumor cell cycle， induce apoptosis and autophagy， reduce the ability of cell invasion and migration， inhibit tumor angiogenesis， and reverse platinum resistance， thereby inhibiting the occurrence and development of ovarian cancer. Such pathways include phosphatidylinositol 3- kinase （PI3K）/protein kinase B （Akt）/mammalian target of rapamycin （mTOR） signaling pathway， Janus kinase （JAK）/signal transducer and activator of transcription 3 （STAT3） signaling pathway， mitogen-activated protein kinase （MAPK） signaling pathway， secreted glycoprotein （Wnt）/β-catenin signaling pathway， Notch signaling pathway， and nuclear factor kappaB （NF-κB） signaling pathway. By reviewing the regulatory effect of flavonoid monomers on the signaling pathways of ovarian cancer， we aim to provide a theoretical basis for the research on the roles of flavonoid monomers in inhibiting the occurrence and development of ovarian cancer.
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Autophagy is a lysosome-mediated catabolic process that captures and degrades dysfunctional organelles and useless proteins during cellular stress process， which plays a dual role in cervical cancer. In the early stage of cervical cancer， autophagy inhibits the occurrence and development of cervical cancer by prohibiting the accumulation of oncogenic p62 protein. In the advanced stage of cervical cancer， inhibition of autophagy of cancer cells enhances the sensitivity of cancer cells to chemotherapeutic drugs， thus inhibiting their proliferation. In recent years， the research on Chinese medicine monomers regulating autophagy in the treatment of cervical cancer has attracted extensive attention from scholars at home and abroad. Chinese medicine monomers regulate the autophagy of cervical cancer cells through multiple pathways and multiple targets， so as to increase the apoptosis rate and reduce the resistance of cancer cells to chemotherapeutic drugs. Therefore， this paper reviewed the mechanism of Chinese medicine monomers in inhibiting cervical cancer through autophagy， expecting to find new breakthroughs in the discovery and development of preventive and therapeutic drugs for cervical cancer. By reviewing the literature， it was found that in the early stage of cervical cancer， Chinese medicine monomers activated autophagy to promote apoptosis of cancer cells， and the main mechanism was to increase lysosomal membrane permeability and chemotherapeutic sensitivity and activate intact autophagy flow. In the advanced stage of cervical cancer， inhibition of autophagy reduced the sensitivity of cancer cells to chemotherapy drugs by inhibiting the formation of autophagosomes and autolysosomes. The treatment of cervical cancer by Chinese medicine monomers regulating autophagy has achieved certain effect， but there are few clinical experimental studies and lack of reliable clinical theoretical basis. Therefore， it is essential to carry out more clinical experimental studies on Chinese medicine monomers regulating autophagy to treat cervical cancer， thus finding more reliable theoretical basis for the treatment of tumors.
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Alzheimer's disease （AD） is currently the most common neurodegenerative disorder characterized by insidious onset and slow progression， which has seriously endangered the physical and mental health of the elderly. It is therefore very important to carry out the early diagnosis and active prevention and treatment. Biomarkers are essential for its diagnosis. Looking for ideal biomarkers is helpful for early identification of this disease. The prevention and treatment of AD with traditional Chinese medicine （TCM） has always been a hot spot in scientific research due to good safety and small side effects. Proteomics is an advanced omics technology that enables the identification and characterization of proteins. Its high-throughput， dynamic， and comprehensive characteristics coincide with the concept of holism emphasized in TCM diagnosis and treatment， which makes proteomics suitable for identifying biomarkers with diagnostic potential， objectifying TCM syndrome differentiation and treatment， and developing new Chinese medicinal prescriptions for precise and targeted treatment. Although the proteomics technology is becoming increasingly mature， it still faces challenges in the diagnosis and treatment of AD. There exist such shortcomings as high heterogeneity and poor reproducibility of protein omics results， requirement for the combination with other advanced omics technologies， and high sequencing cost. In the future， the protein omics technology should be constantly updated and optimized to boost precision medicine， disease prevention， and drug research and development. This paper retrieved related articles from Pubmed， China National Knowledge Infrastructure （CNKI） and reviewed the application of proteomics in the early diagnosis of AD and its prevention and treatment with TCM in recent years， in order to provide reference for the in-depth study of AD diagnosis as well as its prevention and treatment with TCM.
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Synthetic polymer hydrogel nanoparticles(NPs)were developed to function as abiotic affinity reagents for fibrinogen.These NPs were made using both temperature-sensitive N-isopropyl acrylamide(NIPAm)and L-amino acid monomers.Five kinds of L-amino acids were acryloylated to obtain functional mono-mers:L-phenylalanine(Phe)and L-leucine(Leu)with hydrophobic side chains,L-glutamic acid(Glu)with negative charges,and L-lysine(Lys)and L-arginine(Arg)with positive charges.After incubating the NPs with fibrinogen,y-globulin,and human serum albumin(HSA)respectively,the NPs that incorporated N-acryloyl-Arg monomers(AArg@NPs)showed the strongest and most specific binding affinity to fibrin-ogen,when compared with y-globulin and HSA.Additionally,the fibrinogen-AArg binding model had the best docking scores,and this may be due to the interaction of positively charged AArg@NPs and the negatively charged fibrinogen D domain and the hydrophobic interaction between them.The specific adsorption of AArg@NPs to fibrinogen was also confirmed by the immunoprecipitation assay,as the AArg@NPs selectively trapped the fibrinogen from a human plasma protein mixture.AArg@NPs had a strong selectivity for,and specificity to,fibrinogen and may be developed as a potential human fibrinogen-specific affinity reagent.
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The traditional Chinese medicine(TCM) syndrome of blood stasis refers to blood stagnation in meridians and viscera, with the main symptoms of pain, mass, bleeding, purple tongue, and unsmooth pulse. Cardiovascular and cerebrovascular diseases are among the major chronic diseases seriously harming the health of the Chinese. Among the coronary heart disease and stroke patients, most demonstrate the blood stasis syndrome. Platelet is considered to be one of the necessary factors in thrombosis, which closely relates to the TCM syndrome of blood stasis and the occurrence of cardiovascular and cerebrovascular diseases. The clinical and laboratory research on platelet activation and aggregation has been paid more and more attention. Its purpose is to treat and prevent blood stasis syndrome. In this study, the authors analyzed the research on the dysfunctions of platelets in blood stasis syndrome, biological basis of TCM blood stasis syndrome, and the effect of blood-activating stasis-resolving prescriptions on platelets, aiming at providing a reference for exploring the mechanism of platelet intervention in the treatment of TCM blood stasis syndrome and the pathways and targets of Chinese medicine in the prevention and treatment of the syndrome.
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Humans , Blood Platelets , Coronary Disease , Medicine, Chinese Traditional , Platelet Activation , SyndromeABSTRACT
Abstract Polyphenol Extracts (PE) hold antioxidant properties, which might be related to positive effects on human health. It has been stated that PE, obtained from cocoa beans, contain fractions of flavan-3-ols with different degrees of polymerization (DP). However, it is unknown which of the fractions or their mixture drives the best antioxidant activity. This paper reports the study conducted to elucidate the role of each fraction (with different DP) on Antioxidant Capacity (AC). First, the process of extraction and separation of polyphenols' fractions in cocoa beans was executed; afterward, AC was determined for each fraction individually and their combinations (monomers, dimers and oligomers). Solid-liquid extraction was made by using a 50% (v/v) ethanol solution and a mass:solvent ratio of 1:120 in an ultrasound bath. PE were separated into monomers, dimers, and oligomers by HPLC using a semipreparative column. The results obtained show that PE contain 95.35, 7.45, and 21.75 mg EE (epicatechin equivalents) / g ds of monomers, dimers, and oligomers, respectively. Finally, the AC of each fraction was evaluated using a complete cubic model mix design. According to the results, the best AC was obtained for dimers. However, when monomers, dimers and oligomers were mixed, an antagonistic effect on AC was observed.
Resumen Los extractos polifenólicos (PE) tienen propiedades antioxidantes positivas para la salud humana. Se conoce que los PE obtenidos del cacao contienen fracciones de flavan-3-ols con diferentes grados de polimerización (DP). Sin embargo, se desconoce qué fracción o mezcla de ellos posee mayor capacidad antioxidante. Este trabajo se realizó con el fin de evaluar la capacidad antioxidante (AC) de cada fracción polifenólica (con diferentes DP) extraída del cacao. Primero, se realizó un proceso de extracción y separación de las fracciones de polifenoles en los granos de cacao. Luego, se determinó la AC para cada fracción individual y combinada (monómeros, dímeros y oligómeros). La extracción sólido-líquido se realizó utilizando una solución de etanol en agua al 50 % (v/v) y una relación masa:solvente de 1:120 en un baño de ultrasonido. El extracto PE se separó en monómeros, dímeros y oligómeros por HPLC usando una columna semipreparativa. Los resultados obtenidos muestran que el extracto PE contiene 95,35, 7,45 y 21,75 mg EE (equivalentes de epicatequina) / g ds de monómeros, dímeros y oligómeros, respectivamente. Finalmente, se evaluó la CA de cada fracción utilizando un diseño de mezcla de modelo cúbico completo. Según los resultados, se obtuvo una mayor AC para dímeros; sin embargo, se observó un efecto antagonista de la AC cuando se mezclan monómeros, dímeros y oligómeros.
Resumo Os extratos de polifenóis (PE) possuem propriedades antioxidantes, que podem estar relacionadas a efeitos positivos para a saúde humana. Foi afirmado que o PE, obtido a partir de grãos de cacau, contém frações de flavan-3-ols com diferentes graus de polimerização (DP). No entanto, não se sabe qual fração ou mistura deles impulsiona a melhor atividade antioxidante. Este artigo relata os achados de um estudo realizado com o objetivo de elucidar o papel de cada fração (com DP diferente) na capacidade antioxidante (AC). Inicialmente, o processo de extração e separação de frações de polifenóis 'em grãos de cacau é descrito. Posteriormente, é determinada a AC para cada fração isolada e combinada (monômeros, dímeros e oligômeros). A extração sólido-líquido foi realizada utilizando uma solução de etanol a 50% (v/v) e uma razão massa: solvente de 1: 120 em um banho de ultrassom. O PE foi separado em monômeros, dímeros e oligômeros por HPLC usando uma coluna semi-preparativa. Os resultados obtidos mostram que o PE contém 95,35, 7,45 e 21,75 mg EE (equivalentes de epicatequina) / g ds de monômeros, dímeros e oligômeros, respectivamente. Finalmente, o efeito de cada fração na AC foi avaliado usando um modelo de mistura cúbica completo. De acordo com os resultados, a melhor AC foi obtida para os dímeros; no entanto, um efeito antagônico na AC foi observado quando monômeros, dímeros e oligômeros foram misturados.
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Post-traumatic stress disorder (PTSD) is a mental disorder characterized by restitution of trauma and emotional irritability and avoidance caused by sudden, threatening or catastrophic life events. PTSD occurs not only abnormal behavioral indicators but also abnormal neurobiological indicators. Studies on the pathogenesis of PTSD have focused on neuroendocrine system, central nervous system and immune system, mainly finding abnormal levels of stress hormones, pro-inflammatory cytokines, neurotransmitters and neuroprotective factors. Traditional Chinese medicines(TCM) have many advantages in the treatment of PTSD due to their multi-target, multi-component and multi-pathway characteristics. Current studies have showed that a variety of TCM can improve the abnormal behaviors of animals in the models of post-traumatic stress disorder and reverse the neurobiological indicators. As many of these TCM compounds have been used in clinic and have good efficacy, TCM treatment of PTSD has a broad application prospect. However, there is no specific medicine for PTSD, and its mechanisms have not been fully understood. Therefore, this paper reviews the current studies on the treatment of PTSD with TCM, and focuses on the occurrence and treatment progress of PTSD in terms of TCM, mechanisms of action and animal models, so as to provide references for the treatment of PTSD.
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Abstract The aim of this study was to use the isobornyl methacrylate (IBOMA) as a combining or substituent diluent monomer in the resin matrix of dental resin composites. Thus, the resin matrix was formulated with 60 wt% of BisGMA and 40 wt% of diluent monomers. TEGDMA as the only diluent monomer was used as control with 40 wt%, while total substitution of TEGDMA was done with 40 wt% of IBOMA. The combination of IBOMA and TEGDMA was done with 20 wt% of each monomer. To the resin matrix, 65 wt% of filler particles was added. Degree of conversion (DC) using FT-IR, flexural strength (FS), flexural modulus (FM), polymerization shrinkage by gap formation (GF), Knoop hardness (KH) and solvent degradation (SD) were evaluated. Data were analyzed using ANOVA and Tukey's test (α=0.05; b=0.2). The results showed that reducing or substituting TEGDMA using IBOMA did not affect the DC (0.085), FS (p=0.886) or FM (p=0.414). Also, when IBOMA was used, lower GF was found in comparison to the control containing only TEGDMA as the diluent monomer (p=0.032). However, even though all composites presented reduction in KH during the SD test, the combination of IBOMA and TEGDMA showed similar reduction in KHN in comparison to the control group (p=0.001), while the total substitution of TEGDMA with IBOMA decreased KHN after SD (p=0.041). Thus, the combination of IBOMA and TEGDMA seem to reduce SD and GF without affecting the properties of resin composites.
Resumo O objetivo nesse estudo foi utilizar o isobornil metacrilato (IBOMA) como monômero combinante ou substituinte na matriz resinosa de resinas compostas odontológicas. Para tanto, a matriz resinosa foi formulada com 60 % em peso de BisGMA e 40 % em peso de monômero diluente. O TEGDMA foi utilizado como único monômero diluente para o grupo controle com 40 % em peso, enquanto a substituição total de TEGDMA foi feita com 40 % em peso de IBOMA. Na combinação de IBOMA e TEGDMA foram utilizados 20 % em peso de cada monômero. Na matriz resinosa, 65 % em peso de partículas de carga foi adicionado. O grau de conversão (GC) utilizando FT-IR, a resistência flexural (RF), o módulo flexural (MF), a contração de polimerização por formação de gap (FG) utilizando Microscopia Confocal à Laser, a Dureza Knoop (DK) e a degradação em solvente (DS) foram avaliados. Todos os dados foram analisados utilizando ANOVA e teste de Tukey (α=0.05; b=0.2). Os resultados demonstraram que reduzindo ou substituindo o TEGDMA utilizando o IBOMA não afetou o GC (p=0.085), a RF (p=0.886) ou o MF (p=0.414). Ainda, quando o IBOMA foi utilizado como um monômero combinante ou substituinte, menor FG foi observada em comparação ao controle contendo apenas TEGDMA como monômero diluente (p=0.032). Contudo, apesar de todos os compósitos terem apresentados redução na DK durante o teste de DS, a combinação de IBOMA e TEGDMA demonstrou uma redução na DK similar ao grupo (p=0.001), enquanto a substituição total de TEGDMA com IBOMA reduziu a DK após DS (p=0.041). Dessa forma, a combinação do IBOMA e TEGDMA parece reduzir DS e a FG sem afetar as propriedades de resinas compostas.
Subject(s)
Composite Resins , Methacrylates , Polyethylene Glycols , Polymethacrylic Acids , Solvents , Materials Testing , Bisphenol A-Glycidyl Methacrylate , Spectroscopy, Fourier Transform Infrared , PolymerizationABSTRACT
Aim: To screen BRAFV600E CT26 cell inhibitors from monomers of traditional Chinese medicine (TCM). Methods CT26 cell line was constructed with lentivirus plasmid to stably express BRAFV6C0E. The proliferation, migration and expression of related proteins in MEK/ERK signaling pathway were detected. The monomers of TCM were detected for biological activities as potential BRAF inhibitors by Discovery Studio 4. 0, and further evaluated by MTT assay. Results: The proliferation and migration of BRAFV6C0E CT26 cells were obviously strengthened compared with wild type control. The expressions of proteins in MEK/ ERK pathway were also activated in BRAFV6C0E CT26 cells. Compared with wild type control, Aloin, Angoroside C and Cyasterone exhibited the potent effect against BRAFV600E in CT26 cells (P <0. 05), and could down-regulate the expression of BRAFV600E. Conclusion: Aloin, Angoroside C, Cyasterone might be the potent inhibitors against BRAF for colon treatment.
ABSTRACT
Abstract This study evaluated in vitro cell viability and metabolism, nitric oxide release and production of chemokines by cultured human dental pulp fibroblasts (DPF) under contact with HEMA and Single Bond. Cultures of DPF were established by means of an explant technique. Once plated, cells were kept under contact with increasing concentrations of HEMA (10, 100 and 1000 nM) or Single Bond (SB) [10-fold serially diluted in culture medium (10-4, 10-3 and 10-2 v/v)] and also with polymerized SB components. Cytotoxicity was assessed by Trypan Blue exclusion method and MTT [3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] assay. Nitric oxide release on cell supernatant was detected by Griess Method whereas chemokines (CXCL12 and CXCL8) were detected by ELISA. RT-qPCR was employed for chemokines gene expression analysis. Cytotoxic tests showed significant differences for SB 10-2. None of the tested materials significantly altered NO levels. Protein levels of CXCL12 were significantly decreased only by HEMA. On the other hand, while CXCL12 mRNA remained unaltered, gene expression of CXCL8 had significant decrease with all materials, except for polymerized SB. In conclusion, Single Bond and HEMA at various concentrations, decreased expression and production of molecules involved in inflammatory processes and, therefore, the use of adhesive systems such as pulp capping materials must be viewed with caution due to its large cytotoxic effect when in close contact with the pulp.
Resumo Este estudo avaliou in vitro a viabilidade e metabolismo celular, liberação de óxido nítrico e produção de quimiocinas em cultura de fibroblastos de polpa dental humana (DPF) em contato com HEMA e Single Bond. Culturas de DPF foram estabelecidas por meio de uma técnica de explante. Uma vez plaqueadas, as células foram mantidas em contato com concentrações crescentes de HEMA (10, 100 e 1000 nM) ou Single Bond (SB) [10 vezes diluídas em série em meio de cultura (10-4, 10-3 e 10-2 v/v)] e também com SB polimerizado. A citotoxicidade foi avaliada pelo método de exclusão de Trypan Blue e pelo ensaio de 3-(4,5-dimetiltiazol-2-il)-2,5-difeniltetrazólio brometo (MTT). A liberação de óxido nítrico no sobrenadante celular foi detectada pelo método de Griess, enquanto as quimiocinas (CXCL12 e CXCL8) foram detectadas por ELISA. RT-qPCR foi empregada para análise de expressão gênica de quimiocinas. Testes citotóxicos mostraram diferenças significativas para SB 10-2. Nenhum dos materiais testados alterou significativamente os níveis de NO. Os níveis de proteína de CXCL12 foram significativamente diminuídos apenas pelo HEMA. Por outro lado, enquanto o RNAm de CXCL12 permaneceu inalterado, a expressão gênica de CXCL8 teve redução significativa com todos os materiais, com exceção do SB polimerizado. Em conclusão, Single Bond e HEMA, em várias concentrações, diminuíram a expressão e produção de moléculas envolvidas em processos inflamatórios e, portanto, o uso de sistemas adesivos, como o material protetor da polpa, deve ser visto com cautela devido ao seu grande efeito citotóxico quando em contato com a polpa.