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1.
Zhongguo Zhong Yao Za Zhi ; 46(20): 5330-5340, 2021 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-34738437

RESUMO

This paper aims to explore active components and mechanism of Scutellariae Radix(SR)-Phellodendri Chinensis Cortex(PCC) drug pair in treatment of psoriasis by network pharmacology and molecular docking. Specifically, the chemical components of SR and PCC were retrieved from literature and TCMSP, as well as targets of these components from PharmMapper and UniProt, and the targets related to psoriasis from OMIM, TTD, PharmGkb, and DrugBank. Then the chemical component-medicinal target, protein-protein interaction(PPI), and chemical component-psoriasis target networks were constructed by Cytoscape. Gene ontology(GO) term enrichment analysis and Kyoto encyclopedia of genes and genomes(KEGG) pathway enrichment analysis were performed based on Metascape. Finally, molecular docking of the chemical components(high degree) with core therapeutic targets was carried out by AutoDock vina. The results showed 88 compounds of SR and PCC(including baicalin, wogonoside, berberine and phellodendrine) and 30 targets of the pair in the treatment of psoriasis. The 30 targets mainly involved the biological processes such as neutrophil mediated immunity(GO: 0002446) and T cell activation(GO: 0042110), and the signaling pathways such as metabolism of xenobiotics by cytochrome P450(hsa00980), apoptosis(hsa04210), and PI3 K-Akt signaling pathway(hsa04151). The results of molecular docking demonstrated that the main active components can spontaneously bind to the targets and the binding energy of 46 components with epidermal growth factor receptor(EGFR) was less than-8 kcal·mol~(-1). According to the PPI analysis, EGFR may be a key target for the treatment of psoriasis. Active components such as baicalin and berberine had high binding affinity with EGFR. This study preliminarily revealed the multi-component, multi-target and multi-pathway mechanism of SR-PCC drug pair in the treatment of psoriasis, which provided theoretical basis for the research on the mechanism of the drug pair in the treatment of psoriasis.


Assuntos
Medicamentos de Ervas Chinesas , Psoríase , Simulação de Acoplamento Molecular , Psoríase/tratamento farmacológico , Psoríase/genética , Scutellaria baicalensis , Transdução de Sinais
2.
Zhongguo Zhong Yao Za Zhi ; 46(17): 4389-4394, 2021 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-34581041

RESUMO

This paper explored the ecologically suitable areas for growing Scutellaria baicalensis using Geographic Information System for Global Medicinal Plants(GMPGIS), to figure out the resource distribution of S. baicalensis worldwide and provide a scientific basis for its scientific introduction. A total of 349 S. baicalensis sampling sites were selected all over the world for GMPGIS-based analy-sis of the ecologically suitable areas with six ecological factors including annual average temperature, average temperature during the coldest season, average temperature during the warmest season, average annual precipitation, average annual relative humidity, and annual average illumination and soil type as the ecological indexes. The results demonstrated that the ecologically suitable areas for growing S. baicalensis were mostly located in the Northern hemisphere, and the suitable areas in the United States, China, and Russia accounted for 19.25%, 18.66%, and 13.15% of the total area worldwide, respectively. In China, the Inner Mongolia, Heilongjiang province, and Yunnan province occupied the largest proportions of the total area, namely 14.28%, 8.72%, and 6.18%, respectively. As revealed by ecological factors of each sampling site, S. baicalensis was resistant to low temperature but not to high temperature. The adaptive range of average annual precipitation is narrower than that of average annual air humidity. The suitable soils were mainly inceptisol, alfisol, and fluvisol. High temperature and rainy climate or excessively high soil bulk density was not conducive to the growth of S. baicalensis. The adoption of GMPGIS enabled to obtain areas with the greatest ecological similarity for S. baicalensis, which were reliable data supporting the exploration of resource distribution and reasonable introduction of S. baicalensis.


Assuntos
Plantas Medicinais , Scutellaria baicalensis , China , Clima , Solo
3.
Int J Mol Sci ; 22(16)2021 Aug 20.
Artigo em Inglês | MEDLINE | ID: mdl-34445678

RESUMO

Wogonin is one of the most active flavonoids from Scutellaria baicalensis Georgi (baikal skullcap), widely used in traditional Chinese medicine. It exhibits a broad spectrum of health-promoting and therapeutic activities. Together with baicalein, it is considered to be the one of main active ingredients of Chinese medicines for the management of COVID-19. However, therapeutic use of wogonin may be limited due to low market availability connected with its low content in baikal skullcap and lack of efficient preparative methods for obtaining this compound. Although the amount of wogonin in skullcap root often does not exceed 0.5%, this material is rich in wogonin glucuronide, which may be used as a substrate for wogonin production. In the present study, a rapid, simple, cheap and effective method of wogonin and baicalein preparation, which provides gram quantities of both flavonoids, is proposed. The obtained wogonin was used as a substrate for biotransformation. Thirty-six microorganisms were tested in screening studies. The most efficient were used in enlarged scale transformations to determine metabolism of this xenobiotic. The major phase I metabolism product was 4'-hydroxywogonin-a rare flavonoid which exhibits anticancer activity-whereas phase II metabolism products were glucosides of wogonin. The present studies complement and extend the knowledge on the effect of substitution of A- and B-ring on the regioselective glycosylation of flavonoids catalyzed by microorganisms.


Assuntos
Flavanonas/química , Flavanonas/farmacologia , Scutellaria baicalensis/química , Animais , Biotransformação , COVID-19/tratamento farmacológico , Flavanonas/isolamento & purificação , Flavanonas/farmacocinética , Fungos/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Raízes de Plantas/química , SARS-CoV-2/efeitos dos fármacos
4.
Artigo em Inglês | MEDLINE | ID: mdl-34069141

RESUMO

Flavonoids as the largest group of natural phytochemical compounds have received significant attention, as demonstrated by clinical trials, due to their chemotherapeutic and/or pharmacological effects against non-small-cell lung cancer (NSCLC) and asthma. Scutellaria baicalensis (S. baicalensis), known as one of the most popular medicinal plants and used in several countries, contains natural active flavone constituents, with the major compounds of the roots being baicalein, baicalin, wogonin, wogonoside and oroxylin A. S. baicalensis and their compounds are proven to have inhibitory effects on NSCLC cells when used at different concentrations. However, the exact mechanisms by which these compounds exert their therapeutic effects against asthma remain unexplored. Indeed, the mechanisms by which S. baicalensis and its flavone compounds exert a protective effect against nicotine-induced NSCLC and asthma are not yet fully understood. Therefore, this review explores the mechanisms involved in the therapeutic potential of flavone-rich extracts from S. baicalensis in nicotine-induced NSCLC and asthma.


Assuntos
Asma , Carcinoma Pulmonar de Células não Pequenas , Flavanonas , Flavonas , Neoplasias Pulmonares , Asma/induzido quimicamente , Asma/tratamento farmacológico , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Flavonas/uso terapêutico , Flavonoides , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Nicotina , Extratos Vegetais/uso terapêutico , Raízes de Plantas , Scutellaria baicalensis
5.
Int J Mol Sci ; 22(10)2021 May 13.
Artigo em Inglês | MEDLINE | ID: mdl-34068421

RESUMO

Resistance to epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) is a major obstacle in managing lung cancer. The root of Scutellaria baicalensis (SB) traditionally used for fever clearance and detoxification possesses various bioactivities including anticancer effects. The purpose of this study was to investigate whether SB exhibited anticancer activity in EGFR TKI-resistant lung cancer cells and to explore the underlying mechanism. We used four types of human lung cancer cell lines, including H1299 (EGFR wildtype; EGFR TKI-resistant), H1975 (acquired TKI-resistant), PC9/ER (acquired erlotinib-resistant), and PC9/GR (acquired gefitinib-resistant) cells. The ethanol extract of SB (ESB) decreased cell viability and suppressed colony formation in the four cell lines. ESB stimulated nuclear fragmentation and the cleavage of poly(ADP-ribose) polymerase (PARP) and caspase-3. Consistently, the proportion of sub-G1 phase cells and annexin V+ cells were significantly elevated by ESB, indicating that ESB induced apoptotic cell death in EGFR TKI-resistant cells. ESB dephosphorylated signal transducer and activator of transcription 3 (STAT3) and downregulated the target gene expression. The overexpression of constitutively active STAT3 reversed ESB-induced apoptosis, suggesting that ESB triggered apoptosis in EGFR TKI-resistant cells by inactivating STAT3. Taken together, we propose the potential use of SB as a novel therapeutic for lung cancer patients with EGFR TKI resistance.


Assuntos
Resistencia a Medicamentos Antineoplásicos , Neoplasias Pulmonares/patologia , Extratos Vegetais/farmacologia , Inibidores de Proteínas Quinases/farmacologia , Fator de Transcrição STAT3/antagonistas & inibidores , Scutellaria baicalensis/química , Apoptose , Proliferação de Células , Receptores ErbB/antagonistas & inibidores , Regulação Neoplásica da Expressão Gênica , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Neoplasias Pulmonares/metabolismo , Raízes de Plantas/química , Fator de Transcrição STAT3/genética , Fator de Transcrição STAT3/metabolismo , Células Tumorais Cultivadas
6.
J Pharm Biomed Anal ; 202: 114170, 2021 Aug 05.
Artigo em Inglês | MEDLINE | ID: mdl-34062496

RESUMO

Consistency evaluation of Traditional Chinese Medicinal preparations (TCMPs) with complex chemical composition is challenging. Chaihuang granules (CHG), as a well-known TCMP, consists of Chaihu (Bupleuri Radix) and Huangqin (Scutellariae Radix) extract. In this work, we used pharmacokinetics and metabolomics to evaluate consistency of CHG products from two different manufacturers. In the pharmacokinetic study, a liquid chromatography tandem mass spectrometry (LC-MS/MS) method was applied to determine the plasma concentration-time profiles of baicalin in rat plasma. Pharmacokinetic parameters, including the maximum concentration in blood (Cmax), area under the curve (AUC), the time to reach Cmax (Tmax), and half-life (T1/2), were calculated to assess the consistency preliminarily. And there was no significant difference in these pharmacokinetic parameters between the two CHG. In LC-MS-based metabolomics, the metabolic response profiles changes based on relative distance values (RDV) to different CHG products were compared. Meanwhile, the kinetic process of 31 differential endogenous metabolites that altered by CHG were determined. Metabolomics data showed the similar metabolic regulation effects to rats of the two formulations. Both pharmacokinetic and metabolomics results indicated there was no significant difference between CHG products. Furthermore, metabolic pathways significantly altered by CHG were elucidated, including phenylalanine, tyrosine and tryptophan biosynthesis, valine, leucine and isoleucine biosynthesis, phenylalanine metabolism, and sphingolipid metabolism. Pharmacokinetics combined with metabolomics could provide a comprehensive perspective for consistency evaluation of CHG.


Assuntos
Medicamentos de Ervas Chinesas , Espectrometria de Massas em Tandem , Animais , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Metabolômica , Ratos , Ratos Sprague-Dawley , Scutellaria baicalensis
7.
Talanta ; 230: 122328, 2021 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-33934785

RESUMO

Scutellaria baicalensis is one of the widely used Chinese traditional medicines, and wogonin is one of major active components in it. However, the mechanism of action of wogonin has largely remained unclear. In this work, we designed a fluorescent probe, namely ATTO565-WGN, by conjugating wogonin with the fluorophore ATTO565 based on Mannich reaction via a flexible chain linker. In vitro assays verified that the ATTO565-WGN conjugate has a similar anti-proliferative activity to wogonin against human A549 and HeLa cancer cell lines. Combining co-localization and competition studies, confocal fluorescence imaging clearly demonstrated that the fluorescent wogonin probe predominantly located in mitochondrial area of living cells, indicating that wogonin acts at mitochondrion to exert its pharmacological functions. Significantly, the conjugated ATTO565 fluorophore conferred the wogonin probe STED (Stimulated Emission Depletion) feature, enabling STED fluorescence living cell imaging with a 55 nm of ultrahigh spatial resolution. This will greatly beneficial for the in situ investigation of interactions between wogonin and biological targets at the finely organized and dynamic mitochondria of living cells. Moreover, this work also provides novel insights into rational design of mitochondrion targeting fluorescence probes for ultrahigh resolution living cell imaging.


Assuntos
Flavanonas , Flavanonas/farmacologia , Fluorescência , Humanos , Mitocôndrias , Scutellaria baicalensis
8.
Zhongguo Zhong Yao Za Zhi ; 46(8): 2061-2066, 2021 Apr.
Artigo em Chinês | MEDLINE | ID: mdl-33982520

RESUMO

In the pharmacopoeia, many process parameters for the purification process of Scutellariae Radix are unclear. In this study, deterministic screening design combined with design space method was used to optimize the purification process of Scutellariae Radix extract. Nine method parameters such as mass fraction of solution(X_1), first acid precipitation pH(X_2) and first holding time(X_3) in the purification process were firstly studied by definitive screening design. The yield of baicalin was defined as the evaluation index. A stepwise regression method was used then to build quantitative models between evaluation index and method parameters and the three most critical impact parameters were determined. Probability-based design space was calculated and successfully verified with the experimental error simulation method. Finally, the second standing temperature, the first standing temperature and the pH value of the second acid precipitation were determined as the three most critical method parameters. The recommended operating space was as follows: the second standing temperature 5-7 ℃, the first standing temperature 13-15 ℃, and the pH of the second acid precipitation 1.5-1.7. Within this operating space, the baicalin yield in the purification process was over 80%, and the probability of reaching the standard was over 0.96. In this study, we optimized the effect of various parameters for the purification process of the Scutellariae Radix extract in the pharmacopoeia on the yield of baicalin and provided a reference for industrial production of the exact of Scutellariae Radix.


Assuntos
Medicamentos de Ervas Chinesas , Scutellaria baicalensis , Flavonoides , Extratos Vegetais
9.
Sheng Wu Gong Cheng Xue Bao ; 37(4): 1312-1323, 2021 Apr 25.
Artigo em Chinês | MEDLINE | ID: mdl-33973444

RESUMO

Dihydroflavanol-4-reductase (Dfr) is a key enzyme that regulates the synthesis of anthocyanin and proanthocyanidin in the flavonoid biosynthesis pathway. To investigate the difference of dfr gene in Scutellaria baicalensis Georgi with different colors in the same ecological environment, three complete full-length sequences of dfr gene were cloned from the cDNA of S. baicalensis with white, purple-red and purple colors using homologous cloning and RACE techniques. The three genes were named Sbdfr1, Sbdfr2 and Sbdfr3, respectively, and their corresponding structures were analyzed. The results showed that all three Dfr proteins have highly conserved NADPH binding sites and substrate-specific binding sites. Phylogenetic analysis showed that they are closely related to that of the known S. viscidula (ACV49882.1). Analysis of key structural domains and 3D models revealed differences in the catalytically active regions on the surface of all three Dfr proteins, and their unique structural characteristics may provide favorable conditions for studying the substrate specificity of different Dfr proteins. qRT-PCR analysis shows that dfr was expressed at different level in all tissues except the roots of S. baicalensis in full-bloom. During floral development, the expression level of dfr in white and purple-flowered Scutellaria showed an overall upward trend. In purple-red-flowered Scutellaria, the expression first slowly increased, followed by a decrease, and then rapidly increased to the maximum. This research provides a theoretical basis for further exploring the mechanism and function of Dfr substrate selectivity, and are of great scientific value for elucidating the molecular mechanism of floral color variation in S. baicalensis.


Assuntos
Antocianinas , Scutellaria baicalensis , Clonagem Molecular , Cor , Filogenia , Scutellaria baicalensis/genética
10.
Chin J Nat Med ; 19(5): 364-375, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-33941341

RESUMO

Huang-Qin Decoction (HQD) is a classic prescription for diarrhea in Chinese medicine treatment. Recent studies have demonstrated that HQD and its modified formulation PHY906 could ameliorate irinotecan (CPT-11) induced gastrointestinal (GI) toxicity and enhance its anticancer therapeutic efficacy. Nevertheless, which constituents in HQD are effective is still unclear so far. The study aims to screen out the key bioactive components combination from HQD that could enhance the anticancer effect of CPT-11. First, the potential bioactive constituents were obtained through system pharmacology strategy. Then the bioactivity of each constituent was investigated synthetically from the aspects of NCM460 cell migration, TNF-α release of THP-1-derived macrophage and MTT assay in HCT116 cell. The contribution of each constituent in HQD was evaluated using the bioactive index Ei, which taken the content and bioactivity into comprehensive consideration. And then, the most contributing constituents were selected out to form a key-component combination. At last, the bioefficacy of the key-component combination was validated in vitro and in vivo. As a result, a key-component combination (HB4) consisting of four compounds baicalin, baicalein, glycyrrhizic acid and wogonin was screened out. In vitro assessment indicated that HB4 could enhance the effect of CPT-11 on inhibiting cell proliferation and inducing apoptosis in HCT116. Furthermore, the in vivo study confirmed that HB4 and HQD have similar pharmacological activity and could both enhance the antitumor effect of CPT-11 in HCT116 xenograft model. Meanwhile, HB4 could also reduce the CPT-11 induced GI toxicity.


Assuntos
Antineoplásicos/farmacologia , Medicamentos de Ervas Chinesas , Irinotecano/farmacologia , Scutellaria baicalensis , Animais , Apoptose , Proliferação de Células , Modelos Animais de Doenças , Medicamentos de Ervas Chinesas/farmacologia , Células HCT116 , Humanos , Scutellaria baicalensis/química , Ensaios Antitumorais Modelo de Xenoenxerto
11.
Molecules ; 26(8)2021 Apr 16.
Artigo em Inglês | MEDLINE | ID: mdl-33923637

RESUMO

Baicalin which has multiple biological activities is the main active component of the root of Scutellaria baicalensis Georgi (SBG). Although its isolation and purification by adsorption methods have aroused much interest of the scientific community, it suffered from the poor selectivity of the adsorbents. In this work, an environmentally benign method was developed to prepare ionic liquids (ILs) grafted silica by using IL 1-butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide ([C4mim]NTf2) and ethanol as reaction media. The IL 1-propyl-3-methylimidazolium chloride ([C3mim]Cl) grafted silica ([C3mim]+Cl-@SiO2) was used to adsorb and purify baicalin from the root extract of Scutellaria baicalensis Georgi (SBG). Experimental results indicated that the adsorption equilibrium can be quickly achieved (within 10 min). The adsorption behavior of [C3mim]+Cl-@SiO2 for baicalin was in good agreement with Langmuir and Freundlich models and the adsorption was a physisorption process as suggested by Dubinin-Radushkevich model. Compared with commercial resins, [C3mim]+Cl-@SiO2 showed the strongest adsorption ability and highest selectivity. After desorption and crystallization, a purity of baicalin as high as 96.5% could be obtained. These results indicated that the ILs grafted silica materials were promising adsorbents for the adsorption and purification of baicalin and showed huge potential in the purification of other bioactive compounds from natural sources.


Assuntos
Flavonoides/química , Líquidos Iônicos/química , Dióxido de Silício/química , Adsorção , Flavonoides/isolamento & purificação , Extratos Vegetais/química , Scutellaria baicalensis/química
12.
PLoS One ; 16(4): e0250663, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33905439

RESUMO

In a disease-state-dependent manner, the histamine-resistant itch in dry skin-based skin diseases such as atopic dermatitis (AD) and xerosis is mainly due to hyperinnervation in the epidermis. Semaphorin 3A (Sema3A) is a nerve repulsion factor expressed in keratinocytes and it suppresses nerve fiber elongation in the epidermis. Our previous studies have shown that Sema3A ointment inhibits epidermal hyperinnervation and scratching behavior and improves dermatitis scores in AD model mice. Therefore, we consider Sema3A as a key therapeutic target for improving histamine-resistant itch in AD and xerosis. This study was designed to screen a library of herbal plant extracts to discover compounds with potential to induce Sema3A in normal human epidermal keratinocytes (NHEKs) using a reporter gene assay, so that positive samples were found. Among the positive samples, only the extract of S. baicalensis was found to consistently increase Sema3A levels in cultured NHEKs in assays using quantitative real-time PCR and ELISA. In evaluation of reconstituted human epidermis models, the level of Sema3A protein in culture supernatants significantly increased by application of the extract of S. baicalensis. In addition, we investigated which components in the extract of S. baicalensis contributed to Sema3A induction and found that baicalin and baicalein markedly increased the relative luciferase activity, and that baicalein had higher induction activity than baicalin. Thus, these findings suggest that S. baicalensis extract and its compounds, baicalin and baicalein, may be promising candidates for improving histamine-resistant itch via the induction of Sema3A expression in epidermal keratinocytes.


Assuntos
Extratos Vegetais/química , Scutellaria baicalensis/química , Semaforina-3A/metabolismo , Linhagem Celular , Flavanonas/genética , Flavanonas/metabolismo , Flavonoides/genética , Flavonoides/metabolismo , Genes Reporter , Humanos , Queratinócitos/citologia , Queratinócitos/efeitos dos fármacos , Queratinócitos/metabolismo , Modelos Biológicos , Extratos Vegetais/farmacologia , RNA Mensageiro/metabolismo , Scutellaria baicalensis/metabolismo , Semaforina-3A/genética
13.
Biomed Pharmacother ; 138: 111445, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33711551

RESUMO

Whilst the popular use of herbal medicine globally, it poses challenges in managing potential drug-herb interaction. There are two folds of the drug-herb interaction, a beneficial interaction that may improve therapeutic outcome and minimise the toxicity of drug desirably; by contrast, negative interaction may evoke unwanted clinical consequences, especially with drugs of narrow therapeutic index. Scutellaria baicalensis Georgi is one of the most popular medicinal plants used in Asian countries. It has been widely used for treating various diseases and conditions such as cancer, diabetes, inflammation, and oxidative stress. Studies on its extract and bioactive compounds have shown pharmacodynamic and pharmacokinetic interactions with a wide range of pharmaceutical drugs as evidenced by plenty of in vitro, in vivo and clinical studies. Notably, S. baicalensis and its bioactives including baicalein, baicalin and wogonin exhibited synergistic interactions with many pharmaceutical drugs to enhance their efficacy, reduce toxicity or overcome drug resistance to combat complex diseases such as cancer, diabetes and infectious diseases. On the other hand, S. baicalensis and its bioactives also affected the pharmacokinetic profile of many drugs in absorption, distribution, metabolism and elimination via the regulatory actions of the efflux pumps and cytochrome P450 enzymes. This review provides comprehensive references of the observed pharmacodynamic and pharmacokinetic drug interactions of Scutellaria baicalensis and its bioactives. We have elucidated the interaction with detailed mechanistic actions, identified the knowledge gaps for future research and potential clinical implications. Such knowledge is important for the practice of both conventional and complementary medicines, and it is essential to ensure the safe use of related herbal medicines. The review may be of great interest to practitioners, consumers, clinicians who require comprehensive information on the possible drug interactions with S. baicalensis and its bioactives.


Assuntos
Interações Ervas-Drogas/fisiologia , Preparações Farmacêuticas/administração & dosagem , Preparações Farmacêuticas/metabolismo , Extratos Vegetais/metabolismo , Extratos Vegetais/uso terapêutico , Scutellaria baicalensis , Animais , Doenças Transmissíveis/tratamento farmacológico , Doenças Transmissíveis/metabolismo , Diabetes Mellitus/tratamento farmacológico , Diabetes Mellitus/metabolismo , Resistência a Medicamentos/efeitos dos fármacos , Resistência a Medicamentos/fisiologia , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/metabolismo , Medicamentos de Ervas Chinesas/uso terapêutico , Humanos , Neoplasias/tratamento farmacológico , Neoplasias/metabolismo , Extratos Vegetais/isolamento & purificação
14.
Front Cell Infect Microbiol ; 11: 624745, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33763384

RESUMO

Human babesiosis is a CDC reportable disease in the United States and is recognized as an emerging health risk in multiple parts of the world. The current treatment for human babesiosis is suboptimal due to treatment failures and unwanted side effects. Although Babesia duncani was first described almost 30 years ago, further research is needed to elucidate its pathogenesis and clarify optimal treatment regimens. Here, we screened a panel of herbal medicines and identified Cryptolepis sanguinolenta, Artemisia annua, Scutellaria baicalensis, Alchornea cordifolia, and Polygonum cuspidatum to have good in vitro inhibitory activity against B. duncani in the hamster erythrocyte model. Furthermore, we found their potential bioactive compounds, cryptolepine, artemisinin, artesunate, artemether, and baicalein, to have good activity against B. duncani, with IC50 values of 3.4 µM, 14 µM, 7.4 µM, 7.8 µM, and 12 µM, respectively, which are comparable or lower than that of the currently used drugs quinine (10 µM) and clindamycin (37 µM). B. duncani treated with cryptolepine and quinine at their respective 1×, 2×, 4× and 8× IC50 values, and by artemether at 8× IC50 for three days could not regrow in subculture. Additionally, Cryptolepis sanguinolenta 90% ethanol extract also exhibited no regrowth after 6 days of subculture at doses of 2×, 4×, and 8× IC50 values. Our results indicate that some botanical medicines and their active constituents have potent activity against B. duncani in vitro and may be further explored for more effective treatment of babesiosis.


Assuntos
Artemisia annua , Babesia , Euphorbiaceae , Fallopia japonica , Animais , Cricetinae , Cryptolepis , Humanos , Extratos Vegetais , Scutellaria baicalensis
15.
Zhongguo Zhong Yao Za Zhi ; 46(5): 1191-1196, 2021 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-33787114

RESUMO

To explore the effect of Huangqin Decoction on ulcerative colitis(UC) pyroptosis, and to explain the mechanism of pyroptosis based on NOD-like receptor thermoprotein domain 3(NLRP3)/cysteine proteinase 1(caspase-1) pathway. The animal model of UC induced with 3% dextran sodium sulfate(DSS) was established. The experimental animals were divided into control group, model group, low-dose(4.55 g·kg~(-1)), medium-dose(9.1 g·kg~(-1)) and high-dose(18.2 g·kg~(-1)) Huangqin Decoction groups and salazosulfapyridine group(0.45 g·kg~(-1)). While modeling, intragastric administration was given for 7 consecutive days. On the 8 th day, the mice were euthanized, the colon length was collected, and the histopathological changes were observed by HE staining. The content of interleukin-18(IL-18) was observed by ELISA. The content of lactatedehydrogenase(LDH)was determined by microplate method. TUNEL assay kit was used to detect the cell death. The immunohistochemical staining was used to detect the expressions of NLRP3 and apoptosis-associated speck-like protein containing a CARD(ASC). Western blot was used to detect the expressions of interleukin-1ß(IL-1ß), caspase-1 and gasdermin D(GSDMD).The experimental study showed that compared with normal group, the LDH content, TUNEL positive staining, inflammatory factors(IL-18, IL-1ß), and proteins associated with pyroptosis were significantly increased(P<0.05). Compared with model control group, the LDH content, TUNEL positive staining, inflammatory factors(IL-18, IL-1ß), and proteins associated with pyroptosis were decreased, and these results were more significant in high-dose groups(P<0.05). The results of HE staining showed that Huangqin Decoction could improve the pathological changes of colon. Huangqin Decoction could inhibit UC cell pyroptosis, and the mechanism may be closely related to NLRP3/caspase-1 signaling pathway.


Assuntos
Colite Ulcerativa , Piroptose , Animais , Caspase 1/genética , Colite Ulcerativa/tratamento farmacológico , Camundongos , Proteína 3 que Contém Domínio de Pirina da Família NLR/genética , Scutellaria baicalensis
16.
Food Res Int ; 140: 109857, 2021 02.
Artigo em Inglês | MEDLINE | ID: mdl-33648175

RESUMO

This study gives new insights to understand the type of interactions between Ginkgo biloba L. and Scutellaria baicalensis Georgi, two Chinese medicinal plants with well documented neuroprotective effects, on three targets in Alzheimer's disease (AD): acetylcholinesterase (AChE) and butyrylcholnesterase (BuChE) inhibition and hydrogen peroxide scavenging. Individual samples, binary mixtures with different proportions of both plant species, and also a commercial multicomponent combination containing both plants together with unroasted Coffea arabica L. and quercetin-3-O-rutinoside were used to perform this in vitro evaluation. Sample phenolic profiles were also determined by HPLC-DAD, showing the presence of several flavonoid glycosides, phenolic acids and a methylxanthine. In order to investigate the possible synergism/antagonism interaction, data obtained were analyzed by CompuSyn software. The results showed that G. biloba and S. baicalensis alone display better activities than in mixtures, most of the interactions exhibiting different degrees of antagonism. A slight synergism interaction was only observed for the commercial multicomponent mixture tested against H2O2. Further analysis was carried out to understand which compounds could be responsible for the antagonistic interaction. Seventeen single pure compounds present in all extracts were tested against AChE inhibition, most of them displaying weak or no activity. Only caffeine had a remarkable activity. Five different binary and quaternary mixture compositions were design to deepen the interaction between these compounds, revealing mainly phenolic acid-flavonoid, flavonoid-flavonoid and methylxanthine-flavonoid-phenolic acid antagonistic interactions. These results clearly show that, for the targets evaluated, there is no potentiation of the neuroprotective effect by combining S. baicalensis and G. biloba extracts.


Assuntos
Ginkgo biloba , Scutellaria baicalensis , Colinesterases , Peróxido de Hidrogênio , Extratos Vegetais/farmacologia , Espécies Reativas de Oxigênio
17.
Phytother Res ; 35(6): 3194-3204, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-33587321

RESUMO

The current worldwide outbreak of the coronavirus disease 2019 (COVID-19) has been declared a public health emergency. The angiotensin-converting enzyme II (ACE2) has been reported as the primary host-cell receptor for severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), the causative virus of COVID-19. In this study, we screened ACE2 ligands from Radix Scutellariae and investigated its suppressive effect on SARS-CoV-2 spiked pseudotyped virus in vitro. HEK293T cells stably expressing ACE2 receptors (ACE2 cells) were used to provide the receptor for the ACE2/cell membrane chromatography (CMC) method used for analysis. The SARS-CoV-2-spiked pseudotyped virus was used to examine the anti-viropexis effect of the screened compounds in ACE2 cells. Molecular docking and the surface plasmon resonance (SPR) assay were used to determine the binding properties. Oroxylin A exhibited an appreciable suppressive effect against the entrance of the SARS-CoV-2-spiked pseudotyped virus into ACE2 cells, which showed good binding to ACE2 as determined using SPR and CMC. Oroxylin A was shown to be a potential candidate in the treatment for COVID-19 by virtue of its blocking the entrance of SARS-CoV-2 into ACE2 cells by specifically binding to the ACE2 receptor.


Assuntos
COVID-19/tratamento farmacológico , Flavonoides/farmacologia , SARS-CoV-2/efeitos dos fármacos , Scutellaria baicalensis/química , Enzima de Conversão de Angiotensina 2/metabolismo , Membrana Celular/metabolismo , Cromatografia , Células HEK293 , Humanos , Simulação de Acoplamento Molecular , Ligação Proteica/efeitos dos fármacos
18.
Nan Fang Yi Ke Da Xue Xue Bao ; 41(2): 256-263, 2021 Feb 25.
Artigo em Chinês | MEDLINE | ID: mdl-33624600

RESUMO

OBJECTIVE: To explore the effect of Huangqin decoction (HQD) on group 3 innate lymphoid cells (ILC3s) and helper T cells (Th) for treatment of ulcerative colitis (UC). OBJECTIVE: Male Balb/c mice were randomly divided into control group, DSS group, mesalazine group (ME, 400 mg/kg), and 2.275 g/kg, 4.55 g/kg and 9.1 g/kg HQD groups. All the mice were given free access to normal chow. Except for those in the normal control group, all the mice were given 3% DSS solution for 7 days to establish models of UC. The mice in ME group and 3 HQD groups were given mesalazine or HQD via oral gavage at the specified doses once a day. Flow cytometry was performed to analyze the ILC3s, MHC Ⅱ, Th1 and Treg in the lamina propria lymphocytes in the colon. Milliplex was performed to determine cytokine levels of in the colon tissues. OBJECTIVE: Compared with those in DSS group, the mice in the 3 HQD groups all showed obviously lessened symptoms of UC with significantl decreased DAI score (P < 0.001) and macroscopic score (P < 0.001). The results of flow cytometry showed that HQD treatment significantly increased the percentage of ILC3s (P < 0.05) and expression of MHCⅡ (P < 0.05), obviously reduced the proportion of Th1 (P < 0.05) but increased Treg cells (P < 0.05) in the colon tissues. Milliplex showed that HQD treatment significantly reduced the expressions of Th-related pro-inflammatory cytokines including IL-2 (P < 0.05), IL-17A (P < 0.05), IL-23 (P < 0.05), TNF-α (P < 0.05), and IFN-γ (P < 0.05). OBJECTIVE: HQD alleviates DSS- induced UC in mice by increasing ILC3s and MHC Ⅱ expression to suppress the function of Th17 and Th1 cells and promote Treg and Th2 cells.


Assuntos
Colite Ulcerativa , Animais , Contagem de Células , Colite Ulcerativa/tratamento farmacológico , Imunidade Inata , Masculino , Mesalamina/uso terapêutico , Camundongos , Scutellaria baicalensis
19.
Ann Palliat Med ; 10(3): 2979-2989, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33615818

RESUMO

BACKGROUND: Oral medication therapies are more conventional than other non-surgical therapies in the acute phase of Peyronie's disease (PD). Although the commonly used oral drugs for PD have shown poor or indeterminate outcomes, most patients prefer oral medications. The aim of this study was to evaluate the efficacy and safety of Scutellaria baicalensis extract for treating acute-phase PD patients and examine the practicality of treatment strategies for PD according to the disease course. METHODS: This retrospective study was performed at our institution from 2005 to 2015 and analyzed the data of 261 patients with PD. The acute-phase PD patients received Scutellaria baicalensis extract for 6 months. After oral treatment, the patients with persistent curvature underwent surgical correction during the stable phase. RESULTS: During this study period, 183 patients received oral treatment with Scutellaria baicalensis, and 78 patients did not. Compared to the untreated patients, treatment with Scutellaria baicalensis had a significant effect in improving the symptoms of acute-phase PD. The mean time required for stabilization also showed a significant statistical difference. Treatment with Scutellaria baicalensis was safe and well-tolerated. After the disease stabilized, 70 and 31 patients with significant penile curvature underwent surgical correction by 16- dot plication and great saphenous vein grafting procedures, respectively. At the one-year follow-up, complete penile straightening and penile length shortening were observed in 92.86% and 41.43% of the patients after 16-dot plication and in 87.10% and 25.81% of the patients after grafting procedures, respectively. The postoperative Erectile Function domain of the International Index of Erectile Function scales were maintained in all patients after the 16-dot plication procedure and decreased in 54.84% of the patients after the grafting procedure. Overall, 92.86% and 83.87% of the patients who received 16-dot plication and grafting procedures, respectively, were satisfied with the final surgical results. CONCLUSIONS: Treatment with extract of Scutellaria baicalensis seems to be beneficial for improvements in symptoms of acute phase PD and acceleration of the disease stabilization. The 16-dot plication and great saphenous vein grafting procedure seem effective options in the surgical management of the stable phase after Scutellaria baicalensis administration in the acute phase of PD.


Assuntos
Induração Peniana , Scutellaria baicalensis , Humanos , Masculino , Satisfação do Paciente , Induração Peniana/tratamento farmacológico , Induração Peniana/cirurgia , Extratos Vegetais/uso terapêutico , Estudos Retrospectivos , Resultado do Tratamento
20.
Phytomedicine ; 83: 153477, 2021 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-33545549

RESUMO

BACKGROUND: Our previous clinical research showed that the interaction between gut microbiota and bile acids (BAs) in patients with type 2 diabetes mellitus (T2DM) changed significantly. We hypothesized that T2DM could be improved by adjusting this interaction mediated by farnesoid X receptor (FXR). T2DM belongs to the category of "xiaoke" in traditional Chinese medicine. Radix scutellariae has the effects of clearing away heat and eliminating dampness, curing jaundice and quenching thirst and is widely used alone or in combination with other medicines for the treatment of T2DM in China and throughout Asia. Additionally, the interaction between Radix scutellariae and gut microbiota may influence its efficacy in the treatment of T2DM. PURPOSE: This study chose Radix scutellariae to validate that T2DM could improve by adjusting the interaction between gut microbiota and bile acid metabolism. STUDY DESIGN AND METHODS: Radix scutellariae water extract (WESB) was administered to a T2DM rat model established by a high-fat diet combined with streptozotocin. The body weight and blood glucose and insulin levels were measured. The levels of serum lipids, creatinine, uric acid, albumin and total bile acid were also detected. Changes in the pathology and histology of the pancreas, liver and kidney were observed by haematoxylin-eosin staining. The 16S rRNAs of gut microbiota were sequenced, and the faecal and serum BAs were determined by liquid chromatography tandem mass spectrometry. The expression levels of BA metabolism-associated proteins in the liver and intestine were evaluated by immunoblot analysis. RESULTS: The results showed that WESB improved hyperglycaemia, hyperlipaemia, and liver and kidney damage in T2DM rats. In addition, the abundances of key gut microbiota and the concentrations of certain secondary BAs in faeces and serum were restored. Moreover, there was a significant correlation between the restored gut microbiota and BAs, which might be related to the activation of liver cholesterol 7α-hydroxylase (CYP7A1) and the inhibition of FXR expression in the intestine rather than the liver. CONCLUSIONS: This study provided new ideas for the prevention or treatment of clinical diabetes and its complications by adjusting the interaction between gut microbiota and bile acid metabolism.


Assuntos
Ácidos e Sais Biliares/metabolismo , Microbioma Gastrointestinal/efeitos dos fármacos , Hiperglicemia/tratamento farmacológico , Hiperlipidemias/tratamento farmacológico , Scutellaria baicalensis/química , Animais , Colesterol 7-alfa-Hidroxilase/metabolismo , Diabetes Mellitus Experimental/tratamento farmacológico , Diabetes Mellitus Experimental/metabolismo , Diabetes Mellitus Tipo 2/tratamento farmacológico , Diabetes Mellitus Tipo 2/metabolismo , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Microbioma Gastrointestinal/fisiologia , Hiperglicemia/metabolismo , Hiperglicemia/microbiologia , Hiperlipidemias/metabolismo , Hiperlipidemias/microbiologia , Intestinos/efeitos dos fármacos , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Masculino , Ratos Sprague-Dawley
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