Antimicrobial and antioxidant activity of Panax ginseng and Hedysarum neglectum root crop extracts / Atividade antimicrobiana e antioxidante de extratos de raízes de Panax ginseng e Hedysarum neglectum

In order to ensure the timely and uninterrupted supply of medicinal plant raw materials, the methods of cultivation of plant cell cultures, namely, the production of plant root cultures, are relevant. In this paper, the geroprotective potential of Hedysarum neglectum Ledeb and Panax ginseng C. A. Mey root cultures is studied. They were cultured under in vitro conditions by transforming the rhizome (H. neglectum) and seed seedlings (P. ginseng) with Agrobacterium rhizogenes 15834 Swiss. To identify the geroprotective potential, the antimicrobial disc-diffusion method and the antioxidant activity were analyzed by titration of KMnO4 extracts of plant root cultures. The qualitative and quantitative composition was analyzed using high-performance liquid chromatography, thin-layer chromatography, and gas chromatography with mass spectrometry. In the course of the work, the presence of antimicrobial and antioxidant activity of plant root culture extracts was established. Biologically active substances contained in extracts of Hedysarum neglectum Ledeb root crops and Panax ginseng C. A. Mey are characterized by geroprotective potential, so they can act as a source of natural antioxidants in the functional nutrition of the geroprotective orientation.

Para garantir o abastecimento em tempo e ininterrupto de matérias-primas de plantas medicinais, são relevantes os métodos de cultivo de culturas de células vegetais, nomeadamente a produção de culturas de raízes vegetais. Neste trabalho, foi estudado o potencial geroprotetor de culturas de raízes de Hedysarum neglectum Ledeb e Panax ginseng C. A. Mey. Eles foram cultivados em condições in vitro pela transformação do rizoma (H. neglectum) e mudas de sementes (P. ginseng) com Agrobacterium rhizogenes 15834 Swiss. Para identificar o potencial geroprotetor, o método antimicrobiano de difusão em disco e a atividade antioxidante foram analisados por titulação de extratos de KMnO4 de raízes de plantas. A composição qualitativa e quantitativa foi analisada por cromatografia líquida de alta eficiência, cromatografia em camada delgada e cromatografia gasosa com espectrometria de massa. No decorrer do trabalho, foi constatada a presença de atividade antimicrobiana e antioxidante dos extratos de raízes de plantas. Substâncias biologicamente ativas contidas em extratos de raízes de H. neglectum Ledeb e P. ginseng C. A. Mey são caracterizadas pelo potencial geroprotetor, podendo atuar como fonte de antioxidantes naturais na nutrição funcional da orientação geroprotetora.

Efficacy of Citrullus colocynthis seed extract on Earias vittella, Fabricius, (Lepidoptera: Noctuidae): environment sustainable approach

Abstract Earias vittellaFabricius, 1794 (Noctuidae: Lepidoptera) is deliberated to be one of the most destructive pests of cotton and okra vegetation in the world including Asia. The pest has established resistance to various synthetic insecticides. The use of bio-pesticide is one of the unconventional approaches to develop a vigorous ecosystem without harming non- target pests and beneficial natural insect fauna. In the present study, the toxicity levels of Citrullus colocynthis seed extract have been evaluated against the populations of E. vittellaunder standardized laboratory conditions. The toxic effects of C. colocynthis on development periods, protein contents and esterase activity of the life stages of E. vittella were also evaluated. The toxicity levels of methanol, ethanol, hexane, water and profenofos were evaluated on the 1st instar larvae of E. vittella. LC30 and LC80 concentrations exhibited the effectiveness of methanol-based C. colocynthis seed extract against 1st instar larvae of E. vitella. The enhanced larval and pupal periods were revealed in treated samples during the comparison with untreated samples. The intrinsic rate of increase, net reproductive rate in the LC30 and LC80 concentrations exposed larvae remained less than the control treatment. Fecundity, the esterase activity and protein contents were declined in LC30 and LC80 treated samples as compared to the control. The present findings suggest that C. colosynthis extracts based botanical insecticides are beneficial, ecosystem sustainable and can be integrated with insect management programs from environment safety perspective.

Resumo Earias vittella Fabricius, 1794 (Noctuidae: Lepidoptera) é considerada uma das pragas mais destrutivas de algodão e quiabo no mundo, incluindo a Ásia. Essa praga estabeleceu resistência a vários inseticidas sintéticos. O uso de biopesticidas é uma das abordagens não convencionais para desenvolver um ecossistema saudável sem prejudicar as pragas não alvo e a fauna natural benéfica de insetos. No presente estudo, os níveis de toxicidade do extrato de semente de Citrullus colocynthis foram avaliados nas populações de E. vittella em condições de laboratório padronizadas. Os efeitos tóxicos de C. colocynthis nos períodos de desenvolvimento, conteúdo de proteína e atividade esterase das fases de vida de E. vittella também foram avaliados. Os níveis de toxicidade de metanol, etanol, hexano, água e profenofós foram avaliados em larvas de 1º instar de E. vittella. As concentrações de LC30 e LC80 apresentaram eficácia do extrato de sementes de C. colocynthis à base de metanol contra larvas de 1º instar de E. vittella. Os períodos larval e pupal aumentados foram revelados nas amostras tratadas durante a comparação com as amostras não tratadas. A taxa intrínseca de aumento e a taxa reprodutiva líquida nas concentrações de larvas expostas LC30 e LC80 permaneceram menores do que o tratamento controle. A fecundidade, a atividade da esterase e o conteúdo de proteína diminuíram nas amostras tratadas com LC30 e LC80 em comparação com o controle. As presentes descobertas sugerem que os extratos de C. colocynthis à base de inseticidas botânicos são benéficos, sustentáveis para o ecossistema e podem ser integrados com programas de manejo de insetos do ponto de vista da segurança ambiental.

Phenolic compounds and antifungal activity of ethyl acetate extract and methanolic extract from Capsicum chinense Jacq. ripe fruit

Abstract Food loss due to contamination caused by fungi has much impact on agriculture and leads to significant economic losses. Synthetic and natural fungicides have been used for avoiding losses of several food products due to fungal contamination. As a result, species of the genus Capsicum have been used for preserving food because of their chemical compounds with antifungal activity. Therefore, this study aimed at identifying some phenolic compounds found in both ethyl acetate extract (EAE) and methanolic extract (ME) from habanero pepper (C. chinense) ripe fruit by liquid chromatography tandem mass spectrometry with electrospray ionization (LC-ESI-MS/MS) and at evaluating their antifungal activities against fungi Sclerotinia sclerotiorum, Rhizopus stolonifer and Colletotrichum gloeosporioides. Extracts resulted from a sequential process of maceration. Antifungal activity was evaluated by the disk diffusion method (DDM) at the following doses of both diluted extracts: 25 µL, 50 µL, 100 µL and 200 µL. The chemical analysis showed that there were protocatechuic acid, gentisic acid, vanillic acid, kaempferol-3-O-robinobiosideo and naringenin in both extracts. EAE showed high inhibition of mycelial growth at both doses 100µL and 200µL against the three fungi while methanolic exhibited weak activity even at the highest dose under investigation. However, further in-depth studies are needed to reinforce their uses and practical applications to the agricultural field.

Resumo As perdas de alimentos por contaminação causada por fungos são de grande impacto negativo para a agricultura, gerando altos prejuízos econômicos. Para evitar as perdas de diversos produtos alimentícios pela contaminação fúngica são utilizados fungicidas sintéticos e naturais. As espécies do gênero Capsicum são usadas há muitos anos para auxiliar na conservação de alimentos por possuírem substâncias químicas com ação antifúngica entre outras. Neste contexto, o objetivo deste estudo foi identificar alguns compostos fenólicos por cromatografia líquida de alta eficiência acoplada à espectrometria de massas sequencial (LC-ESI-MS/MS) presentes nos extratos acetato de etila (EAE) e metanólico (ME) dos frutos maduros da pimenta biquinho (C. chinense) e avaliar atividade antifúngica de EAE e ME contra os fungos Sclerotinia sclerotiorum, Rhizopus stolonifer e Colletotrichum gloeosporioides. Os extratos foram obtidos de forma sequencial, utilizando o procedimento de maceração. A atividade antifúngica foi avaliada seguindo a metodologia de difusão em disco, nas doses de 25 µL, 50 µL, 100 µL e 200 µL de cada extrato diluído. A análise química evidenciou a presença de ácido protocatequico, ácido gentisico, ácido vanílico, kaempferol-3-O-robinobiosídeo e naringenina em ambos os extratos. EAE revelou maior poder de inibição do crescimento micelial nas doses de 100µL e 200µL contra os três fungos testados, enquanto ME exibiu fraca atividade inclusive na maior dose investigada. Entretanto, estudos mais aprofundados ainda são necessários para consolidar seu uso e aplicação prática na área agronômica.

Antimicrobial and antioxidant activity of Panax ginseng and Hedysarum neglectum root crop extracts

Abstract In order to ensure the timely and uninterrupted supply of medicinal plant raw materials, the methods of cultivation of plant cell cultures, namely, the production of plant root cultures, are relevant. In this paper, the geroprotective potential of Hedysarum neglectum Ledeb and Panax ginseng C. A. Mey root cultures is studied. They were cultured under in vitro conditions by transforming the rhizome (H. neglectum) and seed seedlings (P. ginseng) with Agrobacterium rhizogenes 15834 Swiss. To identify the geroprotective potential, the antimicrobial disc-diffusion method and the antioxidant activity were analyzed by titration of KMnO4 extracts of plant root cultures. The qualitative and quantitative composition was analyzed using high-performance liquid chromatography, thin-layer chromatography, and gas chromatography with mass spectrometry. In the course of the work, the presence of antimicrobial and antioxidant activity of plant root culture extracts was established. Biologically active substances contained in extracts of Hedysarum neglectum Ledeb root crops and Panax ginseng C. A. Mey are characterized by geroprotective potential, so they can act as a source of natural antioxidants in the functional nutrition of the geroprotective orientation.

Resumo Para garantir o abastecimento em tempo e ininterrupto de matérias-primas de plantas medicinais, são relevantes os métodos de cultivo de culturas de células vegetais, nomeadamente a produção de culturas de raízes vegetais. Neste trabalho, foi estudado o potencial geroprotetor de culturas de raízes de Hedysarum neglectum Ledeb e Panax ginseng C. A. Mey. Eles foram cultivados em condições in vitro pela transformação do rizoma (H. neglectum) e mudas de sementes (P. ginseng) com Agrobacterium rhizogenes 15834 Swiss. Para identificar o potencial geroprotetor, o método antimicrobiano de difusão em disco e a atividade antioxidante foram analisados por titulação de extratos de KMnO4 de raízes de plantas. A composição qualitativa e quantitativa foi analisada por cromatografia líquida de alta eficiência, cromatografia em camada delgada e cromatografia gasosa com espectrometria de massa. No decorrer do trabalho, foi constatada a presença de atividade antimicrobiana e antioxidante dos extratos de raízes de plantas. Substâncias biologicamente ativas contidas em extratos de raízes de H. neglectum Ledeb e P. ginseng C. A. Mey são caracterizadas pelo potencial geroprotetor, podendo atuar como fonte de antioxidantes naturais na nutrição funcional da orientação geroprotetora.

Efeito de extratos vegetais de Hamamelis virginiana, Persea americana, Cynara scolymus L e Stryphnodendron barbatiman Msobre a expressão fenotípica dos fatores de virulência em biofilmes de Candida albicans / Effect of Hamamelis virginiana, Persea americana, Cynara scolymus L and Stryphnodendron barbatiman M plant extracts on the phenotypic expression of virulence factors in biofilms of the Candida albicans

Objetivo: Analisar a expressão fenotípica de fatores de virulência em biofilmes de Candida albicans frente a extratos glicólicos de plantas. Material e Métodos: Os biofilmes de Candida albicans (ATCC 18804) obtidos a partir de incubação de 48 horas foram expostos por 5 minutos e 24 horas a diferentes concentrações de extratos glicólicos de Hamamelis virginiana e Persea americana, Cynara scolymus L e Stryphnodendron barbatiman M, a fim de verificar a ação antifúngica da proteinase, fosfolipase e hemolisina. Resultados: Todos os extratos foram eficazes na redução do biofilme. Em contato por 5 minutos. os extratos reduziram 50% do biofilme. Após 24 horas. o extrato de Persea americana apresentou o biofilme em 90%, seguido de Cynara scolymus, que o interrompeu em 85%. Houve mudança na intensidade da proteinase após 5 minutos e 24 horas, com uma atividade enzimática média de 0,69 em comparação com o controle de 0,49. Cynara scolymus foi o extrato com maior concentração média de 100 mg/ml; a intensidade da fosfolipase foi alterada com Stryphnodendron barbatiman sendo mais efetivo em 24 horas em relação ao controle (p< 0,0001). A secreção de hemolisina foi modificada por Hamamelis virginiana (12,5 mg/ml) após 5 minutos de exposição e em 24 horas. todos os extratos foram capazes de causar alterações na secreção. Conclusão: Os extratos testados apresentam potencial antifúngico em biofilmes de Candida albicans, implicando em redução significativa dos fatores de virulência. Assim, estes podem ser indicados como uma ferramenta terapêutica alternativa para reduzir a morbidade dessas infecções, já que em ambos os tempos de exposição investigados, eles foram capazes de reduzir a secreção enzimática do fungo (AU)

Objective: Analyze the phenotypic expression of virulence factors in Candida albicans biofilms against plant glycolicextracts. Material and Methods: The biofilms of Candida albicans (ATCC 18804) obtained from incubation for 48 hours were exposed for 5 minutes and 24 hours to different concentrations of glycolic extracts of Hamamelis virginiana and Persea americana, Cynara scolymus L and Stryphnodendron barbatiman M, in order to verify the antifungal activity of the proteinase, phospholipase and hemolysin. Results: All extracts were effective in reducing biofilm. In contact for 5 minutes. the extracts reduced 50% of the biofilm. After 24 hours, the Persea americanaextract showed the biofilm at 90%, followed by Cynara scolymus, which interrupted it at 85%, There was a change in proteinase intensity after 5 minutes and 24 hours. with an average enzymatic activity of 0.69 compared to the control of 0.49. Cynara scolymus was the extract with the highest mean concentration of 100 mg/ml; the phospholipase intensity was changed with Stryphnodendron barbatiman being more effective in 24 hours compared to the control (p< 0.0001). The hemolysin secretion was modified by Hamamelis virginiana (12.5 mg/ml) after 5 minutes of exposure, and in 24 hours. all extracts were capable to cause changes in secretion. Conclusion: The tested extracts have antifungal potential in Candida albicans biofilms, implying a significant reduction in virulence factors. Thus, these can be indicated as an alternative therapeutic tool to reduce the morbidity of these infections, as in both investigated exposure times. they were able to reduce theenzymatic secretion of the fungus (AU)

Preventive effects of systemic Pistacia eurycarpa Yalt. administration on alveolar bone loss and oxidative stress in rats with experimental periodontitis

Abstract Objective: This study aimed to investigate the effects of systemic administration of P. eurycarpa Yalt. plant extract on alveolar bone loss and oxidative stress biomarkers in gingival tissue in a rat model of experimental periodontitis. Methodology: 32 male Wistar albino rats, weighing 200-250 g, were divided into four groups (n=8): Healthy control (HC), Experimental periodontitis control (EPC), Experimental periodontitis 400 mg/kg (EP400), Experimental periodontitis 800 mg/kg (EP800). Experimental periodontitis was induced using the ligating method. Distilled water was administered to the HC and EPC groups and the plant extract was administered to the EP400 and EP800 groups by oral gavage at doses of 400 mg/kg and 800 mg/kg, respectively. The rats were sacrificed on the 15th day. The values of glutathione peroxidase GSH-Px, malondialdehyde (MDA), superoxide dismustase (SOD), interleukin-1β (IL-1β), interleukin-10 (IL-10), total antioxidant status (TAS), total oxidant status (TOS), oxidative stress index (OSI) in the gingival tissues were analyzed by ELISA tests. Alveolar bone loss was assessed using micro-CT images of the maxilla. Results: Although the IL-1β, TOS, OSI results of the healthy control group were lower than those of the other groups, the TAS values were higher (p<0.05). No significant difference was found in the biochemical parameters among the EPC, EP400, and EP800 groups (p>0.05). Alveolar bone loss was significantly reduced in the extract groups compared to the EPC group (p<0.001). Conclusion: Within the limitations of this study, it was observed that the systemic P. eurycarpa extract application reduced alveolar bone loss in a rat model of experimental periodontitis. Further studies are needed to elucidate the beneficial effects of P. eurycarpa.

Ensayo de citotoxicidad de extractos de Pleurotusostreatus en diferentes líneas celulares para aplicaciones inmunonutricionales

Introducción: Los bioderivados propuestos como candidatos a ingredientes alimentarios suelen requerir ciertas evaluaciones para las aplicaciones inmunonutricionales Los hongos comestibles-medicinales son un surtidor de compuestos con estas potencialidades. Entre ellos, las setas Pleurotus ostreatus contienen metabolitos bioactivos, con importantes usos en la industria alimenticia y en la práctica terapéutica de la industria médico-farmacéutica. Los ensayos de citotoxicidad in vitro constituyen métodos valiosos para evaluarproductos de origen natural, como los extractos fúngicos. Objetivo: Evaluar la citotoxicidad de dos extractos obtenidos de la seta Pleurotus ostreatus en diferentes líneas celulares. Método: Se obtuvieron extractos hidrosolubles a partir del micelio y de los cuerpos fructíferos de Pleurotus ostreatus en laboratorios del Centro de Estudios de Biotecnología Industrial de la Universidad de Oriente. Se evaluó la citotoxicidad de los bioproductos por el ensayo de reducción del colorante resazurina sobre tres líneas celulares en el Laboratorio de Microbiología, Parasitología e Higiene (LMPH) de la Universidad de Amberes, Bélgica. Se utilizaron células no adherentes THP-1 (pre-monocitos de leucemia humana), células adherentes Caco-2 (epitelio de adenocarcinoma de colon humano) y células adherentes RAW 264.7 (macrófagos murinos). Resultados: Los extractos de Pleurotus ostreatus no resultaron citotóxicos para ninguna de las líneas celulares estudiadas humanas o murina, ya que no ocasionaron daños sobre la viabilidad de las célulasepiteliales del sistema gastrointestinal, nisobrelas células del sistema inmune empleadas. Conclusiones: Este resultado demuestra que ambos bioderivados fúngicos pueden ser aplicados con seguridad en estudios inmunonutricionales.

Introduction: Bioderivatives proposed as candidates for food ingredients usually require certain evaluations for immunonutritional applications. Edible-medicinal mushrooms are a source of compounds with these potentials. Among them, Pleurotus ostreatus mushrooms contain bioactive metabolites, with important uses in the food industry and in the therapeutic practice of the medical-pharmaceutical industry. In vitro cytotoxicity assays are valuable methods to evaluate products of natural origin, such as fungal extracts. Objective: To evaluate the cytotoxicity of two extracts obtained from the Pleurotus ostreatus mushroom in different cell lines. Method: Water-soluble extracts were obtained from the mycelium and fruiting bodies of Pleurotus ostreatus in laboratories of the Center for Industrial Biotechnology Studies of the Universidad de Oriente. The cytotoxicity of the bioproducts was evaluated by the resazurin dye reduction assay on three cell lines at the Laboratory of Microbiology, Parasitology and Hygiene (LMPH) of the University of Antwerp, Belgium. Non-adherent THP-1 cells (human leukemia pre-monocytes), Caco-2 adherent cells (human colon adenocarcinoma epithelium) and RAW 264.7 adherent cells (murine macrophages) were used. Results: Pleurotus ostreatus extracts were not cytotoxic for any of the human or murine cell lines studied, since they did not cause damage to the viability of the epithelial cells of the gastrointestinal system, nor to the immune system cells used. Conclusions: This result demonstrates that both fungal bioderivatives can be safely applied in immunonutritional studies.

Introdução: Bioderivados propostos como candidatos a ingredientes alimentícios geralmente requerem determinadas avaliações para aplicações imunonutricionais. Pleurotus ostreatus contêm metabólitos bioativos, com importantes utilizações na indústria alimentícia e na prática terapêutica da indústria médico-farmacêutica. Ensaios de citotoxicidade in vitro são métodos valiosos para avaliar produtos de origem natural, como extratos de fungos. Objetivo: Avaliar a citotoxicidade de dois extratos obtidos do cogumelo Pleurotus ostreatus em diferentes linhagens celulares. Método: Extratos hidrossolúveis foram obtidos do micélio e dos corpos frutíferos de Pleurotus ostreatus nos laboratórios do Centro de Estudos de Biotecnologia Industrial da Universidade de Oriente. A citotoxicidade dos bioprodutos foi avaliada pelo ensaio de redução do corante resazurina em três linhagens celulares no Laboratório de Microbiologia, Parasitologia e Higiene (LMPH) da Universidade de Antuérpia, Bélgica. Foram utilizadas células THP-1 não aderentes (pré-monócitos de leucemia humana), células aderentes Caco-2 (epitélio de adenocarcinoma do cólon humano) e células aderentes RAW 264.7 (macrófagos murinos). Resultados: Os extratos de Pleurotus ostreatus não foram citotóxicos para nenhuma das linhagens celulares humanas ou murinas estudadas, pois não causaram danos à viabilidade das células epiteliais do sistema gastrointestinal, nem às células do sistema imunológico utilizadas. Conclusões: Este resultado demonstra que ambos os bioderivados fúngicos podem ser aplicados com segurança em estudos imunonutricionais.

Plant extracts used in Brazil for treatment of oral ulcers and mucositis: systematic review / Extratos vegetais utilizados no Brasil para tratamento de úlceras orais e mucosite: revisão sistemática

Objective: To identify and analyze plant extracts used in Brazil for the treatment of oral ulcers and oral mucositis. Material and Methods: A systematic review was registered in PROSPERO (CRD 42018102184) and performed following the PRISMA protocol. The databases searched were PubMed, Web of Science, Scopus, Lilacs, Scielo, the Brazilian Dentistry Library. Manual searches were also performed. Results: Initially, 440 studies were found, of which 392 were excluded after reading the titles and abstracts. A total of 29 articles were read in full and 11 studies were excluded, resulting in 18 articles included in the systematic review. Nine plant species were identified in five clinical trials and 13 in vivo studies, with Chamomila recutita being the most used (33.3% of the studies). Chamomila recutita showed more promising results for analgesic, anti-inflammatory, and healing properties. Calotropis procera latex significantly decreased (p<0.05) inflammatory mediators, such as TNF-α and IL-1ß in oral mucositis induced in rats. Eupatorium laevigatum showed anti-inflammatory activity and analgesic action on oral ulcers. Carapa guianensis Aubl. reduced the severity and painful symptoms of oral mucositis and exhibited better results compared to the use of low power laser. Curcuma longa L accelerated re-epithelialization and resolution of inflammatory processes. Spondias mombin reduced oxidative stress and inflammation caused by oral mucositis and helped on healing it. Extracts of Aloe barbadensis Miller or Aloe vera showed anti-inflammatory action but did not help in the healing process of oral ulcers. Copaifera reticulata Ducke oil did not induce improvement in the healing process, nor did it show an anti-inflammatory effect. Malva sylvestrisdid not show an anti-inflammatory action on oral lesions in humans or rats. The assessment of methodological heterogeneity showed the impossibility of performing a meta-analysis. Risk of bias varied from low to high. Conclusion: The plant species most used and with the best results for the treatment of oral ulcerations and oral mucositis was Chamomilla recutita. Spondias mombin L., Curcuma longa L., Carapa guianensis Aubl and Calotropis procera showed good results in the treatment of oral mucositis, while Eupatorium laevigatum was efficient in the treatment of ulcers of traumatic origin. Malva sylvestris, Copaifera reticulata Ducke, and Aloe barbadensis Miller did not exhibit significant results (AU)

Objetivo: Identificar e analisar extratos vegetais utilizados no Brasil para o tratamento de úlceras orais e mucosite oral. Material e Métodos: Uma revisão sistemática foi registrada no PROSPERO (CRD 42018102184) e realizada seguindo o protocolo PRISMA. As bases de dados pesquisadas foram PubMed, Web of Science, Scopus, Lilacs, Scielo, Biblioteca Brasileira de Odontologia. Buscas manuais também foram realizadas. Resultados: Inicialmente, foram encontrados 440 estudos, dos quais 392 foram excluídos após a leitura dos títulos e resumos. Um total de 29 artigos oram lidos na íntegra e 11 estudos foram excluídos, resultando em 18 artigos incluídos na revisão sistemática. Nove espécies vegetais foram identificadas em cinco ensaios clínicos e 13 estudos in vivo, sendo a Chamomila recutita a mais utilizada (33,3% dos estudos). A Chamomila recutita apresentou resultados mais promissores quanto às propriedades analgésicas, anti-inflamatórias e cicatrizantes. O látex de Calotropis procera diminuiu significativamente (p<0,05) os mediadores inflamatórios, como TNF-α e IL-1ß, na mucosite oral induzida em ratos. Eupatorium laevigatumapresentou atividade anti-inflamatória e ação analgésica em úlceras orais. Carapa guianensis Aubl. reduziu a gravidade e os sintomas dolorosos da mucosite oral e apresentou melhores resultados em comparação com o uso do laser de baixa potência. Curcuma longa L. acelerou a reepitelização e resolução de processos inflamatórios. Spondias mombinreduziu o estresse oxidativo e a inflamação causadas pela mucosite oral e ajudou na sua cicatrização. Extratos de Aloe barbadensis Miller ou Aloe vera apresentaram ação anti-inflamatória, mas não auxiliaram no processo de cicatrização de úlceras orais. O óleo de Copaifera reticulata Ducke não induziu melhora no processo cicatricial, nem apresentou efeito anti-inflamatório. Malva sylvestris não apresentou ação anti-inflamatória em lesões orais em humanos ou ratos. A avaliação da heterogeneidade metodológica mostrou a impossibilidade de realizar uma meta-análise. O risco de viés variou de baixo a alto. Conclusão: A espécie vegetal mais utilizada e com melhores resultados para o tratamento de ulcerações orais e mucosite oral foi a Chamomilla recutita. Spondias mombin L., Curcuma longa L., Carapa guianensis Aubl e Calotropis procera apresentaram bons resultados no tratamento da mucosite oral, enquanto Eupatorium laevigatum foi eficiente no tratamento de úlceras de origem traumática. Malva sylvestris, Copaifera reticulata Duckee Aloe barbadensis Miller não apresentaram resultados significativos(AU)

Efficacy of Citrullus colocynthis seed extract on Earias vittella, Fabricius, (Lepidoptera: Noctuidae): environment sustainable approach / Eficácia do extrato de semente de Citrullus colocynthis em Earias vittella Fabricius (Lepidoptera: Noctuidae): abordagem ambiental sustentável

Abstract Earias vittellaFabricius, 1794 (Noctuidae: Lepidoptera) is deliberated to be one of the most destructive pests of cotton and okra vegetation in the world including Asia. The pest has established resistance to various synthetic insecticides. The use of bio-pesticide is one of the unconventional approaches to develop a vigorous ecosystem without harming non- target pests and beneficial natural insect fauna. In the present study, the toxicity levels of Citrullus colocynthis seed extract have been evaluated against the populations of E. vittellaunder standardized laboratory conditions. The toxic effects of C. colocynthis on development periods, protein contents and esterase activity of the life stages of E. vittella were also evaluated. The toxicity levels of methanol, ethanol, hexane, water and profenofos were evaluated on the 1st instar larvae of E. vittella. LC30 and LC80 concentrations exhibited the effectiveness of methanol-based C. colocynthis seed extract against 1st instar larvae of E. vitella. The enhanced larval and pupal periods were revealed in treated samples during the comparison with untreated samples. The intrinsic rate of increase, net reproductive rate in the LC30 and LC80 concentrations exposed larvae remained less than the control treatment. Fecundity, the esterase activity and protein contents were declined in LC30 and LC80 treated samples as compared to the control. The present findings suggest that C. colosynthis extracts based botanical insecticides are beneficial, ecosystem sustainable and can be integrated with insect management programs from environment safety perspective.

Resumo Earias vittella Fabricius, 1794 (Noctuidae: Lepidoptera) é considerada uma das pragas mais destrutivas de algodão e quiabo no mundo, incluindo a Ásia. Essa praga estabeleceu resistência a vários inseticidas sintéticos. O uso de biopesticidas é uma das abordagens não convencionais para desenvolver um ecossistema saudável sem prejudicar as pragas não alvo e a fauna natural benéfica de insetos. No presente estudo, os níveis de toxicidade do extrato de semente de Citrullus colocynthis foram avaliados nas populações de E. vittella em condições de laboratório padronizadas. Os efeitos tóxicos de C. colocynthis nos períodos de desenvolvimento, conteúdo de proteína e atividade esterase das fases de vida de E. vittella também foram avaliados. Os níveis de toxicidade de metanol, etanol, hexano, água e profenofós foram avaliados em larvas de 1º instar de E. vittella. As concentrações de LC30 e LC80 apresentaram eficácia do extrato de sementes de C. colocynthis à base de metanol contra larvas de 1º instar de E. vittella. Os períodos larval e pupal aumentados foram revelados nas amostras tratadas durante a comparação com as amostras não tratadas. A taxa intrínseca de aumento e a taxa reprodutiva líquida nas concentrações de larvas expostas LC30 e LC80 permaneceram menores do que o tratamento controle. A fecundidade, a atividade da esterase e o conteúdo de proteína diminuíram nas amostras tratadas com LC30 e LC80 em comparação com o controle. As presentes descobertas sugerem que os extratos de C. colocynthis à base de inseticidas botânicos são benéficos, sustentáveis ​​para o ecossistema e podem ser integrados com programas de manejo de insetos do ponto de vista da segurança ambiental.

Phenolic compounds and antifungal activity of ethyl acetate extract and methanolic extract from Capsicum chinense Jacq. ripe fruit / Compostos fenólicos e atividade antifúngica dos extratos acetato de etila e metanólico dos frutos maduros de Capsicum chinense Jacq

Food loss due to contamination caused by fungi has much impact on agriculture and leads to significant economic losses. Synthetic and natural fungicides have been used for avoiding losses of several food products due to fungal contamination. As a result, species of the genus Capsicum have been used for preserving food because of their chemical compounds with antifungal activity. Therefore, this study aimed at identifying some phenolic compounds found in both ethyl acetate extract (EAE) and methanolic extract (ME) from habanero pepper (C. chinense) ripe fruit by liquid chromatography tandem mass spectrometry with electrospray ionization (LC-ESI-MS/MS) and at evaluating their antifungal activities against fungi Sclerotinia sclerotiorum, Rhizopus stolonifer and Colletotrichum gloeosporioides. Extracts resulted from a sequential process of maceration. Antifungal activity was evaluated by the disk diffusion method (DDM) at the following doses of both diluted extracts: 25 µL, 50 µL, 100 µL and 200 µL. The chemical analysis showed that there were protocatechuic acid, gentisic acid, vanillic acid, kaempferol-3-O-robinobiosideo and naringenin in both extracts. EAE showed high inhibition of mycelial growth at both doses 100µL and 200µL against the three fungi while methanolic exhibited weak activity even at the highest dose under investigation. However, further in-depth studies are needed to reinforce their uses and practical applications to the agricultural field.

As perdas de alimentos por contaminação causada por fungos são de grande impacto negativo para a agricultura, gerando altos prejuízos econômicos. Para evitar as perdas de diversos produtos alimentícios pela contaminação fúngica são utilizados fungicidas sintéticos e naturais. As espécies do gênero Capsicum são usadas há muitos anos para auxiliar na conservação de alimentos por possuírem substâncias químicas com ação antifúngica entre outras. Neste contexto, o objetivo deste estudo foi identificar alguns compostos fenólicos por cromatografia líquida de alta eficiência acoplada à espectrometria de massas sequencial (LC-ESI-MS/MS) presentes nos extratos acetato de etila (EAE) e metanólico (ME) dos frutos maduros da pimenta biquinho (C. chinense) e avaliar atividade antifúngica de EAE e ME contra os fungos Sclerotinia sclerotiorum, Rhizopus stolonifer e Colletotrichum gloeosporioides. Os extratos foram obtidos de forma sequencial, utilizando o procedimento de maceração. A atividade antifúngica foi avaliada seguindo a metodologia de difusão em disco, nas doses de 25 µL, 50 µL, 100 µL e 200 µL de cada extrato diluído. A análise química evidenciou a presença de ácido protocatequico, ácido gentisico, ácido vanílico, kaempferol-3-O-robinobiosídeo e naringenina em ambos os extratos. EAE revelou maior poder de inibição do crescimento micelial nas doses de 100µL e 200µL contra os três fungos testados, enquanto ME exibiu fraca atividade inclusive na maior dose investigada. Entretanto, estudos mais aprofundados ainda são necessários para consolidar seu uso e aplicação prática na área agronômica.

Actividad antiinflamatoria in vitro de Plantago major L. y Piper aduncum L. sobre la fosfolipasa A2 del veneno de la serpiente Lachesis muta muta / In vitro anti-inflammatory activity of Plantago major L. and Piper aduncum L. on phospholipase A2 from the venom of snake Lachesis muta muta

Objetivo. Evaluar la actividad inhibitoria in vitro de los extractos de Plantago major «llantén» y Piper aduncum «matico» sobre Fosfolipasa A2 (PLA2) del veneno de la serpiente Lachesis muta muta. Materiales y métodos. Esta investigación fue de tipo explicativa con diseño experimental. Se recolectaron hojas de P. major y P. aduncum en la provincia de Huarochirí en Lima, Perú. Se prepararon extractos alcohólicos diluidos en agua destilada y se realizaron los ensayos fitoquímicos, la cuantificación de fenoles y flavonoides, la cromatografía de capa fina (CCF) en celulosa y la actividad enzimática con PLA2. Se analizó la capacidad de inhibir la PLA2 con los extractos en estudio y sus fracciones. Para el análisis estadístico se utilizó la prueba de Kruskal Wallis y comparaciones múltiples de Bonferroni. Resultados. Tanto en P. major como en P. aduncum se identificó cualitativamente la presencia de fenoles, flavonoides y taninos; además, P. aduncum presentó saponinas. La inhibición de la actividad de la PLA2 del veneno por el extracto total de P. major fue del 45,3%, y sus fracciones mostraron valores de inhibición: LLF-1 con 31,1%, LLF-2 con 66,3% y LLF-3 con 65,5%. En P. aduncum, los valores de inhibición para el extracto total fueron de 86,9%, y sus fracciones presentaron inhibiciones: MF-1 con 34,3%, MF-2 con 67,1% y MF-3 con 54,9%. El análisis estadístico demostró diferencias significativas en la inhibición de la PLA2 (p=0,009) por los extractos. Conclusión. Los ensayos realizados demostraron una asociación entre el efecto antiinflamatorio de los extractos y la inhibición de la PLA2.

Objective. To evaluate the in vitro inhibitory activity of Plantago major "llantén" and Piper aduncum "matico" extracts on phospholipase A2 (PLA2) from the venom of the snake Lachesis muta muta. Materials and methods. We carried out an explanatory study with experimental design. Leaves of P. major and P. aduncum were collected in the province of Huarochirí in Lima, Peru. Then, we prepared alcoholic extracts diluted in distilled water and conducted phytochemical assays, quantification of phenols and flavonoids, thin layer chromatography (TLC) on cellulose and enzymatic activity with PLA2. The ability to inhibit PLA2 with the extracts under study and their fractions was analyzed. The Kruskal Wallis test and Bonferroni multiple comparisons were used during statistical analysis. Results. Phenols, flavonoids and tannins were qualitatively identified in both P. major and P. aduncum; in addition, P. aduncum presented saponins. The inhibition of PLA2 activity of the venom by the total extract of P. major was 45.3%, and its fractions showed the following inhibition values: 31.1% for LLF-1, 66.3% for LLF-2 and 65.5% for LLF-3. The inhibition values for the total extract of P. aduncum were 86.9%, and its fractions showed the following inhibition rates: 34.3% for MF-1, 67.1% for MF-2 and 54.9% for MF-3. Statistical analysis showed significant differences in the inhibition of PLA2 (p=0.009) by the extracts. Conclusion. The tests demonstrated an association between the anti-inflammatory effect of the extracts and PLA2 inhibition.

Estimation of Lipid and Fatty Acids Composition over the Ground Part of Nepeta olgae Regel (L.) Plants Growing in Namangan Region

The article is devoted to the study of lipids and fatty acid composition of the above-ground part of the Nepeta olgae Regel (L.) plant of the Laminaceae family. It was found that the content of neutral lipids (NL) is 5.54%, PL - 6.12%, and total lipids (NL, PL) - 11.66%. Of the neutral lipids, the unsaponifiable substances (HB) had a bright yellow color, which is explained by a small amount of carotenoids (88.87 mg%). Glycolipids dominate in PL. Among the unsaponifiable substances were found biologically active components such as hydrocarbons, carotenoids, aliphatic alcohols, sterols and triterpenols. Phytosterols were the main component of unsaponifiable NS. Quantitative and qualitative analysis of fatty acids from the plant Nepeta olgae Regel (L.) was carried out by gas chromatography (GC). 28 acids were identified, of which 11 compounds are saturated, and 7 compounds are unsaturated fatty acids. Of the fatty acids, the main ones are linolenic 18:3 (35.48), palmitic 16:0 (33.38%), as well as ?-3 polyunsaturated fatty acids, including eicosanoic 20:1, cis-11,14-eicosadienoic 20:2, 8,11,14-eicosatriene 20:3 + arachidonic 20:4. Extracts of Nepeta olgae Regel (L.) were distinguished by a high content of polyunsaturated acids, which determines their potential biological activity.

Research progress on the biological activity of pyrrole 1,2-α indole alkaloids / 中国基层医药

Pyrrole [1,2-α] indole is a novel fused heterocyclic skeleton, which is also the basic structural unit and synthetic intermediate of many natural active products and drugs. Pyrrole [1,2-α] indole heterocyclic derivatives have attracted much attention in organic synthesis and medicinal chemistry because of their extensive and marked biological activities. Plant extracts have always been an important source of active compounds. At present, the alkaloids based on the pyrrole [1,2-α] indole heterocyclic structure discovered and isolated from plant extracts include isatisine, isoborreverine, flinderoles, polyavolensin and yuremamine. This paper reviews the research progress on the biological activity of pyrrole [1,2-α] indole heterocyclic derivatives and has found that pyrrole [1,2-α] indole heterocyclic derivatives have a good development prospect in screening active compounds and developing candidate drugs.

Immune enhancement of 30% ethanol elution fraction of Artemisia absinthium ethanol extract with macroporous resin / 国际生物医学工程杂志

Objective:To investigate the effects of 30% ethanol elution fraction of Artemisia absinthium extract with macroporous resin (AAEM-30%) on the dendritic cell (DC) and immunity of mice. Methods:AAEM-30% was obtained from the alcoholic extracts of A. absinthium by AB-8 macroporous resin, and its polysaccharide, flavonoid, and terpenoid contents were determined. The expressions of AAEM-30% on DC surface molecular cluster of differentiation (CD) 40, CD80 and CD86 were detected in vitro by flow cytometry, and the expressions of DC cytokines IL-6 and tumor necrosis factor-α (TNF-α) were detected by enzyme linked immunosorbent assay (ELISA). The effect of AAEM-30% on the immune function of ICR mice was measured in vivo with different doses (50 and 100 mg/kg) and different administration methods (subcutaneous injection, intraperitoneal injection, and gavage). Results:The contents of polysaccharides, flavonoids, and terpenoids in AAEM-30% were 24.30%, 22.50% and 28.19%, respectively. AAEM-30% significantly enhanced the expression of CD40, and CD86 and the secretion of IL-6 and TNF-α (all P<0.001). Compared with the control group, no statistically significant differences were found in the body mass of mice compared with the three administration methods (all P>0.05). The thymus index in the 50 and 100 mg/kg AAEM-30% intraperitoneal injection groups and the spleen index in the 50 mg/kg AAEM-30% gavage group were increased (all P<0.05). CD19 + cells increased in the 100 mg/kg AAEM-30% intraperitoneal injection group ( P<0.01) and in the 50 mg/kg AAEM-30% gavage group ( P<0.05). The CD11b + and CD11c + counts increased in the 100 mg/kg AAEM-30% gavage group ( P<0.05). The number of CD4 + and CD8 + T lymphocytes was increased by both gavage and intraperitoneal administration (all P<0.05). Conclusions:AAEM-30% can promote the maturation of DC and enhanced the immunity of mice without obvious side effects.

Radix Scrophulariae Extracts Exert Effect on Hyperthyroidism via MST1/Hippo Signaling Pathway / 中国结合医学杂志

OBJECTIVE@#To explore the mechanism of Radix Scrophulariae (RS) extracts in the treatment of hyperthyroidism rats by regulating proliferation, apoptosis, and autophagy of thyroid cell through the mammalian sterile 20-like kinase 1 (MST1)/Hippo pathway.@*METHODS@#Twenty-four rats were randomly divided into 4 groups according to a random number table: control, model group, RS, and RS+Hippo inhibitor (XMU-MP-1) groups (n=6 per group). Rats were gavaged with levothyroxine sodium tablet suspension (LST, 8 μ g/kg) for 21 days except for the control group. Afterwards, rats in the RS group were gavaged with RS extracts at the dose of 1,350 mg/kg, and rats in the RS+XMU-MP-1 group were gavaged with 1,350 mg/kg RS extracts and 1 mg/kg XMU-MP-1. After 15 days of administration, thyroid gland was taken for gross observation, and histopathological changes were observed by hematoxylin-eosin staining. The structure of Golgi secretory vesicles in thyroid tissues was observed by transmission electron microscopy. The expression of thyrotropin receptor (TSH-R) was observed by immunohistochemistry. Terminal-deoxynucleoitidyl transferase mediated nick end labeling assay was used to detect cell apoptosis in thyroid tissues. Real-time quantity primer chain reaction and Western blot were used to detect the expressions of MST1, p-large tumor suppressor gene 1 (LATS1), p-Yes1 associated transcriptional regulator (YAP), proliferating cell nuclear antigen (PCNA), G1/S-specific cyclin-D1 (Cyclin D1), B-cell lymphoma-2 (Bcl-2), Caspase-3, microtubule-associated proeins light chain 3 II/I (LC3-II/I), and recombinant human autophagy related 5 (ATG5). Thyroxine (T4) level was detected by enzyme-linked immunosorbent assay.@*RESULTS@#The thyroid volume of rats in the model group was significantly increased compared to the normal control group (P<0.01), and pathological changes such as uneven size of follicular epithelial cells, disorderly arrangement, and irregular morphology occurred. The secretion of small vesicles by Golgi apparatus was reduced, and the expressions of receptor protein TSH-R and T4 were significantly increased (P<0.01), while the expressions of MST1, p-LATS1, p-YAP, Caspase-3, LC3-II/I, and ATG5 were significantly decreased (P<0.01). The expressions of Bcl-2, PCNA, and cyclin D1 were significantly increased (P<0.01). Compared with the model group, RS extracts reduced the volume of thyroid gland, improved pathological condition of the thyroid gland, promoted secretion of the secretory vesicles with double-layer membrane structure in thyroid Golgi, significantly inhibited the expression of TSH-R and T4 levels (P<0.01), upregulated MST1, p-LATS1, p-YAP, Caspase-3, LC3-II/I, and ATG5 expressions (P<0.01), and downregulated Bcl-2, PCNA, and Cyclin D1 expressions (P<0.01). XMU-MP-1 inhibited the intervention effects of RS extracts (P<0.01).@*CONCLUSION@#RS extracts could inhibit proliferation and promote apoptosis and autophagy in thyroid tissues through MST1/Hippo pathway for treating hyperthyroidism.

Antibacterial and antibiotic potentiating capabilities of extracts isolated from Burkillanthus malaccensis, Diospyros hasseltii and Cleisthanthus bracteosus against human pathogenic bacteria

@#Antibiotics which once a boon in medicine and saved millions of lives are now facing an ever-growing menace of antibacterial resistance, which desperately needs new antibacterial drugs which are innovative in chemistry and mode of action. For many years, the world has turned to natural plants with antibacterial properties to combat antibiotic resistance. On that basis, we aimed to identify plants with antibacterial and antibiotic potentiating properties. Seventeen different extracts of 3 plants namely Burkillanthus malaccensis, Diospyros hasseltii and Cleisthanthus bracteosus were tested against multi-drug resistant Acinetobacter baumannii, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Methicillinresistant Staphylococcus aureus (MRSA) and methicillin-susceptible Staphylococcus aureus (MSSA). Antibacterial activity of hexane, methanol and chloroform extracts of bark, seed, fruit, flesh and leaves from these plants were tested using, disk diffusion assay, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) assays. Antibiotic potentiating capabilities were tested using time-kill assay. B. malaccensis fruit chloroform extract showed the biggest zone of inhibition against MRSA (13.00±0.0 mm) but C. bracteosus bark methanol extract showed the biggest inhibition zone against MSSA (15.33±0.6 mm). Interestingly, bark methanol extract of C. bracteosus was active against MRSA (8.7±0.6 mm), MSSA (7.7±0.6 mm) (Gram-positive) and A. baumannii (7.7±0.6 mm) (Gram-negative). Overall, the leaf methanol and bark methanol extract of C. bracteosus warrants further investigation such as compound isolation and mechanism of action for validating its therapeutic use as antibiotic potentiator importantly against MRSA and A. baumannii.

Effects of ethanolic extracts of Euonymus alatus on CCl / 中国药理学通报

Aim To explore the mechanism of ethanolic extracts of euonymus alatus on CCl4-induced hepatic fibrosis in mice by regulating JAK2/STAT3 signaling pathway. Methods Sixty C57BL/6J mice were randomly divided into control group,model group,EAL,EAM),EAH,and Silybin(n=10). Except for the control group,mice in other groups were injected with 25% CCl4 of 1.6 mL·kg

Mechanisms of Euphorbia fischeriana steud. alcohol extracts intreatment of HCC based on network pharmacology and experiment verification / 中国药理学通报

Aim To investigate the molecular mechanisms of alcohol extracts of Euphorbia fischeriana steud. against hepatocellular carcinoma (HCC) through a combination of network pharmacology analysis and experimental validation. Methods The active ingredients and targets of alcohol extracts of Euphorbia fischeriana steud. were determined through TCMSP, Swiss ADME, Swiss Target Prediction database and references. The databases DisGeNET and GeneCards were employed to screen potential HCC-related genes. Venny platform, STRING platform and Cytoscape software were applied to construct active ingredient-target-disease and protein-protein interaction (PPI) network maps. Gene ontology (GO) and kyoto encyclopedia of genes and genomes (KEGG) enrichment analyses were performed using the DAVID database. To assess the effects of Euphorbia fischeriana steud. alcohol extracts on BEL-7402 cells, the proliferation and apoptosis were detected by CCK-8, EdU and flow cytometry assays, and the related protein levels of JAK2/STAT3 pathway were analyzed by Western blot. Additionally, H22 hepatocellular carcinoma mouse model was used to evaluate the in vivo efficacy of Euphorbia fischeriana steud. alcohol extracts. Results A total of 916 HCC targeted genes, 30 active ingredients containing the related 567 potential targeted genes, and 115 intersection targets of disease and compounds were obtained. KEGG enrichment analysis identified JAK2/STAT3 signaling as a critical pathway. In vitro experiments showed the alcohol extracts of Euphorbia fischeriana steud. could inhibit proliferation, promote apoptosis and suppress JAK2/STAT3 signaling pathway in a dose-dependent manner in BEL-7402 cells. In addition, the alcohol extracts of Euphorbia fischeriana steud., either alone or in combination with sorafenib, dramatically blocked tumor growth in in vivo tests. Conclusions Euphorbia fischeriana steud. alcohol extracts have anti-cancer effects in HCC, and the molecular mechanisms may be connected to the regulation of JAK2/STAT3 signaling pathway.

Effects of different extraction parts of Tibetan medicine Pulicaria insignis Drumm ex Dunn on CIA rats / 中国药理学通报

Aim To clarify the anti-rheumatoid arthritis effect of Tibetan medicine Pulicaria insignis (P. insignis),sift out the active parts against rheumatoid arthritis,and investigate the mechanism. Methods Rat rheumatoid arthritis (CIA) model was established with bovine type II collagen and incomplete Freund's adjuvant. The effects of the total extract of P. insignis, macroporous resin eluted parts with different concentrations of ethanol and Tripterygium Glycosides (GTW) on the degree of foot swelling in CIA rats were observed,the levels of tumor necrosis factor (TNF-α), intd rheumaerleukin-1β (IL-1β) antoid factor (RF) in serum of rats were detected, the pathological changes of synovial tissues were investigated, and the effects on MAPK/p38/NF-κB, TLR4/NF-κB protein expressions were explored by Western blot. Results Compared with the model group, the total extract of P. insignis and the eluted part of macroporous resin 60% ethanol could significantly reduce the degree of joint swelling in CIA rats, effectively improve the pathological changes of rats synovium tissues, and significantly reduce the levels of rat tumor necrosis factor (TNF-α), interleukin-1β (IL-1β) and rheumatoid factor (RF) in serum inflammatory factors, and markedly decrease the expression of related inflammatory proteins (TLR4, NF-κB, Myd88, p-p38, p-IκBα, iNOS, etc) in synovial tissue. Conclusions (1) P. insignis can relieve the symptoms of joint inflammation in rats with rheumatoid arthritis, and the eluted part of macroporous resin 60% ethanol of P. insignis is the effective active part for anti-rheumatoid arthritis. (2) The total and partial extracts of P. insignis can relieve arthritis symptoms in CIA rats through inhibiting the MAPK/ p38/NF-κB and TLR4/NF-κB signaling pathways.

Crystallization transformation of amorphous extracts of traditional Chinese medicine and its effect on dissolution behavior — Taking total flavonoids from Pueraria lobata as an example / 中国药科大学学报

@#In order to guarantee the quality of traditional Chinese medicines (TCMs), the crystallization transformation of complex extracts of TCMs and the influence of solid form on their physicochemical properties were studied.The extract of total flavonoids from Pueraria lobata was taken as a model.Crystallization transformation happened when lofting under different conditions, and the intrinsic dissolution tests were carried out.It was found that humidity was the key factor to induce crystallization of total flavonoids from Pueraria lobata.The greater the wettability was, the more the crystallization was.The dissolution rate of total flavonoids from Pueraria lobata with the most crystallization amount significantly decreased by 96.51% compared to the sample without crystallization.After further simulating the preparation process of total flavonoids from Pueraria lobata, it was found that the wet granulation process with introduced water would also lead to crystallization and reduced dissolution rate.As for all crystallization samples, there was an inversely proportional relationship between the dissolution rates and the amount of crystallization.The risk of crystallization existed both in the storage and preparation process of TCM extracts.Crystallization would significantly affect the dissolution rate, and thus the quality of TCM products.In this study, the crystallization transformation of amorphous complex TCM extracts was discovered, and the effect of the crystallization transformation on its dissolution behavior was systematically studied, which provides a new research idea for assuring the quality of TCM products and promoting the improvement of TCM preparation level.