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1.
Mol Med Rep ; 27(1)2023 01.
Artigo em Inglês | MEDLINE | ID: mdl-36331022

RESUMO

Stroke is one of the leading causes of death from diseases. When the blood supply to the brain tissue is interrupted, neuronal core death occurs due to the lack of glucose and oxygen in min. Blood pressure lowering after ischemic stroke was proven to be an effective strategy to achieve neurovascular protection and reduce the risk of recurrent stroke. Astragaloside IV is a pure small molecular compound isolated from Radix Astragali, and it is well documented that astragaloside IV has neuroprotective effect on cerebral ischemia reperfusion (CIR) injury through many mechanisms, including antioxidant, anti­inflammatory and anti­apoptotic. The present study adopted mean arterial pressure (MAP) monitoring, neurological scoring, 2,3,5­triphenyltetrazolium chloride staining, enzyme­linked immuno­sorbent assay, western blotting and other experimental methods to investigate the effect of astragaloside IV on systemic blood pressure during CIR in a middle cerebral artery occlusion animal model. It was demonstrated that astragaloside IV pretreatment significantly alleviated CIR injury as previously reported. In addition, the elevation of MAP during CIR was significantly inhibited by astragaloside IV administration. Moreover, it was revealed that the expression of Na+­K+­2Cl­ cotransporter isoform 1 in the hypothalamus was inhibited and the subsequent synthesis of vasopressin was reduced by astragaloside IV pretreatment in the CIR animal model. In conclusion, astragaloside IV may alleviate CIR injury partially by lowering systemic blood pressure.


Assuntos
Isquemia Encefálica , Traumatismo por Reperfusão , Saponinas , Triterpenos , Ratos , Animais , Ratos Sprague-Dawley , Saponinas/farmacologia , Saponinas/uso terapêutico , Triterpenos/farmacologia , Triterpenos/uso terapêutico , Isquemia Encefálica/tratamento farmacológico , Traumatismo por Reperfusão/tratamento farmacológico , Traumatismo por Reperfusão/prevenção & controle , Reperfusão , Infarto da Artéria Cerebral Média , Modelos Animais de Doenças
2.
Ann Pharmacother ; 57(1): 99-106, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-35502451

RESUMO

OBJECTIVE: To review the pharmacology, efficacy, and safety of ibrexafungerp in the management of vulvovaginal candidiasis (VVC). DATA SOURCES: Literature was sought using PubMed (1966-February 2022) and EMBASE (1973-February 2022), and clinicaltrials.gov. Search terms included ibrexafungerp, SCY-078, and VVC. STUDY SELECTION AND DATA EXTRACTION: All studies including humans and published in English with data assessing the efficacy and safety of ibrexafungerp for the treatment of VVC were evaluated. DATA SYNTHESIS: A phase 2 dose-finding study found ibrexafungerp had similar efficacy to fluconazole in the clinical cure of VVC (51.9% vs 58.3%, respectively). Two phase 3 clinical trials demonstrated ibrexafungerp had statistical superiority over placebo for clinical cure in moderate to severe VVC (P < 0.001 and P = 0.023, respectively). The most frequently reported adverse reactions in the clinical trials were gastrointestinal-related symptoms. To date, data comparing efficacy of ibrexafungerp and topical imidazoles in the treatment of VVC are nonexistent. RELEVANCE TO PATIENT CARE AND CLINICAL PRACTICE: Topical imidazoles and oral fluconazole are effective for the treatment of uncomplicated VVC. Due to increased resistance, limited fluconazole coverage for non-Candida albicans species, and potential for significant drug interactions associated with fluconazole use, alternative treatments for VVC are needed. Ibrexafungerp is a new oral triterpenoid antifungal agent indicated for the treatment of VVC. Additional clinical trials are needed to evaluate long-term safety data as well as efficacy and safety in specialty populations. CONCLUSION: Ibrexafungerp, a recently approved triterpenoid antifungal agent, is an effective and well-tolerated option for the treatment of VVC.


Assuntos
Candidíase Vulvovaginal , Triterpenos , Feminino , Humanos , Candidíase Vulvovaginal/tratamento farmacológico , Fluconazol/efeitos adversos , Antifúngicos/efeitos adversos , Triterpenos/uso terapêutico , Imidazóis/uso terapêutico
3.
J Ethnopharmacol ; 300: 115704, 2023 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-36096345

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Glycyrrhiza uralensis Fisch (RC) and Coptis chinensis Franch (RG) are traditional Chinese medicines, which are classic drug pair in prescriptions to treat gastrointestinal diseases. Multi-herb therapy is one of the most important features of traditional Chinese medicine, but due to the complex components of herbal decoctions, the substances that actually exert their medicinal effects have not been fully elucidated. The discovery of Glycyrrhiza uralensis Fisch and Coptis chinensis Franch supramolecular parts (RC-RG SA) can provide a new perspective for explaining the mechanism of drug-pair compatibility. AIM OF THE STUDY: The purpose of this study was to explore the active composition and identification of chemical constituents of RC-RG SA, and to explore the inhibitory effects of supramolecular parts on S. aureus and biofilm. MATERIALS AND METHODS: The micromorphology of RC-RG SA was characterized by SEM and DLS. Intermolecular forces between Glycyrrhiza uralensis Fisch and Coptis chinensis Franch determined by ITC. The chemical constituents of RC-RG SA were systematically analyzed by UPLC-ESI-MSn. The inhibitory effect of RC-RG SA on S. aureus was determined by turbidimetric method and plate coating method. The scavenging effect of RC-RG SA supramolecular parts on S. aureus biofilm were observed by MTT method, SEM and LSCM, respectively. RESULTS: The microstructure of RC-RG SA was spherical with a particle size of 161.6 nm. ITC proved that the reaction between decoction of RC and RG was exothermic. A total of 70 compounds were preliminarily identified in RC-RG SA, including 34 flavonoids, 34 alkaloids and 2 triterpenoids. The inhibitory effect of RC-RG supramolecular parts on S. aureus proliferation and the ability to clear S. aureus biofilm were better than RC-RG co-decoction and RC-RG non-supramolecular parts. CONCLUSIONS: The Glycyrrhiza uralensis Fisch and Coptis chinensis Franch co-decoctions' supramolecular components were an important substance that exerts its medicinal effect. Current study provided supramolecular strategies to reveal the active ingredients and the medicinal effect of the traditional Chinese medicine decoction.


Assuntos
Alcaloides , Medicamentos de Ervas Chinesas , Glycyrrhiza uralensis , Triterpenos , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Flavonoides , Glycyrrhiza uralensis/química , Medicina Tradicional Chinesa , Staphylococcus aureus
4.
J Ethnopharmacol ; 300: 115723, 2023 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-36115600

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Xiaojin Pills (XJPs), which has the function of dissipating knots and dispersing swelling, removing blood stasis, and relieving pain, is a classic prescription for the treatment of mammary glands hyperplasia. It is also the first choice of Chinese patent medicine for the clinical treatment of mammary glands hyperplasia in contemporary traditional Chinese medicine clinics. Previous studies have shown that the efficacy of XJPs "taken orally after soaked with Chinese Baijiu" in tradition was significantly better than that of taking it orally with water in modern in terms of activating the blood, anti-inflammation, analgesia, anti-mammary gland hyperplasia, anti-breast cancer and its metastasis in vitro and in vivo, especially under low-dose conditions. However, the material basis for the difference in efficacy between XJP&B and XJP&W is still unclear. AIM OF THE STUDY: To analyze the material basis of the significant difference in efficacy between XJP&B and XJP&W from the perspective of serum pharmacochemistry and pharmacokinetics, and clarified the scientific connotation of XJPs "taken orally after soaked with Chinese Baijiu". MATERIALS AND METHODS: Ultra-high performance liquid chromatography-mass spectrometry combined with a multivariate statistical analysis method were used to screen the differential components in the Chinese Baijiu extract and the water extract of XJPs and the corresponding residues, so as to clarify the differential components between XJP&B and XJP&W in vitro. The migrating components in the blood after XJP&B and XJP&W were characterized by serum pharmacochemical methods, in order to clarify the differential components in rats. The pharmacokinetic parameters of the representative components absorbed into the blood were compared between XJP&B and XJP&W by the pharmacokinetics study method, in order to determine the dynamic changes of the representative components in rats. RESULTS: The identification results of different components in vitro showed that there were 34 and 12 different compounds between the Chinese Baijiu extract and water extract of XJPs, and the residues after Chinese Baijiu extraction and water extraction, respectively. The content of different components such as arachidonic acid, ursolic acid, 3-acetyl-11-keto-ß-boswellic acid, 2α-hydroxyursolic acid, and oleanolic acid was higher in the Chinese Baijiu extract, which was more than twice the content in the water extract. The results of the serum pharmacochemistry study indicated that 42 prototype components were identified in the serum of rats after XJP&B and XJP&W, including organic acids, alkaloids, steroids, and terpenoids. And XJP&B increased the absorption of the prototype components of organic acids in XJPs into the blood. The pharmacokinetic study results of representative components demonstrated that the mean plasma concentration-time profile and pharmacokinetic parameters of muscone, aconitine, and 3-acetyl-11-keto-ß-boswellic acid were significantly different between XJP&B and XJP&W. Compared with XJP&W, the Cmax and AUC0-t of muscone and aconitine in XJP&B were higher, and the T1/2 and MRT0-t of 3-acetyl-11-keto-ß-boswellic acid in XJP&B were relatively longer. CONCLUSION: This research proved that "taking XJPs orally after being soaked with Chinese Baijiu" can increase the dissolution and absorption of active ingredients in XJPs, increase the plasma concentration and content of representative ingredients, and prolong its action time, thus enhancing the biological activity of XJPs in vitro and in vivo. To a certain extent, this study revealed the material basis of the significantly better efficacy of XJP&B than XJP&W and clarified the scientific connotation of XJPs "taken orally after soaked with Chinese Baijiu", which can provide a theoretical basis for the optimization of XJPs' clinical administration method.


Assuntos
Alcaloides , Medicamentos de Ervas Chinesas , Ácido Oleanólico , Aconitina/análise , Animais , Ácidos Araquidônicos , China , Cromatografia Líquida de Alta Pressão/métodos , Cicloparafinas , Medicamentos de Ervas Chinesas/química , Hiperplasia , Medicamentos sem Prescrição , Ácido Oleanólico/análise , Ratos , Triterpenos , Água
5.
J Ethnopharmacol ; 301: 115823, 2023 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-36220512

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Glycyrrizae Radix et Rhizoma has various effects, including tonifying the spleen and qi, clearing heat and toxic substances, eliminating phlegm, relieving cough and pain, and harmonizing the effects of other medicines. It is widely used in the pharmaceutical and food industries. AIMS OF THE STUDY: This review systematically collates the identification of Glycyrrhiza Linn. species with medicinal value and their distributions. The morphological and genetic characteristics, distribution, quantity of reserves in China, suitable environment, and area of suitable habitat of important medicinal species were reviewed. The effects of the natural environment and cultivation management (water and nutrients) on the growth and quality of licorice were reviewed. The aim is to make people have a systematic understanding of the status of medicinal plant resources of the G. Linn., and understand the natural and human factors that affect its quality, so as to provide help for the collection of resources of the important medicinal licorice and the human control of its quality in the future. MATERIALS AND METHODS: We conducted extensive searches of the primary literature, master's and doctoral theses, and pharmacopeias of many countries using PubMed, Geenmedical, CNKI, Web of Science, SCI-hub and other databases. The keywords used in searches included "classification of Glycyrrhiza," "medicinal Glycyrrhiza," "distribution of Glycyrrhiza," and "suitable environment for Glycyrrhiza" The results of research conducted by our research group on the morphological and genetic characteristics, natural distribution, and effects of artificial regulation on the growth and quality of licorice were summarized. RESULTS: There are approximately 29 species of G. Linn. worldwide, including 15 species with medicinal value. These species occur on all continents except Antarctica across 41 countries. Only one licorice is recorded in Indian pharmacopoia,two species are recorded in US and Japanese pharmacopoeias,and three species are recorded in most national pharmacopoeias: G. glabra Linn., G. uralensis Fisch. and G. inflata Batalin. These three medicinal licorice species are mainly distributed in Eurasia, especially Central Asia. The main morphological differences between these three medicinal licorice species are in the leaves, inflorescences, pods, and seeds, and they can be distinguished by ITS and psbA-trnH sequences. The reserves of wild licorice in China have decreased annually to 1.04 million(t) in 2010. The cultivation area of G. uralensis Fisch in China is currently approximately 26,900 hm2. Soil conditions have a substantial effect on the yield and quality of G. uralensis Fisch, especially water and nutrients. Appropriate irrigation and fertilization measures can enhance the quality of G. uralensis Fisch. CONCLUSIONS: G. Linn. species and their natural distributions were summarized. The morphology, genetic characteristics, suitable environment, and area of suitable habitat of three medicinal licorice species collected in major countries were described. The main environmental conditions and cultivation measures affecting their growth and medicinal quality were determined. This article provides a comprehensive review on G. Linn. medicinal plant resources to enhance the future use of these resources.


Assuntos
Glycyrrhiza , Plantas Medicinais , Triterpenos , Humanos , Extratos Vegetais , Água
6.
J Ethnopharmacol ; 301: 115819, 2023 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-36228891

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Crataegus pinnatifida belongs to the Rosaceae family and extensively distribute in North China, Europe, and North America. Its usage was first described in "Xinxiu Ben Cao." The dried fruits of Crataegus pinnatifida Bunge or Crataegus pinnatifida var. major N. E. Br., also known as "Shanzha," is a famous medicine and food homology herb with a long history of medicinal usage in China. C. pinnatifida has the functions for digestive promotion, cardiovascular protection, and lipid reduction. It was traditionally used to treat indigestion, cardiodynia, thoracalgia, hernia, postpartum blood stagnation, and hemafecia. In recent years, C. pinnatifida has attracted worldwide attention as an important medicinal and economical crop due to its multiple and excellent health-promoting effects on cardiovascular, nervous, digestive, endocrine systems, and morbigenous microorganisms of the human body due to its medicinal and nutritional values. AIM OF THE REVIEW: The current review aims to provide a comprehensive analysis of the geographical distribution, traditional usage, phytochemical components, pharmacological actions, clinical settings, and toxicities of C. pinnatifida. Moreover, the connection between the claimed biological activities and the traditional usage, along with the future perspectives for ongoing research on this plant, were also critically summarized. MATERIALS AND METHODS: We collected the published literature on C. pinnatifida using a variety of scientific databases, including Web of Science, ScienceDirect, PubMed, Wiley, Springer, Taylor & Francis, ACS Publications, Google Scholar, Baidu Scholar, CNKI, The Plant List Database, and other literature sources (Ph.D. and MSc dissertations) from 2012 to 2022. RESULTS: In the last decade, over 250 phytochemical compounds containing lignans, phenylpropanoids, flavonoids, triterpenoids, and their glycosides, as well as other compounds, have been isolated and characterized from different parts, including the fruit, leaves, and seeds of C. pinnatifida. Among these compounds, flavonoids and triterpenoids were major bioactive components of C. pinnatifida. They exhibited a broad spectrum of pharmacological actions with low toxicity in vitro and in vivo, such as cardiovascular protection, neuroprotection, anti-inflammatory, antioxidant, antibacterial, antiviral, anti-diabetes, anti-cancer, anti-mutagenic, anti-osteoporosis, anti-aging, anti-obesity, and hepatoprotection and other actions. CONCLUSION: A long history of traditional uses and abundant pharmacochemical and pharmacological investigations have demonstrated that C. pinnatifida is an important medicine and food homology herb, which displays outstanding therapeutic potential, especially in the digestive system and cardiovascular disease. Nevertheless, the current studies on the active ingredients or crude extracts of C. pinnatifida and the possible mechanism of action are unclear. More evidence-based scientific studies are required to verify the traditional uses of C. pinnatifida. Furthermore, more efforts must be paid to selecting index components for quality control research and toxicity and safety studies of C. pinnatifida.


Assuntos
Crataegus , Triterpenos , Humanos , Crataegus/química , Etnofarmacologia , Compostos Fitoquímicos/uso terapêutico , Compostos Fitoquímicos/toxicidade , Flavonoides , Extratos Vegetais/farmacologia
7.
J Ethnopharmacol ; 300: 115725, 2023 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-36115602

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Cimicifuga foetida L. is a well-established traditional Chinese medicine with heat-clearing and detoxifying effects and has good therapeutic effect on oral mucosal ulcer and pharyngitis. The rhizome of this herb is rich in triterpenoid glycosides, including 23-O-acetylshengmanol-3-o-α-L-arabinoside (DA). AIM OF THE STUDY: Whether and how DA attenuates acute lung injury (ALI) are unclear. Accordingly, we focused on its anti-inflammatory effects and underlying molecular mechanisms in lipopolysaccharide (LPS)-stimulated ALI mice and RAW264.7 cells. MATERIALS AND METHODS: The model of ALI mice was established by exposed intratracheal instillation of LPS. Lung pathological changes were evaluated by hematoxylin and eosin staining. Pulmonary function was assessed by whole-body plethysmography. Total protein content in bronchoalveolar lavage fluid (BALF) was detected by bicinchoninic acid method. Wet/dry lung ratio was used to evaluate the degree of pulmonary edema in mice. The levels of pro-inflammatory mediators were measured using enzyme-linked immunosorbent assay. The relative expression of pro-inflammatory gene mRNA was examined by RT-qPCR. The expression of inflammatory-related proteins was detected by Western blot. RAW264.7 cells were used to test the anti-inflammatory effects of DA in vitro. Cytotoxicity was assessed using a MTT assay. Nitric oxide production was measured by Griess assay. The production and expression of inflammatory mediators and the protein levels of inflammatory signaling molecules in the NF-κB and MAPK pathways were measured. Furthermore, immunofluorescence staining was used to analyze the expression of p-IκBα, p-ERK, and p-p38 in lung macrophages and the nuclear translocation of NF-κB p65 and AP-1 in cells. RESULTS: DA evidently alleviated histopathological changes and ameliorated pulmonary edema. Moreover, DA could reduce excessive inflammatory reaction in lung tissue as manifested by the reduction of proinflammatory mediators (IL-1ß, IL-6, TNF-α, MCP-1, iNOS, and COX-2) in BALF, serum, and lung tissues. Further, DA inhibited the activation of the NLRP3/caspase-1 pathway in the lung. DA reduced the production and expression of the proinflammatory mediators above in RAW264.7 cells. Mechanistically, DA remarkably blocked the nuclear translocation of NF-κB p65, suppressed IκBα phosphorylation, and markedly reduced the nuclear translocation of AP-1 and the phosphorylation of ERK and p38. CONCLUSIONS: The findings demonstrated that DA exerts anti-inflammatory effects in LPS-stimulated ALI mice and macrophages by downregulating the NLRP3/caspase-1 signaling pathway in lung tissue and the IκB/NF-κB and MAPKs/AP-1 pathways in macrophages, suggesting that DA may be promising in ALI treatment.


Assuntos
Lesão Pulmonar Aguda , Edema Pulmonar , Triterpenos , Lesão Pulmonar Aguda/induzido quimicamente , Lesão Pulmonar Aguda/tratamento farmacológico , Animais , Anti-Inflamatórios , Caspases/metabolismo , Ciclo-Oxigenase 2/metabolismo , Amarelo de Eosina-(YS) , Glicosídeos/farmacologia , Hematoxilina/farmacologia , Hematoxilina/uso terapêutico , Proteínas I-kappa B/metabolismo , Mediadores da Inflamação/metabolismo , Interleucina-6 , Lipopolissacarídeos/toxicidade , Camundongos , Proteínas Quinases Ativadas por Mitógeno/metabolismo , Inibidor de NF-kappaB alfa/metabolismo , NF-kappa B/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR , Óxido Nítrico/metabolismo , RNA Mensageiro , Transdução de Sinais , Fator de Transcrição AP-1/metabolismo , Fator de Necrose Tumoral alfa/farmacologia
8.
J Ethnopharmacol ; 300: 115745, 2023 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-36162548

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Anadenanthera colubrina (Vell.) Brenan is an endemic tree to South America and different parts of it are used by the population for the treatment of various diseases, as well as in indigenous rituals. This species has high pharmacological potential but may present toxic potential due to the presence of psychotropic compounds. AIM OF THE STUDY: To review published studies with the species A. colubrina regarding ethnobotanical, phytochemical, pharmacological and toxicological aspects, as well as discuss perspectives for new research and protection of this species. MATERIALS AND METHODS: A literature review was performed by accessing published articles on databases such as: PubMed, Science Direct, Scielo, Scopus, Taylor and Francis online, Springer Link, National Center for Biotechnology Information (NCBI), ACS Publications, Chemspider and Google Scholar. The keywords used were: "Anadenanthera colubrina" or "Mimosa colubrina" or "Piptadenia colubrina" or "Piptadenia macrocarpa" or "Piptadenia grata" or "Anadenanthera macrocarpa" and "medicinal plants" or "pharmacological" or "phytochemicals" or "traditional use" or "toxicological" or "ethnobotanical" or "pre-clinical trial" or "clinical". Articles found by database searches and search engines were screened at four stages: (i) title screening, (ii) locality screening, (iii) abstract screening, and (iv) full text. Other articles found through supplementary searches were screened in the full text whenever available. Each article was assessed by three reviewers at the title and abstract screening stages, except for those found in Portuguese databases that were assessed by the native reviewer. RESULTS: This robust tree has been popularly useful for agroeconomic, medicinal and as a hallucinogen in religious rituals. According to the published studies, the main parts of the plant are the bark and seeds that are mostly used for respiratory conditions and as entheogens, respectively. It is a rich traditional herbal medicine with many pharmacological properties such as anti-inflammatory, antinociceptive, antidiarrheal, wound healing, antimicrobial, antitumoral, antioxidant, antiaddictive, insecticide and allelopathic that were described in in vitro and in vivo assays, and approximately 56 compounds were identified, suggesting a therapeutic potential for this species. Although most relate to medicinal uses, these are preliminaries and do not show the mechanism of action. The phytochemical assays showed the presence of phenolic compounds, flavonoids, triterpenes, steroids and alkaloids. Some of the compounds are anadanthoflavone, which is exclusive to this species, and no pharmacological or toxicological studies have yet demonstrated this compound. Another important compound is bufotenine which was isolated from seeds and is related to hallucinogenic and antiviral activity. The extracts made from leaves, bark, gum, and fruits appear to be safe, according to both in vivo and in vitro toxicology testing, which all shown low toxicity. Due to the presence of bufotenine in the seeds, it can be toxic, however, it was not found in toxicological assays with the seed extracts. CONCLUSIONS: Therefore, part of the studies confirms the popular use of A. colubrina, however, more assays with isolated compounds and with the different extracts are necessary to corroborate other uses and the mechanism of action of their pharmacological effects needs to discuss in more detail. Therefore, the present review would be identified the gaps and suggests further studies oriented to validate the popular use. Thus, it must be noted that the use of this species must be controlled in order to minimize the environmental impact, as most of the pharmacological potential was shown with the bark and seeds. Due to its wide use in folk medicine, it is part of the Brazilian medicinal species with priority for conservation.


Assuntos
Alcaloides , Colubrina , Fabaceae , Alucinógenos , Inseticidas , Plantas Medicinais , Triterpenos , Analgésicos , Anti-Inflamatórios , Antidiarreicos , Antioxidantes , Antivirais , Brasil , Bufotenina , Etnofarmacologia , Flavonoides , Compostos Fitoquímicos/uso terapêutico , Compostos Fitoquímicos/toxicidade , Fitoterapia , Extratos Vegetais/química , Extratos Vegetais/toxicidade
9.
J Ethnopharmacol ; 300: 115740, 2023 Jan 10.
Artigo em Inglês | MEDLINE | ID: mdl-36162549

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Antrodia camphorata is a genus of wood-rot basidiomycete in the family Fomitopsidaceae. It is a valuable medicinal fungus in China that contains more than 78 kinds of active compounds. A. camphorata has good protection effects on the liver, especially on alcoholic liver injury (ALI). AIM: This paper summarizes the complex occurrence and development of alcoholic liver disease (ALD). In addition, the effect of ALD on the intestine through the gut-liver axis is summarized. The protective mechanism of A. camphorata on ALI is reviewed to reveal its therapeutic potential, offering insights into future research. MATERIALS AND METHODS: A comprehensive search in the literature was obtained from books and online databases such as Web of Science, Google Scholar, PubMed, Scopus, Science direct, ACS Publications and Baidu Scholar. RESULTS: The pathogenesis of ALD mainly includes oxidative stress injury, intestinal microflora imbalance, inflammatory mediator injury and nutritional imbalance. A. camphorata contains rich active components (e.g. polysaccharides, triterpenoids, maleic and succinic acid derivatives, amino acids, superoxide dismutase, vitamins, lignin and sterols). These components have good antioxidant, anti-inflammatory and intestinal protection activities. Therefore, A. camphorata has a wide application in the prevention and treatment of ALI. CONCLUSIONS: ALD develops from a mild disease to alcoholic hepatitis and cirrhosis, which is the main reason of global morbidity and mortality. At present, there is no effective drug for the treatment of ALD. A. camphorata, as a valuable medicinal fungus unique to Taiwan, has a great protective effect on the liver. It is expected to be an effective drug for ALI treatment. Although many studies have performed the protective effects of A. camphorata on ALI, its regulatory effects on the gut-liver axis of ALD patients need to be further explored.


Assuntos
Antrodia , Hepatopatias Alcoólicas , Triterpenos , Aminoácidos/metabolismo , Anti-Inflamatórios/farmacologia , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Antrodia/química , Humanos , Mediadores da Inflamação/metabolismo , Lignina , Hepatopatias Alcoólicas/tratamento farmacológico , Hepatopatias Alcoólicas/prevenção & controle , Polyporales , Esteróis , Succinatos , Superóxido Dismutase/metabolismo , Triterpenos/uso terapêutico , Vitaminas/metabolismo
10.
Oxid Med Cell Longev ; 2022: 4564471, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35308167

RESUMO

The polarization of microglia is recognized as a crucial factor in reducing neuroinflammation and promoting hematoma clearance after intracerebral hemorrhage (ICH). Previous studies have revealed that redox components participate in the regulation of microglial polarization. Recently, the novel Nrf2 activator omaveloxolone (Omav) has been validated to improve neurological function in patients with neurodegenerative disorders by regulating antioxidant responses. In this study, we examined the efficacy of Omav in ICH. Omav significantly promoted Nrf2 nuclear accumulation and the expression of HO-1 and NQO1 in BV2 cells. In addition, both in vitro and in vivo experiments showed that Omav treatment inhibited M1-like activation and promoted the activation of the M2-like microglial phenotype. Omav inhibited OxyHb-induced ROS generation and preserved the function of mitochondria in BV2 cells. Intraperitoneal administration of Omav improved sensorimotor function in the ICH mouse model. Importantly, these effects were blocked by pretreatment with ML385, a selective inhibitor of Nrf2. Collectively, Omav modulated microglial polarization by activating Nrf2 and inhibiting ROS generation in ICH models, suggesting that it might be a promising drug candidate for the treatment of ICH.


Assuntos
Lesões Encefálicas , Microglia , Animais , Lesões Encefálicas/tratamento farmacológico , Hemorragia Cerebral/complicações , Hemorragia Cerebral/tratamento farmacológico , Hemorragia Cerebral/metabolismo , Humanos , Camundongos , Microglia/metabolismo , Fator 2 Relacionado a NF-E2/metabolismo , Fenótipo , Triterpenos
11.
Biomed Pharmacother ; 156: 113989, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36411656

RESUMO

Atopic disease is a kind of abnormal immune reaction caused by tissue damage and physiological dysfunction caused by allergens. Atopic diseases involve many systems and have obvious genetic tendencies, threatening the quality of life, health, and life safety of human beings. Astragalus membranaceus is an ancient and commonly used traditional Chinese medicine widely used in allergic diseases. Astragaloside IV is one of the main active ingredients in Astragalus membranaceus and is an important index component for evaluating the quality of Astragalus membranaceus and Astragalus membranaceus preparations at present. It has good antiallergic and immunomodulatory effects. Therefore, this paper reviews and summarizes the mechanism of action, pharmacokinetics, and drug optimization research progress of astragaloside IV in the treatment of atopic diseases.


Assuntos
Hipersensibilidade , Saponinas , Triterpenos , Humanos , Qualidade de Vida , Saponinas/farmacologia , Saponinas/uso terapêutico , Triterpenos/uso terapêutico , Astragalus propinquus
12.
Molecules ; 27(21)2022 Nov 02.
Artigo em Inglês | MEDLINE | ID: mdl-36364287

RESUMO

Propolis, popularly known as bee glue, is a resinous, sticky substance produced by different bee species across the globe. Studies on the biological properties of propolis from the Philippines are rare. Hence, the current study aims at the chemical characterization of propolis produced by the stingless bees Tetragonula biroi Friese from the Philippines and to investigate its antitrypanosomal and anticancer properties. The determination of the chemical composition and characterization of propolis samples was achieved using liquid chromatography-mass spectrometry (LC-MS), -high-performance liquid chromatography-evaporative light scattering detector (HPLC-ELSD), and nuclear magnetic resonance (NMR) spectroscopy. Three major triterpenes were isolated and identified using HRESI-MS and 1H/13C NMR techniques. The spectral studies confirmed the presence of compounds such as isomangiferolic acid, 27-hydoxymangiferonic acid, and 27-hydroxyisomangiferolic acid. All crude propolis samples, isolated fractions, and pure compounds demonstrated moderate antitrypanosomal and anticancer properties compared to control drugs. Amongst the tested compounds, 27-hydoxymangiferonic acid exhibited the highest antitrypanosomal activity at a concentration of 11.6 µg/mL. The highest anticancer effect was demonstrated by the Ph-2 fraction, followed by 27-hydroxyisomangiferolic acid, with IC50 values of 129.6 and 153.3 µg/mL. Thus, it can be concluded that the observed biological activity of Philippine propolis is due to the combinatorial effect or synergistic action of the active compounds 27-hydoxymangiferonic acid and 27-hydroxyisomangiferolic acid.


Assuntos
Antineoplásicos , Própole , Triterpenos , Animais , Própole/química , Triterpenos/farmacologia , Triterpenos/análise , Cromatografia Líquida de Alta Pressão/métodos , Antineoplásicos/farmacologia
13.
Molecules ; 27(21)2022 Nov 02.
Artigo em Inglês | MEDLINE | ID: mdl-36364289

RESUMO

Lung cancer is the leading cause of cancer-related deaths globally. Despite current treatment approaches that include surgery, chemotherapy, radiation and immunotherapies, lung cancer accounted for 1.79 million deaths worldwide in 2020, emphasizing the urgent need to find novel agents and approaches for more effective treatment. Traditionally, chemicals derived from plants, such as paclitaxel and docetaxel, have been used in cancer treatment, and in recent years, research has focused on finding other plant-derived chemicals that can be used in the fight against lung cancer. Ursolic acid is a polyphenol found in high concentrations in cranberries and other fruits and has been demonstrated to have anti-inflammatory, antioxidant and anticancer properties. In this review, we summarize recent research examining the effects of ursolic acid and its derivatives on lung cancer. Data from in vitro cell culture and in vivo animal studies show potent anticancer effects of ursolic acid and indicate the need for clinical studies.


Assuntos
Neoplasias Pulmonares , Triterpenos , Animais , Proliferação de Células , Triterpenos/farmacologia , Triterpenos/uso terapêutico , Triterpenos/química , Neoplasias Pulmonares/tratamento farmacológico , Paclitaxel/farmacologia
14.
Molecules ; 27(21)2022 Nov 07.
Artigo em Inglês | MEDLINE | ID: mdl-36364484

RESUMO

Five new triterpene (4,4,14-trimethylsterol) di-, tri- and tetrasulfated pentaosides, chilensosides A (1), A1 (2), B (3), C (4), and D (5) were isolated from the Far-Eastern sea cucumber Paracaudina chilensis. The structures were established on the basis of extensive analysis of 1D and 2D NMR spectra and confirmed by HR-ESI-MS data. The structural variability of the glycosides concerned the pentasaccharide chains. Their architecture was characterized by the upper semi-chain consisting of three sugar units and the bottom semi-chain of two sugars. Carbohydrate chains of compounds 2-5 differed in the quantity and positions of sulfate groups. The interesting structural features of the glycosides were: the presence of two sulfate groups at C-4 and C-6 of the same glucose residue in the upper semi-chain of 1, 2, 4, and 5 and the sulfation at C-3 of terminal glucose residue in the bottom semi-chain of 4 that makes its further elongation impossible. Chilensoside D (5) was the sixth tetrasulfated glycoside found in sea cucumbers. The architecture of the sugar chains of chilensosides A-D (1-5), the positions of sulfation, the quantity of sulfate groups, as well as the aglycone structures, demonstrate their similarity to the glycosides of the representatives of the order Dendrochirotida, confirming the phylogenetic closeness of the orders Molpadida and Dendrochirotida. The cytotoxic activities of the compounds 1-5 against human erythrocytes and some cancer cell lines are presented. Disulfated chilensosides A1 (2) and B (3) and trisulfated chilensoside C (4) showed significant cytotoxic activity against human cancer cells.


Assuntos
Antineoplásicos , Neoplasias , Pepinos-do-Mar , Triterpenos , Animais , Humanos , Pepinos-do-Mar/química , Triterpenos/farmacologia , Triterpenos/química , Filogenia , Glicosídeos/farmacologia , Glicosídeos/química , Antineoplásicos/farmacologia , Antineoplásicos/química , Açúcares , Sulfatos , Glucose , Estrutura Molecular
15.
Int J Mol Sci ; 23(21)2022 Oct 29.
Artigo em Inglês | MEDLINE | ID: mdl-36361934

RESUMO

Carbon monoxide (CO), a product of organic oxidation processes, arises in vivo principally from the enzymatic reaction of heme oxygenase (HO, transcription gene named HMX1). HO/CO has been found to exert many salutary effects in multiple biological processes, including the stress response. However, whether HO/CO is involved in the regulation of the heat-stress (HS) response of Ganoderma lucidum (G. lucidum) is still poorly understood. In this paper, we reported that under heat stress, the HMX1 transcription level, HO enzyme activity, and CO content increased by 5.2-fold, 6.5-fold and 2-fold, respectively. HMX1 silenced strains showed a 12% increase in ganoderic acid (GA) content under HS as analyzed by HPLC. Furthermore, according to Western blot analysis of the protein phosphorylation levels, HMX1 attenuated the increase in phosphorylation levels of slt2, but the phosphorylation levels were prolonged over a 3 h HS time period. The chitin and glucan content in HMX1 silenced strains increased by 108% and 75%, respectively. In summary, these findings showed that the HO/CO system responds to heat stress and then regulates the HS-induced GA biosynthesis and the cell-wall integrity mediated by the Slt-MAPK phosphorylation level in G. lucidum.


Assuntos
Reishi , Triterpenos , Reishi/genética , Reishi/metabolismo , Monóxido de Carbono/metabolismo , Heme Oxigenase (Desciclizante)/metabolismo , Triterpenos/farmacologia , Resposta ao Choque Térmico
16.
Int J Mol Sci ; 23(21)2022 Oct 31.
Artigo em Inglês | MEDLINE | ID: mdl-36362079

RESUMO

Cancer has been a major health problem in the world in the past decades. It is urgent to develop new, effective and safe drugs for the treatment of cancer. There are many pentacyclic triterpenoids with positive anti-tumor activity and safety in nature. Oleanolic acid (OA), as one of the pentacyclic triterpenoids, also has broad biological activities including liver protection, anti-inflammatory, hypoglycemic, antiviral and anti-tumor. Therefore, to investigate its anti-tumor activity and mechanism, many OA derivatives have been developed. Some derivatives are less toxic to normal hepatocytes, which may be due to the strong liver protection ability of OA. However, the poor water solubility of OA is one of the main reasons for the weak anti-tumor activity. It is reported that some OA derivatives could enhance solubility by chemically linking some hydrophilic groups to improve anti-tumor activity. This review not only summarizes the highly water-soluble OA derivatives that can improve anti-tumor activity reported in recent years, but also introduces their possible anti-tumor mechanisms.


Assuntos
Neoplasias , Ácido Oleanólico , Triterpenos , Humanos , Solubilidade , Triterpenos/química , Neoplasias/tratamento farmacológico , Água
17.
Int J Mol Sci ; 23(21)2022 Nov 06.
Artigo em Inglês | MEDLINE | ID: mdl-36362380

RESUMO

Neurotrophins such as nerve growth factor (ngf) and brain-derived neurotrophic factor (bdnf) play important roles in the central nervous system. They are potential therapeutic drugs for the treatment of neurodegenerative diseases, including Alzheimer's disease and Parkinson's disease. In this study, we investigated the neurotrophic properties of triterpenes isolated from fruiting bodies of Laetiporus sulphureus and a mycelial culture of Antrodia sp. MUCL 56049. The structures of the isolated compounds were elucidated based on nuclear magnetic resonance (NMR) spectroscopy in combination with high-resolution electrospray mass spectrometry (HR-ESIMS). The secondary metabolites were tested for neurotrophin (ngf and bdnf) expression levels on human astrocytoma 1321N1 cells. Neurite outgrowth activity using rat pheochromocytoma (PC-12) cells was also determined. Twelve triterpenoids were isolated, of which several potently stimulated the expression of neurotrophic factors, namely, ngf (sulphurenic acid, 15α-dehydroxytrametenolic acid, fomefficinic acid D, and 16α-hydroxyeburicoic acid) and bdnf (sulphurenic acid and 15α-dehydroxytrametenolic acid), respectively. The triterpenes also potentiated ngf-induced neurite outgrowth in PC-12 cells. This is, to the best of our knowledge, the first report on the compound class of lanostanes in direct relation to bdnf and ngf enhancement. These compounds are widespread in medicinal mushrooms; hence, they appear promising as a starting point for the development of drugs and mycopharmaceuticals to combat neurodegenerative diseases. Interestingly, they do not show any pronounced cytotoxicity and may, therefore, be better suited for therapy than many other neurotrophic compounds that were previously reported.


Assuntos
Basidiomycota , Doenças Neurodegenerativas , Triterpenos , Animais , Ratos , Humanos , Fator de Crescimento Neural/farmacologia , Fator de Crescimento Neural/metabolismo , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Triterpenos/farmacologia , Triterpenos/química , Madeira/metabolismo , Basidiomycota/química
18.
Molecules ; 27(21)2022 Oct 24.
Artigo em Inglês | MEDLINE | ID: mdl-36364025

RESUMO

Euphorbia officinarum L. is a Moroccan endemic plant known as "Tikiout" and "Daghmus" that can also be found in Mauritania, Western Sahara, and Algeria. In the present review, "Euphorbia officinarum", "metabolites" "hemisynthesis" were the keywords used for the research in the Web search engine Google Scholar and in the database Web of Science. Triterpenes, phytosterols and ingol diterpenes were isolated and identified in the latex of Moroccan E. officinarum. More than sixty triterpenes were obtained by hemisynthesis from natural triterpenes. Some of these derivatives had insecticidal and antimicrobial activity (phytopathogenic bacteria). The total phenol content and the antioxidant and anti-α-glucosidase activities were dependent on the time and temperature of extractions and also on the plant solvent ratio. The antioxidant activity of monofloral honey of E. officinarum origin was attributed to the phenol fraction (this fraction, previously isolated from honey samples, had better activity than the entire honey).


Assuntos
Diterpenos , Euphorbia , Triterpenos , Abelhas , Animais , Látex , Antioxidantes/farmacologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia
19.
J Tradit Chin Med ; 42(6): 877-884, 2022 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-36378044

RESUMO

OBJECTIVE: To investigate the in-depth pharma-cological mechanisms of celastrol in children neuro-blastoma treatment. METHODS: In the current study, we examined the effects of celastrol on children neuroblastoma cells viability and proliferation by cell counting kit-8 assay and colony formation assay. Annexin V-FTIC and PI staining were applied to determine cell apoptosis after celastrol treatment. ROS generation levels were examined by 2', 7'-dichloroflfluorescin diacetate. RESULTS: We found that celastrol could suppress the proliferation of children neuroblastoma cells with few effects on normal cell lines . Further mechanisms studies have shown that celastrol inhibited cell cycle progression and induced cell apoptosis in QDDQ-NM and SH-SY5Y cells. In addition, ROS production might involve in celastrol-mediated apoptotic cell death in children neuroblastoma cells by activating caspase death pathway. CONCLUSIONS: Our findings demonstrated that celastrol could promote ROS generation-induced apoptosis in neuroblastoma cell by activating caspase death pathway. These findings suggested that celastrol might be a potential novel anti-neuroblastoma agent with minor cytotoxicity.


Assuntos
Neuroblastoma , Triterpenos , Criança , Humanos , Caspases/genética , Espécies Reativas de Oxigênio/metabolismo , Neuroblastoma/tratamento farmacológico , Neuroblastoma/genética , Neuroblastoma/metabolismo , Triterpenos/farmacologia , Linhagem Celular Tumoral , Apoptose , Sobrevivência Celular , Proliferação de Células , Caspase 3/metabolismo
20.
Int J Med Mushrooms ; 24(10): 15-29, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36374827

RESUMO

Considering the impact of oxidative stress on the development of many diseases, together with the role of natural antioxidants in maintaining physiological balance in humans, medicinal mushrooms are potential sources of bioactive compounds against many diseases. In the present work, in vitro evaluation of the biological activities of the alcoholic extracts of two wild tree mushrooms, namely, Ganoderma applanatum and Fomitopsis pinicola, has been performed. Extraction of G. applanatum (GAE) and F. pinicola (FPE) was conducted with 60% ethanol and 100% ethanol sequentially. UPLC-MS/MS identification was conducted on the two mushrooms extracts. A total of 15 substances were identified in GAE, including 3 spiro meroterpenoids and 12 triterpenoids; a total of 14 chemical constituents were iden¬tified in FPE, including 8 triterpenoids, 4 triterpene glycosides, 1 lanosterol, and 1 lanostanoid. The resulting extracts were examined for their in vitro antioxidative and cytoprotective effects against AAPH-induced oxidative damage. Our results demonstrated that both extracts have potent antioxidative activities, when GAE was 0.2 mg/mL, the clearance rates of DPPH and ABTS have reached 93.34% and 99.93%, respectively. When FPE was 1.4 mg/mL and 0.6 mg/mL, the scavenging rates of DPPH and ABTS have reached 91.76% and 100%, respectively. Both the alcoholic extracts of G. applanatum and F. pinicola were able to protect the AAPH-induced damage and could effectively inhibit cell aging via ß-galactosidase (SA ß-gal) staining activity test and scanning electron microscopy analysis.


Assuntos
Neoplasias das Glândulas Suprarrenais , Agaricales , Ganoderma , Feocromocitoma , Triterpenos , Humanos , Antioxidantes/química , Cromatografia Líquida , Espectrometria de Massas em Tandem , Agaricales/química , Triterpenos/química , Etanol
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