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1.
Mini Rev Med Chem ; 2021 Oct 22.
Artigo em Inglês | MEDLINE | ID: mdl-34719362

RESUMO

Natural products have remarkable structural diversity and biological characteristics, providing researchers with more possibilities to develop novel drugs for disease therapeutics. Andrographolide, an ent-labdane diterpenoid from traditional Chinese medicines, Andrographis paniculata, exhibits a broad range of biological activities, which has been a hot area of research for several years. Up to now, lots of its derivatives with multiple bioactivities have been prepared through chemical modification. This review summarizes andrographolide derivatives prepared in the last ten years (2006-present), classifies them by different biological activities, and provides some discussion about the design of novel and potent derivatives.

2.
Nat Prod Rep ; 2021 Nov 24.
Artigo em Inglês | MEDLINE | ID: mdl-34816854

RESUMO

Covering: March 2010 to December 2020. Previous review: Nat. Prod. Rep., 2011, 28, 705This review summarizes the latest progress and perspectives on the structural classification, biological activities and mechanisms, metabolism and pharmacokinetic investigations, biosynthesis, chemical synthesis and structural modifications, as well as future research directions of the promising natural withanolides. The literature from March 2010 to December 2020 is reviewed, and 287 references are cited.

3.
Curr Top Med Chem ; 2021 Nov 04.
Artigo em Inglês | MEDLINE | ID: mdl-34749614

RESUMO

Natural products have been proven as the main source of biologically active compounds, which are potentially useful for drug development. As one of the most studied pentacyclic triterpenes, oleanolic acid (OA) exhibits a broad range of biological activities and serves as a good scaffold for the development of novel derivatives that could be vital in drug discovery for various ailments. Up to now, many of its derivatives with multiple bioactivities have been prepared through chemical modification. This review summarizes the recent reports of OA derivatives (2016-present) and their biological effects and action mechanisms in vitro and in vivo models, and discusses the design of novel and potent derivatives.

4.
J Neuroimaging ; 2021 Oct 14.
Artigo em Inglês | MEDLINE | ID: mdl-34648213

RESUMO

BACKGROUND AND PURPOSE: To explore the application value and clinical significance of transcranial Doppler(TCD)in assessing leptomeningeal collateral flow (LMF) status in patients with unilateral middle cerebral artery (MCA) occlusion. METHODS: Medical records of patients with unilateral MCA occlusion confirmed by digital subtraction angiography (DSA) were analyzed retrospectively. The patients were divided into three groups according to LMF status, and the laboratory and imaging results were collected. Cerebral blood flow velocity (CBFV) of MCA, anterior cerebral artery (ACA), and posterior cerebral artery (PCA) on the affected side (ipsilateral, i) and the healthy side (contralateral, c) were measured and recorded by TCD. The results of CBFV changes detected by TCD were compared with those of DSA, and the correlation between CBFV changes and LMF status was analyzed. RESULTS: Eighty-four patients with unilateral MCA occlusion were included. CBFViACA and CBFViPCA were significantly faster than CBFVcACA and CBFVcPCA in patients with good LMF status (p<.05). There was a significant positive correlation between CBFViACA and LMF status (r = 0.697, p<.001). There was statistical significance in receiver operating characteristic curve analysis of CBFViACA and CBFViPCA (p<.05). The area under the curve of CBFViACA and CBFViPCA, respectively, was 0.879 and 0.678, and the best cutoff value was 82 and 60.5 cm/s. CONCLUSIONS: TCD can assess LMF status by detecting the changes of flow velocity of intracranial vessels. CBFV of ACA and PCA in patients with MCA occlusion is significantly correlated with LMF status by DSA. Assessing LMF status, CBFViACA, CBFViACA/CBFVcACA, and CBFViACA/CBFViMCA has the great diagnostic value, which is of great significance in guiding MCA occlusion patients to choose individualized treatment.

5.
J Agric Food Chem ; 69(42): 12433-12444, 2021 Oct 27.
Artigo em Inglês | MEDLINE | ID: mdl-34664962

RESUMO

Two previously undescribed compounds, moranigrine A (1) and morusamine (2), along with 18 known compounds were isolated from the fruits of Morus nigra Linn. and structurally characterized using spectroscopic data and electronic circular dichroism analyses. All isolates were evaluated for their inhibitory effects on the 3-phosphoglycerate dehydrogenase (PHGDH) enzyme, which catalyzes the first committed step for the synthesis of glucose-derived serine and is associated with many kinds of cancers. Among these compounds, methyl caffeate (3) exhibited effective inhibition against PHGDH and was directly bound to PHGDH based on the microscale thermophoresis method and the cellular thermal shift assay. Further biochemical assays revealed that 3 was a noncompetitive inhibitor with respect to the substrate of 3-phosphoglycerate and exhibited a concentration-dependent inhibition. Molecular docking demonstrated that 3 coordinated in an allosteric site of PHGDH with low binding energy. Meanwhile, 3 was selectively toxic to high PHGDH-expressing cancer cell lines and could cause apoptosis of cervical cancer cells in micromolar concentrations and could obviously inhibit tumor growth in the HeLa xenograft mouse model with low toxicities. Therefore, 3 could be developed as a potential inhibitor of PHGDH for the treatment of cancers. Our present study provides information about M. nigra as a functional food or pharmaceutical supplement in the application of cancer prevention and treatment.


Assuntos
Antineoplásicos , Morus , Animais , Antineoplásicos/farmacologia , Ácidos Cafeicos , Linhagem Celular Tumoral , Proliferação de Células , Frutas , Humanos , Camundongos , Simulação de Acoplamento Molecular , Fosfoglicerato Desidrogenase , Serina/farmacologia
6.
Virol Sin ; 2021 Oct 27.
Artigo em Inglês | MEDLINE | ID: mdl-34704222

RESUMO

Porcine reproductive and respiratory syndrome virus (PRRSV) continues to cause significant economic loss worldwide and remains a serious threat to the pork industry. Currently, vaccination strategies provide limited protection against PRRSV infection, and consequently, new antiviral strategies are urgently required. Andrographolide (Andro) and its derivative potassium dehydrographolide succinate (PDS) have been used clinically in China and other Asian countries as therapies for inflammation-related diseases, including bacterial and viral infections, for decades. Here, we demonstrate that Andro and PDS exhibit robust activity against PRRSV replication in Marc-145 cells and primary porcine alveolar macrophages (PAMs). The two compounds exhibited broad-spectrum inhibitory activities in vitro against clinically circulating type 2 PRRSV GD-HD, XH-GD, and NADC30-like HNhx strains in China. The EC50 values of Andro against three tested PRRSV strain infections in Marc-145 cells ranged from 11.7 to 15.3 µmol/L, with selectivity indexes ranging from 8.3 to 10.8, while the EC50 values of PDS ranged from 57.1 to 85.4 µmol/L, with selectivity indexes ranging from 344 to 515. Mechanistically, the anti-PRRSV activity of the two compounds is closely associated with their potent suppression on NF-κB activation and enhanced oxidative stress induced by PRRSV infection. Further mechanistic investigations revealed that PDS, but not Andro, is able to directly interact with PRRSV particles. Taken together, our findings suggest that Andro and PDS are promising PRRSV inhibitors in vitro and deserves further in vivo studies in swine.

7.
Phytochemistry ; 192: 112971, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34628107

RESUMO

Six undescribed diterpenoid alkaloids including five C19-diterpenoid alkaloids forrestlines A-E, and one C20-diterpenoid alkaloid forrestline F, together with nine known alkaloids have been isolated from the whole herbs of Delphinium forrestii var. vride. Their structures were elucidated by spectroscopic data, and their inhibitory activities on NO production stimulated by LPS in RAW264.7 macrophage cells were determined. Then, forrestline F, with the strongest inhibitory activity (IC50 of 9.57 ± 1.43 µM), was selected to study its possible anti-inflammatory mechanism. ELISA results showed that forrestline F suppressed inflammatory cytokines, including interleukin-1ß (IL-1ß), tumor necrosisfactor-α (TNF-α), and interleukin-6 (IL-6). Moreover, forrestline F could down-regulate LPS-induced expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) by western blotting assay. It also inhibited expression of phosphorylation of MAPKs (including p-p38, p-ERK and p-JNK), and NF-κB p65, and decreased ROS accumulation by upregulating the expression of HO-1 expression via nuclear translocation of Nrf2. In conclusion, forrestline F showed anti-inflammatory effect by inhibiting NF-κB/MAPK and Nrf2/HO-1 signaling pathway. Therefore, forrestline F could be a promising molecule for the development of anti-inflammatory agents in the future.


Assuntos
Alcaloides , Delphinium , Diterpenos , Alcaloides/farmacologia , Anti-Inflamatórios/farmacologia , Ciclo-Oxigenase 2/metabolismo , Diterpenos/farmacologia , Heme Oxigenase-1/metabolismo , Lipopolissacarídeos , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo
8.
Med Ultrason ; 2021 Sep 11.
Artigo em Inglês | MEDLINE | ID: mdl-34508616

RESUMO

AIMS: To investigate the positional relationship between the ovary and Fallopian tube and the relationship between the ovarian position and tubal morphology. MATERIAL AND METHODS: A total of 195 patients with 338 fallopian tubes were enrolled in this retrospective study. The ovarian and tubal positions were defined relative to the uterus in all directions. Tubal morphology was classified as smooth or tortuous. RESULTS: The distribution of the Fallopian tubes corresponded to the positions of the ipsilateral ovaries in the superoinferior direction (χ2 =197.653, p<0.001), mediolateral direction (χ2 =237.447, p <0.001) and anteroposterior direction (χ2 =109.746, p<0.001). Tubal morphology differed according to ovarian position in the superoinferior (χ2 =21.804, p<0.001), mediolateral directions (χ2 =4.679, p=0.031) but not in the anteroposterior direction (χ2 =0.793, p=0.373). CONCLUSIONS: Evaluating the ovarian position can provide preliminary information on the distribution and shapeof the Fallopian tube, helping the operator choose the appropriate initial plane and the necessary approaches for inspection.

9.
Macromol Rapid Commun ; 42(21): e2100431, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34480770

RESUMO

The hydrogels composed of decamethylcucurbit[5]uril (Me10 Q[5]) and para-phenylenediamine (p-PDA) are first reported herein. They are the first Q[5]-based supramolecular hydrogels, the formation of which is driven by portal exclusion between Me10 Q[5] and p-PDA. The composition, structure, and properties of the Me10 Q[5]/p-PDA-based hydrogels are investigated by various techniques. Since the 1D supramolecular chain forms via portal exclusion between Me10 Q[5] and p-PDA is the key to the formation of the hydrogels, any competitive species, such as metal ions, organic molecules, and amino acids, which can affect the portal exclusion, can change the behavior of the Me10 Q[5]/p-PDA-based hydrogels. Hence, the hydrogels can be used for various applications. Importantly, the results may provide a new research direction for the preparation of Q[n]-based hydrogels via portal exclusion of Q[n]s with guests.


Assuntos
Hidrogéis , Fenilenodiaminas , Íons
10.
J Ethnopharmacol ; 281: 114563, 2021 Dec 05.
Artigo em Inglês | MEDLINE | ID: mdl-34438033

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: The genus Amomum belonging to the family Zingiberaceae, is mainly distributed in tropical regions of Asia and Oceania. Their fruits and seeds are valuable traditional medicine and used extensively, particularly in South China, India, Malaysia, and Vietnam. The genus Amomum has long been used for treating gastric diseases, digestive disorder, cancer, hepatopathy, malaria, etc. AIMS OF THE REVIEW: The main purpose of this review is to provide the available information on the traditional medicinal uses, phytochemistry, and pharmacology aspects of the genus Amomum in order to explore the trends and perspectives for further studies on its non-volatile constituents. MATERIALS AND METHODS: The present review collected the literatures published prior to 2020 on the traditional medicinal uses, phytochemistry, and pharmacology of the genus Amomum. The available literatures were extracted from scientific databases, such as Sci-finder, PubMed, Web of Science, Google Scholar, Baidu Scholar, and CNKI, books, and others. RESULTS: Herein, we summarize all 166 naturally occurring non-volatile compounds from 16 plants of the genus Amomum reported in 171 references, including flavonoids, terpenoids, diarylheptanoids, coumarins, etc. Triterpenes and flavonoids are the main constituents among these compounds and maybe play an important role in the activities directly or indirectly. As traditional medicine, the plants from the genus Amomum have been usually used in some traditional herbal prescriptions, and pharmacological researches in vitro and in vivo revealed that the extracts possessed significant antioxidant, anti-inflammatory, anti-allergic activities, etc. CONCLUSION: The review systematically summarizes current studies on traditional medicinal uses, phytochemistry, pharmacological activity on the plants from the genus Amomum. To date, the majority of publications still focused on the research of volatile constituents. However, the promising preliminary data of non-volatile constituents indicated the research potential of this genus in phytochemical and pharmacological aspects. Furthermore, the further in-depth investigations on the safety, efficacy, as well as the stereo-chemistry and structure-activity relationships of pure compounds from this genus are essential in the future.

11.
J Sep Sci ; 44(19): 3646-3653, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34350710

RESUMO

A chiral analytical method was proposed based on capillary electrophoresis with laser-induced fluorescence detection coupled with microwave-assisted derivatization for the simultaneous baseline separation and sensitive detection of four stereoisomers of 3-hydroxyaspartate. The derivatization reaction of 3-hydroxyaspartate with 4-chloro-7-nitrobenzo-2-oxa-1,3-diazole was greatly accelerated by microwave irradiation. Under the optimized conditions, the derivatization yield was increased by 20% and the derivatization time was shortened by 20 min when compared with those from conventional water bath heating. In addition, the sensitivity was improved by online sample concentration methods. The detection limit of l-threo-3-hydroxyaspartate obtained by large-volume sample stacking with polarity switching was 5.3 nmol/L, which was around 1000-fold lower than that of the capillary electrophoresis/laser-induced fluorescence without stacking. The excellent analytical performance in terms of linearity and precision was also achieved. Furthermore, the developed method was successfully applied to the determination of 3-hydroxyaspartate in the spiked urine, and satisfactory recoveries were obtained ranging from 90.5 to 107.0%.

12.
Int Immunopharmacol ; 100: 108070, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34454292

RESUMO

RESEARCH QUESTION: In previous studies, we demonstrated that the human decidua and decidual stromal cells express high levels of CCL2 (chemokine (C-C motif) ligand 2, also known as monocyte chemotactic protein-1) and its receptor CCR2 (chemokine receptor 2). DSC-derived CCL2 interacts with CCR2 on DICs, causing the production and secretion of Th2-type cytokines, which promotes a Th2 bias at the maternal-foetal interface. Many pathogens may be present in the genital tract during pregnancy, but whether they affect immune regulation, especially Th2 regulation remains unknown. Toll-like receptors (TLRs) are a family of pattern-recognition receptors that recognise specific components of microbes and certain host molecules and play an important role in the host innate immune response. We examined TLR expression and evaluated whether TLRs could affect CCL2 secretion and subsequently induce Th1/Th2 responses. DESIGN: We used quantitative real-time PCR to measure TLR expression in the decidua and DSCs (decidual stromal cells). DSCs were cultured in the presence or absence of the TLR2 agonists PAM3CSK4, PGN-Sa, and zymosan, the TLR3 agonist poly (I:C) and the TLR4 agonist LPS. Then, the supernatants were assayed for CCL2 secreted by DSCs and IL-4, IFN-γ, IL-10, and TNF-α produced by DICs. RESULTS: Costimulation with TLR2, TLR3 and TLR4 agonists resulted in enhancing CCL2 production compared with that in the controls. Additionally, these TLR2, 3, and 4 agonists stimulated CD80/CD86 on DSCs and regulated IL-4 and IL-10 secretion on DICs. TLR2 and TLR3 agonists may promote Th1/Th2 immune bias. CONCLUSIONS: TLRs may induce Th1/Th2 responses by affecting the secretion of CCL2 at the maternal-foetal interface.

13.
J Chromatogr A ; 1654: 462446, 2021 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-34384924

RESUMO

Through an appropriate computational protocol and environmental simulation, a satisfactory fit was observed for the theoretical electronic circular dichroism (ECD) spectra of 19 chiral amino acids (AAs), which correspondeds to the forms of the AAs in aqueous solution. Methods for enantioseparation of these chiral AAs by capillary electrophoresis (CE) and high-performance liquid chromatography (HPLC) were developed. Combining ECD with chromatographic separation methods, enantiomers were identified and quantified independent of a single enantiomer standard.


Assuntos
Aminoácidos , Cromatografia Líquida de Alta Pressão , Dicroísmo Circular , Eletroforese Capilar , Aminoácidos/química , Aminoácidos/isolamento & purificação , Eletrônica , Estereoisomerismo
15.
Eur J Med Chem ; 224: 113696, 2021 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-34274828

RESUMO

The antimicrobial resistance (AMR) is an intractable problem for the world. Metal ions are essential for the cell process and biological function in microorganisms. Many metal-based complexes with the potential for releasing ions are more likely to be absorbed for their higher lipid solubility. Hence, this review highlights the clinical potential of organometallic compounds for the treatment of infections caused by bacteria or fungi in recent five years. The common scaffolds, including antimicrobial peptides, N-heterocyclic carbenes, Schiff bases, photosensitive-grand-cycle skeleton structures, aliphatic amines-based ligands, and special metal-based complexes are summarized here. We also discuss their therapeutic targets and the risks that should be paid attention to in the future studies, aiming to provide information for researchers on metal-based complexes as antimicrobial agents and inspire the design and synthesis of new antimicrobial drugs.

16.
BMC Pregnancy Childbirth ; 21(1): 470, 2021 Jun 30.
Artigo em Inglês | MEDLINE | ID: mdl-34193061

RESUMO

BACKGROUND: The Pelvic Girdle Questionnaire (PGQ) is the only specific instrument designed to evaluate pain and activity limitations in pregnant or postpartum women with pelvic girdle pain (PGP). This study aimed to translate and culturally adapt the PGQ for Chinese patients and to verify the validation of the psychometric items of the PGQ in the Chinese population. METHODS: First, the translation and cultural adaptation process of the PGQ was conducted on the basis of international guidelines. Eighteen women suffering from PGP (11 pregnant women and 7 postpartum women) were enrolled in the pilot tests. Second, a total of 130 pregnant and postpartum women with PGP were enrolled to evaluate the validation of the psychometric items of the Chinese version. RESULTS: The calculated Cronbach's alphas demonstrated a high level of internal consistency for the Chinese version of the PGQ, ranging from 0.77 to 0.93. The convergent validity showed a high positive correlation between the PGQ total score and the Oswestry Disability Index (0.84) and Numeric Rating Scale (0.73) for pain intensity. Furthermore, a good discriminatory ability was found for the Chinese version of the PGQ for distinguishing women who needed treatment from those not (area under the curve [AUC] = 0.843, p < 0.001), but not for discriminating the pregnant and postpartum states (AUC = 0.488, p = 0.824). The results of test-retest showed good reproducibility for the total PGQ (ICC = 0.93), the PGQ activity subscale (ICC = 0.92), and the PGQ symptom subscale (ICC = 0.77). CONCLUSION: Our study presents the translation, validation and psychometric features of the Chinese version of the PGQ, showing good construct validity and discriminative power for assessing the consequences of PGP among pregnant or postpartum Chinese women.


Assuntos
Dor da Cintura Pélvica/diagnóstico , Inquéritos e Questionários/normas , Traduções , Adulto , China , Assistência à Saúde Culturalmente Competente/normas , Feminino , Humanos , Medição da Dor , Período Pós-Parto , Gravidez , Complicações na Gravidez/diagnóstico , Psicometria , Reprodutibilidade dos Testes , Adulto Jovem
17.
Exp Cell Res ; 406(1): 112722, 2021 09 01.
Artigo em Inglês | MEDLINE | ID: mdl-34242623

RESUMO

Breast cancer is one of the most frequently diagnosed cancers and the leading cause of cancer death in women. MIER3 (Mesoderm induction early response 1, family member3) is considered as a potential oncogene for breast cancer. However, the role of MIER3 in breast cancer remain largely unknown. The expression of MIER3 was detected and the relationship between its expression and clinicopathological characteristics was also analyzed. The effect of MIER3 on proliferation and migration of breast cancer cells was detected in vitro and in vivo. Western blot, IF, and Co-IP were employed to detect the relationship between MIER3, HDAC1, HDAC2, and Snail. ChIP assay was performed to determine the binding of MIER3/HDAC1/HDAC2/Snail complex to the promoter of E-cadherin. In this study, we found that MIER3 was upregulated in breast cancer tissue and closely associated with poor prognosis of patients. MIER3 could promote the proliferation, migration, and epithelial-mesenchymal transition (EMT) of breast cancer cells. Further studies showed that MIER3 interacted with HDAC1/HDAC2 and Snail to form a repressive complex which could bind to E-cadherin promoter and was related to its deacetylation. Our study concluded that MIER3 was involved in forming a co-repressor complex with HDAC1/HDAC2/Snail to promote EMT by silencing E-cadherin.


Assuntos
Neoplasias da Mama/genética , Histona Desacetilase 1/genética , Histona Desacetilase 2/genética , Proteínas Nucleares/genética , Fatores de Transcrição da Família Snail/genética , Idoso , Animais , Antígenos CD/genética , Antígenos CD/metabolismo , Neoplasias da Mama/mortalidade , Neoplasias da Mama/patologia , Neoplasias da Mama/terapia , Caderinas/genética , Caderinas/metabolismo , Linhagem Celular Tumoral , Movimento Celular , Proliferação de Células , Células Epiteliais/metabolismo , Células Epiteliais/patologia , Transição Epitelial-Mesenquimal/genética , Feminino , Regulação Neoplásica da Expressão Gênica , Histona Desacetilase 1/metabolismo , Histona Desacetilase 2/metabolismo , Humanos , Camundongos Nus , Pessoa de Meia-Idade , Proteínas Nucleares/antagonistas & inibidores , Proteínas Nucleares/metabolismo , Regiões Promotoras Genéticas , Ligação Proteica , RNA Interferente Pequeno/genética , RNA Interferente Pequeno/metabolismo , Transdução de Sinais/genética , Fatores de Transcrição da Família Snail/metabolismo , Análise de Sobrevida , Carga Tumoral , Ensaios Antitumorais Modelo de Xenoenxerto
18.
Artigo em Inglês | MEDLINE | ID: mdl-34265810

RESUMO

STUDY DESIGN: A prospective study. OBJECTIVE: To investigate the factors associated with cardiopulmonary exercise testing (CPET) measurements in patients with adolescent idiopathic scoliosis (AIS). SUMMARY OF BACKGROUND DATA: Patients with AIS display restrictive pulmonary dysfunction on pulmonary function testing (PFT). It remains unknown whether thoracic spinal deformity affects exercise performance. METHODS: One hundred and sixty-eight patients with AIS from January 2014 to December 2019 were included. They underwent preoperative spinal radiological assessment, PFT, and CPET. The effects of the thoracic curve magnitude, body mass index, physical activity level and history of bracing on pulmonary function and exercise performance were analyzed. The Student t test and two-tailed Pearson test were used in data analysis. RESULTS: We found significantly reduced forced expiratory volume in 1 s (FEV1) in patients with a larger magnitude of the proximal thoracic curve (P < 0.001) and the main thoracic curve (P < 0.001). There was a negative correlation between forced vital capacity (FVC) and the magnitude of the main thoracic curve (P < 0.001) and thoracic hypokyphosis (P < 0.001). In CPET, exercise capacity indicators such as the work rate, peak oxygen intake, and heart rate were not affected by the thoracic curve magnitude. Patients with moderate or severe pulmonary dysfunction had decreased tidal volume (P = 0.01) and ventilatory reserve (P < 0.001), as well as increased respiratory frequency at maximal exercise (P = 0.01). Patients with a moderate or high physical activity level had better exercise capacity, which was reflected by a higher work rate (P = 0.009) and oxygen intake (P < 0.001). CONCLUSIONS: There was no significant correlation between radiographic parameters and exercise capacity indicators. When the thoracic curve increased, patients had restrictive ventilatory dysfunction, which led to a tachypneic breathing pattern and reduction of ventilatory reserve during exercise. A physiological change of improved peak oxygen intake was demonstrated in patients with a moderate or high physical activity level.Level of Evidence: 3.

19.
Phytochemistry ; 190: 112846, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34229224

RESUMO

Euphorbiaceae is one of the largest families of higher plants, including 7500 species, and many of them are used as medicines in China. From 2013 to 2019, a total of 455 previously undescribed diterpenoids were isolated from 53 species of Euphorbia, and some skeleton types were first discovered from the genus Euphorbia. Most of the diterpenoids isolated from Euphorbia spp. have been tested for their biological activity, and some of them were first reported for Euphorbia diterpenoids in recent years, such as neuroprotection, antimalarial activity and inhibition of osteoclast formation. In this review, we summarize all the isolated diterpenoids from the genus Euphorbia according to their skeleton types, classify all these diterpenoids into 26 normal classes and 37 novel skeleton types, and summarize their biological activity.


Assuntos
Diterpenos , Euphorbia , China , Diterpenos/farmacologia , Estrutura Molecular
20.
Chem Biol Interact ; 345: 109571, 2021 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-34217688

RESUMO

Soluble epoxide hydrolase (sEH) is a potential drug target to treat inflammation and neurodegenerative diseases. In this study, we found that the extract of Inula britanica exhibited significantly inhibitory effects against sEH, therefore, we investigated its phytochemical constituents to obtain seven new compounds together with sixteen known ones (1-20), including two pairs of novel enantiomers, (2S,3S)-britanicafanin A (1a), (2R,3R)-britanicafanin A (1b), (2R,3S)-britanicafanin B (2a), and (2S,3R)-britanicafanin B (2b), and three new lignans britanicafanins C-E (3-5). Their structures were determined by HRESIMS, 1D and 2D NMR, and electronic circular dichroism (ECD) spectra as well as quantum chemical computations. All the isolates were evaluated for their inhibitory effects against sEH, compounds 1-3, 5-7, 9, 10, 13, 14, and 17-20 showed significant inhibitory effects against sEH with IC50 values from 3.56 µM to 26.93 µM. The inhibition kinetics results indicated that compounds 9, 10, 13, and 19 were all uncompetitive inhibitors, and their inhibition constants (Ki) values were 7.11, 1.99, 4.06, and 8.78 µM, respectively. Their potential interactions were analyzed by molecular docking and molecular dynamics (MD), which suggested that amino acid residues Asp335 and Asn359, especially Gln384, played an important role in the inhibition of compounds 10 and 13 on sEH, and compounds 10 and 13 could be considered as the potential candidates for the development of sEH inhibitors.


Assuntos
Produtos Biológicos/metabolismo , Produtos Biológicos/farmacologia , Epóxido Hidrolases/antagonistas & inibidores , Epóxido Hidrolases/metabolismo , Inula/química , Simulação de Dinâmica Molecular , Inibidores Enzimáticos/metabolismo , Inibidores Enzimáticos/farmacologia , Epóxido Hidrolases/química , Cinética , Simulação de Acoplamento Molecular , Ligação Proteica , Conformação Proteica , Solubilidade
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