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1.
Chem Biol Drug Des ; 103(3): e14506, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38480508

RESUMO

A series of new betulin, lupeol, erythrodiol, and oleanolic acid phosphoryloxy- and furoyloxy-derivatives has been synthesized and their structure was confirmed by NMR spectroscopy. Synthesized compounds were subjected to Ellman's assays to determine their ability to inhibit the enzymes AChE and BChE. Among them, diethoxyphosphoryloxy-oleanolic acid inhibited BChE with a value of 99%, thereby acting as a mixed-type inhibitor holding very low Ki values of Ki = 6.59 nM and Ki ' = 1.97 nM, respectively.


Assuntos
Ácido Oleanólico , Triterpenos , Butirilcolinesterase/química , Inibidores da Colinesterase/farmacologia , Inibidores da Colinesterase/química , Acetilcolinesterase/metabolismo , Ácido Oleanólico/farmacologia , Triterpenos/farmacologia , Triterpenos/química , Relação Estrutura-Atividade
2.
Molecules ; 29(5)2024 Feb 29.
Artigo em Inglês | MEDLINE | ID: mdl-38474596

RESUMO

Euphorbia is a large genus of the Euphorbiaceae family. Around 250 species of the Euphorbia genus have been studied chemically and pharmacologically; different compounds have been isolated from these species, especially diterpenes and triterpenes. Several reports show that several species have anti-inflammatory activity, which can be attributed to the presence of diterpenes, such as abietanes, ingenanes, and lathyranes. In addition, it was found that some diterpenes isolated from different Euphorbia species have anti-cancer activity. In this review, we included compounds isolated from species of the Euphorbia genus with anti-inflammatory or cytotoxic effects published from 2018 to September 2023. The databases used for this review were Science Direct, Scopus, PubMed, Springer, and Google Scholar, using the keywords Euphorbia with anti-inflammatory or cytotoxic activity. In this review, 68 studies were collected and analyzed regarding the anti-inflammatory and anti-cancer activities of 264 compounds obtained from 36 species of the Euphorbia genus. The compounds included in this review are terpenes (95%), of which 68% are diterpenes, especially of the types ingenanes, abietanes, and triterpenes (approximately 15%).


Assuntos
Antineoplásicos , Diterpenos , Euphorbia , Triterpenos , Euphorbia/química , Abietanos , Estrutura Molecular , Diterpenos/química , Triterpenos/química , Anti-Inflamatórios
3.
Molecules ; 29(5)2024 Feb 29.
Artigo em Inglês | MEDLINE | ID: mdl-38474591

RESUMO

A new glucosyl flavone, 5,7,2',5'-tetrahydroxyflavone 7-O-ß-d-glucopyranoside, named loeflingiin, together with apigenin 6-C-glucoside (isovitexin), coumarins citropten and isompinellin, triterpenoids betulin and betulinic acid, and a mixture of phytosterols ß-sitosterol, stigmasterol and campesterol were isolated for the first time from the leaves of wild Plantago loeflingii L. (Plantaginaceae) collected in the Iraqi Kurdistan region. The plant is used by local people to treat wounds and as a vulnerary remedy. The structures of isolated compounds were determined by spectroscopic analysis. The activities of isovitexin and loeflingiinon the viability of breast (MCF7), ovarian (BG-1), endometrial (Ishikawa), and mesothelioma (IST-MES1) human cancer cells and two normal cell lines were determined with an MTT assay. Notably, the new 7-O-glucosyl flavone showed effects higher than cisplatin against the Ishikawa and IST-MESI cell lines. The significant biological activities exhibited by all the compounds isolated from P. loeflingii provided scientific evidence to support the use of the plant in the Kurdish traditional medicine.


Assuntos
Neoplasias , Plantago , Triterpenos , Humanos , Sobrevivência Celular , Plantas , Extratos Vegetais/química , Triterpenos/farmacologia
4.
Cell Mol Biol (Noisy-le-grand) ; 70(2): 128-136, 2024 Feb 29.
Artigo em Inglês | MEDLINE | ID: mdl-38430031

RESUMO

As the main active ingredient of Astragalus, Astragaloside IV (AS-IV) can ameliorate pulmonary fibrosis. In this experiment, we studied how AS-IV reduces idiopathic pulmonary fibrosis (IPF). Bleomycin (BLM) or TGF-ß1 was treated in mice or alveolar epithelial cells to mimic IPF in vivo as well as in vitro. ASV-IV alleviated levels of inflammatory cytokines and fibrosis markers in IPF model. Through detection of autophagy-related genes, ASV-IV was observed to induce autophagy in IPF. Besides, ASV-IV inhibited miR-21 expression in IPF models, and overexpression of miR-21 could reverse the protective potential of ASV-IV on IPF. PTEN was targeted by miR-21 and was up-regulated by ASV-IV in IPF models. In addition, levels of inflammatory cytokines and fibrosis markers, autophagy, as well as the PI3K/AKT/mTOR pathway regulated by ASV-IV could be neutralized after treatment with autophagy inhibitors, miR-21 mimics, or si-PTEN. Our study demonstrates that ASV-IV inhibits IPF through activation of autophagy by miR-21-mediated PTEN/PI3K/AKT/mTOR pathway, suggesting that ASV-IV could be acted to be a promising therapeutic method for IPF.


Assuntos
Fibrose Pulmonar Idiopática , MicroRNAs , Saponinas , Triterpenos , Animais , Camundongos , Autofagia/efeitos dos fármacos , Fibrose , Fibrose Pulmonar Idiopática/tratamento farmacológico , Fibrose Pulmonar Idiopática/genética , Fibrose Pulmonar Idiopática/metabolismo , MicroRNAs/genética , MicroRNAs/metabolismo , Fosfatidilinositol 3-Quinases/efeitos dos fármacos , Fosfatidilinositol 3-Quinases/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Saponinas/farmacologia , Saponinas/uso terapêutico , Transdução de Sinais , Serina-Treonina Quinases TOR/metabolismo , Triterpenos/farmacologia , Triterpenos/uso terapêutico , PTEN Fosfo-Hidrolase/efeitos dos fármacos , PTEN Fosfo-Hidrolase/metabolismo
5.
Mycoses ; 67(3): e13706, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38438313

RESUMO

BACKGROUND: Fluconazole-resistant Candida parapsilosis is a matter of concern. OBJECTIVES: To describe fluconazole-resistant C. parapsilosis genotypes circulating across hospitals in Spain and Rome and to study their azole-resistance profile associated with ERG11p substitutions. PATIENTS/METHODS: We selected fluconazole-resistant C. parapsilosis isolates (n = 528 from 2019 to 2023; MIC ≥8 mg/L according to EUCAST) from patients admitted to 13 hospitals located in five Spanish cities and Rome. Additionally, we tested voriconazole, posaconazole, isavuconazole, amphotericin B, micafungin, anidulafungin and ibrexafungerp susceptibility. RESULTS: Of the 53 genotypes found, 49 harboured the Y132F substitution, five of which were dominating city-specific genotypes involving almost half the isolates. Another genotype involved isolates harbouring the G458S substitution. Finally, we found two genotypes with the wild-type ERG11 gene sequence and one with the R398I substitution. All isolates were fully susceptible/wild-type to amphotericin B, anidulafungin, micafungin and ibrexafungerp. The azole-resistance patterns found were: voriconazole-resistant (74.1%) or voriconazole-intermediate (25.2%), posaconazole-resistant (10%) and isavuconazole non-wild-type (47.5%). Fluconazole-resistant and voriconazole non-wild-type isolates were likely to harbour substitution Y132F if posaconazole was wild type; however, if posaconazole was non-wild type, substitution G458S was indicated if isavuconazole MIC was >0.125 mg/L or substitution Y132F if isavuconazole MIC was ≤0.125 mg/L. CONCLUSIONS: We detected a recent clonal spread of fluconazole-resistant C. parapsilosis across some cities in Spain, mostly driven by dominating city-specific genotypes, which involved a large number of isolates harbouring the Y132F ERG11p substitution. Isolates harbouring substitution Y132F can be suspected because they are non-susceptible to voriconazole and rarely posaconazole-resistant.


Assuntos
Azóis , Fluconazol , Glicosídeos , Nitrilas , Piridinas , Triazóis , Triterpenos , Humanos , Azóis/farmacologia , Fluconazol/farmacologia , Candida parapsilosis/genética , Cidades , Voriconazol/farmacologia , Anfotericina B , Anidulafungina , Micafungina , Itália , Hospitais , Genótipo
6.
Drug Dev Res ; 85(2): e22174, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38494997

RESUMO

Cucurbitacins, natural compounds highly abundant in the Cucurbitaceae plant family, are characterized by their anticancer, anti-inflammatory, and hepatoprotective properties. These compounds have potential as therapeutic agents in the treatment of liver cancer. This study investigated the association of cucurbitacin D, I, and E (CuD, CuI, and CuE) with the caspase cascade, Bcl-2 family, and oxidative stress modulators in the HepG2 cell line. We evaluated the antiproliferative effects of CuD, CuI, and CuE using the MTT assay. We analyzed Annexin V/PI double staining, cell cycle, mitochondrial membrane potential, and wound healing assays at different doses of the three compounds. To examine the modulation of the caspase cascade, we determined the protein and gene expression levels of Bax, Bcl-xL, caspase-3, and caspase-9. We evaluated the total antioxidant status (TAS), total oxidant status (TOS), superoxide dismutase (SOD), glutathione (GSH), Total, and Native Thiol levels to measure cellular redox status. CuD, CuI, and CuE suppressed the proliferation of HepG2 cells in a dose-dependent manner. The cucurbitacins induced apoptosis by increasing caspase-3, caspase-9, and Bax activity, inhibiting Bcl-xL activation, causing loss of ΔΨm, and suppressing cell migration. Furthermore, cucurbitacins modulated oxidative stress by increasing TOS levels and decreasing SOD, GSH, TAS, and total and native Thiol levels. Our findings suggest that CuD, CuI, and CuE exert apoptotic effects on the hepatocellular carcinoma cell line by regulating Bax/Bcl-xL, caspase-3/9 signaling, and causing intracellular ROS increase in HepG2 cells.


Assuntos
Cucurbitacinas , Proteínas Proto-Oncogênicas c-bcl-2 , Triterpenos , Humanos , Células Hep G2 , Proteína X Associada a bcl-2 , Caspase 9/metabolismo , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Caspase 3/metabolismo , Cucurbitacinas/farmacologia , Estresse Oxidativo , Antioxidantes/farmacologia , Glutationa/metabolismo , Superóxido Dismutase/metabolismo , Compostos de Sulfidrila
7.
Chem Biodivers ; 21(3): e202301779, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38426669

RESUMO

Plant-insect interactions are a driving force into ecosystem evolution and community dynamics. Many insect herbivores enter diapause, a developmental arrest stage in anticipation of adverse conditions, to survive and thrive through seasonal changes. Herein, we investigated the roles of medium- to non-polar metabolites during larval development and diapause in a specialist insect herbivore, Chlosyne lacinia, reared on Aldama robusta leaves. Varying metabolites were determined using gas chromatography-mass spectrometry (GC-MS)-based metabolomics. Sesquiterpenes and steroids were the main metabolites putatively identified in A. robusta leaves, whereas C. lacinia caterpillars were characterized by triterpenes, steroids, fatty acids, and long-chain alkanes. We found out that C. lacinia caterpillars biosynthesized most of the identified steroids and fatty acids from plant-derived ingested metabolites, as well as all triterpenes and long-chain alkanes. Steroids, fatty acids, and long-chain alkanes were detected across all C. lacinia instars and in diapausing caterpillars. Sesquiterpenes and triterpenes were also detected across larval development, yet they were not detected in diapausing caterpillars, which suggested that these metabolites were converted to other molecules prior to the diapause stage. Our findings shed light on the chemical content variation across C. lacinia development and diapause, providing insights into the roles of metabolites in plant-insect interactions.


Assuntos
Diapausa , Lepidópteros , Sesquiterpenos , Triterpenos , Animais , Cromatografia Gasosa-Espectrometria de Massas , Ecossistema , Metabolômica/métodos , Esteroides/metabolismo , Sesquiterpenos/metabolismo , Ácidos Graxos/metabolismo , Alcanos , Triterpenos/metabolismo , Larva
8.
Artigo em Inglês | MEDLINE | ID: mdl-38428624

RESUMO

Reduced blood flow (hypoxia) to the brain is thought to be the main cause of strokes because it deprives the brain of oxygen and nutrients. An increasing amount of evidence indicates that the Centella-Asiatica (HA-CA) hydroalcoholic extract has a variety of pharmacological benefits, such as antioxidant activity, neuroprotection, anti-inflammatory qualities, and angiogenesis promotion. Intermittent fasting (IF) has neurological benefits such as anti-inflammatory properties, neuroprotective effects, and the ability to enhance neuroplasticity. The current study evaluates the combined effect of IF (for 1, 6, and 12 days) along with HA-CA (daily up to 12 days) in adult zebrafish subjected to hypoxia every 5 min for 12 days followed by behavioral (novel tank and open-field tank test), biochemical (SOD, GSH-Px, and LPO), inflammatory (IL-10, IL-1ß, and TNF-α), mitochondrial enzyme activities (Complex-I, II, and IV), signaling molecules (AMPK, MAPK, GSK-3ß, Nrf2), and imaging/staining (H&E, TTC, and TEM) analysis. Results show that sub-acute hypoxia promotes the behavioral alterations, and production of radical species and alters the oxidative stress status in brain tissues of zebrafish, along with mitochondrial dysfunction, neuroinflammation, and alteration of signaling molecules. Nevertheless, HA-CA along with IF significantly ameliorates these defects in adult zebrafish as compared to their effects alone. Further, imaging analysis significantly provided evidence of infarct damage along with neuronal and mitochondrial damage which was significantly ameliorated by IF and HA-CA. The use of IF and HA-CA has been proven to enhance the physiological effects of hypoxia in all dimensions.


Assuntos
Centella , AVC Isquêmico , Triterpenos , Animais , Peixe-Zebra/metabolismo , Centella/química , Centella/metabolismo , Jejum Intermitente , Glicogênio Sintase Quinase 3 beta/farmacologia , Antioxidantes/metabolismo , Estresse Oxidativo , Extratos Vegetais/farmacologia , Anti-Inflamatórios/farmacologia , Hipóxia
9.
J Contemp Dent Pract ; 25(2): 118-127, 2024 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-38514408

RESUMO

AIM: This study aims to evaluate the impact of asiaticoside (AC) on the viability and proliferation of dental pulp stem cells (DPSCs), considering the known negative effects of routinely used intracanal medicaments. This evaluation will be compared with the outcomes from using traditional intracanal medicaments, specifically triple antibiotic paste (TAP) and calcium hydroxide [Ca(OH)2]. MATERIALS AND METHODS: The DPSCs were obtained from the third molars of an adult donor. The application of flow cytometry was employed to do a phenotypic analysis on DPSCs using CD90, CD73, CD105, CD34, CD14, and CD45 antibodies. The methylthiazol tetrazolium (MTT) assay was employed to assess cellular viability. The cells were treated with different concentrations of TAP and Ca(OH)2 (5, 2.5, 1, 0.5, and 0.25 mg/mL), along with AC (100, 50, 25, 12.5, and 6.25 µM). A cell proliferation rate was performed at 3, 5, and 7 days. RESULTS: The characterization of DPSCs was conducted by flow cytometry analysis, which verified the presence of mesenchymal cell surface antigen molecules (CD105, CD73, and CD90) and demonstrated the absence of hematopoietic markers (CD34, CD45, and CD14). Cells treated with concentrations over 0.5 mg/mL of TAP and Ca(OH)2 showed a notable reduction in cell viability in comparison to the untreated cells (p < 0.05). Additionally, the cells treated with different concentrations of AC 12.5, 6.25, 25, and 50 µM did not differ significantly from the untreated cells (p > 0.05). Nevertheless, cells treated with concentrations of 100 µM showed a significant reduction in viability compared to the untreated cells (p < 0.05). After a period of 7 days, it was noted that cells exposed to three different concentrations of AC (50, 25, and 12.5 µM) had a notable rise in cell density in comparison to TAP and Ca(OH)2 (p < 0.05). Furthermore, cells that were exposed to a concentration of 12.5 µM exhibited the highest cell density. CONCLUSION: The cellular viability of the AC-treated cells was superior to that of the TAP and Ca(OH)2-treated cells. Moreover, the AC with a concentration of 12.5 µM had the highest degree of proliferation. CLINICAL SIGNIFICANCE: This study underscores the importance of evaluating alternative root canal medicaments and their effects on DPSCs' growth and vitality. The findings on AC, particularly its influence on the survival and proliferation of DPSCs, offer valuable insights for its probable use as an intracanal medication. This research contributes to the ongoing efforts to identify safer and more effective intracanal treatments, which are crucial for enhancing patient outcomes in endodontic procedures. How to cite this article: Alazemi MJ, Badawi MF, Elbeltagy MG, et al. Examining the Effects of Asiaticoside on Dental Pulp Stem Cell Viability and Proliferation: A Promising Approach to Root Canal Treatment. J Contemp Dent Pract 2024;25(2):118-127.


Assuntos
Cavidade Pulpar , Polpa Dentária , Triterpenos , Humanos , Sobrevivência Celular , Antibacterianos/farmacologia , Hidróxido de Cálcio/farmacologia , Proliferação de Células
10.
Chem Biol Drug Des ; 103(3): e14508, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38514749

RESUMO

Pulmonary Fibrosis (PF) is a fatal lung disease with complicated pathogenesis. Astragaloside IV (ASV) has been discovered to alleviate PF progression, and the potential molecular mechanism of ASV in the development of PF need to be further clarified. Bleomycin (BLM) was used to construct PF in vivo model. Expression levels of circ_0008898, miR-211-5p, high mobility group protein B1 (HMGB1), alpha smooth muscle Actin (α-SMA) and Collagen I were examined by Quantitative real time polymerase chain reaction (qRT-PCR) and western blot. Cell survival was analyzed using Cell Counting Kit-8 (CCK-8) and EdU (5-ethynyl-2'-deoxyuridine) assay. The invasion abilities were investigated by transwell assay. The levels of inflammatory factors were tested via using Enzyme-linked immunosorbent assay (ELISA). The relationship between circ_0008898 or HMGB1 and miR-211-5p was identified by dual-luciferase reporter assay. The results showed that ASV attenuated BLM-induced pulmonary fibrosis in vivo. In vitro study, ASV alleviated TGF-ß1-induced fibrogenesis in HFL1 cells. Circ_0008898 was increased in TGF-ß1-induced HFL1 cells. ASV-induced impacts were abrogated by circ_0008898 overexpression in TGF-ß1-induced HFL1 cells. Mechanistically, circ_0008898 competitively bound to miR-211-5p to increase the expression of its target HMGB1. MiR-211-5p deficiency rescued ASV-mediated effects in TGF-ß1-induced HFL1 cells. In addition, HMGB1 overexpression partially overturned circ_0008898 interference-induced impacts in HFL1 cells upon TGF-ß1 treatment. In conclusion, our work manifested that ASV hindered PF process by mediating the circ_0008898/miR-211-5p/HMGB1 network.


Assuntos
Proteína HMGB1 , MicroRNAs , Fibrose Pulmonar , Saponinas , Triterpenos , Humanos , Fibrose Pulmonar/induzido quimicamente , Fibrose Pulmonar/tratamento farmacológico , Fibrose Pulmonar/genética , Fator de Crescimento Transformador beta1/genética , Proteína HMGB1/genética , MicroRNAs/genética , Proliferação de Células
11.
Nan Fang Yi Ke Da Xue Xue Bao ; 44(2): 280-288, 2024 Feb 20.
Artigo em Chinês | MEDLINE | ID: mdl-38501413

RESUMO

OBJECTIVE: To investigate the mechanism underlying the inhibitory effects of Demethylzeylasteral (T-96) on non-small cell lung cancer (NSCLC) cells. METHODS: We first examined the effects of different concentrations (1, 3, 10, and 30 µmol/L) of demethylzeylasteral on morphology and cell number of A549 and H1299 cells. The changes in proliferation, cell viability, migration, invasion, and apoptosis of A549 and H1299 cells following demethylzeylasteral treatment were detected using clone formation, CCK-8, cell scratch, Transwell, and flow cytometric assays, and the effect of SC79 treatment against demethylzeylasteral-induced cell apoptosis was assessed. Western blotting was performed to detect the changes in expressions of E-cadherin, N-cadherin, vimentin, Bax, Bcl-2 and cleaved caspase-3 and phosphorylation of AKT/CREB in demethylzeylasteral-treated A549 and H1299 cells and the cellular expressions of apoptotic proteins following treatment with both demethylzeylasteral and SC79. RESULTS: T-96 treatment caused elongation of the cell body and widening of the intercellular space and significantly inhibited cell viability, proliferation, migration and invasion of A549 and H1299 cells (P < 0.05). Flow cytometry showed that demethylzeylasteral induced apoptosis in both A549 and H1299 cells, whereas SC79 treatment obviously attenuated its pro-apoptotic effect (P < 0.05). Western blotting revealed up-regulated expressions of Bax and cleaved caspase-3 proteins and lowered Bcl-2 expression level in demethylzeylasteral-treated A549 and H1299 cells, but cotreatment with SC79 obviously attenuated the expressions of the apoptotic proteins. T-96 significantly up-regulated the expression level of E-cadherin, down-regulated the expressions of N-cadherin and vimentin, and inhibited the phosphorylation of AKT and CREB in the two cell lines (P < 0.05). CONCLUSION: T-96 inhibits the proliferation, migration and invasion and induces apoptosis of NSCLC cells possibly by inhibiting the AKT/CREB signaling pathway.


Assuntos
Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Triterpenos , Humanos , Carcinoma Pulmonar de Células não Pequenas/metabolismo , Neoplasias Pulmonares/metabolismo , Proteínas Proto-Oncogênicas c-akt/metabolismo , Caspase 3/metabolismo , Vimentina/metabolismo , Proteína X Associada a bcl-2 , Linhagem Celular Tumoral , Células A549 , Proliferação de Células , Transdução de Sinais , Apoptose , Proteínas Proto-Oncogênicas c-bcl-2/metabolismo , Caderinas , Movimento Celular
12.
BMC Oral Health ; 24(1): 352, 2024 Mar 19.
Artigo em Inglês | MEDLINE | ID: mdl-38504287

RESUMO

BACKGROUND: AH Plus, an epoxy resin-based sealer, is widely used in endodontic practice, owing to its good physical properties that confers longstanding dimensional stability and good adhesion to dentin. Nevertheless, its propensity to trigger inflammation, especially in its freshly mixed state, has been extensively documented. Phytochemicals such as Petasin, Pachymic acid, Curcumin, and Shilajit are known for their anti-inflammatory and analgesic effects. This study aimed to analyze and determine the effect of these natural products on the physical properties of AH Plus sealer when incorporated with the sealer. METHODS: AH Plus (AHR) sealer was mixed with 10% petasin, 0.75% pachymic, 0.5% and 6%shilajit to obtain AHP, AHA, AHC and AHS in the ratio of 10:1 and 5:1 respectively. Five samples of each material were assessed for setting time, solubility, flow, and dimensional stability in accordance with the ISO 6876:2012 standardization. Sealers were characterized through scanning electron microscopy (SEM), X-ray energy dispersive spectroscopy, X-ray diffraction (XRD), and Fourier transform infrared (FTIR) spectroscopy. Statistical evaluation involved the Kolmogorov-Smirnov and Shapiro-Wilks tests for normality and the one-way ANOVA test for analysis. RESULTS: In this investigation, the characterisation analysis revealed a relatively similar microstructure in all the experimental root canal sealers. All experimental groups, excluding the control group, exhibited an increase in flow ranging from 11.9 to 31.4% at a 10:1 ratio. Similarly, for the 5:1 ratio, the increase ranged from 12.02 to 31.83%. In terms of dimensional stability, all groups at the 10:1 ratio showed a decrease compared to the control group. The addition of natural agents to AHR in 10:1 ratio led to a reduction in setting time by 8.9-31.6%, and at a 5:1 ratio, the reduction ranged from 8.1 to 31.5%. However, regarding solubility, the addition of natural agents did not induce any significant alterations. CONCLUSION: Based on the results of this study, it can be concluded that all tested root canal sealers exhibited properties that met the acceptable criteria outlined in the ISO 6876:2012 standardization.


Assuntos
Curcumina , Minerais , Resinas Vegetais , Materiais Restauradores do Canal Radicular , Sesquiterpenos , Triterpenos , Humanos , Materiais Restauradores do Canal Radicular/química , Curcumina/farmacologia , Resinas Epóxi , Teste de Materiais , Silicatos/química , Compostos de Cálcio/química
13.
Se Pu ; 42(3): 234-244, 2024 Mar 08.
Artigo em Chinês | MEDLINE | ID: mdl-38503700

RESUMO

Ziziphi Spinosae Semen refers to the dried seed of Ziziphus jujuba Mill. var. spinosa (Bunge) Hu ex H. F. Chou. The seed is composed of a reddish brown coat and a yellow kernel. A comparative study was conducted to investigate differences in the chemical composition and their relative contents between the seed coat and kernel of Ziziphi Spinosae Semen. First, the chemical compounds found in the seed coat and kernel were characterized and identified using ultra performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS). The analytical results tentatively identified 57 chemical compounds based on reference-compound comparison, literature retrieval, and chemical-database (e. g., MassBank) searches; these compounds included 14 triterpenes, 23 flavonoids, 7 alkaloids, 6 carboxylic acids, and 7 other types of compounds. The mass error of the identified compounds was within the mass deviation range of 5×10-6 (5 ppm). Next, two methods of multivariate statistical analysis, namely, principal component analysis (PCA) and orthogonal partial least squares-discriminant analysis (OPLS-DA), were used to compare the differential compounds between the two seed parts. A total of 17 differential compounds were screened out via OPLS-DA based on a variable importance in projection (VIP) value of >5. The results revealed that betulinic acid, betulonic acid, alphitolic acid, and jujuboside Ⅰ mainly existed in the seed coat whereas the 13 other compounds, such as spinosin, jujuboside A, and 6‴-feruloylspinosin, mainly existed in the seed kernel. Therefore, these 17 differential compounds can be used to distinguish between the two seed parts. Finally, a semiquantitative method was established using UPLC and a charged aerosol detector (CAD) with inverse gradient compensation in the mobile phase. Six representative compounds with different types were selected to examine the CAD response consistency: magnoflorine (alkaloid), spinosin (flavone), 6‴-feruloylspinosin (flavone), jujuboside A (triterpenoid saponin), jujuboside B (triterpenoid saponin), and betulinic acid (triterpenoid acid). The results showed that the relative standard deviation (RSD) of the average response factors at different levels of these six compounds was 7.04% and that their response intensities were similar. Moreover, each compound in the fingerprint demonstrated good response consistency, and the peak areas obtained directly reflected the contents of each compound. Based on the semiquantitative fingerprints obtained, betulinic acid and oleic acid were considered the main components of the seed coat. The betulinic acid content in the seed coat was approximately 7 times higher than that in the seed kernel. Spinosin, jujuboside A, linoleic acid, betulinic acid, and oleic acid were the main components of the seed kernel. The spinosin content in the seed kernel was 18 times higher than that in the seed coat. In addition, the jujuboside A content in the seed kernel was 24 times higher than that in the seed coat. The proposed method can accurately determine the main components and compare the relative contents of these components in different seed parts. In summary, this study identified the differences in chemical components between the seed coat and kernel of Ziziphi Spinosae Semen and clarified the main components and their relative contents in these parts. The findings can not only provide a basis for the identification of chemical compounds and quality research on different parts of Ziziphi Spinosae Semen but also promote the development and utilization of this traditional Chinese medicine.


Assuntos
Alcaloides , Medicamentos de Ervas Chinesas , Flavonas , Saponinas , Triterpenos , Ziziphus , Medicamentos de Ervas Chinesas/química , Ácido Betulínico , Saponinas/química , Ácidos Oleicos , Cromatografia Líquida de Alta Pressão , Ziziphus/química , Sementes
14.
Artigo em Inglês | MEDLINE | ID: mdl-38442634

RESUMO

In this work, a high-speed shear extraction off-line coupling high-speed countercurrent chromatography method was developed to separate maslinic acid and oleanolic acid from olive pomace. To improve extraction efficiency, the polar disparity between maslinic acid and oleanolic acid necessitated the concurrent utilization of both polar and non-polar solvents during high-speed shear extraction. Then, the high-speed shear extraction was directly feed to high-speed countercurrent chromatography for subsequently separation. A total of 250 min were needed to complete the extraction and separation process. This yielded two molecules from 3.3 g of defatted olive pomace: 7.2 mg of 93.8 % pure maslinic acid and 2.3 mg of 90.1 % pure oleanolic acid, both determined by HPLC at 210 nm. Furthermore, the compounds exhibited inhibitory activity against Escherichia coli and Staphylococcus aureus. At a concentration of 100 µg/mL, its efficacy in inhibiting hyaluronidase was comparable to that of the standard drug indomethacin. Compared with the conventional separation method, this coupled technique reduced the whole time due to the direct injection of sample extraction solution. This technique provides a useful approach for the separation of natural products with significant polarity differences.


Assuntos
Olea , Ácido Oleanólico , Ácido Oleanólico/análogos & derivados , Triterpenos , Ácido Oleanólico/análise , Olea/química , Distribuição Contracorrente , Antibacterianos/farmacologia , Triterpenos/química , Cromatografia Líquida de Alta Pressão , Extratos Vegetais/farmacologia , Extratos Vegetais/análise
15.
CNS Neurosci Ther ; 30(3): e14642, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-38430464

RESUMO

BACKGROUND: Inhibiting secondary inflammatory damage caused by glial cells and creating a stable microenvironment is one of the main strategies to investigate drugs for the treatment of spinal cord injury. Acetyl-11-keto-beta-boswellic acid (AKBA) is the active component of the natural drug boswellia, which has anti-inflammatory and antioxidant effects and offers a possible therapeutic option for spinal cord injury. METHODS: In this study, a spinal cord injury model was established by crushing spinal cord, respectively, to detect the M1 macrophage inflammatory markers: iNOS, TNF-α, IL-1ß, and the M2 macrophage markers CD206, ARG-1, IL-10, and the detection of antioxidant enzymes and MDA. In vitro, macrophages were cultured to verify the main mechanism of the macrophage switch from Nrf2/HO-1 to M2 type by flow cytometry, immunofluorescence, and other techniques. Macrophage and Schwann cell co-culture validated the migration mechanism of Schwann cells promoted by AKBA. RESULTS: AKBA significantly enhanced the antioxidant enzyme activities of CAT, GSH-Px, T-AOC, and SOD, reduced MDA content, and reduced oxidative damage caused by spinal cord injury via the Nrf2/HO-1 signaling pathway; AKBA mediates Nrf2/HO-1/IL-10, converts macrophages from M1 to M2 type, reduces inflammation, and promotes Schwann cell migration, thereby accelerating the repair of spinal cord injury in rats. CONCLUSIONS: Our work demonstrates that AKBA can attenuate oxidative stress as well as the secondary inflammatory injury caused by macrophages after SCI, promote Schwann cell migration to the injury site, and thus accelerate the repair of the injured spinal cord.


Assuntos
Interleucina-10 , Traumatismos da Medula Espinal , Triterpenos , Ratos , Animais , Interleucina-10/metabolismo , Antioxidantes/farmacologia , Fator 2 Relacionado a NF-E2/metabolismo , Traumatismos da Medula Espinal/metabolismo , Macrófagos/metabolismo , Medula Espinal/metabolismo , Movimento Celular
16.
BMC Plant Biol ; 24(1): 170, 2024 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-38443797

RESUMO

BACKGROUND: Panax notoginseng (Burk) F. H. Chen is one of the most famous Chinese traditional medicinal plants. The taproot is the main organ producing triterpenoid saponins, and its development is directly linked to the quality and yield of the harvested P. notoginseng. However, the mechanisms underlying the dynamic metabolic changes occurring during taproot development of P. notoginseng are unknown. RESULTS: We carried out metabolomic and transcriptomic analyses to investigate metabolites and gene expression during the development of P. notoginseng taproots. The differentially accumulated metabolites included amino acids and derivatives, nucleotides and derivatives, and lipids in 1-year-old taproots, flavonoids and terpenoids in 2- and 3-year-old taproots, and phenolic acids in 3-year-old taproots. The differentially expressed genes (DEGs) are related to phenylpropanoid biosynthesis, metabolic pathway and biosynthesis of secondary metabolites at all three developmental stages. Integrative analysis revealed that the phenylpropanoid biosynthesis pathway was involved in not only the development of but also metabolic changes in P. notoginseng taproots. Moreover, significant accumulation of triterpenoid saponins in 2- and 3-year-old taproots was highly correlated with the up-regulated expression of cytochrome P450s and uridine diphosphate-dependent glycosyltransferases genes. Additionally, a gene encoding RNase-like major storage protein was identified to play a dual role in the development of P. notoginseng taproots and their triterpenoid saponins synthesis. CONCLUSIONS: These results elucidate the molecular mechanism underlying the accumulation of and change relationship between primary and secondary metabolites in P. notoginseng taproots, and provide a basis for the quality control and genetic improvement of P. notoginseng.


Assuntos
Panax notoginseng , Saponinas , Triterpenos , Panax notoginseng/genética , Metaboloma , Perfilação da Expressão Gênica
17.
Physiol Plant ; 176(2): e14260, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38511471

RESUMO

Bacosides are dammarane-type triterpenoidal saponins in Bacopa monnieri and have various pharmacological applications. All the bacosides are diversified from two isomers, i.e., jujubogenin and pseudojujubogenin. The biosynthetic pathway of bacoside is not well elucidated. In the present study, we characterized a UDP-glycosyltransferase, UGT79A18, involved in the glycosylation of pseudojujubogenin. UGT79A18 shows higher expression in response to 5 h of wounding, and 3 h of MeJA treatment. The recombinant UGT79A18 shows in vitro activity against a wide range of flavonoids and triterpenes and has a substrate preference for protopanaxadiol, a dammarane-type triterpene. Secondary metabolite analysis of overexpression and knockdown lines of UGT79A18 in B. monnieri identify bacopasaponin D, bacopaside II, bacopaside N2 and pseudojujubogenin glucosyl rhamnoside as the major bacosides that were differentially accumulated. In the overexpression lines of UGT79A18, we found 1.7-fold enhanced bacopaside II, 8-fold enhanced bacopasaponin D, 3-fold enhanced pseudojujubogenin glucosyl rhamnoside, and 1.6-fold enhanced bacopaside N2 content in comparison with vector control plant, whereas in the knockdown lines of UGT79A18, we found 1.4-fold reduction in bacopaside II content, 3-fold reduction in the bacopasaponin D content, 2-fold reduction in the pseudojujubogenin glucosyl rhamnoside content, and 1.5-fold reduction in bacopaside N2 content in comparison with vector control. These results suggest that UGT79A18 is a significant UDP glycosyltransferase involved in glycosylating pseudojujubogenin and enhancing the pseudojujubogenin-derived bacosides.


Assuntos
Acetatos , Bacopa , Ciclopentanos , Oxilipinas , Saponinas , Triterpenos , Bacopa/genética , Bacopa/química , Glicosiltransferases/genética , Vias Biossintéticas , Triterpenos/química , Triterpenos/farmacologia , Triterpenos/uso terapêutico , Difosfato de Uridina , Extratos Vegetais/química
18.
Appl Microbiol Biotechnol ; 108(1): 195, 2024 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-38324205

RESUMO

Pentacyclic triterpenoids exhibit a wide range of biological activities which have wide applications in the food, cosmetics, and pharmaceutical industries. High-performance chassis strains have been developed for the production of various pentacyclic triterpenoids, e.g., lupane-type and oleanane-type triterpenoids. The production of common pentacyclic triterpenes and their derivatives is limited by the poor activity of typical pentacyclic triterpene synthases (PTSs). However, a general strategy applicable to typical PTSs is still lacking. As typical pentacyclic triterpenes are derived from the baccharenyl cation, engineering the non-active-site residues in the MXXXXR motif might be beneficial for the catalytic efficiencies of typical PTSs by the stabilization of the baccharenyl cation. Here, we develop a general strategy for improving the activity of typical PTSs. As a proof of concept, the activity of three PTSs such as lupeol synthase, ß-amyrin synthase, and α-amyrin synthases was significantly increased up to 7.3-fold by site-directed saturation mutagenesis. This strategy could be applied to improve the activity of various typical PTSs. KEY POINTS: • The strategy could be applied to typical PTSs for improving the activity. • The catalytic activity of typical PTSs was significantly increased.


Assuntos
Triterpenos , Aminoácidos , Triterpenos Pentacíclicos , Catálise , Cátions
19.
BMC Complement Med Ther ; 24(1): 79, 2024 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-38326823

RESUMO

BACKGROUND: Chemotherapies target the PfEMP-1 and PfPKG proteins in Plasmodium falciparum, the parasite that causes malaria, in an effort to prevent the disease's high fatality rate. This work identified the phytochemical components of Nauclea latifolia roots and docked the chemical compounds against target proteins, and examined the in vivo antiplasmodial effect of the roots on Plasmodium berghei-infected mice. METHODS: Standard protocols were followed for the collection of the plant's roots, cleaning, and drying of the roots, extraction and fraction preparation, assessment of the in vivo antiplasmodial activity, retrieval of the PfEMP-1 and PfPKG proteins, GCMS, ADME, and docking studies, chromatographic techniques were employed to separate the residual fraction's components, and the Swis-ADME program made it possible to estimate the drug's likeness and pharmacokinetic properties. The Auto Dock Vina 4.2 tool was utilized for molecular docking analysis. RESULTS: The residual fraction showed the best therapeutic response when compared favorably to amodiaquine (80.5%) and artesunate (85.1%). It also considerably reduced the number of parasites, with the % growth inhibition of the parasite at 42.8% (D2) and 83.4% (D5). Following purification, 25 compounds were isolated and characterized with GCMS. Based on their low molecular weights, non-permeation of the blood-brain barrier, non-inhibition of metabolizing enzymes, and non-violation of Lipinski's criteria, betulinic and ursolic acids were superior to chloroquine as the best phytochemicals. Hence, they are lead compounds. CONCLUSION: In addition to identifying the bioactive compounds, ADME, and docking data of the lead compounds as candidates for rational drug design processes as observed against Plasmodium falciparum target proteins (PfEMP-1 and PfPKG), which are implicated in the pathogenesis of malaria, the study has validated that the residual fraction of N. latifolia roots has the best antiplasmodial therapeutic index.


Assuntos
Antimaláricos , Malária , Rubiaceae , Triterpenos , Camundongos , Animais , Antimaláricos/química , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Malária/tratamento farmacológico , Malária/parasitologia , Triterpenos/farmacologia , Plasmodium falciparum , Rubiaceae/química
20.
Eur J Med Res ; 29(1): 106, 2024 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-38326876

RESUMO

Scientists have been compelled to search for alternative treatments due to the increasing prevalence of chemoresistance as well as the agonising and distressing side effects of both chemotherapy and radiation. Plant extracts have been exploited to treat various medical conditions for ages. Considering this fact, the main focus of various recent studies that are being conducted to find new and potent anticancer drugs involves the identification and utilisation of potential therapeutic chemicals present in plant extracts. Koetjapic acid (KJA), which belongs to the family of triterpenes, is primarily isolated from Sandoricum koetjape. Ongoing investigations into its therapeutic applications have revealed its tendency to impede the growth and proliferation of cancer cells. Koetjapic acid activates the intrinsic apoptotic pathway and promotes the death of cancer cells. Moreover, it inhibits angiogenesis and the dissemination of tumour (metastasis) by targeting the VEGF signalling cascade. Therefore, this study aims to elucidate the underlying mechanism of anticancer activity of koetjapic acid, providing significant insight into the compound's potential as an anticancer agent.


Assuntos
Antineoplásicos , Triterpenos , Humanos , Triterpenos/farmacologia , Triterpenos/uso terapêutico , Triterpenos/química , Apoptose , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Extratos Vegetais/farmacologia
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