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1.
Anal Chim Acta ; 1239: 340661, 2023 Jan 25.
Artigo em Inglês | MEDLINE | ID: mdl-36628701

RESUMO

A column prepared using a unique three-membered phenanthrene skeleton of rosin has complementary selectivity to a C18 column for some separation tasks. In this study, propylene pimaric acid (16-hydroxyethyl acrylate-34-n-butyl) ester (BRB) and propylene pimaric acid (16-hydroxyethyl acrylate-34-dodecyl) ester (BRLA) were used as functional ligands to prepare two novel stationary phases, namely BRB@SiO2 and BRLA@SiO2, through a "thiol-ene" click chemistry reaction. The characterization results of Fourier transform infrared spectroscopy, thermogravimetric analysis, nitrogen adsorption-desorption measurements, and contact angle tests showed that the BRB@SiO2 and BRLA@SiO2 stationary phases were successfully prepared. In addition, the performance of the columns was evaluated using the Tanaka test and hydrophobic subtraction model, which showed that the stationary phases exhibited typical reversed-phase chromatography performance and good hydrophobicity, hydrophobic selectivity, and steric selectivity. The changes in the retention of Panax notoginseng saponins on a column under different chromatographic conditions (acetonitrile content, flow rate, and column temperature) were investigated. The separation effect of BRB@SiO2 and BRLA@SiO2 columns on P. notoginseng saponins was better than that of the C18 column and the BRLA@SiO2 column could replace the C18 column for the detection of P. notoginseng saponins.


Assuntos
Panax notoginseng , Saponinas , Dióxido de Silício/química , Panax notoginseng/química , Ésteres , Interações Hidrofóbicas e Hidrofílicas
2.
J Ethnopharmacol ; 305: 116128, 2023 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-36623754

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Myocardial fibrosis (MF) is a common pathological manifestation of many cardiovascular diseases at a certain stage, with excessive accumulation of collagen fibers, excessive increase in collagen content, and a significant increase in collagen volume as the main pathological changes. There are currently no effective drugs for the treatment of myocardial fibrosis. Traditional Chinese medicine (TCM), the main component of the medical practice used for more than 5000 years, especially in China, often exerts a wider action spectrum than previously attempted options in treating human diseases. In recent times, the great potential of TCM in the treatment of MF has received much attention. Especially many experimental studies on the treatment of MF by Astragalus mongholicus Bunge have been conducted, and the effect is remarkable, which may provide more comprehensive database and theoretical support for the application of Astragalus mongholicus Bunge in the treatment of MF and could be considered a promising candidate drug for preventing MF. AIM OF THE REVIEW: This review summarizes the chemical components of Astragalus mongholicus Bunge, Astragalus mongholicus Bunge extract, Astragalus mongholicus Bunge single prescription, and Astragalus mongholicus Bunge compound preparation in the treatment of MF, and provides comprehensive information and a reliable basis for the exploration of new treatment strategies of botanical drugs in the therapy of MF. METHODS: The literature information was obtained from the scientific databases on ethnobotany and ethnomedicines (up to August 2022), mainly from the PubMed, Web of Science, and CNKI databases. The experimental studies on the anti-myocardial fibrosis role of the effective active components of Astragalus mongholicus Bunge and the utility of its compound preparation and the involved mechanisms were identified. The search keywords for such work included: "myocardial fibrosis" or "Cardiac fibrosis ", and "Astragalus mongholicus Bunge", "extract," or "herb". RESULTS: Several studies have shown that the effective active components of Astragalus mongholicus Bunge and its formulas, particularly Astragaloside IV, Astragalus polysaccharide, total saponins of Astragalus mongholicus Bunge, triterpenoid saponins of Astragalus mongholicus Bunge, and cycloastragenol, exhibit potential benefits against MF, the mechanisms of which appear to involve the regulation of inflammation, oxidant stress, and pro-fibrotic signaling pathways, etc. Conclusion: These research works have shown the therapeutic benefits of Astragalus mongholicus Bunge in the treatment of MF. However, further research should be undertaken to clarify the unconfirmed chemical composition and regulatory mechanisms, conduct standard clinical trials, and evaluate the possible side effects. The insights in the present review provided rich ideas for developing new anti-MF drugs. THESIS: Myocardial fibrosis (MF) with excessive accumulation of collagen fibers, excessive increase in collagen content, and a significant increase in collagen volume as the main pathological changes is a common pathological manifestation of many cardiovascular diseases at a certain stage, which seriously affects cardiac function. At present, there is still a lack of effective drugs for the treatment of MF. Traditional Chinese medicine (TCM), the main component of the medical practice used for more than 5000 years especially in China, often exerts wider action spectrum than previously attempted options in treating human diseases. In recent times, the great potential of TCM in the treatment of MF has received much attention. Especially many experimental studies on the treatment of MF by Astragalus mongholicus Bunge have been conducted, and the effect is remarkable, which may provide more comprehensive data base and theoretical support for the application of Astragalus mongholicus Bunge in the treatment of MF and could be considered a promising candidate drug for preventing MF.


Assuntos
Doenças Cardiovasculares , Medicamentos de Ervas Chinesas , Saponinas , Humanos , Astragalus propinquus/química , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Medicamentos de Ervas Chinesas/química , Doenças Cardiovasculares/tratamento farmacológico , Fibrose , Saponinas/química
3.
Int J Mol Sci ; 24(2)2023 Jan 16.
Artigo em Inglês | MEDLINE | ID: mdl-36675303

RESUMO

Stroke, one of the leading causes of disability and death worldwide, is a severe neurological disease that threatens human life. Protopanaxatriol (PPT), panaxatriol-type saponin aglycone, is a rare saponin that exists in Panax ginseng and Panax Noto-ginseng. In this study, we established an oxygen-glucose deprivation (OGD)-PC12 cell model and middle cerebral artery occlusion/reperfusion (MCAO/R) model to evaluate the neuroprotective effects of PPT in vitro and in vivo. In addition, metabolomics analysis was performed on rat plasma and brain tissue samples to find relevant biomarkers and metabolic pathways. The results showed that PPT could significantly regulate the levels of LDH, MDA, SOD, TNF-α and IL-6 factors in OGD-PC12 cells in vitro. PPT can reduce the neurological deficit score and infarct volume of brain tissue in rats, restore the integrity of the blood-brain barrier, reduce pathological damage, and regulate TNF-α, IL-1ß, IL-6, MDA, and SOD factors. In addition, the results of metabolomics found that PPT can regulate 19 biomarkers involving five metabolic pathways, including amino acid metabolism, arachidonic acid metabolism, sphingolipid metabolism, and glycerophospholipid metabolism. Thus, it could be inferred that PPT might serve as a novel natural agent for MCAO/R treatment.


Assuntos
Isquemia Encefálica , Fármacos Neuroprotetores , Traumatismo por Reperfusão , Saponinas , Ratos , Humanos , Animais , Isquemia Encefálica/metabolismo , Fármacos Neuroprotetores/farmacologia , Fármacos Neuroprotetores/uso terapêutico , Fator de Necrose Tumoral alfa , Interleucina-6 , Infarto da Artéria Cerebral Média/patologia , Glucose , Traumatismo por Reperfusão/metabolismo , Saponinas/farmacologia , Saponinas/uso terapêutico , Superóxido Dismutase
4.
BMC Complement Med Ther ; 23(1): 13, 2023 Jan 18.
Artigo em Inglês | MEDLINE | ID: mdl-36653797

RESUMO

BACKGROUND: Metabolic hypertension (MH) has become the most common type of hypertension in recent years due to unhealthy eating habits and lifestyles of people, such as over-eating alcohol, high fat, and sugar diets (ACHFSDs). Therefore, effective means to combat MH are needed. Previous studies have shown that Panax notoginseng (Burkill) F. H. Chen flower saponins (PNFS) can lower blood pressure in spontaneously hypertensive rats (SHR). However, whether it acts on MH and its mechanism of action remain unclear.  METHODS: The pharmacodynamic effects of PNFS were evaluated in rats with ACHFSDs-induced MH. The blood pressure, blood biochemical, grip strength, face temperature, vertigo time, and liver index were estimated. The histological changes in the liver and aorta were observed using hematoxylin and eosin staining. The levels of ET-1, TXB2, NO, PGI2, Renin, ACE, Ang II, and ALD in plasma were detected using ELISA. The levels of C3, KLF5, LXRα, and Renin in kidney tissues were measured using qRT-PCR.The expression levels of C3, KLF5, LXRα, and Renin in kidney tissues were examined using Western blotting. RESULTS: In the present study, PNFS was found to reduce blood pressure, face temperature, and vertigo time, increase grip strength and improve dyslipidemia in rats with MH. In addition, PNFS decreased the plasma levels of ET-1 and TXB2, elevated the levels of NO and PGI2, and improved pathological aortic injury. Meanwhile, PNFS decreased the plasma levels of Renin, ACE, Ang II, and ALD. QRT-PCR and Western bolt showed that PNFS downregulated C3, KLF5, LXRα, and Renin protein and mRNA expression in the kidneys of rats with MH. CONCLUSION: The finding of the present study suggested that PNFS could downregulate C3 and KLF-5 expression in rats with MH, thereby inhibiting the overactivation of the renin-angiotensin-aldosterone system, while improving vascular endothelial function and ultimately reducing blood pressure in rats with MH.


Assuntos
Hipertensão , Panax notoginseng , Saponinas , Ratos , Animais , Sistema Renina-Angiotensina , Renina/genética , Renina/metabolismo , Renina/farmacologia , Complemento C3/genética , Complemento C3/metabolismo , Complemento C3/farmacologia , Saponinas/farmacologia , Hipertensão/tratamento farmacológico , Hipertensão/metabolismo , Ratos Endogâmicos SHR , Flores/química , Vertigem
5.
Phytomedicine ; 109: 154580, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36610132

RESUMO

BACKGROUND: Flavonoids and saponins are important bioactive compounds that have attracted wide research interests. This review aims to summarise the state of the art of the pharmacology, toxicology and clinical efficacy of these compounds. METHODS: Data were retrieved from PubMed, Cochrane Library, Web of Science, Proquest, CNKI, Chongqing VIP, Wanfang, NPASS and HIT 2.0 databases. Meta-analysis and systematic reviews were evaluated following the PRISMA guideline. Statistical analyses were conducted using SPSS23.0. RESULTS: Rising research trends on flavonoids and saponins were observed since the 1990s and the 2000s, respectively. Studies on pharmacological targets and activities of flavonoids and saponins represent an important area of research advances over the past decade, and these important resources have been documented in open-access specialised databases and can be retrieved with ease. The rising research on flavonoids and saponins can be attributed, at least in part, to their links with some highly investigated fields of research, e.g., oxidative stress, inflammation and cancer; i.e., 6.88% and 3.03% of publications on oxidative stress cited by PubMed in 1990 - 2021 involved flavonoids and saponins, respectively, significantly higher than the percentage involving alkaloids (1.88%). The effects of flavonoids concern chronic venous insufficiency, cervical lesions, diabetes, rhinitis, dermatopathy, prostatitis, menopausal symptoms, angina pectoris, male pattern hair loss, lymphocytic leukaemia, gastrointestinal diseases and traumatic cerebral infarction, etc, while those of saponins may have impact on venous oedema in chronic deep vein incompetence, erectile dysfunction, acute impact injuries and systemic lupus erythematosus, etc. The volume of in vitro research appears way higher than in vivo and clinical studies, with only 10 meta-analyses and systematic reviews (involving 290 interventional and observational studies), and 36 clinical studies on flavonoids and saponins. Data are sorely needed on pharmacokinetics, in vitro pan-assay interferences, purity of tested compounds, interactions in complex herbal extracts, real impact of anti-oxidative strategies, and mid- and long-term toxicities. To fill these important gaps, further investigations are warranted. On the other hand, drug interactions may cause adverse effects but might also be useful for synergism, with the goals of enhancing effects or of detoxifying. Furthermore, the interactions between phytochemicals and the intestinal microbiota are worth investigating as the field may present a promising potential for novel drug development.


Assuntos
Medicamentos de Ervas Chinesas , Saponinas , Humanos , Masculino , Medicamentos de Ervas Chinesas/farmacologia , Etnofarmacologia , Flavonoides/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Saponinas/farmacologia , Metanálise como Assunto , Revisões Sistemáticas como Assunto
6.
J Adv Res ; 43: 247-257, 2023 01.
Artigo em Inglês | MEDLINE | ID: mdl-36585112

RESUMO

INTRODUCTION: Triterpenoids and saponins have a broad range of pharmacological activities. Unlike most legumes which contain mainly oleanane-type scaffold, Astragalus membranaceus contains not only oleanane-type but also cycloartane-type saponins, for which the biosynthetic pathways are unknown. OBJECTIVES: This work aims to study the function and catalytic mechanism of oxidosqualene cyclases (OSCs), one of the most important enzymes in triterpenoid biosynthesis, in A. membranaceus. METHODS: Two OSC genes, AmOSC2 and AmOSC3, were cloned from A. membranaceus. Their functions were studied by heterologous expression in tobacco and yeast, together with in vivo transient expression and virus-induced gene silencing. Site-directed mutagenesis and molecular docking were used to explain the catalytic mechanism for the conserved motif. RESULTS: AmOSC2 is a ß-amyrin synthase which showed higher expression levels in underground parts. It is associated with the production of ß-amyrin and soyasaponins (oleanane-type) in vivo. AmOSC3 is a cycloartenol synthase expressed in both aerial and underground parts. It is related to the synthesis of astragalosides (cycloartane-type) in the roots, and to the synthesis of cycloartenol as a plant sterol precursor. From AmOSC2/3, conserved triad motifs VFM/VFN were discovered for ß-amyrin/cycloartenol synthases, respectively. The motif is a critical determinant of yield as proved by 10 variants from different OSCs, where the variant containing the conserved motif increased the yield by up to 12.8-fold. Molecular docking and mutagenesis revealed that Val, Phe and Met residues acted together to stabilize the substrate, and the cation-π interactions from Phe played the major role. CONCLUSION: The study provides insights into the biogenic origin of oleanane-type and cycloartane-type triterpenoids in Astragalus membranaceus. The conserved motif offers new opportunities for OSC engineering.


Assuntos
Saponinas , Triterpenos , Astragalus propinquus/metabolismo , Simulação de Acoplamento Molecular , Triterpenos/metabolismo
7.
J Agric Food Chem ; 71(1): 469-479, 2023 Jan 11.
Artigo em Inglês | MEDLINE | ID: mdl-36576094

RESUMO

Panax notoginseng saponins (PNS) are the most important bioactive components of P. Notoginseng. In this paper, an evaluation of the pharmacokinetics and oral absolute bioavailability of PNS was carried out following intravenous and oral administration of PNS to Sprague-Dawley rats. The plasma concentration of 28 PNS was determined using a validated UPLC-MS/MS system. The results demonstrated that Rb1(32.8%), Rg1(41.4%), R1(9.4%), Re(4.5%), and Rd(3.5%) are the five main ingredients of PNS for administration. After oral administration, it was found that the area under the curve (AUC0-72 h) for these five major saponins was significantly different. AUC0-72 h of Rb1 and Rd accounted for about 60% of all PNS exposure, while AUC0-72 h of Rg1 and R1 only accounted for 0.7%, and Re was undetectable in plasma. Also, PPD, PPT, and CK were detected as the major PNS metabolites in vivo. Furthermore, it was shown that the total oral bioavailability of PNS was only 1.2%.


Assuntos
Panax notoginseng , Saponinas , Ratos , Animais , Ratos Sprague-Dawley , Disponibilidade Biológica , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia Líquida , Espectrometria de Massas em Tandem/métodos
8.
J Pharm Biomed Anal ; 225: 115202, 2023 Feb 20.
Artigo em Inglês | MEDLINE | ID: mdl-36586383

RESUMO

Bupleurum scorzonerifolium (BS) is one of the sources of Bupleuri Radix, which was first recorded in Shennong's classic of materia medica. It has a medicinal history of 2000 years and is now widely used for the treatment of depression clinically. However, the material basis of antidepressant effects is unclear, and the quality evaluation method is lacking. The paper aims to investigate the antidepressant quality markers (Q-markers) of BS by electrospray ionization quadrupole time-of-flight tandem mass spectrometry (UPLC-ESI-Q-TOF-MS). Firstly, the rat depression model was established by using chronic unpredictable mild stress (CUMS) combined with the solitary confinement method to evaluate the pharmacodynamics of BS. After verification of the antidepressant effect of BS, UPLC-ESI-Q-TOF-MS was used to analyze BS and the blood components of BS. A total of 34 components were identified in BS, in which 8 components, including saikosaponin a (SSa), saikosaponin c (SSc), saikosaponin d (SSd), saikosaponin b1 (SSb1), saikosaponin b2 (SSb2), glycyrrhetinic acid, nootkatone and valerenic acid, were detected in serum. SSa, SSc, SSd, SSb1 and SSb2 were found as metabolites, and glycyrrhetinic acid, nootkatone and valerenic Acid were identified as the prototypes in the blood. The depression model of zebrafish was established with reserpine to verify the antidepressant effect of the potential eight active components. The results showed that all these components could markedly improve the depressive behavior of zebrafish, increase the content of 5-HT and reduce the cortisol content. Finally, according to the principles of effectiveness, accessibility and measurability for Q-markers, SSa, SSc, and SSd were confirmed as Q-markers of BS, and the contents of 3 Q-markers in 10 batches of BS from different origins were determined to be 0.0728-1.465%. In addition, the total contents of 3 Q-markers in BS produced in Lindian, Heilongjiang Province, were higher than those in other origins. This paper provided a reliable method for the quality evaluation of BS for depression treatment.


Assuntos
Bupleurum , Medicamentos de Ervas Chinesas , Ácido Glicirretínico , Saponinas , Ratos , Animais , Medicamentos de Ervas Chinesas/química , Bupleurum/química , Peixe-Zebra , Saponinas/química , Controle de Qualidade , Antidepressivos , Ácido Glicirretínico/análise , Cromatografia Líquida de Alta Pressão/métodos
9.
J Ethnopharmacol ; 305: 116074, 2023 Apr 06.
Artigo em Inglês | MEDLINE | ID: mdl-36577490

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Astragali Radix (AR) is the dried root of Astragalus membranaceus (Fisch.) Bge. var. mongholicus (Bge.) Hsiao or A. membranaceus (Fisch.) Bge. AR was the main medicine in a Chinese traditional prescription called Fangji Huangqi Decoction, and it has been used to treating nephrotic syndrome (NS) for thousands of years in China. In recent years, AR has been evidenced to have anti-inflammatory activity, antihyperglycemic activity, antioxidant activity, etc. There are two mainstream commodities for ARs in the market including the imitation wild AR and transplanted AR. However, it is not clear whether the imitation wild AR or transplanted AR and which kind of component, astragalus saponin, astragalus flavonoid or astragalus polysaccharide, makes a bigger contribution in treating NS. And the exact molecular mechanism is not fully understood. AIM OF THE STUDY: To explore which kind of AR and which kind of component in AR makes the bigger contribution in treating NS, and exploring the molecular mechanism. MATERIALS AND METHODS: Firstly, HPLC-UV/ELSD was used for quantitative determination of the constituents in different ARs. Secondly, the efficacy of different ARs treating doxorubicin-induced nephropathy (DN) was compared by metabolomics. Thirdly, the protective effects of different constituents from ARs on the damage of MPC5 cells induced by adriamycin are validated. Finally, the effective constituents and mechanism of ARs against doxorubicin-induced nephropathy were investigated by network pharmacology and molecular docking. RESULTS: Quantitative determination experiment and pharmacological experiment indicated that the AR produced from Gansu province (China) (transplanted AR) with a higher proportion of total saponins, has better efficacy in the treatment for DN. And the cell experiment validated the result that astragalus saponins has the better efficacy in protecting the podocyte against injury than astragalus flavonoids and polysaccharides. The network pharmacology and molecular docking study indicated that astragalus saponins were the main constituent of AR in the treatment for DN. The mechanism may involve in GnRH signaling pathway, VEGF signaling pathway and metabolic pathways, especially of bilirubin metabolism. CONCLUSIONS: Transplanted AR has better efficacy in the treatment for NS than imitation wild AR, astragalus saponins have better efficacy in the treatment for NS than astragalus flavonoids and polysaccharides.


Assuntos
Astrágalo (Planta) , Medicamentos de Ervas Chinesas , Nefropatias , Saponinas , Humanos , Simulação de Acoplamento Molecular , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Doxorrubicina , Saponinas/farmacologia , Saponinas/uso terapêutico , Flavonoides/farmacologia , Polissacarídeos
10.
Bioorg Chem ; 131: 106316, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36508939

RESUMO

The recent global Omicron epidemics underscore the great need for the development of small molecule therapeutics with appropriate mechanisms. The trimeric spike protein (S) of SARS-CoV-2 plays a pivotal role in mediating viral entry into host cells. We continued our efforts to develop small-molecule SARS-CoV-2 entry inhibitors. In this work, two sets of BA derivatives were designed and synthesized based on the hit BA-1 that was identified as a novel SARS-CoV-2 entry inhibitor. Compound BA-4, the most potent one, showed broad inhibitory activities against pOmicron and other pseudotyped variants with EC50 values ranging 2.73 to 5.19 µM. Moreover, pSARS-CoV-2 assay, SPR analysis, Co-IP assay and the cell-cell fusion assay coupled with docking and mutagenesis studies revealed that BA-4 could stabilize S in the pre-fusion step to interfere with the membrane fusion, thereby displaying promising inhibition against Omicron entry.


Assuntos
COVID-19 , Inibidores da Fusão de HIV , Ácido Oleanólico , Saponinas , Viroses , Humanos , SARS-CoV-2 , Ácido Oleanólico/farmacologia
11.
Anal Bioanal Chem ; 415(5): 887-897, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36571591

RESUMO

Characterization of structural isomers of bioactive molecules is important for recognizing their functions, but it has been challenging due to their highly similar structures. As the main bioactive constituents of Panax ginseng, ginsenosides have different structural isomers attributed to the aglycone structure and glycosylation sites as well as stereochemistry of sugar groups attached. This work demonstrated a simple and robust in situ methylation reaction with tetramethylammonium hydroxide (TMAH) using ambient ionization source of direct analysis in real time (DART) to characterize saponin structural isomers. The DART ion source provides favorable conditions to methylate hydroxyl groups of ginsenoside instantaneously with TMAH, and it can ionize the methylated products at the same time. Methylated ginsenoside stereoisomers even with subtle structure differences generated very different mass signals from full-scan MS and tandem MS. High-resolution mass spectrometry aided the assignment of molecular structures of the various precursor and fragment ions from different ginsenosides, which provided structural information for both the aglycone skeleton and the sugar moieties in ginsenosides. The presented method was successfully used for the identification of ginsenosides in Panax ginseng, and saponin isomers were characterized without the need for chromatographic separation and/or tedious offline sample pretreatment.


Assuntos
Ginsenosídeos , Panax , Saponinas , Espectrometria de Massas em Tandem , Ginsenosídeos/análise , Metilação , Cromatografia Líquida de Alta Pressão/métodos , Panax/química , Açúcares
12.
Bioorg Chem ; 131: 106305, 2023 02.
Artigo em Inglês | MEDLINE | ID: mdl-36495679

RESUMO

Phytochemical investigation on the rhizomes of Paris fargesii var. petiolata (Baker ex C. H. Wright) Wang et Tang led to the isolation of five previously undescribed steroidal saponins, parpetiosides A-E (1-5), and six known analogs (6-11). Their structures were established by extensive spectroscopic data analysis and chemical methods. Compound 5 was a rare steroidal saponin with disaccharide moiety linked at C-26 of dehydrokryptogenin that was hardly seen in the genus Paris. The cytotoxicities of the isolated compounds against three human cancer cell lines (U87, HepG2 and SGC-7901) were evaluated, and compound 1 displayed certain inhibitory effect with IC50 values of 8.02 ± 0.45, 8.24 ± 0.57 and 6.20 ± 0.79 µM, respectively. Moreover, the preliminary mechanism of 1 inhibiting the proliferation of the three cancer cell lines might be related to cell cycle distribution and the induction of S phase arrest.


Assuntos
Antineoplásicos , Liliaceae , Neoplasias , Saponinas , Humanos , Rizoma/química , Antineoplásicos/farmacologia , Antineoplásicos/análise , Liliaceae/química , Esteroides/farmacologia , Esteroides/química , Saponinas/farmacologia , Saponinas/química
13.
Appl Microbiol Biotechnol ; 107(2-3): 473-489, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36481800

RESUMO

In vitro culture of a plant cell, tissue and organ is a marvellous, eco-friendly biotechnological strategy for the production of phytochemicals. With the emergence of recent biotechnological tools, genetic engineering is now widely practiced enhancing the quality and quantity of plant metabolites. Triterpenoid saponins especially asiaticoside and madecassoside of Centella asiatica (L.) Urb. are popularly known for their neuroprotective activity. It has become necessary to increase the production of asiaticoside and madecassoside because of their high pharmaceutical and industrial demand. Thus, the review aims to provide efficient biotechnological tools along with proper strategies. This review also included a comparative analysis of various carbon sources and biotic and abiotic elicitors. The vital roles of a variety of plant growth regulators and their combinations have also been evaluated at different in vitro growth stages of Centella asiatica. Selection of explants, direct and callus-mediated organogenesis, root organogenesis, somatic embryogenesis, synthetic seed production etc. are also highlighted in this study. In a nutshell, this review will present the research outcomes of different biotechnological interventions used to increase the yield of triterpenoid saponins in C. asiatica. KEY POINTS: • Critical and updated assessment on in vitro biotechnology in C. asiatica. • In vitro propagation of C. asiatica and elicitation of triterpenoid saponins production. • Methods for mass producing C. asiatica.


Assuntos
Centella , Saponinas , Triterpenos , Centella/genética , Centella/metabolismo , Triterpenos/metabolismo , Extratos Vegetais/metabolismo , Biotecnologia , Saponinas/metabolismo
14.
Eur J Pharmacol ; 940: 175468, 2023 Feb 05.
Artigo em Inglês | MEDLINE | ID: mdl-36566009

RESUMO

Metabolic associated fatty liver disease (MAFLD) is one of the most common chronic liver diseases and may develop into non-alcoholic steatohepatitis (NASH), fibrosis, cirrhosis, and even hepatocellular carcinoma, which has threatened human health. Although NLRP3 inflammasome is widely recognized in the pathogenesis of MAFLD, there are currently no drugs targeting NLRP3 inflammasome approved by regulatory agencies. Panax ginseng and its main saponin components have been used to regulate inflammatory and metabolic disorders. Notably, 20(S)-protopanaxatriol (PPT) is an active metabolite of protopanaxatriol saponins with prominent anti-inflammatory activity. However, the mechanism by which PPT ameliorates MAFLD has not been fully elucidated. Therefore, this study explored the efficacy and mechanism of PPT in treating MAFLD based on the inhibition of NLRP3 inflammasome activation. First, we screened potential NLRP3 inflammasome blockers from protopanaxadiol saponins in mouse primary bone marrow-derived macrophages (BMDMs) stimulated by LPS and different inflammasome inducers. Second, LPS-primed mouse BMDMs, mouse primary hepatocytes, mouse primary Kupffer cells and human peripheral blood mononuclear cells (PBMCs) stimulated by cholesterol and ATP were used to evaluate the effect of PPT in inhibiting NLRP3 inflammasome. Finally, MCD-induced mouse MAFLD were established to verify the therapeutic effect of PPT by inhibiting NLRP3 inflammasome. Our results showed that PPT of ginseng saponins significantly inhibited NLRP3 inflammasome activation in multiple primary cells, suppressed systemic inflammation, restored liver function, and attenuated liver inflammation as well as fibrosis in MCD--induced mouse MAFLD. Collectively, protopanaxatriol saponins metabolite PPT, may serve as a potent therapeutic agent for MAFLD by inhibiting NLRP3 inflammasome activation.


Assuntos
Hepatopatia Gordurosa não Alcoólica , Saponinas , Humanos , Animais , Camundongos , Inflamassomos/metabolismo , Hepatopatia Gordurosa não Alcoólica/metabolismo , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Lipopolissacarídeos , Leucócitos Mononucleares/metabolismo , Inflamação/patologia , Fibrose , Saponinas/farmacologia , Saponinas/uso terapêutico , Camundongos Endogâmicos C57BL
15.
Pak J Pharm Sci ; 35(5): 1287-1294, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-36451555

RESUMO

Aristolochia bracteolatais utilized in confronting multiple and complicated disease conditions such as cancer, lung inflammation, dysentery, syphilis, gonorrhea, arthritis, skindiseases, snake bite and oxidative stress relating to humans due to their acceptability, affordability and proximity. This investigation seeks to determine the antioxidant and anti-diabetic effects of methanol extract of A. bracteolate root bark in vitro. The phytochemical screening, antioxidant, and enzymes inhibitory (alpha-amylase and alpha-glucosidase) properties of root bark extract were evaluated by standard procedures. The methanol extract indicated the presence of diverse phytochemicals (tannins, saponins, flavonoids, alkaloids, phenols, glycosides and terpenoids) and contained a remarkable amount of saponins (8.20±0.03%), phenols (6.82±0.01%), alkaloids (4.71±0.03%) and flavonoids (3.50±0.12%). The extract showed not only strong antioxidant properties against DPPH, FRAP and TBARS radicals with IC50 value of 57.87, 54.64 and 47.54 mg/ml, respectively but also anti-diabetic activity by inhibiting alpha-amylase (IC50=53.70 mg/ml) and alpha-glucosidase (IC50=49.18 mg/ml). GC-MS chromatogram identified a diverse array of active metabolites in the methanol extract of A. bracteolate root bark. This study suggested that the methanol extract of A. bracteolate root bark possessed anti-oxidative and anti-diabetic activities.


Assuntos
Aristolochia , Saponinas , Humanos , Metanol , Antioxidantes/farmacologia , Cromatografia Gasosa-Espectrometria de Massas , alfa-Glucosidases , Casca de Planta , Fenóis , Flavonoides/farmacologia , alfa-Amilases , Amilases , Extratos Vegetais/farmacologia
16.
Zhongguo Zhong Yao Za Zhi ; 47(22): 6005-6019, 2022 Nov.
Artigo em Chinês | MEDLINE | ID: mdl-36471951

RESUMO

Patrinia villosa, regarding its functions in clearing heat and detoxification and eliminating carbuncles and pus, is widely used as a traditional medicinal herb that contains rich nutrition and substances such as various amino acids, vitamins, and soluble su-gar, and it is also an edible wild herb in Chinese folk tradition for 2 000 years. In 1973, Japanese scholars firstly separated three iridoids from Japanese P. villosa, and by 2021, chemical components such as flavonoids, iridoids, organic acids, triterpenoids, phenylpropanoids, and steroids have been found, which have multiple pharmacological effects, including antioxidant, antitumor, anti-diarrhea, antibacterial, sedative, and liver protection capabilities. Studies indicate that flavonoids, saponins, phenylpropanoids, and triterpenoids in P. villosa are vital substances for its pharmacological activities. However, the quality of this medicinal material cannot be controlled due to the unclear records in ancient books in the past dynasties and different drug use habits in different places, and thus its circulation is chaotic. At present, researchers have used flavonoids, organic acids, phenylpropanoids, triterpenoid saponins, and other compounds to conduct studies in this regard. Therefore, on the basis of the existing literature resources, we comprehensively summarize the chemical constituents, pharmacological activities, and quality control of P. villosa to further provide a reference for the safety and effectiveness of clinical drug use and lay a foundation for the follow-up experimental research.


Assuntos
Patrinia , Saponinas , Triterpenos , Patrinia/química , Flavonoides/farmacologia , Triterpenos/farmacologia , Iridoides , Controle de Qualidade
17.
Zhongguo Zhong Yao Za Zhi ; 47(19): 5246-5255, 2022 Oct.
Artigo em Chinês | MEDLINE | ID: mdl-36472031

RESUMO

The present study quickly identified the ginsenosides in fresh Panax ginseng and specified the effects of different drying methods(50 ℃-drying, 80 ℃-drying, and-70 ℃ freeze-drying) on ginsenosides.Three P.ginseng products by different drying methods were prepared, and the UHPLC-Q-Exactive Orbitrap high-resolution liquid mass spectrometry(MS) technique was applied to perform gradient elution using water-acetonitrile as the mobile phase, and the data collected in the negative ion mode were analyzed using X Calibur 2.2.The results showed that 57 saponins were identified from fresh P.ginseng.As revealed by the comparison with the fresh P.ginseng, in terms of the loss of ginsenosides, the dried products were ranked as the dried product at 50 ℃, freeze-dried products at-70 ℃, and the dried product at 80 ℃ in the ascending order.This study elucidated the effects of different drying methods on the types and relative content of ginsenosides, which can provide references for the processing of P.ginseng in the producing areas.


Assuntos
Ginsenosídeos , Panax , Saponinas , Ginsenosídeos/análise , Cromatografia Líquida de Alta Pressão/métodos , Espectrometria de Massas/métodos
18.
Front Biosci (Landmark Ed) ; 27(11): 300, 2022 Nov 03.
Artigo em Inglês | MEDLINE | ID: mdl-36472098

RESUMO

BACKGROUND: The mitophagy/NLRP3 inflammasome pathway is a promising therapeutic target for cerebral ischemia-reperfusion (I/R). Panax notoginseng (Burkill) F.H. Chen, one of the most valuable components of traditional Chinese medicine, and Panax notoginseng saponins (PNS), the main active ingredients of P. notoginseng, are patent medicines commonly used to treat cardio- and cerebrovascular diseases. However, their effects on the mitophagy and the NLRP3 inflammasome activation in I/R remain unclear. Therefore, in this study, we investigated how PNS might affect the mitophagy/NLRP3 inflammasome pathway in I/R. METHODS: Cerebral I/R injury was induced by middle cerebral-artery occlusion, and expression levels of NLRP3 inflammasome signaling pathway-associated proteins were detected by western blot. We tested I/R injury using a neurological-deficit score, infarct volume, and hematoxylin and eosin staining, after which we detected both mitophagy- and NLRP3 inflammasome-related proteins in PNS-treated rats to determine whether PNS could attenuate I/R injury and the possible mechanisms involved. RESULTS: Our results showed that cerebral I/R could induce activation of the NLRP3 inflammasome, aggravating brain injury, whereas PNS effectively alleviated cerebral I/R injury in rats by inhibiting the NLRP3 inflammasome and promoting mitophagy via the PINK1/Parkin pathway. Moreover, mitophagy inhibited the NLRP3 inflammasome and mediated the anti-injury effects of PNS. CONCLUSIONS: In conclusion, PNS could promote mitophagy via the PINK1/Parkin pathway by inhibiting activation of the NLRP3 inflammasome, alleviating cerebral I/R injury in rats.


Assuntos
Isquemia Encefálica , Panax notoginseng , Traumatismo por Reperfusão , Saponinas , Animais , Ratos , Saponinas/farmacologia , Inflamassomos , Proteína 3 que Contém Domínio de Pirina da Família NLR , Mitofagia , Traumatismo por Reperfusão/tratamento farmacológico , Traumatismo por Reperfusão/prevenção & controle , Traumatismo por Reperfusão/metabolismo , Isquemia Encefálica/tratamento farmacológico , Ubiquitina-Proteína Ligases , Proteínas Quinases
19.
Eur Rev Med Pharmacol Sci ; 26(22): 8539-8550, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36459035

RESUMO

OBJECTIVE: Autism is a disorder that manifests itself in early childhood. Early diagnosis of autism may not only help the affected children themselves, but also affect family well-being and social stability. The natural drug Albizia bark has been reported to have some effect in the prevention and treatment of autism in children. Therefore, we used network pharmacology and molecular docking to explore the possible mechanism. MATERIALS AND METHODS: TCMID and BATMAN-TCM was used to retrieve the chemical constituents of Albizia bark, and then obtained the relevant targets about autism by TTD, Gene Cards and OMIM. The resulting ingredients and targets were predicted, then a protein interaction network was constructed, and finally bioinformatics analysis was performed. Finally, molecular docking was used to verify the effective ingredients and targets obtained from the screening. RESULTS: Leucaena saponin B, luteolin, 3', 4', 7-trihydroxyflavone, which may be the key compounds for the treatment of autism. BP mainly involving signal transduction, G protein coupled receptor signal pathway, protein phosphorylation. CC, mainly involving plasma membrane, integral component of plasma membrane, MF, including protein binding, adenosine triphosphate binding, protein kinase activity. Molecular docking showed that AKT1, HRAS, PIK3CA, PIK3R1 and SRC, five potential targets, had good binding ability to Leucaena saponin B. CONCLUSIONS: The natural drug Albizia bark exerts pharmacological effects in a multi-component, multi-target and multi-channel manner, including neural regulation, inflammatory response and immune regulation.


Assuntos
Albizzia , Transtorno Autístico , Saponinas , Criança , Pré-Escolar , Humanos , Simulação de Acoplamento Molecular , Transtorno Autístico/tratamento farmacológico , Farmacologia em Rede , Casca de Planta
20.
Biomed Res Int ; 2022: 5489553, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36467888

RESUMO

Saikosaponin D (SSD), a saponin derivative, is extracted from Bupleurum falcatum. It exhibits an inhibitory effect on a number of tumor cells and is relatively safe when used at therapeutic doses. However, its effects on glioblastoma multiforme (GBM) have not been fully explored. This study is aimed at investigating the cytotoxic effects of SSD in GBM cell lines. SSD induces apoptosis and autophagy by activating endoplasmic reticulum (ER) stress in GBM cells. GBM cell proliferation activity and morphology were observed using the Cell Counting Kit-8 assay and hematoxylin and eosin staining. Hoechst 33258 fluorescence staining and flow cytometry were performed to assess apoptosis. Western blotting and immunocytochemical staining were used to detect protein expression and distribution. SSD significantly inhibited the proliferation of RG-2, U87-MG, and U251 cells in a dose-dependent manner, and the proportion of apoptotic cells increased significantly. Additionally, the expressions of ER-, apoptosis-, and autophagy-related proteins were significantly upregulated and distributed in the cytoplasm and nucleus. Therefore, SSD may be considered a novel treatment option for GBM. This study demonstrated the anti-GBM effect of SSD from the perspectives of cell apoptosis and autophagy.


Assuntos
Glioblastoma , Saponinas , Humanos , Estresse do Retículo Endoplasmático , Glioblastoma/tratamento farmacológico , Saponinas/farmacologia , Autofagia , Apoptose
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