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1.
PLoS One ; 18(3): e0282443, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36893115

RESUMO

Saussurea costus is from medicinal plants and have therapeutic properties that were recorded in a variety of medical functions. The usage of biomaterials in the synthesis of nanoparticles is an essential strategy in green nanotechnology. Iron oxide nanoparticles (IONPs) were composed in the stage of (2:1, FeCl2: FeCl3) solution by using the aqueous extract of Saussurea costus peel in an eco-friendly method to evaluate their antimicrobial property. The properties of the obtained IONPs were evaluated using a scanning (SEM) and transmission (TEM) electron microscope. The mean size of IONPs discovered by Zetasizer varies between 100 and 300 nm, with a mean particle size of 295 nm. The morphology of IONPs (γ-Fe2O3) was determined to be nearly spherical and prismatic-curved. Moreover, the antimicrobial property of IONPs was assessed with nine pathogenic microbes, revealing that the nanoparticles have antimicrobial activities with Pseudomonas aeruginosa, Escherichia coli, Shigella sp., Staphylococcus sp. and Aspergillus niger, with possible applications in the therapeutic and biomedical fields.


Assuntos
Anti-Infecciosos , Nanopartículas Metálicas , Saussurea , Compostos Férricos/farmacologia , Extratos Vegetais/farmacologia , Anti-Infecciosos/farmacologia , Nanopartículas Magnéticas de Óxido de Ferro
2.
Molecules ; 28(4)2023 Feb 04.
Artigo em Inglês | MEDLINE | ID: mdl-36838515

RESUMO

BACKGROUND: Saussurea pulchella (SP) is a traditional medicinal plant that is widely used in folk medicine because of its diverse biological activities, particularly its anti-inflammatory effects. However, the alleviation effect of SP on ulcerative colitis (UC) has not yet been realized. PURPOSE: To investigate the chemical composition and therapeutic effect of SP extract against UC. METHODS: First, qualitative and quantitative analysis of SP 75% ethanol extract was performed by UPLC-Q/TOF-MS. Second, a dextran sodium sulfate (DSS) model of UC mice was developed to study the effects of SP on the symptoms, inflammatory factors, oxidative stress indexes and colon histopathology. Third, an integration of network pharmacology with metabolomics was performed to investigate the key metabolites, biological targets and metabolisms closely related to the effect of SP. RESULTS: From the SP ethanol extract, 149 compounds were identified qualitatively and 20 were determined quantitatively. The SP could dose-dependently decrease the DAI score, spleen coefficient and the levels of TNF-α, IL-6, iNOS, MPO and MDA; increase the colon length, GSH level and SOD activity; and protect the intestinal barrier in the UC mice. Moreover, 10 metabolite biomarkers,18 targets and 5 metabolisms were found to play crucial roles in the treatment of UC with SP. CONCLUSIONS: SP 75% ethanol extract could effectively alleviate the progression of UC and, therefore, could be classified as a novel natural treatment for UC.


Assuntos
Colite Ulcerativa , Saussurea , Fator de Necrose Tumoral alfa , Animais , Camundongos , Colite Ulcerativa/tratamento farmacológico , Colo/metabolismo , Sulfato de Dextrana , Modelos Animais de Doenças , Camundongos Endogâmicos C57BL , Estresse Oxidativo , Saussurea/química , Fator de Necrose Tumoral alfa/metabolismo , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Compostos Fitoquímicos/química
3.
Artigo em Inglês | MEDLINE | ID: mdl-36773385

RESUMO

Saussurea obvallata (S. obvallata) is widely used in Qinghai-Tibet Plateau with high medicinal and edible values of reducing inflammation. But, the individual components and mechanisms of action still ill-defined. In this work, an integrated method using affinity ultrafiltration combined with preparative liquid chromatography was developed to identify and separate cyclooxygenase-2 (COX-2) inhibitors from S. obvallata. The sample was pretreated using on-line medium pressure liquid chromatography to yield the active fraction. Then, the potential COX-2 ligands were screened out using affinity ultrafiltration from the targeted fraction and the identified compounds were isolated via preparative liquid chromatography. As a result, four main compounds, coniferin (1), syringin (2), roseoside (3) and grasshopper ketone (4) were targeted isolated with IC50 values of 12.34 ± 1.81, 4.04 ± 0.43, 13.91 ± 2.46 and 7.97 ± 1.21 µM, respectively. Results of this work demonstrated that the developed strategy was effective for the targeted separation of COX-2 inhibitors from natural product extracts.


Assuntos
Inibidores de Ciclo-Oxigenase 2 , Saussurea , Inibidores de Ciclo-Oxigenase 2/química , Cromatografia Líquida de Alta Pressão/métodos , Ultrafiltração , Ciclo-Oxigenase 2 , Cromatografia Líquida
4.
Plant Physiol Biochem ; 195: 155-162, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36638605

RESUMO

S. involucratae, an endemic and endangered plant, is a valuable and traditional Chinese medicinal herb. In order to control the flowering time of S. involucratae, we used the well-known stress inducible RD29A promoter to drive Hd3a (a FT ortholog from rice) expression in S. involucratae. Unexpectedly, the majority of regenerated buds in RD29A::Hd3a transgenic lines (S-RH) produced flowers in tissue culture stage under normal growth (25 ± 2 °C) condition. Their flowering time was not further influenced by salt treatment. Hd3a in S-RH was strongly expressed in MS media supplemented with or without 50 mM NaCl. RD29A::GUS transgenic experiments further revealed that RD29A constitutively promoted GUS expression in both S. involucrate and halophyte Thellungiella halophile, in contrast to glycophic plants Oryza sativa L. 'Zhonghua 11', in which its expression was up-regulated by cold, salinity, and drought stress. The results supported the hypothesis that RD29A promoter activity is inducible in stress-sensitive plants, but constitutive in stress-tolerant ones. Importantly, S-RH plants produced pollen grains and seeds under normal conditions. Additionally, we found that OsLEA3-1::Hd3a and HSP18.2::Hd3a could not promote S. involucrate to flower under either normal conditions or abiotic stresses. Taken together, we demonstrated the potential of RD29A::Hd3a might be served as a feasible approach in breeding S. involucrate under normal condition.


Assuntos
Oryza , Saussurea , Oryza/genética , Oryza/metabolismo , Saussurea/genética , Saussurea/metabolismo , Proteínas de Plantas/genética , Proteínas de Plantas/metabolismo , Regulação da Expressão Gênica de Plantas , Melhoramento Vegetal , Flores/genética , Flores/metabolismo
5.
Molecules ; 28(2)2023 Jan 09.
Artigo em Inglês | MEDLINE | ID: mdl-36677724

RESUMO

Saussurea costus (Falc) Lipsch is a traditional herb used to treat kidney stone problems because it contains several molecules used to treat this health problem, such as quercitrin. Infectious stones are the most painful of all urinary tract disorders, with ammonium phosphate (struvite) and carbapatite stones being the most common, caused by a bacterial infection with urease activity. These stones are treated with antibiotics, but antibiotic resistance is on the rise. The current study investigated the anti-urolithic activities of S. costus aqueous and ethanolic extracts of against struvite crystals synthesized using microscopic crystallization and turbidimetric methods, respectively. The utilized methods indicated that the ethanolic extract of this plant has a significant inhibitory effect on struvite crystallization, with a percentage inhibition of (87.45 ± 1.107) (p < 0.001) for a concentration of 1 mg mL−1 and a decrease in the number of struvite crystals, reaching values less than 100/mm3. For the number of struvite crystals inhibited by cystone, we found a value of 400/mm3 and with the aqueous extract we found 700/mm3. The antibacterial activity of the plant extracts studied was examined against several urease-producing bacteria, and this activity was evaluated by qualitative and quantitative evaluation methods; the highest minimum inhibitory concentration was seen in the ethanolic extract, with an MIC of 50 mg mL−1 for Staphylococcus aureus followed by an MIC of 200 mg mL−1 for Klebsiella pneumoniae. It showed a minimal bactericidal concentration (MBC) against S. aureus and K. pneumoniae (>50 mg mL−1 and >200 mg mL−1, respectively). Furthermore, to determine the extract's anti-inflammatory activity, in vivo anti-inflammatory activity was investigated in rats. The results show that at a dose of 400 mg kg−1, the ethanolic extract has a maximum edema inhibition of 66%.


Assuntos
Anti-Infecciosos , Asteraceae , Saussurea , Ratos , Animais , Saussurea/química , Staphylococcus aureus , Estruvita , Urease , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Anti-Infecciosos/farmacologia , Etanol/farmacologia , Antibacterianos/farmacologia , Antibacterianos/química , Água/farmacologia , Anti-Inflamatórios/farmacologia , Testes de Sensibilidade Microbiana
6.
Phytochemistry ; 206: 113557, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36496006

RESUMO

An LC-HRMS/MS-based molecular networking strategy was applied to investigate the potential sesquiterpene dimers of Aucklandia lappa, leading to the isolation of three undescribed guaiane-guaiane dimers and one guaiane-eudesmane dimer together with six known sesquiterpenes. The structures were determined by analyzing their 1D, 2D NMR, and HRESIMS data as well as ECD calculations. The biogenetic pathway of the sesquiterpene dimers was postulated to involve the Diels-Alder cycloaddition as the key step. All compounds exhibited their inhibitory effects on LPS-induced nitric oxide production in RAW 264.7 macrophages with IC50 values ranging from 0.3 to 25.1 µM.


Assuntos
Saussurea , Sesquiterpenos , Estrutura Molecular , Saussurea/metabolismo , Sesquiterpenos/química , Lactonas/química , Óxido Nítrico
7.
Chem Biodivers ; 20(1): e202200885, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36524455

RESUMO

The snow lotus is an endangered traditional Chinese medicinal herb. Saussurea involucrata, Saussurea laniceps, and Saussurea medusa, the three main snow lotus species (five herbs and two S. involucrata cell cultures), were selected for this study. Snow lotus (XLs) was extracted using 75 % (v/v) ethanol. Two reversed phase-high performance liquid chromatography-diode array detector methods were developed and validated for the determination of 10 representative components in XLs. The antioxidant efficacy of XLs and their components was investigated using DPPH, ABTS free radical scavenging, and ROS inhibition experiments. The results showed that the IC50 for DPPH scavenging ranged from 0.06-0.29 mg/mL for XLs and from 0.13-0.63 mg/mL for ABTS, and could downregulate ROS to varying degrees. The results of the antioxidant activity showed that rutin, quercetin, and isochlorogenic acid A contributed to the antioxidant capacity of XLs. The high content and activity of the cell cultures indicate that they can serve as an effective alternative to snow lotus, thus providing a theoretical basis for the selection of herbs and cell cultures to fulfil various needs.


Assuntos
Lotus , Saussurea , Antioxidantes/farmacologia , Antioxidantes/química , Espécies Reativas de Oxigênio , Saussurea/química , Etanol
8.
Nutrients ; 14(23)2022 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-36501075

RESUMO

As one of the prominent medicinal plants listed in the Chinese pharmacopoeia (2020), Saussurea involucrata (Kar. et Kir.) Sch.-Bip was demonstrated to possess various therapeutic effects. In our recent research, we extracted the polysaccharides from S. involucrata (SIP) at optimal conditions and conducted further structure elucidation on the main fraction as well as the confirmation of its possible anti-inflammatory activity. Hence, in this work, we assessed the in vitro antioxidant activity and anti-melanogenesis effects of the crude SIP in forskolin-induced B16F10 melanoma cells. The results show that SIP possessed strong antioxidant activity and was effective in concentration-dependently decreasing melanin formation and inhibiting tyrosinase activity in forskolin-induced B16F10 cells. Based on these results, the inhibitory mechanism of melanogenesis was investigated by measuring Tyrosinase (TYR), Tyrosinase related protein-1 (TRP-1), Tyrosinase related protein-2 (TRP-2), Microphthalmia-associated transcription factor (MITF), cAMP-response element binding protein (CREB), mitogen-activated protein kinases (MAPK) signaling protein members, and ß-catenin degradation in forskolin-induced B16F10 cells. The anti-melanogenesis response of SIP might be attributed to the regulation of c-Jun N-terminal kinase (JNK) phosphorylation and ß-catenin degradation pathways. These results suggest that polysaccharides from S. involucrata possess a strong anti-melanogenic effect, and thus could be used as a high-value natural material for skin whitening in cosmeceutical industries.


Assuntos
Melanoma Experimental , Melanoma , Saussurea , Animais , beta Catenina , Antioxidantes/farmacologia , Colforsina/farmacologia , Colforsina/uso terapêutico , Linhagem Celular Tumoral , Melanoma/tratamento farmacológico , Polissacarídeos/farmacologia , Polissacarídeos/uso terapêutico , Melanoma Experimental/metabolismo
9.
BMC Plant Biol ; 22(1): 550, 2022 Nov 29.
Artigo em Inglês | MEDLINE | ID: mdl-36443690

RESUMO

BACKGROUND: Saussurea is one of the most species-rich genera in the Cardueae, Asteraceae. There are approximately 40 Saussurea species distributed in Korea, with nearly 40% of them endemics. Infrageneric relationships remain uncertain due to insufficient resolutions and low statistical support. In this study, we sequenced the plastid genomes of five Korean endemic Saussurea (S. albifolia, S. calcicola, S. diamantica, S. grandicapitula, and S. seoulensis), and comparative analyses including two other endemics (S. chabyoungsanica and S. polylepis) were conducted. RESULTS: The plastomes of Korean endemics were highly conserved in gene content, order, and numbers. Exceptionally, S. diamantica had mitochondrial DNA sequences including two tRNAs in SSC region. There were no significant differences of the type and numbers of SSRs among the seven Korean endemics except in S. seoulensis. Nine mutation hotspots with high nucleotide diversity value (Pi > 0.0033) were identified, and phylogenetic analysis suggested that those Korean endemic species most likely evolved several times from diverse lineages within the genus. Moreover, molecular dating estimated that the Korean endemic species diverged since the late Miocene. CONCLUSIONS: This study provides insight into understanding the plastome evolution and evolutionary relationships of highly complex species of Saussurea in Korean peninsula.


Assuntos
Asteraceae , Genomas de Plastídeos , Saussurea , Saussurea/genética , Filogenia , República da Coreia
10.
Int J Mol Sci ; 23(22)2022 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-36430559

RESUMO

Three pairs of novel enantiomeric 8-O-4' type neolignans (1a/1b-3a/3b), together with seven known analogues (4-10), were isolated from the whole plants of Saussurea&nbsp;medusa. Their structures were elucidated by extensive spectroscopic data analysis and electric circular dichroism (ECD) calculations after chiral separations. All compounds were obtained from S. medusa for the first time, and compounds 1-3 and 5-10 had never been obtained from the genus Saussurea previously. The anti-inflammatory activities of the compounds were evaluated by determining their inhibitory activities on the production of NO and inducible nitric oxide synthase (iNOS) expression in LPS-stimulated RAW 264.7 cells. Compounds (+)-1a, (-)-1b and 5-7 inhibited NO production and had IC50 values ranging from 14.3 ± 1.6 to 41.4 ± 3.1 µM. Compound 7 induced a dose-dependent reduction in the expression of iNOS in LPS-treated RAW 264.7 cells. Molecular docking experiments showed that all active compounds exhibited excellent docking scores (<-7.0 kcal/mol) with iNOS. Therefore, compounds (+)-1a, (-)-1b and 5-7 isolated from the whole plants of S. medusa may have therapeutic potential in inflammatory diseases.


Assuntos
Lignanas , Saussurea , Simulação de Acoplamento Molecular , Lipopolissacarídeos/toxicidade , Lignanas/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/química
11.
J Chromatogr A ; 1683: 463522, 2022 Nov 08.
Artigo em Inglês | MEDLINE | ID: mdl-36198213

RESUMO

The hyphenation of high-performance thin-layer chromatography to effect-directed assays is a very straightforward way to detect individual bioactive zones, and at the same time, to investigate several samples simultaneously. The combination of the separation technique with adherent human cells applied on the same surface was recently shown to be possible. Since on-surface adherent cell assays are in their infancy, a planar bioluminescent cytotoxicity assay was developed to expand the possibilities. Human embryonic kidney (HEK) 293 or HeLa (cervical carcinoma) cells were chosen because of their fast growth rates and high rates of successful transfection, being suitable for the generation of genetically modified reporter cells. For the first time, HeLa cells were visualized on the wettable reversed phase plate surface using digital microscopy. For the generation of bioluminescent reporter cells, vectors for the expression of three luciferase enzymes of various origins were tested. The genetically modified HEK 293T-CMV-ELuc cells were the best suitable for the new planar cytotoxicity assay due to the faster growth rate, robustness, and stronger bioluminescence signal. The stable expression of luciferase under the control of a strong constitutive promoter allowed the cells to be used for the determination of the cytotoxicity of Saussurea costus root samples obtained from the market and to assess the authenticity of these samples. Any cytotoxic zone was detected as a dark zone inhibiting the cell bioluminescence. Five replicates of the dose-response curve confirmed the good assay performance and the cytotoxicity of a zone, which was assigned to costunolide and dehydrocostus lactone. By this, the proof-of-principle of the new planar bioluminescent cytotoxicity assay, which does not require expensive licensing, was successful.


Assuntos
Medições Luminescentes , Saussurea , Humanos , Células HEK293 , Células HeLa , Luciferases/genética , Luciferases/metabolismo , Medições Luminescentes/métodos , Saussurea/química , Saussurea/metabolismo , Saussurea/toxicidade
12.
Int J Biol Macromol ; 222(Pt A): 154-166, 2022 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-36122780

RESUMO

The optimum extraction condition for the Saussurea involucrata polysaccharide (SIP) was determined to be a temperature of 80 °C, time 2 h, and a liquid-solid ratio of 30 mL/g with a yield of 11.37 %. An acidic homogenous polysaccharide, namely SIP-II was isolated from Saussurea involucrate through anion exchange and gel permeation column chromatography. The structure of the SIP-II was elucidated through the combination of HPLC, GC-MS, IC, peroxide oxidation, smith degradation, methylation, NMR analysis, it was mainly composed of arabinose, rhamnose, galactose, galacturonic acid, and glucose with the molar ratio of 19.85:20.30: 27.12:11.95:8.69 with a molecular weight of 237,570 Da. The glycosidic linkages of SIP-II mainly composed of →1)-α-L-Rhap-(2→, T-Araf, →1)-ß-D-GalpA-(4→, →1)-ß-D-Galp-(3,6→, →1)-ß-D-Galp-(6→, →1)-α-L-Rhap-(2,4→, T-Galp, and →1)-α-L-Araf-(5→. Meanwhile, the structures were characterized through extensive analysis of UV, FT-IR, SEM-EDX, CD, XRD, and TG. SIP-II possessed a remarkable anti-inflammatory activity by effectively inhibiting the expression of pro-inflammatory cytokines and inflammation-related mediators in LPS-stimulated RAW264.7 macrophages, and the anti-inflammatory response of SIP-II might be attributed to the regulation of the NF-κB, MAPK and JAK/STAT pathways. The results showed that polysaccharides from Saussurea involucrate could be a potential ingredient in the functional food and pharmaceutical industry.


Assuntos
Saussurea , Saussurea/química , Espectroscopia de Infravermelho com Transformada de Fourier , Polissacarídeos/química , Galactose/análise , Peso Molecular
13.
Pak J Pharm Sci ; 35(4): 1153-1158, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-36008914

RESUMO

Saussurea heteromalla is the one of specie of Saussurea plant belonging to family Asteraceae. The Saussurea heteromalla found extensively in Pakistan. The literature review highlights numerous biological aspects of Saussurea heteromalla. This research therefore aims to assess its potential anti-inflammatory, antioxidant, anti-cancer. Carrageenan induced rat paw edema model was used for the evaluation of anti-inflammatory activity. DPPH method was used to evaluate anti-oxidant activity. The MTT (3- [4, 5-dimethylthiazol-2-yl]-2, 5 diphenyl tetrazolium bromide) test was used to assess the viability of the cells for the assessment of the cytotoxic effect of the extract. Methanolic Saussurea heteromalla flowers extract analysis carried by GC-MS, result 19 different peaks. The methanolic extract of Saussurea heteromalla at 400mg/kg dose have equal anti-inflammatory action when compare with standard that is diclofenac sodium. Anti-oxidant activity of methanolic extract is also very good. IC50 value of methanol extract was 25µg/ml. 18.72% cell survive out of 100 when methanolic flower extract of Saussurea heteromalla was given at the dose of 400mg, which shows the cytotoxic effect. This activity shows that plant Saussurea heteromalla methanolic flowers extract have anti-inflammatory, anti-oxidant, cytotoxic effect. The isolation and characterization-based investigations proclaiming the biologically leading active molecule are worthy for further study in this regard.


Assuntos
Saussurea , Animais , Anti-Inflamatórios , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Edema/induzido quimicamente , Edema/tratamento farmacológico , Flores , Metanol/uso terapêutico , Compostos Fitoquímicos/uso terapêutico , Extratos Vegetais , Ratos , Saussurea/química
14.
J Ethnopharmacol ; 298: 115648, 2022 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-35987408

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Saussurea involucrata Kar.et Kir. (S.I.) has long been used as a precious national medicine and clinically proven to be an effective treatment for rheumatoid arthritis (RA) and cardiovascular diseases. In clinical practice, two extraction methods of S.I., including water decoction and alcohol extraction, are prescribed to treat the same conditions. Nevertheless, no study has been performed on the exposure differences of the pharmacodynamic material basis in vivo caused by different extraction methods. AIM OF THE STUDY: Based on the integrated strategy of metabolism, network pharmacology, and pharmacokinetics, we aimed to reveal exposure differences in pharmacodynamic substances caused by different extraction methods. MATERIALS AND METHODS: Ultra-high-performance liquid chromatography-high-resolution mass spectrometry (UPLC-HRMS) was employed to identify the chemical constituents of S.I. extracts and the metabolites in vivo after administration. Based on the analysis of prototype components in vivo, the major exposure active constituents, potential therapeutic targets and possible pharmacological mechanisms in RA treatment were investigated using network pharmacological analysis. Seven critical active components, including quercetin, hispidulin, apigenin, chlorogenic acid, arctigenin, syringin, and umbelliferone, were quantitatively compared between the alcohol, and aqueous extraction methods, which had been confirmed by the reference substance. RESULTS: The chemical comparison demonstrated that the types of chemicals in the two extracts were identical, mainly flavonoids, phenylpropanoids, coumarins, lignins, sesquiterpene lactones, and others, but the contents of the primary constituents in the aqueous extract were lower than those of the alcohol extract. A total of 30 prototype components and 174 metabolites were analyzed and identified in rat plasma, urine, fecal, and bile samples. Twenty-three prototype components were analyzed by network pharmacology, and seven critical active components were selected as representative markers for the pharmacokinetic study. Pharmacokinetic studies had shown that the Tmax values of apigenin, hispidulin, chlorogenic acid, arctigenin, and syringin after the oral administration of the alcohol extract were lower than those after the oral administration of the aqueous extract, and the above components in the alcohol extract could increase the absorption. Compared with the aqueous extract group, the Tmax and T1/2 of quercetin and umbelliferone were longer; it was suggested that alcohol extraction might have a slow-release and long-term effect on these two components. The relative bioavailability of apigenin, hispidulin, quercetin, chlorogenic acid, and umbelliferone in the alcohol extract group were higher than those in the aqueous extract group, which was consistent with the traditional clinical experience that alcohol extract could improve the efficacy of S.I. CONCLUSIONS: The major exposure active constituents in vivo were screened. The representative components that could be used in pharmacokinetics were determined by integrating network pharmacology and metabolism studies. The critical active compounds were quantitatively compared between the alcohol and aqueous extraction methods. This study clarified that flavonoids, coumarin, and phenylpropanoids might be the primary material basis that caused the exposure differences between aqueous and alcoholic extracts from S.I.. This research aimed to provide the basis of metabolism in vivo for further studying these pharmacodynamic differences.


Assuntos
Medicamentos de Ervas Chinesas , Saussurea , Animais , Apigenina , Ácido Clorogênico , Cromatografia Líquida de Alta Pressão , Medicamentos de Ervas Chinesas/farmacologia , Flavonoides , Farmacologia em Rede , Extratos Vegetais/uso terapêutico , Quercetina , Ratos , Saussurea/química , Umbeliferonas
15.
Molecules ; 27(15)2022 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-35956858

RESUMO

Siddha medicine is one of the oldest medical systems in the world and is believed to have originated more than 10,000 years ago and is prevalent across ancient Tamil land. It is undeniable that inhibitor preferences rise with increasing solubility in water due to the considerations pertaining to the bioavailability and the ease of which unabsorbed residues can be disposed of. In this study, we showed the phytochemical discrimination of Saussurea costus extracted with water at room temperature as a green extraction procedure. A total of 48 compounds were identified using gas chromatography-mass spectrometry (GC-MS). The fatty acids had a high phytochemical abundance at 73.8%, followed by tannins at 8.2%, carbohydrates at 6.9%, terpenoids at 4.3%, carboxylic acids at 2.5%, hydrocarbons at 2.4%, phenolic compounds at 0.2%, and sterols at 1.5%. Of these compounds, 22 were docked on the active side and on the catalytic dyad of His41 and Cys145 of the main protease of SARS-CoV-2 (Mpro). Eight active inhibitors were carbohydrates, five were fatty acids, three were terpenoids, two were carboxylic acids, one was a tannin, one was a phenolic compound, and one was a sterol. The best inhibitors were 4,8,13-Cyclotetradecatriene-1,3-diol, 1,5,9-trimethyl-12-(1-methylethyl), Andrographolide, and delta.4-Androstene-3.beta.,17.beta.-diol, with a binding affinity that ranged from -6.1 kcal/mol to -6.5 kcal/mol. The inhibitory effect of Saussurea costus of SARS-CoV-2 entry into the cell was studied using a pseudovirus with Spike proteins from the D614G variant and the VOC variants Gamma and Delta. Based on the viral cycle of SARS-CoV-2, our results suggest that the Saussurea costus aqueous extract has no virucidal effect and inhibits the virus in the events after cell entry. Furthermore, the biological activity of the aqueous extract was investigated against HSV-1 virus and two bacterial strains, namely Staphylococcus aureus ATCC BAA 1026 and Escherichia coli ATCC 9637. According to this study, an enormous number of water-soluble inhibitors were identified from Saussurea costus against the Mpro, and this is unprecedented as far as we know.


Assuntos
Saussurea , Carboidratos , Ácidos Carboxílicos , Ácidos Graxos , Humanos , Índia , Simulação de Acoplamento Molecular , Simulação de Dinâmica Molecular , Peptídeo Hidrolases/metabolismo , Compostos Fitoquímicos/farmacologia , Inibidores de Proteases/química , SARS-CoV-2 , Saussurea/química , Terpenos , Água
16.
Int J Mol Sci ; 23(13)2022 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-35806462

RESUMO

Saussurea involucrata has been reported to have potential therapeutic effects against myocardial ischemia. The pharmacological effects of oral natural medicines may be influenced by the participation of gut microbiota. In this study, we aimed to investigate the bidirectional regulation of gut microbiota and the main components of Saussurea involucrata. We first established a quantitative method for the four main components (chlorogenic acid, syringin, acanthoside B, rutin) which were chosen by fingerprint using liquid chromatography tandem mass spectrometry (LC-MS/MS), and found that gut microbiota has a strong metabolic effect on them. Meanwhile, we identified five major rat gut microbiota metabolites (M1-M5) using liquid chromatography tandem time-of-flight mass spectrometry (LC/MSn-IT-TOF). The metabolic properties of metabolites in vitro were preliminarily elucidated by LC-MS/MS for the first time. These five metabolites of Saussurea involucrata may all have potential contributions to the treatment of myocardial ischemia. Furthermore, the four main components (10 µg/mL) can significantly stimulate intestinal bacteria to produce short chain fatty acids in vitro, respectively, which can further contribute to the effect in myocardial ischemia. In this study, the therapeutic effect against myocardial ischemia of Saussurea involucrata was first reported to be related to the intestinal flora, which can be useful in understanding the effective substances of Saussurea involucrata.


Assuntos
Microbioma Gastrointestinal , Saussurea , Animais , Cromatografia Líquida , Interações Medicamentosas , Isquemia , Ratos , Saussurea/metabolismo , Espectrometria de Massas em Tandem
17.
Chemosphere ; 305: 135335, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-35724723

RESUMO

Membrane technology has been adopted as a prospective and promising alternative to the standard technology used for biodiesel production since the time when it had some limitations. During this research project, the inedible seed oil generating feedstock known as Saussurea heteromalla was put through a biodiesel production process that utilized membrane technology with an effort to increase the yield of methyl ester. The transesterification process was mediated by zirconium oxide nanoparticles that were generated using an aqueous extract of Portulaca oleracea leaf. With an oil to methanol ratio of 1:9, a catalyst concentration of 0.88 (wt. %), temperature of 87 °C, and reaction time of 180 min, the highest possible biodiesel yield of 93% was achieved. The findings of the catalyst characterization demonstrated the purity of the zirconium oxide nano particles and their nanoscale nature with average particle size of 31 nm. Using gas chromatography and mass spectrometry (GC/MS), an examination of biodiesel revealed the presence of four different peaks of methyl esters. Using Fourier-transform infrared spectroscopy (FTIR) and nuclear magnetic resonance, we were able to verify that the production of methyl esters in the biodiesel sample was successful (NMR). Zerconium oxide nanoparticles were found reusable up to five consecutive cycles of transesterification. The fuel-related properties of methyl ester have been determined and are in line with the requirements of the international standards ASTM D-6571 and EN 14214. In the course of our ongoing research, we made use of membrane technology, which led to the production of biodiesel from the seed oil of Saussurea heteromalla that was better for the environment, more cost effective, and produced in greater quantities.


Assuntos
Biocombustíveis , Saussurea , Biocombustíveis/análise , Catálise , Esterificação , Ésteres/química , Óleos de Plantas/química
18.
Food Chem Toxicol ; 166: 113225, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-35691462

RESUMO

The goal of this study was to investigate the effects of three different extracts of Saussurea costus roots (ethanol, methanol, and water) as a food additive in alleviating the harmful effect of sodium nitrite in rat meals. Thirty-five adult male rats were divided into five groups as follows: control, sodium nitrite (NaNO2; 75 mg/kg BW, single oral dose), S. costus 70% ethanol, 70% methanol, and aqueous extracts (300 mg/kg BW), respectively for four weeks followed by a single dose of NaNO2 24h before decapitation. Results showed that the 70% ethanol extract of S. costus has a higher concentration of total phenolic content, total flavonoids, and antioxidant effect than the 70% methanol and water extracts. Rats pretreated with S. costus extracts reduced the harmful effects induced by NaNO2 and improved the hematological parameters, liver, and kidney function biomarkers as well as lipid profile as compared to the NaNO2 group. Furthermore, S. costus improved the histopathological alterations in the liver and kidney induced by NaNO2 and improved meat sensory evaluation. Conclusively, the 70% ethanol extract of S. costus roots is the most effective extract as an antioxidant against the toxicity of sodium nitrite in male rats and might be used safely as a natural additive in the food industry.


Assuntos
Costus , Saussurea , Animais , Antioxidantes/farmacologia , Etanol/toxicidade , Aditivos Alimentares , Masculino , Metanol , Extratos Vegetais/farmacologia , Estudos Prospectivos , Ratos , Nitrito de Sódio/toxicidade , Água
19.
Comput Biol Med ; 146: 105549, 2022 07.
Artigo em Inglês | MEDLINE | ID: mdl-35751193

RESUMO

OBJECTIVE: Based on bioinformatics and network pharmacology, the treatment of Saussurea involucrata (SAIN) on novel coronavirus (COVID-19) was evaluated by the GEO clinical sample gene difference analysis, compound-target molecular docking, and molecular dynamics simulation. role in the discovery of new targets for the prevention or treatment of COVID-19, to better serve the discovery and clinical application of new drugs. MATERIALS AND METHODS: Taking the Traditional Chinese Medicine System Pharmacology Database (TCMSP) as the starting point for the preliminary selection of compounds and targets, we used tools such as Cytoscape 3.8.0, TBtools 1.098, AutoDock vina, R 4.0.2, PyMol, and GROMACS to analyze the compounds of SAIN and targets were initially screened. To further screen the active ingredients and targets, we carried out genetic difference analysis (n = 72) through clinical samples of COVID-19 derived from GEO and carried out biological process (BP) analysis on these screened targets (P ≤ 0.05)., gene = 9), KEGG pathway analysis (FDR≤0.05, gene = 9), protein interaction network (PPI) analysis (gene = 9), and compounds-target-pathway network analysis (gene = 9), to obtain the target Point-regulated biological processes, disease pathways, and compounds-target-pathway relationships. Through the precise molecular docking between the compounds and the targets, we further screened SAIN's active ingredients (Affinity ≤ -7.2 kcal/mol) targets and visualized the data. After that, we performed molecular dynamics simulations and consulted a large number of related Validation of the results in the literature. RESULTS: Through the screening, analysis, and verification of the data, it was finally confirmed that there are five main active ingredients in SAIN, which are Quercitrin, Rutin, Caffeic acid, Jaceosidin, and Beta-sitosterol, and mainly act on five targets. These targets mainly regulate Tuberculosis, TNF signaling pathway, Alzheimer's disease, Pertussis, Toll-like receptor signaling pathway, Influenza A, Non-alcoholic fatty liver disease (NAFLD), Neuroactive ligand-receptor interaction, Complement and coagulation cascades, Fructose and mannose metabolism, and Metabolic pathways, play a role in preventing or treating COVID-19. Molecular dynamics simulation results show that the four active ingredients of SAIN, Quercitrin, Rutin, Caffeic acid, and Jaceosidin, act on the four target proteins of COVID-19, AKR1B1, C5AR1, GSK3B, and IL1B to form complexes that can be very stable in the human environment. Tertiary structure exists. CONCLUSION: Our study successfully explained the effective mechanism of SAIN in improving COVID-19, and at the same time predicted the potential targets of SAIN in the treatment of COVID-19, AKR1B1, IL1B, and GSK3B. It provides a new basis and provides great support for subsequent research on COVID-19.


Assuntos
Medicamentos de Ervas Chinesas , Saussurea , Aldeído Redutase , Biologia Computacional , Medicamentos de Ervas Chinesas/farmacologia , Medicamentos de Ervas Chinesas/uso terapêutico , Humanos , Medicina Tradicional Chinesa , Simulação de Acoplamento Molecular , Terapia de Alvo Molecular , Farmacologia em Rede , Rutina
20.
Molecules ; 27(9)2022 Apr 28.
Artigo em Inglês | MEDLINE | ID: mdl-35566153

RESUMO

Saussurea costus is a plant traditionally used for the treatment of several ailments. Our study accomplished the UPLC/T-TOF-MS/MS analysis of a methanol extract of Saussurea costus roots (MESC), in addition to lipoidal matter determination and assessment of its in vivo hepatoprotective activity. In this study, we were able to identify the major metabolites in MESC rather than the previously known isolated compounds, improving our knowledge of its chemical constituents. The flavones apigenin, acacetin, baicalein, luteolin, and diosmetin, and the flavonol aglycones quercetin, kaempferol, isorhamnetin, gossypetin, and myricetin and/or their glycosides and glucuronic derivatives were the major identified compounds. The hepatoprotective activity of MESC was evaluated by measuring catalase activity using UV spectrophotometry, inflammatory cytokines and apoptotic markers using ELISA techniques, and genetic markers using PCR. Paracetamol toxicity caused a significant increase in plasma caspase 2, cytokeratin 18 (CK18), liver tumor necrosis factor-α (TNF-α), interleukin 6 (IL-6), miRNA-34a, and miRNA-223, as well as a significant decrease in liver catalase (CAT) activity and in the levels of liver nuclear factor 1α (HNF-1α), sirtuin-1, and C/ebpα. Oral pretreatment with MESC (200 mg/kg) showed a significant decrease in caspase 2, CK18, TNF-α, IL-6 and a significant increase in liver CAT activity. MESC decreased the levels of liver miRNA-34a and miRNA-223 and induced HNF-1α, sirtuin-1, and C/ebpα gene expression. The histological examination showed a significant normalization in rats pretreated with MESC. Our findings showed that Saussurea costus may exert a potent hepatoprotective activity through the modulation of the expression of cellular cytokines, miRNA-34a, and miRNA-223.


Assuntos
MicroRNAs , Saussurea , Animais , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Proteína alfa Estimuladora de Ligação a CCAAT/metabolismo , Caspase 2/metabolismo , Catalase/metabolismo , Fator 1-alfa Nuclear de Hepatócito/metabolismo , Interleucina-6/metabolismo , MicroRNAs/genética , MicroRNAs/metabolismo , Extratos Vegetais/química , Raízes de Plantas , Ratos , Saussurea/química , Sirtuína 1/genética , Sirtuína 1/metabolismo , Espectrometria de Massas em Tandem , Fator de Necrose Tumoral alfa/metabolismo
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