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1.
J Sci Food Agric ; 103(1): 164-175, 2023 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-35837792

RESUMO

BACKGROUND: Sophora alopecuroides L. is a leguminous plant commonly found in northwest China. In Xinjiang, the fresh herb of S. alopecuroides is often applied as a green fertilizer to the rhizosphere of melon (Cucumis melo) plants at the end of their flowering period, to improve the taste of the fruits. However, the effects of S. alopecuroides-based fertilizers on the microbial community structure of soil and crop-root systems are unclear. In order to study the sweetening mechanism of the S. alopecuroides organic fertilizer, three different varieties of melon were selected. The untreated plants were used as the control (CK) group, and the plants treated with S. alopecuroides-based organic fertilizer were selected as the treatment (T) group. The physical and chemical properties, enzyme activities and microbial community structure of the rhizosphere samples were also determined, and a correlation analysis with the fruit sweetness index was conducted. RESULTS: Sugar content of group T was at least 40% higher than that of group CK. The increase in fruit sugar content positively correlated with the increase in the abundance of beneficial microorganisms, including Pseudomonas, Bacillus, Mycobacterium, Burkholderia, Streptomyces, Acinetobacter, Proteobacteria, Lysobacter, Actinomycetes, Penicillium and Aspergillus. CONCLUSION: Sophora alopecuroides organic fertilizer could alter the composition and function of bacterial and fungal communities and promote the growth of beneficial bacteria in the melon plant rhizosphere. Further, it could increase the content of soluble solids and sugar in the fruits to achieve a sweetening effect. This fertilizer can be applied as a fruit sweetener in melon cultivation, improving the sugar content of the fruit and consequently the sweetness. © 2022 Society of Chemical Industry.


Assuntos
Cucurbitaceae , Microbiota , Sophora , Fertilizantes/análise , Rizosfera , Frutas/química , Microbiologia do Solo , Solo/química , Bactérias/genética , Açúcares
2.
J Ethnopharmacol ; 301: 115799, 2023 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-36216196

RESUMO

ETHNOPHARMACOLOGY RELEVANCE: Sophora flavescens is a frequently used traditional Chinese medicine (TCM) for the treatment of skin disorders, diarrhea, vaginal itching and inflammatory diseases. In particular, the root of S. flavescens combination with other herbs mainly treat eczema ailment in the clinical applications. However, a holistic network pharmacology approach to understanding the mechanism by which alkaloids in S. flavescens treat eczema has not been pursued. AIM OF THE STUDY: To examine the network pharmacological potential effect of S. flavescens on eczema, we studied the alkaloids, performed protein targets prediction and investigated interacting signal pathways. Furthermore, animal experiment was carried out to evaluate its efficacy and real-time quantitative polymerase chain reactions (RT-qPCR) analysis was explored the mechanism of action. MATERIALS AND METHODS: The detail information on alkaloids from S. flavescens were obtained from a handful of public databases on the basis of oral bioavailability (OB ≥ 30%) and drug-likeness (DL ≥ 0.18). Then, correlations between compounds and protein targets were linked using the STRING database, and targets associated with eczema were gathered by the GeneCards database. Human genes were identified and subjected to Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis and Gene Ontology (GO) functional enrichment analysis. Particularly, matrine, the crucial alkaloid from S. flavescens, was estimated using a 2,4-dinitrochlorobenzene (DNCB)-induced eczema Kunming (KM) mice model, administered (50 mg/kg and 10 mg/kg) to mice for 22 days. On the last day, the activities of serum tumor necrosis factor α (TNF-α), interleukin-4 (IL-4) and histopathologic examinations were determined. For further to elucidate the mechanisms, the mRNA levels of TNF-α, STAT3, TP53, AKT1, IL-6, JUN and EGFR in dorsal skin tissues were also tested. RESULTS: Network analysis collected and identified 35 alkaloids from S. flavescens. Among them, in total 10 dominating alkaloids, including matrine, oxymatrine, sophoridine, sophocarpine, oxysophocarpine, allomatrine, sophoramine, anagyrine, cytisine and N-methylcytisine. And 71 related targets were provided of alkaloids for the treatment of eczema from S. flavescens. Furthermore, matrine dose-dependently (50 or 10 mg/kg, 22 days, apply to dorsal skin) remarkable decreased the serum levels of TNF-α and IL-4, and significantly alleviated the skin lesions. The effects of 50 mg/kg of matrine were almost identical to those of 200 mg/kg of the positive drug dexamethasone (DXM). The further RT-qPCR analyses could reveal that matrine down-regulate TNF-α, STAT3 and TP53 at transcriptional level in dorsal skin tissues. CONCLUSION: Pharmacological network analysis can utilize to illuminate the pharmacodynamic substances and the potential molecular mechanism of S. flavescens for treating eczema. Matrine, as the crucial alkaloid from S. flavescens, could be a promising drug candidate for the treatment of eczema ailment.


Assuntos
Alcaloides , Eczema , Sophora , Humanos , Camundongos , Animais , Interleucina-4 , Fator de Necrose Tumoral alfa , Farmacologia em Rede , Quinolizinas/farmacologia , Quinolizinas/uso terapêutico , Alcaloides/farmacologia , Alcaloides/uso terapêutico , Alcaloides/análise
3.
BMC Plant Biol ; 22(1): 144, 2022 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-35337273

RESUMO

Sophora davidii is an important plant resource in the karst region of Southwest China, but S. davidii plant-height mutants are rarely reported. Therefore, we performed phenotypic, anatomic structural, transcriptomic and metabolomic analyses to study the mechanisms responsible for S. davidii plant-height mutants. Phenotypic and anatomical observations showed that compared to the wild type, the dwarf mutant displayed a significant decrease in plant height, while the tall mutant displayed a significant increase in plant height. The dwarf mutant cells were smaller and more densely arranged, while those of the wild type and the tall mutant were larger and loosely arranged. Transcriptomic analysis revealed that differentially expressed genes (DEGs) involved in cell wall biosynthesis, expansion, phytohormone biosynthesis, signal transduction pathways, flavonoid biosynthesis and phenylpropanoid biosynthesis were significantly enriched in the S. davidii plant-height mutants. Metabolomic analysis revealed 57 significantly differential metabolites screened from both the dwarf and tall mutants. A total of 8 significantly different flavonoid compounds were annotated to LIPID MAPS, and three metabolites (chlorogenic acid, kaempferol and scopoletin) were involved in phenylpropanoid biosynthesis and flavonoid biosynthesis. These results shed light on the molecular mechanisms of plant height in S. davidii mutants and provide insight for further molecular breeding programs.


Assuntos
Sophora , Transcriptoma , Perfilação da Expressão Gênica , Metabolômica , Reguladores de Crescimento de Plantas/metabolismo , Sophora/genética , Sophora/metabolismo
4.
Molecules ; 27(17)2022 Aug 29.
Artigo em Inglês | MEDLINE | ID: mdl-36080327

RESUMO

The roots of Sophora tonkinensis Gagnep., a traditional Chinese medicine, is known as Shan Dou Gen in the Miao ethnopharmacy. A large number of previous studies have suggested the usage of S. tonkinensis in the folk treatment of lung, stomach, and throat diseases, and the roots of S. tonkinensis have been produced as Chinese patent medicines to treat related diseases. Existing phytochemical works reported more than 300 compounds from different parts and the endophytic fungi of S. tonkinensis. Some of the isolated extracts and monomer compounds from S. tonkinensis have been proved to exhibit diverse biological activities, including anti-tumor, anti-inflammatory, antibacterial, antiviral, and so on. The research progress on the phytochemistry and pharmacological activities of S. tonkinensis have been systematically summarized, which may be useful for its further research.


Assuntos
Sophora , Anti-Inflamatórios/análise , Anti-Inflamatórios/farmacologia , Fungos , Medicina Tradicional Chinesa , Compostos Fitoquímicos/análise , Raízes de Plantas/química , Sophora/química
5.
J Am Chem Soc ; 144(35): 15938-15943, 2022 09 07.
Artigo em Inglês | MEDLINE | ID: mdl-36006400

RESUMO

(+)-Matrine and (+)-isomatrine are tetracyclic alkaloids isolated from the plant Sophora flavescens, the roots of which are used in traditional Chinese medicine. Biosynthetically, these alkaloids are proposed to derive from three molecules of (-)-lysine via the intermediacy of the unstable cyclic imine Δ1-piperidine. Inspired by the biosynthesis, a new dearomative annulation reaction has been developed that leverages pyridine as a stable surrogate for Δ1-piperidine. In this key transformation, two molecules of pyridine are joined with a molecule of glutaryl chloride to give the complete tetracyclic framework of the matrine alkaloids in a single step. Using this dearomative annulation, isomatrine is synthesized in four steps from inexpensive commercially available chemicals. Isomatrine then serves as the precursor to additional lupin alkaloids, including matrine, allomatrine, isosophoridine, and sophoridine.


Assuntos
Alcaloides , Sophora , Alcaloides/química , Piperidinas , Piridinas , Quinolizinas/química , Sophora/química
6.
Contrast Media Mol Imaging ; 2022: 1250755, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36017023

RESUMO

For the treatment of trichomonas vaginitis, a combination therapy of metronidazole vaginal effervescent tablet combined with Flavescentis Sophora suppository is proposed. The patients diagnosed with trichomonas vaginitis are divided into the conventional treatment group and the joint group. The conventional group is treated with metronidazole vaginal effervescent tablets, and the joint group is treated with metronidazole vaginal effervescent tablets combined with sophora bolt. Both groups are treated for 3 months to observe the therapeutic effect of the two treatment methods. The expressions of IL-2 and IL-13 in serum of patients are detected by the ELISA. The changes in the vaginal pH value and cleanliness at each time point are observed. The patients are followed up for 6 months after treatment in order to observe the recurrence of trichomonas vaginitis in both groups. Experimental results show that the combination of the two tablets can further improve the clinical efficacy and reduce the inflammatory response and effectively improve the PH value and cleanliness of the vagina, and the recurrence rate is lower, which is worthy of clinical application.


Assuntos
Sophora , Vaginite por Trichomonas , Feminino , Humanos , Metronidazol/metabolismo , Metronidazol/uso terapêutico , Comprimidos/metabolismo , Comprimidos/uso terapêutico , Vaginite por Trichomonas/tratamento farmacológico , Vaginite por Trichomonas/metabolismo , Vagina/metabolismo
7.
J Ethnopharmacol ; 297: 115500, 2022 Oct 28.
Artigo em Inglês | MEDLINE | ID: mdl-35863614

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: Ulcerative colitis (UC) is relevant to dysregulation of inflammation and immune processes. Sophora flavescens Aiton is a classic medicine widely used in the treatment of UC in ancient and modern China, alkaloids and flavonoids are the main components. Previous studies reveal that Sophora flavescens Aiton total flavonoids extracts (SFE) exert an anti-UC effect by regulating the intestinal microbe structure and restoring the balance of the "host-microbe" co-metabolic network in UC mice. However, whether SFE influences immune inflammation remains unclear, which is the core link to UC disease. It also remains to be verified flavonoids are the material basis that plays a role in SFE. AIM OF THE STUDY: To identify the action mechanism of the immune-inflammatory regulation of SFE and its main active component Kurarinone against UC. METHODS: This study constructed UC mice and abnormal immune RAW 264.7 cell models, and subsequently used western blotting and flow cytometry (FCM) to evaluate the effects of SFE on the NF-κB pathway and the regulation of immunity in UC mice. Kurarinone was screened from flavonoid compounds of SFE by lipopolysaccharide (LPS)-induced RAW 264.7 cells, and its effect was subsequently investigated in UC mice. Western blotting, ELISA, FCM, and RT-PCR were used to determine the regulation of Kurarinone on the Th17/Treg differentiation and the JAK2/STAT3 signaling pathway. RESULTS: SFE regulated the differentiation of Th17/Treg in peripheral blood and inhibited immune-inflammatory response to treat UC. Various flavonoid components in SFE inhibited the synthesis of IL-6 and TNF-α in RAW 264.7 cells, among which Kurarinone had better effect. This study revealed the therapeutic effects of Kurarinone in UC mice for the first time. Kurarinone promoted the secretion of SIgA to improve the regulation of the intestinal mucosal barrier and resistance to pathogens. It also regulated the transcription level of RORγt and Foxp3 in colon, decreased the expression of pro-inflammatory factor IL-17A and up-regulated the expression of immunosuppressive factors TGF-ß1 and IL-10 in colon. Furthermore, Kurarinone restored intestinal immune system homeostasis by down-regulating the JAK2/STAT3 signaling pathway and regulating the balance of Th17/Treg cell differentiation in UC. CONCLUSIONS: SFE, especially the flavonoid ingredients represented by Kurarinone, has significant effects on immunoregulation against UC. And their mechanism of effect is related to inhibiting the activation of JAK2/STAT3 signaling pathway and regulating differentiation of Th17/Treg cells. KEYWORK: Immunoregulatory; Kurarinone; Th17 cells; Treg cells; Ulcerative colitis.


Assuntos
Colite Ulcerativa , Colite , Sophora , Animais , Colite/metabolismo , Colite Ulcerativa/induzido quimicamente , Colite Ulcerativa/tratamento farmacológico , Modelos Animais de Doenças , Flavonoides/metabolismo , Flavonoides/farmacologia , Flavonoides/uso terapêutico , Homeostase , Inflamação/metabolismo , Camundongos , Linfócitos T Reguladores , Células Th17
8.
Plant Sci ; 322: 111347, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35700842

RESUMO

Sophora japonica is a leguminous tree species native to China. To explore the nitrogen (N) source preference and its impact on stress tolerance, a hydroponic experiment was designed in which S. japonica seedlings were supplied with sole ammonium (NH4+) or sole nitrate (NO3-) nutrition under 75 mM NaCl-induced salt stress. The growth and N metabolism performance were investigated. In the absence of NaCl, plants fed NH4+ showed better root growth than those fed NO3-, but there was no difference in aerial part growth. Salinity inhibited the root growth of NH4+-fed plants and the shoot growth of NO3--fed plants, while the total N accumulation was suppressed under either N form. Specifically, in NH4+-fed plants, salinity significantly increased the net photosynthetic rate, root NH4+ content and root antioxidant enzyme activities. Higher nitrate reductase (NR) activities but lower glutamate synthetase (GS) activities were observed in both leaves and roots. Leaf AMT1.1 and AMT2.1a in NH4+-fed plants positively reacted to salt stress, whereas the expression of four AMTs was reduced or remained unchanged in roots. In contrast, salinity suppressed the net photosynthetic rate, antioxidant enzyme activities, and GS activity in the leaves of NO3--fed plants. Upregulation of NPF1.2, NPF2.11, NPF4.6 and NPF7.3, as well as unaltered NR activity, caused higher NO3- content in the leaves. Moreover, NR and glutamate synthase (GOGAT) activities together with the transcription of most NRTs were promoted by salinity in the roots of NO3--fed plants. Additionally, compared to those treated with NH4+, in response to salinity, NO3--treated seedlings showed more intensive repression of the net photosynthetic rate, chlorophyll content, and both shoot and root growth. Overall, these results suggest that S. japonica plants grew better in NH4+ medium than in NO3- medium, and the different N metabolism responses improved S. japonica tolerance to salinity with NH4+ application. This study provides new insights for understanding the mechanism of salt tolerance, breeding resistant varieties of S. japonica, and developing scientific fertilization management strategies during the seedling cultivation period.


Assuntos
Compostos de Amônio , Sophora , Compostos de Amônio/metabolismo , Antioxidantes/metabolismo , Glutamato-Amônia Ligase/metabolismo , Nitratos/metabolismo , Nitrogênio/metabolismo , Melhoramento Vegetal , Raízes de Plantas/metabolismo , Salinidade , Plântula , Cloreto de Sódio/metabolismo , Cloreto de Sódio/farmacologia , Sophora/metabolismo
9.
Food Chem ; 393: 133395, 2022 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-35691061

RESUMO

Sophora japonica flower, rich in rutin, is a homology of medicine and food that can be used as an anti-inflammatory agent. Its effects and mechanisms against intestinal inflammation are unknown. In this study, S. japonica flower extracts (SFE) or rutin were administrated to chemically induced-colitic mice. The results showed that SFE or rutin regulated inflammation and oxidative stress in colitic mice. The colonic permeability was significantly improved by SFE or rutin, which was characterized by the higher levels of tight junction proteins and serum lower levels of FITC-Dextran and endotoxins. The inactivation of the NF-κB pathway by SFE or rutin may contribute to the anti-colitis effects. In colitic mice, SFE or rutin partially restored gut microbiota dysbiosis, as seen by increases in potential probiotics (e.g., Faecalibaculum rodentium) and decreases in potentially disease-related bacteria (e.g., Romboutsia ilealis and Eubacterium fissicatena group).


Assuntos
Colite , Microbioma Gastrointestinal , Sophora , Animais , Colite/induzido quimicamente , Colite/tratamento farmacológico , Colite/genética , Sulfato de Dextrana , Modelos Animais de Doenças , Flores/química , Inflamação/tratamento farmacológico , Camundongos , NF-kappa B/genética , NF-kappa B/metabolismo , Compostos Fitoquímicos/análise , Rutina/análise , Rutina/farmacologia , Transdução de Sinais , Sophora/química
10.
Vet Parasitol ; 306: 109731, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-35643574

RESUMO

Ichthyophthirius multifiliis, a global distributed protozoan parasite, causes "White spot disease" and leads to serious mortality of freshwater fish in aquaculture. The present study was conducted to assess the anti-I. multifiliis efficacy of active compound isolated from Sophora flavescens. The isolated active compound was identified as sophoraflavanone G (SG) with ESI-MS and NMR. In vitro tests, SG at concentrations of 0.5 mg/L and 2 mg/L resulted in death of all theronts and tomonts, respectively; SG at concentrations of 0.125 mg/L and 0.25 mg/L notably decreased theronts infectivity (p < 0.05). Additionally, the in vivo test results showed that a cumulative delivery of SG at concentration of 2 mg/L for 7 days protected fish from I. multifiliis infection. The 96-h LC50 (median lethal concentration) and safety concentration of SG to grass carp were 46.6 mg/L and 11.3 mg/L, respectively. The present work indicated that SG was a potential safe and effectively therapeutic agent in treating I. multifiliis.


Assuntos
Infecções por Cilióforos , Doenças dos Peixes , Hymenostomatida , Parasitos , Sophora , Animais , Infecções por Cilióforos/tratamento farmacológico , Infecções por Cilióforos/parasitologia , Infecções por Cilióforos/veterinária , Doenças dos Peixes/tratamento farmacológico , Doenças dos Peixes/parasitologia , Flavanonas
11.
Int J Mol Sci ; 23(11)2022 May 29.
Artigo em Inglês | MEDLINE | ID: mdl-35682783

RESUMO

Sophoraflavanone G (SG), isolated from Sophora flavescens, has anti-inflammatory and anti-tumor bioactive properties. We previously showed that SG promotes apoptosis in human breast cancer cells and leukemia cells and reduces the inflammatory response in lipopolysaccharide-stimulated macrophages. We investigated whether SG attenuates airway hyper-responsiveness (AHR) and airway inflammation in asthmatic mice. We also assessed its effects on the anti-inflammatory response in human tracheal epithelial cells. Female BALB/c mice were sensitized with ovalbumin, and asthmatic mice were treated with SG by intraperitoneal injection. We also exposed human bronchial epithelial BEAS-2B cells to different concentrations of SG to evaluate its effects on inflammatory cytokine levels. SG treatment significantly reduced AHR, eosinophil infiltration, goblet cell hyperplasia, and airway inflammation in the lungs of asthmatic mice. In the lungs of ovalbumin-sensitized mice, SG significantly promoted superoxide dismutase and glutathione expression and attenuated malondialdehyde levels. SG also suppressed levels of Th2 cytokines and chemokines in lung and bronchoalveolar lavage samples. In addition, we confirmed that SG decreased pro-inflammatory cytokine, chemokine, and eotaxin expression in inflammatory BEAS-2B cells. Taken together, our data demonstrate that SG shows potential as an immunomodulator that can improve asthma symptoms by decreasing airway-inflammation-related oxidative stress.


Assuntos
Asma , Hipersensibilidade Respiratória , Sophora , Animais , Anti-Inflamatórios/metabolismo , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/uso terapêutico , Asma/metabolismo , Líquido da Lavagem Broncoalveolar , Citocinas/metabolismo , Eosinófilos/metabolismo , Feminino , Flavanonas , Inflamação/patologia , Pulmão/patologia , Camundongos , Camundongos Endogâmicos BALB C , Ovalbumina/metabolismo , Estresse Oxidativo , Hipersensibilidade Respiratória/metabolismo , Sophora/metabolismo
12.
Bioorg Med Chem ; 64: 116724, 2022 06 15.
Artigo em Inglês | MEDLINE | ID: mdl-35468537

RESUMO

Quinolizidine alkaloids, as essential active ingredients extracted from Sophora alopecuroides Linn (SAL), have been proven to be pharmacologically active in a variety of cancers including non-small cell lung cancer (NSCLC). However, whether these alkaloids have substantial benefits in combination with immune checkpoint blockade (ICB) for the treatment of NSCLC is unknown. Here, we explore the potential of these alkaloids in combination with ICB therapy based on a systems pharmacology and bioinformatics approach. We found that 37 alkaloids in SAL have highly similar characteristics in the molecular skeleton, pharmacological properties, and targets. The expression of targets of these alkaloids are significantly correlated with the infiltration level of tumor infiltrating lymphocytes and the expression levels of multiple immune checkpoints in NSCLC. They share similar molecular mechanisms in antitumor immunity. Sophocarpine (Sop) is one of the most representative constituents of these alkaloids. We demonstrated that the Sop promotes PD-L1 expression to improve the effects of PD-L1 blockade treatment via the ADORA1-ATF3 axis. In conclusion, our study identified these alkaloids as promising candidates for the treatment of NSCLC, either alone or in combination with ICB, with potential value for drug development and may provide a promising strategy for improving the survival of NSCLC patients.


Assuntos
Alcaloides , Carcinoma Pulmonar de Células não Pequenas , Neoplasias Pulmonares , Sophora , Alcaloides/farmacologia , Alcaloides/uso terapêutico , Antígeno B7-H1 , Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Humanos , Inibidores de Checkpoint Imunológico , Neoplasias Pulmonares/tratamento farmacológico , Farmacologia em Rede
13.
Sheng Wu Gong Cheng Xue Bao ; 38(4): 1565-1575, 2022 Apr 25.
Artigo em Chinês | MEDLINE | ID: mdl-35470627

RESUMO

8-prenylnaringenin (8-PN) is a potent estrogen with high medicinal values. It also serves as an important precursor for many prenylated flavonoids. Microbial synthesis of 8-PN is mainly hindered by the low catalytic activity of prenyltransferases (PTS) and insufficient supply of precursors. In this work, a SfN8DT-1 from Sophora flavescens was used to improve the efficiency of (2S)-naringenin prenylation. The predicted structure of SfN8DT-1 showed that its main body is comprised of 9 α-helices and 8 loops, along with a long side chain formed by nearly 120 amino acids. SfN8DT-1 mutants with different side-chain truncated were tested in Saccharomyces cerevisiae. A mutant expressing the truncated enzyme at K62 site, designated as SfND8T-1-t62, produced the highest 8-PN titer. Molecular docking of SfN8DT-1-t62 with (2S)-naringenin and dimethylallyl diphosphate (DMAPP) showed that K185 was a potentially crucial residue. Alanine scanning within a range of 0.5 nm around these two substrates showed that the mutant K185A may decrease its affinity to substrates, which also indicated K185 was a potentially critical residue. Besides, the mutant K185W enhanced the affinity to ligands implied by the simulated saturation mutation, while the saturated mutation of K185 showed a great decrease in 8-PN production, indicating K185 is vital for the activity of SfN8DT-1. Subsequently, overexpressing the key genes of Mevalonate (MVA) pathway further improved the titer of 8-PN to 31.31 mg/L, which indicated that DMAPP supply is also a limiting factor for 8-PN synthesis. Finally, 44.92 mg/L of 8-PN was produced in a 5 L bioreactor after 120 h, which is the highest 8-PN titer reported to date.


Assuntos
Dimetilaliltranstransferase , Flavanonas/biossíntese , Sophora , Dimetilaliltranstransferase/genética , Dimetilaliltranstransferase/metabolismo , Flavonoides/metabolismo , Simulação de Acoplamento Molecular , Prenilação , Saccharomyces cerevisiae/genética , Saccharomyces cerevisiae/metabolismo , Sophora/genética , Sophora/metabolismo
14.
Artigo em Inglês | MEDLINE | ID: mdl-35395445

RESUMO

Diabetic retinopathy (DR) is the most common microvascular complication of diabetes and a leading cause of vision impairment and blindness, which lacks effective diagnostic measures and therapeutic options. Sophora flavescens Aiton or "Kushen" is a traditional Chinese medicine used since ancient times, either alone or in combination, to clear heat, dampness, and tearing, and to treat ocular diseases and improve eyesight. Additionally, the flavonoids of Sophora flavescens Aiton extracted using ethyl acetate (EtOAc) (SFE) is effective in managing diabetes and diabetic vascular complications. In this study, we explored the pharmacodynamic effects and material basis of action of SFE on DR for the first time and elucidated the mechanism based on untargeted retinal metabolomics. Results from the pharmacodynamic studies showed that SFE could reduce blood glucose levels in rats, regulate serum lipopolysaccharide, tauroursodeoxycholic acid, and trimethylamine oxide levels, and significantly improve the structure of retina in rats with DR. Moreover, SFE could protect the blood-retinal barrier, reduce angiogenesis and capillary formation, and inhibit retinal nerve cell apoptosis. A total of 13 compounds were identified in the aqueous humor and retina, which were dihydroflavonoid, isoflavonoid, pterostane flavonoid, chalcone, and dihydroflavonol derivatives. In addition, 39 differential metabolites were screened based on retinal metabolomics data and 23 were found to be affected by SFE, indicating its anti-DR effect by regulating the synthetic metabolic pathways, including lactose, bile acid, glycerophospholipid, arginine, purine, and pyrimidine metabolism pathways. Collectively, our findings elucidated the effects, material basis, and treatment mechanism of SFE on DR systematically and could lay the foundation for promoting the clinical application of Sophora flavescens Aiton.


Assuntos
Diabetes Mellitus , Retinopatia Diabética , Sophora , Acetatos , Animais , Retinopatia Diabética/tratamento farmacológico , Flavonoides/química , Flavonoides/farmacologia , Metabolômica/métodos , Extratos Vegetais/química , Ratos , Retina , Sophora/química
15.
Bioorg Med Chem ; 61: 116723, 2022 05 01.
Artigo em Inglês | MEDLINE | ID: mdl-35396127

RESUMO

Alopecurosines A and B (CMs 1 and 2, respectively) are two novel cytisine-type alkaloid dimers first isolated from the aerial parts of Sophora alopecuroides L. CMs 1 and 2 are new dimeric alkaloids whose piperidine matrine ring is cleaved and connected via the N'-1 bond. Their chemical structures have been confirmed by IR, UV, HR-ESI-MS, and NMR. Preliminary screening shows that they have topoisomerase I (Topo I)-based anti-tumor activity. Their Topo I inhibitory activities and mechanism have been evaluated by agarose gel electrophoresis assay and a molecular docking study. The results show that the inhibition rate of CM 1 is 82.26% at 1 mM concentration and that it exhibits significantly Topo I inhibitory activity. Further research has illustrated that CMs 1 and 2 exert inhibitory activity by stabilising the Topo I-DNA cleavage complex, implying that they have the potential to be developed as novel Topo I inhibitors.


Assuntos
Alcaloides , Sophora , Alcaloides/química , Azocinas , Simulação de Acoplamento Molecular , Quinolizinas , Sementes/química , Sophora/química
16.
DNA Res ; 29(3)2022 May 27.
Artigo em Inglês | MEDLINE | ID: mdl-35466378

RESUMO

Sophora japonica is a medium-size deciduous tree belonging to Leguminosae family and famous for its high ecological, economic and medicinal value. Here, we reveal a draft genome of S. japonica, which was ∼511.49 Mb long (contig N50 size of 17.34 Mb) based on Illumina, Nanopore and Hi-C data. We reliably assembled 110 contigs into 14 chromosomes, representing 91.62% of the total genome, with an improved N50 size of 31.32 Mb based on Hi-C data. Further investigation identified 271.76 Mb (53.13%) of repetitive sequences and 31,000 protein-coding genes, of which 30,721 (99.1%) were functionally annotated. Phylogenetic analysis indicates that S. japonica separated from Arabidopsis thaliana and Glycine max ∼107.53 and 61.24 million years ago, respectively. We detected evidence of species-specific and common-legume whole-genome duplication events in S. japonica. We further found that multiple TF families (e.g. BBX and PAL) have expanded in S. japonica, which might have led to its enhanced tolerance to abiotic stress. In addition, S. japonica harbours more genes involved in the lignin and cellulose biosynthesis pathways than the other two species. Finally, population genomic analyses revealed no obvious differentiation among geographical groups and the effective population size continuously declined since 2 Ma. Our genomic data provide a powerful comparative framework to study the adaptation, evolution and active ingredients biosynthesis in S. japonica. More importantly, our high-quality S. japonica genome is important for elucidating the biosynthesis of its main bioactive components, and improving its production and/or processing.


Assuntos
Sophora , Cromossomos , Genoma , Humanos , Filogenia , Sequências Repetitivas de Ácido Nucleico , Sophora/genética
17.
Curr Comput Aided Drug Des ; 18(3): 228-239, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35388762

RESUMO

BACKGROUND: The compound Sophora flavescenes (Kushen) decoction was found to reduce the inflammatory symptom of Ulcerative Colitis (UC). However, there exists a very limited understanding of the molecular pharmacological mechanisms. OBJECTIVE: This study aimed to explore the mechanism of compound Sophora flavescens (Kushen) decoction in treating ulcerative colitis from the perspective of network pharmacology. METHODS: Active components and potential targets of compound Sophora flavescens (Kushen) decoction were obtained through the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP) database. GeneCards and other databases were used to predict and screen ulcerative colitis-related genes. Cytoscape software was applied to construct the "drugactive component-disease-target" network. GO function and KEGG pathway enrichment analyses revealed the potential pathway of the compound Sophora flavescenes (Kushen) decoction for UC. RESULTS: After the screening, a total of 124 active ingredients and 163 potential therapeutic targets for UC were obtained from the compound Sophora flavescens (Kushen) decoction. Protein interaction network analysis showed that 15 key targets could be identified for the possible treatment of UC. GO and KEGG analyses showed that the active ingredients in the compound Sophora flavescens (Kushen) decoction were mainly enriched in 2556 biological processes and 172 signaling pathways. CONCLUSION: The study showed that the compound Sophora flavescens (Kushen) decoction has therapeutic effects on UC through multi-component, multi-target, and multi-pathway.


Assuntos
Colite Ulcerativa , Sophora , Colite Ulcerativa/tratamento farmacológico , Colite Ulcerativa/genética , Medicamentos de Ervas Chinesas , Simulação de Acoplamento Molecular , Farmacologia em Rede , Tecnologia
18.
Lett Appl Microbiol ; 75(1): 70-80, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35322896

RESUMO

Natural products, including honey, total alkaloids of Sophora alopecuroides (TASA) and matrine have been used in combination with antibiotics against various pathogenic bacteria. However, there are limited data on the antibacterial activity of these natural products in combination against multidrug-resistant Pseudomonas aeruginosa strains. The in vitro activity of honey, TASA and matrine alone and in combination with antibiotics against P. aeruginosa isolates was investigated. In this study, four biofilm-producing P. aeruginosa isolates, which were resistant to multiple antibiotics, were used. These natural products were not the most effective single agent against four isolates. The fractional inhibitory concentration index method revealed the synergistic effect of matrine and TASA-honey in combination with ciprofloxacin (Cip) against all tested isolates. When these combinations were used, the resistance of isolates to Cip was decreased significantly (six to eightfold reduction in the minimum inhibitory concentration of Cip. The disk diffusion method showed that all isolates were resistant to ß-lactams. Combinations of these antibiotics with TASA and matrine changed slightly the activity of either antibiotic used as a single agent. All isolates produced metallo-ß-lactamase enzymes (MBL). Pretreatment isolates with Cip-matrine and Cip-TASA-honey resulted in a statistically downregulated expression of the mexA gene. These natural products can be used against overactivating MexAB-OprM but not MBL-producing P. aeruginosa isolates.


Assuntos
Alcaloides , Produtos Biológicos , Mel , Sophora , Alcaloides/metabolismo , Alcaloides/farmacologia , Antibacterianos/metabolismo , Produtos Biológicos/farmacologia , Ciprofloxacina/farmacologia , Testes de Sensibilidade Microbiana , Pseudomonas aeruginosa , Quinolizinas , beta-Lactamases/genética
19.
Phytomedicine ; 100: 154054, 2022 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-35358931

RESUMO

BACKGROUND: Sophora flavescens Aiton (SF), also known as Kushen (Chinese:), has been an important species in Chinese medicine since the Qin and Han dynasties. It is also recognized as a plant resource suitable for the globalization of Chinese medicine. Traditionally, it has been used in various ethnic medical systems in East Asia, especially in China, to kill insects and dispel dampness. Sophora flavescens is commonly used for clearing heat-clearing, killing worms, and diuretic. Nowdays, accumulating studies demonstrated its anticancer and cardioprotection. OBJECTIVE OF THE REVIEW: This paper aims to systematically review information on the genus, pharmacological and toxicological significance, chemical composition and biological activity of Sophora flavescens. To promoting its development and application. To summarize recent findings regarding to the metabolism, pharmacological/toxicological effects of Sophora flavescens. MATERIAL AND METHODS: Online academic databases (including PubMed, Google Scholar, Web of Science and CNKI) were searched using search terms of "Sophora flavescens Aiton", "Ku shen", "Pharmacology", "Active ingredient", "Toxicology" and combinations to include published studies of Sophora flavescens Aiton primarily from 1970-2021. Several critical previous studies beyond this period were also included and other related terms. CONCLUSION: Sophora flavescens has a broad spectrum of biological activities associated with Sophora flavescens has been considered a valuable resource in both traditional and modern medicine. However, there is a lack of in-depth studies on the medicinal uses of Sophora flavescens. Moreover, further studies on single chemical components should be conducted based on the diversity of chemical structures, significant biological activities and clinical applications. The discovery of its bioactive molecules and multi-component interactions would be of great importance for the clinical application of Sophora flavescens spp. Detailed pharmacological and toxicological studies on the classic prescriptions of Sophora flavescens are also needed. It is more beneficial to the wide application of SF plant and facilitates the worldwide promotion of modern Chinese medicine. However, an increasing number of reports indicate that the administration of Sophora flavescens has serious adverse effects. Its main toxic effects are neurotoxicity and acute toxicity, which have caused widespread concern worldwide. In addition, the alkaloids of Sophora flavescens are distributed in the heart, liver, stomach and large intestine. They are excreted from the body through gluconeogenesis, which is the mode of action of certain therapeutic mechanisms of action such as anticancer. The detailed metabolic study of alkaloids and other components of Sophora flavescens in vivo needs to be further investigated. It is important to improve the pharmacological effects and reduce the toxicity of Sophora flavescens. For this purpose, structural modification of active components of Sophora flavescens or combination with other drugs is very essential.


Assuntos
Alcaloides , Antineoplásicos , Sophora , Alcaloides/farmacologia , Biodiversidade , China , Etnofarmacologia , Medicina Tradicional Chinesa , Compostos Fitoquímicos/farmacologia , Sophora/química
20.
Sci Rep ; 12(1): 3301, 2022 02 28.
Artigo em Inglês | MEDLINE | ID: mdl-35228632

RESUMO

The total alkaloids extracted from the seeds of Sophora moorcroftiana (TAs-SM) have the potential to treat alveolar echinococcosis, a disease included by the WHO in a list of 17 key neglected diseases world-wide. The aims of the current study were first to develop a supercritical fluid extraction (SFE) method for optimizing TAs-SM extraction, and second, to develop an optimized method for evaluating TAs-SM pharmacokinetics in vivo. The Box-Behnken response surface method was used to optimize the extraction process, and ultra-high liquid chromatography coupled with high resolution electrospray mass spectrometry (UPLC-HR-ESI-MS) was used to determine the pharmacokinetics of TAs-SM in SD rats. The results indicated the following optimal SFE extraction conditions: pressure = 31 MPa, temperature = 70 °C, time = 162.18 min. With these parameters, total alkaloids could be extracted from each gram of S. moorcroftiana, with the total content being 68.88 µg. The linear range of UPLC-HR-ESI-MS is 0.78-200.00 ng/ml, R2 > 0.99, and the sample recovery is 99-113%. The precision, accuracy, selectivity and stability of the method meet the requirements of US FDA guidelines. To our knowledge this study is the first to establish an SFE method for extracting TAs-SM and the first to employ UPLC-HR-ESI-MS for measuring TAs-SM in rats. These findings provide important contributions for using TAs-SM in further drug development and clinical applications.


Assuntos
Alcaloides , Cromatografia com Fluido Supercrítico , Sophora , Alcaloides/química , Animais , Dióxido de Carbono/análise , Cromatografia Líquida de Alta Pressão/métodos , Cromatografia com Fluido Supercrítico/métodos , Ratos , Ratos Sprague-Dawley , Sementes/química , Sophora/química
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