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1.
Food Res Int ; 159: 111643, 2022 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-35940816

RESUMO

Trichosanthes kirilowii Maxim seed is a primary source of edible vegetable oil and possesses a high nutritional value, making them extremely beneficial to humanity. To promote the extraction process of Trichosanthes kirilowii Maxim seed oil, the effect of microwave heating time (700 W for 0, 2, 4, and 6 min) on lipid composition, chemical properties, and antioxidant activity of oils was studied. The results showed that the oil yield of the seed increased with the microwave heating time. Besides, microwave heating time significantly affects (p < 0.05) DPPH and tocopherols, and the IC50 value of DPPH was highest with microwave heating for 6 min, whatever the shells are reserved. The tocopherol content was highest with microwave heating for 2 min in the seed shell oil, which was 1930.60 mg/kg. The longer microwave heating time could improve the oil yield and antioxidant activity of Trichosanthes kirilowii Maxim seed oil. The seed shell also affects chemical properties, fatty acid composition, antioxidant activity, and tocopherol contents of the Trichosanthes kirilowii Maxim seed oil. The Trichosanthes kirilowii Maxim seed shell oil has higher DPPH and tocopherols contents than seed kernel oil, while seed kernel oils showed higher oil yield and acid value. Our finding is valuable for manufacturers to choose suitable means to produce Trichosanthes kirilowii Maxim seed oil of required qualities and chemical compositions for targeted use.


Assuntos
Trichosanthes , Antioxidantes/análise , Calefação , Micro-Ondas , Óleos Vegetais/análise , Sementes/química , Tocoferóis/análise , Trichosanthes/química
2.
Genet Res (Camb) ; 2022: 1792977, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35919037

RESUMO

Background: Oxidative stress is an important cause of liver disease and atherosclerosis. Natural substances with antioxidant activity are good drugs for treating liver disease and atherosclerosis. Trichosanthes kirilowii Peel Polysaccharide (TKPP) can remove DPPH (2,2-Diphenyl-1-picrylhydrazyl) free radicals and hydroxyl free radicals in vitro, which shows antioxidant activity. Therefore, it is speculated that it can protect human hepatoma cell line (HepG2) and umbilical artery smooth muscle cell (HUASMC) against oxidative damage by hydrogen peroxide (H2O2). Methods: Oxidative damage cell models of HepG2 and HUASMC were induced by H2O2. HepG2 and HUASMC were divided into blank group, H2O2 injury group, TKPP treatment group, and glutathione (GSH) positive control group. Cell Counting Kit-8 (CCK-8) was used to detect cell viability. The level of total GSH and the amount of Nitric oxide (NO) secreted by cells were detected by specific kits. The gene and protein expressions of catalase (CAT) and superoxide dismutase (SOD) were detected by fluorescence quantitative PCR and Western Blot. Results: In these two kinds of cells, compared with the control group, the survival rate, total GSH level, and NO secretion, CAT and SOD gene and protein expressions were significantly decreased in the H2O2 damaged group. In the TKPP treatment group, the cell survival rate was significantly elevated with the increase of the polysaccharide concentration, and the total GSH level, NO secretion, CAT and SOD gene expression, and protein expression levels were also significantly increased. Conclusion: TKPP can improve the activities of HepG2 and HUASMC cells damaged by H2O2 and protect the cellular antioxidant system.


Assuntos
Aterosclerose , Trichosanthes , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Glutationa/metabolismo , Glutationa/farmacologia , Humanos , Peróxido de Hidrogênio/toxicidade , Estresse Oxidativo , Polissacarídeos/farmacologia , Superóxido Dismutase/metabolismo , Superóxido Dismutase/farmacologia , Trichosanthes/metabolismo
3.
J Oleo Sci ; 71(6): 823-827, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35661064

RESUMO

Trichosanthes cucumerina seed and seed oil have been investigated for their chemical, physico-chemical properties, characterization and fatty acid profile. The properties were assessed by standard methods and the fatty acid profile was carried out using gas chromatography fatty acid methyl ester analysis. The seed was found to contain 71.1% crude oil, 1.6% Crude Protein, 2.9% carbohydrate, 2.8% crude Fiber, and 1.6% Ash. Iodine, Peroxide, and Acid the molecular weights of the seed oil are 0.84 gI2 of oil, 2.0 meq O2/kg oil and 4.0 mg/KOH/g, respectively, with 4.0 Free Fatty Acid and a Saponification Value of 379.12 mg/g. The oil is rich in polyunsaturated fatty acids that are vital for growth, maintenance of the cell membrane, development, and boosting of the immune system in humans. It qualifies to be classified as an edible vegetable oil and can also be useful in the soap and cosmetic industry.


Assuntos
Trichosanthes , Ácidos Graxos/análise , Ácidos Graxos não Esterificados/análise , Humanos , Óleos Vegetais/química , Sementes/química
4.
Nan Fang Yi Ke Da Xue Xue Bao ; 42(3): 384-391, 2022 Mar 20.
Artigo em Chinês | MEDLINE | ID: mdl-35426802

RESUMO

OBJECTIVE: To screen the effective antioxidant components in Trichosanthes extract based on the mean value of Deng's correlation degree and assess the antioxidant activity of the identified components. METHOD: High-performance liquid chromatography (HPLC) was used to obtain the fingerprints of Trichosanthes extract, and the clearance rates of DPPH · and O2-· by 3, 9 and 27 mg/mL Trichosanthes extract were determined. The antioxidant spectrum effect of Trichosanthes extract was analyzed by calculating the mean value of Deng's correlation degree to screen the effective antioxidant component group. According to the contents of each known components in the antioxidant effective component group, mixed solutions of the components were prepared and tested for their clearance rates of DPPH · and O2-·. RESULTS: The 36 common peaks in HPLC fingerprints of Trichosanthes extract showed different degrees of correlation with DPPH · and O2-· clearance. The common peaks with a correlation degree greater than the median value included peaks 21, 36, 8, 31, 14, 5, 27, 2, 24, 15, 18, 33, 22, 34, 35, 19, 28 and 25. The 5 components, namely kaempferol (peak 36), isoquercitrin (peak 8), luteolin (peak 31), rutin (peak 5) and apigenin (peak 35), were tentatively identified to constitute the effective antioxidant component group with a mass ratio 3∶2∶2∶ 1∶1 in Trichosanthes extract. The prepared mixed solutions of antioxidant effective component group (6.12, 2.04, and 0.68 µg/mL) showed clearance rates of DPPH · of 65.4%, 64.0% and 61.0%, and clearance rates of O2-· of 12.9%, 9.5% and 8.3%, respectively. CONCLUSION: We identified the material basis for the antioxidant activity of Trichosanthes and screened the antioxidant effective component group in Trichosanthes extract.


Assuntos
Trichosanthes , Antioxidantes/farmacologia , Cromatografia Líquida de Alta Pressão/métodos , Luteolina , Extratos Vegetais/farmacologia , Trichosanthes/química
5.
J Diabetes Res ; 2022: 3250016, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35224106

RESUMO

This study investigates the effects of the water-soluble and organic-soluble Trichosanthes extracts on the hyperglycemic condition in streptozotocin- (STZ-) induced diabetic rats. The blood glucose levels, body weights, water intake, and urine volumes of rats in different experimental groups were monitored throughout the experiment, and the results obtained indicate that the two extracts can effectively reduce blood sugar levels, increase body weights, and improve water intake and urine volumes in diabetic rats. Based on blood biochemical analyses, the two extracts play an important role in regulating the diabetes-induced lipid metabolism disorder, increasing the levels of insulin and C-peptide, and alleviating the symptoms of diabetes. The variation in the liver glycogen contents of the water-soluble fraction and ethanol fraction groups suggests that the mechanisms underlying the hypoglycemic effects of the two extracts are different. Indeed, the water-soluble fraction alleviates diabetes symptoms in rats mainly by antioxidative activity, unlike the ethanol fraction.


Assuntos
Diabetes Mellitus Tipo 1/tratamento farmacológico , Extratos Vegetais/metabolismo , Trichosanthes/metabolismo , Animais , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Antioxidantes/uso terapêutico , Glicemia/metabolismo , Diabetes Mellitus Tipo 1/fisiopatologia , Modelos Animais de Doenças , Hipolipemiantes/metabolismo , Hipolipemiantes/farmacologia , Hipolipemiantes/uso terapêutico , Insulina/sangue , Insulina/metabolismo , Insulina/uso terapêutico , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Ratos
6.
J Ethnopharmacol ; 285: 114893, 2022 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-34875347

RESUMO

ETHNOPHARMACOLOGICAL RELEVANCE: A mixture (SH003) of Astragalus membranaceus (Fisch.) Bunge, Angelica gigas Nakai, and Trichosanthes Kirilowii (Maxim.) has beneficial effects against several carcinomas. There have been few reports on an immune-enhancing activity of SH003 and its active constituent nodakenin. AIM OF THE STUDY: This study aimed at identifying the immune-enhancing effect of SH003 and nodakenin. MATERIALS AND METHODS: The immune-enhancing effect was evaluated using RAW264.7 macrophages, mouse primary splenocytes, and a cyclophosphamide (CP)-induced immunosuppression murine model. RESULTS: The results show that SH003 or nodakenin stimulated the production levels of granulocyte colony-stimulating factor, IL-12, IL-2, IL-6, TNF-α, and nitric oxide (NO) and the expression levels of iNOS in RAW264.7 macrophages. SH003 or nodakenin also enhanced NF-κB p65 activation in RAW264.7 macrophages. SH003 or nodakenin stimulated the production levels of IFN-γ, IL-12, IL-2, TNF-α, and NO and the expression levels of iNOS in splenocytes. SH003 or nodakenin increased the splenic lymphocyte proliferation and splenic NK cell activity. In addition, SH003 or nodakenin increased the levels of IFN-γ, IL-12, IL-2, IL-6, and TNF-α in the serum and spleen of CP-treated mice, alleviating CP-induced immunosuppression. CONCLUSION: Taken together, the results of this study show that SH003 improved immunosuppression through the activation of macrophages, splenocytes, and NK cells. These findings suggest that SH003 could be applied as a potential immunostimulatory agent for a variety of diseases caused or exacerbated by immunodeficiency.


Assuntos
Angelica/química , Astrágalo (Planta)/química , Cumarínicos/farmacologia , Glucosídeos/farmacologia , Fitoterapia , Trichosanthes/química , Animais , Cumarínicos/química , Ciclofosfamida/toxicidade , Citocinas/genética , Citocinas/metabolismo , Regulação da Expressão Gênica/efeitos dos fármacos , Glucosídeos/química , Imunossupressores/toxicidade , Células Matadoras Naturais/efeitos dos fármacos , Macrófagos , Camundongos , NF-kappa B , Baço/citologia
7.
Nutr Cancer ; 74(1): 333-345, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-33544002

RESUMO

AIM: Hepatocellular carcinoma (HCC) is one of the most common malignant tumors. TKP is a serine protease extracted from the fruit of Trichosanthes kirilowii. We investigated the impact of TKP on the proliferation of HCC cells and its underlying mechanisms. METHODS: Bel-7402 and HepG2 cell viability and colony formation capacity were evaluated using MTT and colony formation assays, respectively. Glucose uptake and lactate production were determined using glucose and lactate assay kits. The mRNA expressions of GLUT1, PDK, LDHA, PKM2, ß-catenin, c-Myc, and HnRNPA1 were assessed using real-time PCR analysis. Protein expression and the distribution of PKM2 were examined by western blot assay. RESULTS: TKP significantly inhibited Bel-7402 and HepG2 cell survival and colony formation capacity. The IC50 values of TKP against Bel-7402 and HepG2 cells were 31.37 ± 1.33 and 27.41 ± 0.81 µg/mL, respectively. TKP restrained aerobic glycolysis. TKP decreased the expression level, nuclear protein level and pyruvate kinase activity of PKM2, whereas overexpression PKM2 reversed the suppression of TKP on glycolysis. TKP inhibited the ß-catenin/c-Myc/HnRNPA1 pathway. LiCl treatment partly rescued the inhibitory effects of TKP on PKM2, aerobic glycolysis, and cell viability. CONCLUSION: TKP suppresses HCC cell proliferation via blocking PKM2-dependent glycolysis, which is regulated by inhibiting the ß-catenin/c-Myc/HnRNPA1 pathway.


Assuntos
Carcinoma Hepatocelular , Neoplasias Hepáticas , Trichosanthes , Carcinoma Hepatocelular/patologia , Linhagem Celular Tumoral , Proliferação de Células , Glicólise , Humanos , Neoplasias Hepáticas/patologia , Oligopeptídeos , Serina Proteases/farmacologia
8.
Toxins (Basel) ; 13(12)2021 12 14.
Artigo em Inglês | MEDLINE | ID: mdl-34941735

RESUMO

Neuroinflammation, which is mediated by microglia that release various inflammatory cytokines, is a typical feature of neurodegenerative diseases (NDDs), such as Alzheimer's disease and Parkinson's disease. Hence, alleviating neuroinflammation by downregulating pro-inflammatory action, and upregulating anti-inflammatory action of microglia is an efficient therapeutic target for NDDs. In this study, we evaluated whether trichosanthis semen (TS), a dried ripe seed of Trichosanthes kirilowii Maximowicz, reduces lipopolysaccharide (LPS)-induced neuroinflammation by regulating microglial responses in vitro and in vivo. Our results presented that TS reduced the release of pro-inflammatory mediators, such as nitric oxide (NO), inducible NO synthase, tumor necrosis factor-α, interleukin-1ß, and interleukin-6 via inhibition of the nuclear factor kappa B (NF-κB) signaling pathway in LPS-treated BV2 microglial cells. Moreover, TS induced anti-inflammatory mediators, such as interleukin-10, found in inflammatory zone 1, and chitinase 3-like 3 by the upregulation of heme oxygenase 1 (HO-1). We further confirmed that TS administration suppressed microglial activation, but enhanced HO-1 expression in LPS-injected mice. These results suggest that TS has anti-neuroinflammatory effects via inhibition of NF-κB signaling through the activation of HO-1, and that TS may be a therapeutical candidate for NDDs treatment.


Assuntos
Inflamação/tratamento farmacológico , Lipopolissacarídeos/toxicidade , NF-kappa B/metabolismo , Extratos Vegetais/farmacologia , Sementes/química , Trichosanthes/química , Animais , Regulação da Expressão Gênica/efeitos dos fármacos , Heme Oxigenase-1/genética , Heme Oxigenase-1/metabolismo , Inflamação/induzido quimicamente , Proteínas de Membrana/genética , Proteínas de Membrana/metabolismo , Camundongos , Microglia/efeitos dos fármacos , NF-kappa B/genética , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo II/metabolismo , Extratos Vegetais/química , Ratos , Transdução de Sinais/efeitos dos fármacos
9.
Int J Mol Sci ; 22(16)2021 Aug 05.
Artigo em Inglês | MEDLINE | ID: mdl-34445110

RESUMO

Epidermal growth factor receptor (EGFR) is overexpressed in lung cancer patients. Despite treatment with various EGFR tyrosine kinase inhibitors, recurrence and metastasis of lung cancer are inevitable. Docetaxel (DTX) is an effective conventional drug that is used to treat various cancers. Several researchers have studied the use of traditional herbal medicine in combination with docetaxel, to improve lung cancer treatment. SH003, a novel herbal mixture, exerts anticancer effects in different cancer cell types. Here, we aimed to investigate the apoptotic and anticancer effects of SH003 in combination with DTX, in human non-small-cell lung cancer (NSCLC). SH003, with DTX, induced apoptotic cell death, with increased expression of cleaved caspases and cleaved poly (ADP-ribose) polymerase in NSCLC cells. Moreover, SH003 and DTX induced the apoptosis of H460 cells via the suppression of the EGFR and signal transducer and activator of transcription 3 (STAT3) signaling pathways. In H460 tumor xenograft models, the administration of SH003 or docetaxel alone diminished tumor growth, and their combination effectively killed cancer cells, with increased expression of apoptotic markers and decreased expression of p-EGFR and p-STAT3. Collectively, the combination of SH003 and DTX may be a novel anticancer strategy to overcome the challenges that are associated with conventional lung cancer therapy.


Assuntos
Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico , Docetaxel/farmacologia , Neoplasias Pulmonares/tratamento farmacológico , Extratos Vegetais/farmacologia , Transdução de Sinais/efeitos dos fármacos , Células A549 , Angelica , Inibidores da Angiogênese/farmacologia , Animais , Apoptose/efeitos dos fármacos , Astrágalo (Planta) , Biomarcadores Tumorais/metabolismo , Carcinoma Pulmonar de Células não Pequenas/metabolismo , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Receptores ErbB/metabolismo , Humanos , Neoplasias Pulmonares/metabolismo , Camundongos , Recidiva Local de Neoplasia/tratamento farmacológico , Recidiva Local de Neoplasia/metabolismo , Inibidores de Proteínas Quinases/farmacologia , Fator de Transcrição STAT3/metabolismo , Trichosanthes , Ensaios Antitumorais Modelo de Xenoenxerto/métodos
10.
Plant Cell Rep ; 40(10): 1845-1858, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34228189

RESUMO

KEY MESSAGE: De novo transcriptome analysis from callus, leaf, and fruit of Trichosanthes cucumerina L. for the identification of genes associated with triterpenoid biosynthesis, especially bryonolic acid and cucurbitacin B. Trichosanthes cucumerina L. (TC) has been used as a medicinal plant in Thailand with various potential functions. Two major triterpenoids found in this plant, bryonolic acid and cucurbitacin B, are receiving increased attention for their activities. Here, we provide TC transcriptome data to identify genes involved in the triterpenoid biosynthetic pathway through callus, where was previously suggested as a novel source for bryonolic acid production as opposed to leaf and fruit. A de novo assembly of approximately 290-thousand transcripts generated from these tissues led to two putative oxidosqualene cyclases: isomultiflorenol synthase (IMS) and cucurbitadienol synthase (CBS). TcIMS and TcCBS, genes that encode substrates for two characteristic triterpenoids in cucurbitaceous plants, were identified as isomultiflorenol synthase and cucurbitadienol synthase, respectively. These two genes were functionally characterised in mutant yeast Gil77 systems, which led to the productions of isomultiflorenol and cucurbitadienol. Moreover, the callus-specific gene expression profiles were also presented. These obtained information showed candidate cytochrome P450s with predicted full-length sequences, which were most likely associated with triterpenoid biosynthesis, especially bryonolic acid. Our study provides useful information and a valuable reference for the further studies on cucurbitaceous triterpenoids.


Assuntos
Proteínas de Plantas/genética , Trichosanthes/genética , Trichosanthes/metabolismo , Triterpenos/metabolismo , Clonagem Molecular , Sistema Enzimático do Citocromo P-450/genética , Sistema Enzimático do Citocromo P-450/metabolismo , Perfilação da Expressão Gênica , Regulação da Expressão Gênica de Plantas , Transferases Intramoleculares/genética , Transferases Intramoleculares/metabolismo , Filogenia , Folhas de Planta/genética , Folhas de Planta/metabolismo , Proteínas de Plantas/metabolismo , Saccharomyces cerevisiae/genética , Saccharomyces cerevisiae/metabolismo
11.
J Food Biochem ; 45(5): e13714, 2021 05.
Artigo em Inglês | MEDLINE | ID: mdl-33817805

RESUMO

Trichosanthes dioica seed lectin (TDSL), having a molecular mass of 57 ± 2 kDa was purified in an alternative way. For the purification process, the galactose-sepharose-4B affinity column was used. The purified TDSL agglutinated human and mouse erythrocytes at the minimum concentration of 8  µg/ml. d-lactose and d-galactose were the most potent inhibitory sugars as observed. The purified lectin was a glycoprotein having 3.0% of a neutral sugar. The lectin exhibited maximum activity up to 60°C and pH range from 7.0 to 10.0 and stable up to 4.0 M urea as tested. The lectin demonstrated mild toxicity when administered against brine shrimp nauplii, and the LC50 value was calculated to be 84.0 µg/ml. Minimum agglutination of Ehrlich ascites carcinoma (EAC) cells caused by the lectin was found at the protein concentration of 1.56 µg/ml. TDSL inhibited 7, 50.2%, and 60.3% of the EAC cells growth in vivo in mice when administered with 0.75, 1.5, and 3.0 mg kg-1  day-1 (i.p.), respectively, for five consecutive days. After lectin treatment, red blood cell (RBC) and hemoglobin levels were increased significantly toward the normal compared with EAC cells-bearing control and normal mice. The tumor burden reduced to 29.5% and 67% after treatment with 1.5 and 3.0 mg kg-1  day-1 of the lectin. TDSL triggered the cell cycle arrest at the G0 /G1 phase, which was observed using flow cytometry. In conclusion, TDSL can be a candidate for the potent anticancer agents that exerts low toxicity toward brine shrimp nauplii. PRACTICAL APPLICATIONS: A 57 ± 2 kDa lectin (designated TDSL) was purified from Trichosanthes dioica seeds using a galactose-sepharose-4B affinity column. The lectin demonstrated mild toxicity and agglutinated Ehrlich ascites carcinoma (EAC) cells. The lectin inhibited 50.2% and 60.3% of the EAC cell growth in vivo in mice when administered with 1.5 and 3.0 mg kg-1  day-1 (i.p.), respectively, for five consecutive days. The lectin increased RBC and hemoglobin level toward the normal compared with lectin-treated EAC cells-bearing, EAC cells-bearing control and normal mice. The tumor burden reduced to 29.5% and 67% after treatment with 1.5 and 3.0 mg kg-1  day-1 lectin. TDSL triggered the cell cycle arrest at the G0 /G1 phase. The lectin can be a candidate for potent anticancer agents.


Assuntos
Carcinoma de Ehrlich , Trichosanthes , Animais , Ascite , Carcinoma de Ehrlich/tratamento farmacológico , Pontos de Checagem do Ciclo Celular , Lectinas/farmacologia , Camundongos , Sementes
12.
Nat Prod Res ; 35(23): 5132-5137, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32744101

RESUMO

The peel of Trichosanthes kirilowii Maxim is clinically used to treat cardiovascular diseases in China. In this study, the NF-κB inhibitory activity of the peel of T. kirilowii Maxim extracts was determined by Dual-Luciferase Reporter Assay System, and the results showed 70% ethanol extract could significantly inhibit the activation of NF-κB (p < 0.001). Further, 21 compounds were isolated from 70% ethanol extract. One new compound, namely (2 R)-(2-amino-2-hydroxymethyl-3-[(4-hydroxy-3-methoxybenzoyl)-O-]-propanoic acid (1), and 20 known compounds were elucidated by comprehensive spectroscopic analyses. The isolated compounds were tested in the anti-inflammatory assay, and the results indicated compounds 5, 8, 11, 14, 15, 17 and 21 could inhibit the activation of NF-κB (p <0 .05, p < 0.001) at concentration of 1 µM.


Assuntos
Trichosanthes , China , NF-kappa B
13.
J Nat Prod ; 83(12): 3536-3544, 2020 12 24.
Artigo em Inglês | MEDLINE | ID: mdl-33269591

RESUMO

In the ongoing efforts to discover natural cholesterol-lowering compounds, dihydrocucurbitacin B, isolated from Trichosanthes cucumeroides roots, was found to promote LDL uptake by upregulating LDLR protein in a PCSK9-dependent process. In this study, an in-depth investigation of T. cucumeroides roots afforded 27 cucurbitacins (1-27), including seven new cucurbitacins (1-7), and their structures were elucidated by spectroscopic data analyses. In order to gain insight into their structure-activity relationship, cucurbitacin derivatives (B1-11 and DB1-11) were synthesized. Evaluation of lipid-lowering activities of these cucurbitacins by an LDL uptake assay in HepG2 cells revealed that most of the compounds improved the LDL uptake rate, among which hexanorisocucurbitacin D (6) and isocucurbitacin D (21) exhibited the highest activities (rates of 2.53 and 2.47, respectively), which were comparable to that of the positive control, nagilactone B (rate of 2.07). According to a mechanistic study by Western blot analysis, compounds 6 and 21 dose-dependently increased LDLR protein levels and reduced PCSK9 protein levels, representing promising new lipid-lowering drug candidates.


Assuntos
Cucurbitacinas/farmacologia , Hipercolesterolemia/sangue , Trichosanthes/química , Cucurbitacinas/química , Células Hep G2 , Humanos , Extratos Vegetais/química , Raízes de Plantas/química , Análise Espectral/métodos , Relação Estrutura-Atividade
14.
Sci Rep ; 10(1): 17815, 2020 10 20.
Artigo em Inglês | MEDLINE | ID: mdl-33082402

RESUMO

The present study explores the methodology for the synthesis of bio-oil from waste trichosanthes cucumerina seeds by the solvent extraction method. It investigates the yield percentage, concentration of free fatty acids and acid contents in the extracted bio-oil. Effects of size of the crushed seeds, moisture content, extraction time, solvent to seed ratio and extraction temperatures were examined. The non-polar hexane solvent resulted in a higher percentage of oil yield (28.4 ± 0.4%) for the crushed seed size of 0.21 mm, 6% moisture content, 270 min extraction time, 68 °C temperature and 6:1(ml/g) of solvent to seed ratio. The synthesized bio-oil was characterized using Fourier Transform Infra-Red spectrum and Gas Chromatography-Mass Spectroscopy analysis. The properties of the bio-oil and biodiesel were assessed according to the American Society for Testing and Materials and the Association of Official Analytical Chemists standards. The obtained methyl-ester by trans-esterification process results in the fuel properties closer to the conventional fuel. Thus, Trichosanthes cucumerina bio-diesel can be used as a potential substitute.


Assuntos
Óleos Vegetais/síntese química , Polifenóis/síntese química , Energia Renovável , Trichosanthes/fisiologia , Biocombustíveis , Catálise , Esterificação , Cromatografia Gasosa-Espectrometria de Massas , Gasolina , Sementes , Espectroscopia de Infravermelho com Transformada de Fourier
15.
PLoS One ; 15(10): e0239230, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-33057394

RESUMO

Trichosanthes kirilowii Maxim. (TK) is a dioecious plant in the Cucurbitaceae for which different sexes have separate medicinal uses. In order to study the genes related to sex determination, transcriptome sequencing was performed on flower buds of male and female plants using the high-throughput sequencing technology. A total of 145,975 unigenes and 7110 DEGs were obtained. There were 6776 DEGs annotated to 1234 GO terms and enriched to 18 functional groups, including five biological processes related to sugar metabolism. KEGG pathway analysis indicated genes involved in hormone transduction, hormone synthesis and carbohydrate metabolism. Many DEGs of TK are involved in reproductive organ formation, hormone signal transduction and regulatory networks. Combining the results of GO, KEGG and qRT-PCR, 11 sex determining candidate genes of TK were selected, including MYB80, MYB108, CER1, CBL9, ABCB19, SERK1, HSP81-3, ACS9, SEP3, AUX1 and YUC6. The results provide a foundation for the study of sex differentiation in TK.


Assuntos
Proteínas de Plantas/genética , Transcriptoma , Trichosanthes/genética , Metabolismo dos Carboidratos/genética , Regulação da Expressão Gênica de Plantas , Redes Reguladoras de Genes/genética , Sequenciamento de Nucleotídeos em Larga Escala , Anotação de Sequência Molecular , Reguladores de Crescimento de Plantas/genética , Reguladores de Crescimento de Plantas/metabolismo , Proteínas de Plantas/metabolismo , RNA de Plantas/química , RNA de Plantas/isolamento & purificação , RNA de Plantas/metabolismo , Transdução de Sinais/genética , Trichosanthes/crescimento & desenvolvimento
16.
Medicine (Baltimore) ; 99(38): e22228, 2020 Sep 18.
Artigo em Inglês | MEDLINE | ID: mdl-32957363

RESUMO

INTRODUCTION: Cancer is the second leading cause of death, and the burden of cancer continues to grow globally. Research on the efficacy of combined administration of herbal medicine and anticancer drugs is also increasing. SH003 is a new herbal medicine composed of Astragalus membranaceus, Angelica gigas, and Trichosanthes kirilowii. SH003 alone up to 4800 mg daily was found to be safe. Preclinical studies have shown SH003 to have a synergistic effect with coadministration of anticancer drugs. This study aimed to determine the maximum tolerated dose of SH003 combined with docetaxel in patients with lung or breast cancer. METHODS: This is an open-label, dose-escalation study to evaluate the safety of SH003 combined with docetaxel. Patients with lung or breast cancer will be recruited. The participants will be divided into 3 groups based on SH003 daily dose (2400, 3600, and 4800 mg); the medication will be taken orally for 21 days. The traditional 3 + 3 design will be adopted for the dose escalation. Dose-limiting toxicities are defined as grade 3 or 4 adverse events according to the Common Terminology Criteria for Adverse Events. The highest dose at which no more than 1 of the 6 patients experience dose-limiting toxicity will be determined as the maximum tolerated dose of SH003 combined with docetaxel. DISCUSSION: This study investigates the safety of SH003 when combined with docetaxel. The results of this study will provide a safe dose range for conducting therapeutic exploratory trials. TRIAL REGISTRATIONS: ClinicalTrials.gov NCT04360317.


Assuntos
Antineoplásicos Fitogênicos/administração & dosagem , Neoplasias da Mama/tratamento farmacológico , Docetaxel/administração & dosagem , Neoplasias Pulmonares/tratamento farmacológico , Extratos Vegetais/administração & dosagem , Angelica , Protocolos de Quimioterapia Combinada Antineoplásica , Astrágalo (Planta) , Ensaios Clínicos Fase I como Assunto , Humanos , Fitoterapia , Trichosanthes
17.
Nan Fang Yi Ke Da Xue Xue Bao ; 40(7): 995-1000, 2020 Jul 30.
Artigo em Chinês | MEDLINE | ID: mdl-32895151

RESUMO

OBJECTIVE: To study the plasma concentration and pharmacokinetics of 3, 29-Dibenzoyl Karounitriol (3, 29-DK) from sustained- release pellets and extracts of Trichosanthes at different time points in rats using high-performance liquid chromatography- tandem mass spectrometry (LC-MS/MS). METHODS: Healthy male SD rats were given a single gavage of Trichosanthes sustained-release pellets or Trichosanthes extract, and orbital blood samples were taken at different time points within 48 h after drug administration in the pellet group and within 5 h in Trichosanthes extract group for determination of the plasma concentrations of 3, 29-DK using LC-MS/MS. The standard curve of 3, 29-DK content was established, and the specificity, minimum detection limit, precision and accuracy, extraction recovery, stability and matrix effect of LC-MS/MS analysis were assessed. The mean plasms levels of 3, 29-DK at different time points after the drug administration were determined and its pharmacokinetic parameters were calculated using Das 2.0 software. RESULTS: LC-MS/MS analysis showed a good linearity of 3, 29-DK concentration within the range of 0.5-32 ng/mL, and the results of methodological validation confirmed the validity of this method for biological sample determination. Trichosanthes sustained-release pellets and Trichosanthes extract showed significant differences in their AUC(0-t), AUC(0-∞), MRT(0-t), MRT(0-∞), t1/2z and Tmax of 3, 29-DK after administration in rats (P < 0.05). CONCLUSIONS: Trichosanthes sustained-release pellets are capable of sustained-release of 3, 29-DK in rats, and thus provides a basis for the study of new dosage forms of Trichosanthes.


Assuntos
Trichosanthes , Animais , Cromatografia Líquida de Alta Pressão , Preparações de Ação Retardada , Masculino , Ratos , Ratos Sprague-Dawley , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem
18.
Cell Death Dis ; 11(8): 717, 2020 09 02.
Artigo em Inglês | MEDLINE | ID: mdl-32879309

RESUMO

In gastric cancer (GC), hypoxia is one of the greatest obstacles to cancer therapy. In this present study, we report that SH003, an herbal formulation, induces ER stress via PERK-ATF4-CHOP signaling in GC. SH003-mediated ER stress inhibits G9a, a histone methyltransferase, by reducing STAT3 phosphorylation and activates autophagy, indicating to the dissociation of Beclin-1 and autophagy initiation from Bcl-2/Beclin-1 complex. However, the inhibition of PERK and CHOP inhibited SH003-induced cell death and autophagy activation. Moreover, targeting autophagy using specific siRNAs of LC3B or p62 or the autophagy inhibitor 3-MA also inhibited SH003-induced cell death in GC. Interestingly, SH003 induces BNIP3-mediated autophagic cell death under hypoxia than normoxia in GC. These findings reveal that SH003-induced ER stress regulates BNIP3-induced autophagic cell death via inhibition of STAT3-G9a axis under hypoxia in GC. Therefore, SH003 may an important tumor therapeutic strategy under hypoxia-mediated chemo-resistance.


Assuntos
Autofagia/efeitos dos fármacos , Extratos Vegetais/farmacologia , Neoplasias Gástricas/metabolismo , Fator 4 Ativador da Transcrição/metabolismo , Angelica , Astrágalo (Planta) , Morte Celular Autofágica/efeitos dos fármacos , Proteína Beclina-1 , Hipóxia Celular/efeitos dos fármacos , Hipóxia Celular/fisiologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Estresse do Retículo Endoplasmático/efeitos dos fármacos , Antígenos de Histocompatibilidade/metabolismo , Histona-Lisina N-Metiltransferase/metabolismo , Humanos , Proteínas de Membrana/metabolismo , Extratos Vegetais/metabolismo , Proteínas Proto-Oncogênicas/metabolismo , Fator de Transcrição STAT3/metabolismo , Transdução de Sinais/efeitos dos fármacos , Trichosanthes
19.
Int J Biol Macromol ; 164: 2861-2872, 2020 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-32810537

RESUMO

Microwave-assisted extraction of polysaccharides from Trichosanthes kirilowii Maxim seeds (TKMSP) was optimized using Response surface methodology (RSM) base on Central composite design (CCD). The optimum extraction conditions are detailed as follows: liquid-solid ratio 42 mL/g, extraction temperature 80 °C, microwave power 570 W, extraction time 26 min. Under this conditions, the mean value of TKMSP yield 2.43 ± 0.45% (n = 3), which was consistent closely with the predicted value (2.44%). The five polysaccharides (TKMSP-1, TKMSP-2, TKMSP-3, TKMSP-4 and TKMSP-5) were isolated from TKMSP by DEAE-52. TKMSP-1, TKMSP-2 and TKMSP-4 were common in containing Man, Rib, Rha, GluA, GalA, Glu, Gal, Xyl, Arab and Fuc. However, there was no Fuc in TKMSP-3, while TKMSP-5 lacked GluA, GalA and Fuc. UV-vis and FT-IR analysis combined with molecular weight determination further indicated that the five fractions were polydisperse polysaccharides. A significant difference was achieved in the structural characterization of these five fractions. TKMSP exhibited immunosuppressive activity on RAW264.7 cells. It can be applied as a potential immunosuppressant agent in medicine.


Assuntos
Fatores Imunológicos/química , Polissacarídeos/química , Trichosanthes/química , Animais , Sobrevivência Celular , Fatores Imunológicos/farmacologia , Camundongos , Micro-Ondas , Peso Molecular , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Polissacarídeos/isolamento & purificação , Polissacarídeos/farmacologia , Células RAW 264.7 , Sementes/química , Espectroscopia de Infravermelho com Transformada de Fourier
20.
Bull Entomol Res ; 110(6): 756-766, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-32484147

RESUMO

Diaphania indica (Saunders) (Lepidoptera: Crambidae) is an important phytophagous pest of Trichosanthes anguina L. in India. We studied life table parameters by age-stage, two-sex, amylolytic and proteolytic activities, and food utilization parameters of D. indica on the leaves of three T. anguina cultivars (Baruipur Long, Polo No. 1 and MNSR-1). Further, nutrients (total carbohydrates, proteins, lipids, amino acids and nitrogen) and antinutrients (total phenols, flavonols and tannins) in leaves were determined. The development time (egg to adult emergence) was the shortest on MNSR-1 (19.79 d) and the longest on Polo No. 1 (25.72 d). Fecundity was the highest and lowest on MNSR-1 (259 eggs) and Polo No. 1 (151.22 eggs), respectively. The lowest intrinsic rate of increase (rm) and net reproductive rate (R0) of D. indica on Polo No. 1 were 0.1112 d-1 and 27.22 offspring individual-1, respectively. The mean generation time (T) was the shortest on MNSR-1 (23.99 days) and the longest on Polo No. 1 (29.70 d). The larvae of D. indica fed with MNSR-1 had the highest level of amylolytic and proteolytic activities, and the lowest activities were in the larvae fed with Polo No. 1. The fifth-instar larvae fed with Polo No. 1 had the lowest consumption index and growth rate. The higher larval development time and lower fecundity of D. indica on Polo No. 1 were due to the lower level of nutrients and a higher level of antinutrients than other cultivars. Our results concluded that Polo No. 1 cultivar could be suggested for cultivation.


Assuntos
Mariposas/crescimento & desenvolvimento , Mariposas/fisiologia , Trichosanthes/química , Fenômenos Fisiológicos da Nutrição Animal , Animais , Fenômenos Fisiológicos do Sistema Digestório , Feminino , Fertilidade , Larva/crescimento & desenvolvimento , Larva/fisiologia , Tábuas de Vida , Masculino , Trichosanthes/classificação
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