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1.
China Pharmacy ; (12): 1448-1454, 2022.
Article in Chinese | WPRIM | ID: wpr-927191

ABSTRACT

OBJECTIVE To in vestigate inhibitory effect s of gallic acid (GA)on human esophageal cancer TE- 1 cells in vitro and its potential mechanism. METHODS The effects of GA on the proliferation of TE- 1 cells were determined by MTT assay after treated with GA for 24 h and 48 h. Cell fluorescence counting (CCK-F)method and inverted fluorescence microscope were used to observe the changes in the number and morphology of TE- 1 cells after treated with GA. The change of cell migration ability was detected by scratch test. The effects of GA on the colony-forming ability of TE- 1 cells were tested by plate colony formation experiment. Cell apoptosis was detected by flow cytometry. Fluorescence probe (DCFH-DA)method was used to observe reactive oxygen species (ROS)production. Western blot assay was used to detect the expression of caspase- 3,caspase-9,Bcl-2,Bcl-2 associated X protein (Bax),cyclin D 1 and cyclin D 3. RESULTS GA significantly reduced the proliferation ability of TE- 1 cells in time and concentration dependent manner. the IC 50 of GA to TE- 1 cells were (281.22±26.81)μmol/L(24 h)and(220.90±31.15) μ mol/L(48 h),respectively. Compared with control group ,the cells in the administration group showed shrinkage ,sparse arrangement and nuclear pyknosis ,and the number of cells decreased significantly. Compared with control group ,the cell migration ability and colony formation ability were decreased significantly in administration groups (P<0.01 or P<0.05). The apoptosis rates of TE- 1 cells were (6.21±0.32)%,(12.59±0.58)% and(15.41±0.41)% after treated with 100,300 and 500 μmol/L GA for 24 h,all of which were significantly higher than (5.29±0.28)% of control group (P<0.01 or P<0.05). Except for GA 100 μmol/L group,the level of ROS in other administration groups were significantly increased (P<0.01 or P<0.05). Compared with control group,the expressions of Bcl- 2(only GA 200 μmol/L group),Bax(except for GA 100 μmol/L),caspase-3 and caspase- 9(except for GA 100 μmol/L)were increased significantly (P<0.01 or P<0.05),while the protein expressions of Bcl- 2(except GA 100, 200 μmol/L group),cyclin D 1 and cyclin D 3 were significantly decreased (P<0.01 or P<0.05). CONCLUSIONS GA can inhibit the proliferation of esophageal cancer TE- 1 cells, E-mail:1209364115@qq.com restrict their migration ability and colony-forming ability ,and promote apoptosis. The mechanism may be related to the increase of ROS level ,up-regulation of the expressions of pro-apoptotic proteins caspase- 3,caspase-9 and Bax ,and down-regulation of the expressions of anti-apoptotic protein Bcl- 2,cyclin D1 and cyclin D 3.

2.
Article in Chinese | WPRIM | ID: wpr-940522

ABSTRACT

ObjectiveTo investigate the effects of gallic acid (GA) on human colon cancer HCT-116 and Caco-2 cell activities, intracellular Janus kinase (JAK)/signal transducer and activator of transcription factor (STAT) signaling pathway, and the expression of anti-apoptotic protein B-cell lymphoma-2 (Bcl-2) and pro-apoptotic protein B-cell lymphoma-2-associated X protein (Bax), so as to explore its underlying molecular mechanism. MethodFollowing the classification of cells into GA group, blank group, and 5-fluorouracil (5-FU, 0.05 g·L-1) group, the HCT-116 and Caco-2 cells were treated with GA (0.02, 0.05, 0.1, 0.15, 0.2 g·L-1) for 12, 24, 48, and 72 h, respectively, and the cell proliferation inhibition rats were determined by cell counting kit-8 (CCK-8) assay to select the GA concentration that effectively inhibited proliferation. The colony formation ability was detected by crystal violet staining and the migration of cells by scratch test. The level of reactive oxygen species (ROS) was measured using a fluorescent probe (DCFH-DA). The expression of interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) in cell supernatant were determined using the enzyme-linked immunosorbent assay (ELISA) kits. The expression levels of JAK2, phosphorylated (p)-JAK2, STAT3, p-STAT3, Bcl-2, and Bax were assayed by Western blot. ResultCCK-8 assay showed that after 12, 24, 48, and 72 h of treatment, GA (0.02, 0.05, 0.1, 0.15, 0.2 g·L-1) inhibited the proliferation of HCT-116 and Caco-2 cells in a dose- and time-dependent manner, and the inhibition rates were higher than those in the blank control group. Compared with the 5-FU group, GA (0.2 g·L-1) enhanced the inhibition of cell proliferation in a time-dependent manner. Compared with the blank control group, GA (0.1, 0.15, and 0.2 g·L-1) significantly decreased the number of cell colonies (P<0.01), increased the inhibition rate of cell colony formation (P<0.01), diminished the scratch healing rate (P<0.05, P<0.01), elevated the fluorescence intensity of intracellular ROS (P<0.01), and down-regulated the expression of IL-6 and TNF-α in the supernatant (P<0.01) in a dose-dependent manner. Compared with the 5-FU group, GA (0.2 g·L-1) decreased the scratch healing rate (P<0.01), enhanced the fluorescence intensity of intracellular ROS (P<0.01), and down-regulated the levels of IL-6 and TNF-α in cell supernatant (P<0.01). According to Western blot analysis, compared with the blank control group, GA (0.1, 0.15, 0.2 g·L-1) obviously lowered the expression of p-JAK2, p-STAT3, Bcl-2, p-JAK2/JAK2, p-STAT3/STAT3, and Bcl-2/Bax (P<0.01) and raised Bax protein expression (P<0.05, P<0.01) in a dose-dependent manner. Compared with the 5-FU group, GA (0.2 g·L-1) down-regulated the expression of p-JAK2, p-STAT3, Bcl-2, p-JAK2/JAK2, p-STAT3/STAT3, and Bcl-2/Bax (P<0.05, P<0.01) and up-regulated the expression of Bax protein (P<0.05, P<0.01). ConclusionGA significantly inhibits the proliferation of HCT-116 and Caco-2 cells, which may be related to the increased accumulation of intracellular ROS, down-regulation of inflammatory factors IL-6 and TNF-α, p-JAK2 and p-STAT3 protein expression in JAK/STAT signaling pathway, and Bcl-2, and up-regulation of Bax.

3.
Article in English | WPRIM | ID: wpr-939779

ABSTRACT

Cancer is one of the most devastating diseases worldwide and definitive therapeutics for treating cancer are not yet available despite extensive research efforts. The key challenges include limiting factors connected with traditional chemotherapeutics, primarily drug resistance, low response rates, and adverse side-effects. Therefore, there is a high demand for novel anti-cancer drugs that are both potent and safe for cancer prevention and treatment. Gallic acid (GA), a natural botanic phenolic compound, can mediate various therapeutic properties that are involved in anti-inflammation, anti-obesity, and anti-cancer activities. More recently, GA has been shown to exert anti-cancer activities via several biological pathways that include migration, metastasis, apoptosis, cell cycle arrest, angiogenesis, and oncogene expression. This review discusses two aspects, one is the anti-cancer potential of GA against different types of cancer and the underlying molecular mechanisms, the other is the bibliometric analysis of GA in cancer and tumor research. The results indicated that lung cancer, prostate cancer, stomach cancer, and colon adenocarcinoma may become a hot topic in further research. Overall, this review provides evidence that GA represents a promising novel, potent, and safe anti-cancer drug candidate for treating cancer.


Subject(s)
Adenocarcinoma/drug therapy , Antineoplastic Agents/therapeutic use , Apoptosis , Cell Line, Tumor , Colonic Neoplasms , Gallic Acid/therapeutic use , Humans , Male
4.
Bol. latinoam. Caribe plantas med. aromát ; 20(3): 226-243, may. 2021. ilus, tab
Article in English | LILACS | ID: biblio-1342815

ABSTRACT

Several species of the Myrcia genus have been used in folk medicine to treat diabetes. Therefore, the aim of this work was to investigate the inhibitory activity of α-glucosidase and pancreatic lipase in the crude extract (EBF) and in the ethyl acetate fraction (FFA) of Myrcia hatschbachii, as well as to identify isolated phenolic compounds and to evaluate the antioxidant property and preliminary in vitro toxicity against Artemia salina. EBF (IC50: 3.21 µg/mL) and FFA (IC50: 1.14 µg/mL) showed inhibitory activity superior to acarbose (IC50: 193.65 µg/mL). In addition, they showed inhibitory effects of pancreatic lipase (IC50: 556.58 µg/mL for EBF and 532.68 µg/mL for FFA), antioxidant potential, absence of preliminary toxicity and presence of gallic andellagic acids in FFA. The relevant results in the inhibition of α-glucosidase and pancreatic lipase motivate new studies for the development of herbal medicines that assist in the treatment of diabetic patients.


Varias especies del género Myrcia se han utilizado en la medicina popular para tratar la diabetes. Por lo tanto, el objetivo de este trabajo fue investigar la actividad inhibitoria de la α-glucosidasa y la lipasa pancreática en el extracto crudo (EBF) y en la fracción de acetato de etilo (FFA) de Myrcia hatschbachii, así como identificar compuestos fenólicos aislados y evaluar la propiedad antioxidante y toxicidad in vitro preliminar contra Artemia salina. EBF (IC50: 3.21 µg/mL) y FFA (IC50: 1.14 µg/mL) mostraron una actividad inhibitoria superior a la acarbosa (IC50: 193.65 µg/mL). Además, mostraron efectos inhibitorios de la lipasa pancreática (IC50: 556.58 µg/mL para EBF y 532.68 µg/mL para FFA), potencial antioxidante, ausencia de toxicidad preliminar y presencia de ácidos gálico y elágico en FFA. Los resultados relevantes en la inhibición de la α-glucosidasa y la lipasa pancreática motivan nuevos estudios para el desarrollo de medicamentos a base de hierbas que ayudan en el tratamiento de pacientes diabéticos.


Subject(s)
Plant Extracts/pharmacology , Myrtaceae/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Lipase/drug effects , Antioxidants/pharmacology , Pancreas/enzymology , Phenols/analysis , X-Ray Diffraction , In Vitro Techniques , Plant Extracts/toxicity , Plant Extracts/chemistry , Free Radical Scavengers , Complex Mixtures , Ellagic Acid , Gallic Acid , Antioxidants/chemistry
5.
Braz. arch. biol. technol ; 64: e21210023, 2021. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-1355828

ABSTRACT

Abstract In this study, physicochemical, microbiological, and sensory properties, antibacterial and antifungal effects of kombucha teas produced with some small berry fruits (blackberry, raspberry, and red goji berry) were investigated. During fermentation, titratable acidity and pellicle biomass weights increased whereas water activity, brix, viscosity, L* and b* values decreased. At the end of fermentation, the highest minerals determined in the samples were potassium and magnesium. Also, catechin and gallic acid were detected in all samples. Samples produced with blackberry were the most appreciated ones in all criteria. The highest antibacterial and antifungal effects were determined in samples containing blackberries on Staphylococcus aureus and Rhizopus nigricans (24.36 and 20.53 mm zone diameters). The antibacterial effect, MIC, and MBC values (0.023 and 0.016 mg/L) on Staphylococcus aureus. Regarding the antifungal effect, the MIC and MFC values were determined in tea produced with blackberry on Rhizopus nigricans with 0.035 mg/L, and 0.023 mg/L.

6.
China Pharmacy ; (12): 933-939, 2021.
Article in Chinese | WPRIM | ID: wpr-876262

ABSTRACT

OBJECTIVE:To esta blish a method for si multaneous determination of 5 components in the branch and root of Juglans mandshurica as gallic acid ,ellagic acid ,1,6-di-O-galloyl-β-D-glucose,1,2,6-tri-O-galloyl-β-D-glucose and 1,2,3, 6-tetra-O-galloyl-β-D-glucose,and to analyze the content difference of above 5 components between the branch and root samples. METHODS:HPLC method was adopted. The determination was performed on Agilent Poroshell 120 SB-C18 column with mobile phase consisted of water (containing 0.2% formic acid )-acetonitrile (containing 0.2% formic acid ). A gradient elution was performed at a flow rate of 0.3 mL/min. The column temperature was 30 ℃ and the detection wavelength was 270 nm. The sample size was 5 μL. Independent samples t-test and partial least squares-discriminant analysis (PLS-DA)were applied for statistical analysis of 5 components. RESULTS :The linear range of gallic acid ,ellagic acid ,1,6-di-O-galloyl-β-D-glucose,1,2, 6-tri-O-galloyl-β-D-glucose and 1,2,3,6-tetra-O-galloyl-β-D-glucose were 0.989-63.3,1.58-101,1.01-64.7,3.31-212,3.34-214 μg/mL (r≥0.997 3),respectively. RSDs of precision ,reproducibility and stability tests (12 h)were all lower than 3.2%. The average recoveries of the 5 components were 103.2%(RSD=4.85%),99.1%(RSD=2.80%),101.5%(RSD=1.31%),102.9%(RSD= 2.73%)and 104.7%(RSD=1.28%),respectively. The average contents of the above components in the branch of J. mandshurica were 0.296 5,0.621 1,0.562 5,3.111 7 and 3.451 3 mg/g,respectively. The average contents of above components in the root were 0.673 4,2.755 5,0.964 0,2.946 6 and 4.836 4 mg/g,respectively. The total contents of the 5 components in the branch and roo t of J. mandshurica were 8.043 2 and 12.175 9 mg/g,respectively. The contents of gallic acid ,ellagic acid and 1,6-di-O-galloyl- β-D-glucose in roots were significantly higher than those in branches (P<0.05 or P<0.01). There were no significant differences in the contents of the other 2 components and the total contents of the 5 components in branches and roots (P>0.05). The cumulative interpretability (R 2X,R 2Y) and cumulative predictability (Q 2) of the model established by PLS-DA were 0.943,0.745,and 0.710 respectively. The model load diagram showed that the distance between the ellagic acid and the origin was the farthest ,and only variable projection importance of the content of the ellagic acid was greater than 1. CONCLUSIONS:The established method can be used for the content determination of 5 components in the branch and root of J. mandshurica . Except for 1,2,6-tri-O-galloyl-β-D-glucose,the contents of other 4 components and total contents of the 5 components in the root of J. mandshurica are higher than those of the branch. Ellagic acid is selected as the potential marker for discriminating the branch and root samples.

7.
Article in Chinese | WPRIM | ID: wpr-909252

ABSTRACT

Objective:To investigate the inhibitory effect of gallic acid on Pseudomonas aeruginosa biofilm. Methods:From January to June 2020, crystal violet staining was used to screen clinically isolated Pseudomonas aeruginosa biofilm strains in Taizhou Hospital of Integrated Traditional Chinese and Western Medicine. The minimal inhibitory concentration (MIC) of gallic acid against Pseudomonas aeruginosa was detected by the microdilution method. The adhesiveness of gallic acid to Pseudomonas aeruginosa and the minimum inhibitory membrane concentration (SMIC) were determined by (2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide) (XTT) assay. Results:PA08, PA12, PA18, PA35, PA53 and ATCC27853 strains were screened and used as test strains. The MIC of gallic acid against PA08, PA12, PA18, PA35, PA53 and ATCC27853 strains was 150 mg/L, 150 mg/L, 75 mg/L, 150 mg/L, 150 mg/L and 150 mg/L, respectively. Gallic acid at 75 mg/L could significantly inhibit the early adhesion of PA18 strain ( t = 3.766, P < 0.05). Gallic acid at 150 mg/L could significantly inhibit the early adhesion of PA08, PA12, PA18, PA35, PA53, ATCC27853 ( t = 4.562, 3.787, 6.769, 11.29, 5.719 and 7.251, all P < 0.05). Gallic acid at 300 mg/L could significantly inhibit the adhesion of PA18 strain at 6 hours ( t = 6.012, P < 0.05). The SMIC 50 of PA12, PA35, PA53 was 75 mg/L, and that of PA08, PA18, ATCC27853 was 150 mg/L. Conclusion:Gallic acid can effectively inhibit the early adhesion of Pseudomonas aeruginosa and affect its biofilm formation.

8.
Article in Chinese | WPRIM | ID: wpr-907682

ABSTRACT

Objective:To establish the HPLC fingerprint method for assessing the quality of Moutan Cortex, and to determine the contents of paeonol, paeoniflorin, gallic acid, hydroxyl-paeoniflorin and benzoyl-paeoniflorin of Moutan Cortex in different growth period. Methods:Diamonsil Plus C18 column (250 mm × 4.6 mm, 5 μm) was used with the mobile phase comprising acetonitrile-0.05% formic acid solution and the flow rate of 1.0 ml/min with gradient elution manner. The detected wavelength was 230 nm for paeoniflorin and benzoyl-paeoniflorin, 267 nm for gallic acid, 258 nm for hydroxyl-paeoniflorin and 274 nm for paeonol with temperature column of 25 ℃. Then putting chromatograms into Similarity Evaluation System for Chromatographic Fingerprint of Chinese Materia Medica (2012A) to evaluate the similarity of Moutan Cortex in different growth period; then putting peak area data into SPSS software for cluster analysis and the clustering effect was determined. Results:The HPLC fingerprints established with this method has 23 shared peaks and 5 of them were identified, namely, paeonol, paeoniflorin, gallic acid, hydroxyl-paeoniflorin and benzoylpaeoniflorin. The similarity of Moutan Cortex in different years was between 0.850-0.991. This method has good linear relation ( r≥0.999 5), RSDs of precision, stability tests and reproducibility were lower than 1.6% ( n=6). Different growth periods of Moutan Cortex have obvious influence on the concentration of five compounds. Conclusion:This method is useful to evaluate and discriminate Moutan Cortex at different growth periods so as toprovide scientific reference on the harvest,industrialization and evaluation of Moutan Cortex.

9.
Article in Chinese | WPRIM | ID: wpr-906438

ABSTRACT

Objective:To provide a scientific basis for the classification of Phyllanthi Fructus product grades. Method:A total of 30 batches of Phyllanthi Fructus currently available in the market were collected for quantification based on such appearance indexes as diameter, thickness, grain weight, and crust colour (<italic>L</italic><sup>*</sup>, <italic>a</italic><sup>*</sup>, and <italic>b</italic><sup>*</sup> values). The contents of gallic acid, corilagin, chebulagic acid, and ellagic acid were measured by high performance liquid chromatography (HPLC), followed by descriptive statistical analysis (DSA), analysis of variance (ANOVA), and principal component analysis (PCA) to determine the importance of each main index and explore the correlations between the appearance indexes and internal components. The classification standard of Phyllanthi Fructus product grades was formulated, and its scientificity was verified in hepatocelular carcinoma HepG2 cells. Result:The correlation analysis revealed that the crust colour <italic>L</italic><sup>*</sup>, <italic>a</italic><sup>*</sup>, and <italic>b</italic><sup>*</sup> values were significantly negatively correlated with corilagin, chebulagic acid, and ellagic acid (<italic>|r|</italic>>0.5, <italic>P</italic><0.01), but irrelevant to gallic acid (<italic>|r|</italic><0.1). Considering the variable coefficient of each index, PCA results, and the requirement of gallic acid as quality indicator for Phyllanthi Fructus in <italic>Chinese Pharmacopoeia</italic>, the crust colour <italic>L</italic><sup>*</sup>, <italic>a</italic><sup>*</sup>, and <italic>b</italic><sup>*</sup> values and gallic acid content were determined to be the classification indexes. The K-means cluster analysis confirmed that products with crust colour <italic>L</italic><sup>*</sup><44, <italic>a</italic><sup>*</sup><7, and <italic>b</italic><sup>*</sup><10 and gallic acid content >1.6% could be classified into the first class, and those failing to meet the above requirements into the second class. The cell experiment demonstrated that the half-maximal inhibitory concentration (IC<sub>50</sub>) of the first-class product against hepatocelular carcinoma HepG2 cells was lower than that of the second-class product. A colourimetric card was developed based on crust colour <italic>L</italic><sup>*</sup>, <italic>a</italic><sup>*</sup>, and <italic>b</italic><sup>*</sup> values to provide a visual tool for on-site evaluation of Phyllanthi Fructus products. Conclusion:This study has initially established the classification standard of Phyllanthi Fructus product grades, which contributes to guiding price negotiation of Phyllanthi Fructus products based on quality grade and thus ensuring high quality and high price.

10.
China Pharmacy ; (12): 2619-2623, 2021.
Article in Chinese | WPRIM | ID: wpr-904520

ABSTRACT

OBJECTIVE:To study the hepatotoxicity of main components of Polygonum multiflorum ,and investigate its toxic mechanism based on metabolic enzymes. METHODS :ADMETlab 2.0 platform was used to forecast the toxic or carcinogenic effects of emodin ,physcion,rhein,stilbene glycoside and gallic acid on liver ,skin and heart. The effects of those components on cytochrome P 450 enzyme system (CYP1A2,CYP2C9,CYP2C19,CYP2D6,CYP3A4)were evaluated. The effects of different concentrations of emodin ,rhein,stilbene glycoside and gallic acid (10,20,40,80 μmol/L)on the survival rate of normal hepatocyte L 02 were detected. The effects of major components of P. multiflorum on the activity of UGT 1A1 enzyme were studied by in vitro reaction system ,using bilirubin as substrate. RESULTS :Main components of P. multiflorum ,ie. emodin ,physcion, rhein and gallic acid ,showed strong toxic effects on the liver ,while stilbene glycosides possessed weak toxic effects on the liver. Emodin and physcion had strong inhibitory effects on CYP 1A2 and medium inhibitory effects on CYP 2C9,CYP2D6 and CYP3A4;rhein showed medium inhibitory effects on CYP 1A2 and CYP 2C9,while stilbene glycoside and gallic acid possessed weak inhibitory effects on the above enzymes. Emodin (40,80 μmol/L)and gallic acid (40,80 μmol/L)could significantly reduce the survival rate of L 02 cells(P<0.01). The inhibition rate of 5,10,20,40,80 μmol/L emodin and gallic acid(except for 5 μmol/L emodin)on UGT 1A1 enzyme increased significantly (P<0.01),and the inhibition effect of emodin on UGT 1A1 enzyme was reversible competitive inhibition. CONCLUSIONS :The main components of P. multiflorum ,ie. emodin ,rhein and physcion , are hepatotoxic ;the mechanism of it may be associated with inhibiting the activity of CYP 1A2 and CYP 2C9 and competitively blocking rate-limiting enzyme UGT 1A1 in the process of bilirubin metabolism.

11.
Article in Chinese | WPRIM | ID: wpr-921735

ABSTRACT

Phyllanthi Fructus, a unique Chinese and Tibetan medicinal plant with both edible and medical values, has high potential of cultivation and development. The resources of Phyllanthi Fructus in China are rich, mainly distributed in Yunnan, Sichuan, Fujian, Guangdong, Guangxi, etc. Phyllanthi Fructus is widely used in the clinical practice of Chinese medicine and plays an important role in Tibetan medicine, Uyghur medicine, Yi medicine, and Mongolian medicine. Phyllanthi Fructus mainly contains phenolic acids,tannins, terpenes, sterols, fatty acids, flavonoids, amino acids and other compounds. Modern pharmacological studies show that Phyllanthi Fructus has antioxidant, anticancer, blood lipid-lowering, liver protective, antimicrobial, anti-inflammatory, and immune regulatory activities. In this paper, the research status of Phyllanthi Fructus was reviewed from the aspects of herbal textual research,chemical composition, and pharmacological action. The quality markers(Q-markers) of Phyllanthi Fructus were predicted and analyzed from the aspects of biogenic pathway, specificity and measurability of chemical components, efficacy, properties, new clinical uses, drug-food homology, and transformation of polyphenols. The results will provide a scientific basis for the quality control, quality evaluation, and standard formulation of Phyllanthi Fructus.


Subject(s)
China , Drugs, Chinese Herbal , Fruit , Medicine, Tibetan Traditional , Quality Control
12.
J Ayurveda Integr Med ; 44013; 11(3): 294-300
Article | IMSEAR | ID: sea-214037

ABSTRACT

Background: Regulatory guidelines recommend shelf life of herbal products to be established throughsystematic stability studies.Objective: The study was designed to establish shelf life of Syzygium cumini extract through acceleratedand long-term stability testing as per WHO guidelines.Material and methods: The extract was stored under accelerated (40_x005F_x005F_x0001_C/75 %RH) and long-term (25_x005F_x005F_x0001_C/60%RH) stability conditions for 6 and 30 months, respectively. Samples were withdrawn at periodic intervals and analysed through two validated HPLC-UV methods (I and II) for fingerprint and quantitativeanalysis of markers. Antidiabetic activity of control and stability samples was evaluated by a-glucosidaseinhibitory model.Results: Method I generated a well resolved fingerprint of the control sample that was found to containgallic acid (GA, 1.45 % w/w) and ellagic acid (EA, 3.97 % w/w). The content of GA did not change underboth the stability conditions, but that of EA varied insignificantly (3.97e4.77 % w/w) under long-termconditions up to 24 months and subsequently decrease to 3.15 % w/w after 30 months. There was novisible change in LC-UV fingerprint of any stability sample with respect to control. a-Glucosidaseinhibitory activity of all stability samples also remained unaltered as compared to control sample (IC501.48 mg/mL). GA and EA did not elicit any activity at the concentrations present in the extract.Conclusion: Phytochemical composition and antidiabetic efficacy of S. cumini extract remain unchangedduring its storage under both accelerated and long-term stability conditions, which suggest its shelf lifeto be 30 months. Also, GA and EA are not appropriate anti-diabetic markers

13.
Int J Pharm Pharm Sci ; 2020 Jun; 12(6): 76-80
Article | IMSEAR | ID: sea-206113

ABSTRACT

Objective: The objective of the present work was to establish a simple, precise, accurate and robust method for simultaneous estimation of gallic acid, curcumin and piperine from the marketed ayurvedic formulation by liquid chromatography. Methods: The separation was carried out on Hemochrom C18 Column (250 mm × 4.6 mm ID, 5 µm pore size) with a mobile phase methanol: acetonitrile: water (pH 3.2adjusted by using orthophosphate acid) in the ratio 70:20:10v/v by isocratic elution modeat 25 °C and the flow rate was setat0.8 ml/min. The analysis was carried out atisoabsorptive wavelength of 295 nm. Results: The retention time of gallic acid, curcumin and piperine was found to be 3.3(±0.2), 4.7 (±0.2) and 5.6 (±0.2) min, respectively. The linearity range for gallic acid, curcumin and piperine was found to be 10-70 μg/ml, 20-80 µg/ml and 2-14 µg/ml, respectively with the coefficient of linear regression greater than 0.99 for all markers. Mean percent recoveries for gallic acid, curcumin, and piperine were found within the limit of acceptance (99-100%). The percent relative standard deviation (%RSD) for precision and robustness was found less than 2%, which indicates the method is precise and robust. The developed method applied for quantification of these markers from the marketed ayurvedic formulation of Dekofcyn tablet. Conclusion: The developed method was found to be simple, rapid, precise and reproducible for standardization of Dekofcyn tablet and can be useful for other formulations containing these three markers.

14.
Article | IMSEAR | ID: sea-203782

ABSTRACT

Objective: The aim of the paper is to assess the anti-inflammatory potential of three medicinal plants using two rat models. Materials and Methods: Soxhlet extraction approaches utilized to separatethe constituents of interest. Quantitative analysis has been performed to determine the total phenolic and flavonoid content. Three plants extract employed for the ointment formulation by addition of the extract of Artocarpus heterophyllus (AH), Murraya koenigii (MK), and Punica granatum (PG) inpolyethylene glycol (PEG) ointment base, a blend of PEG 600 and PEG 4000, and ratio 7:3, respectively.Two rat models based on chemical induced animals employed for the anti-inflammatory potential. Results and Discussion: All three plants including AH Lam., MK Linn., and PG Linn. extracted for the major component and have shown the gallic acid and quercetin as major component for flavonoid and phenol content. The ointment formulation F3 has showed maximum inhibition (80.95%) at 50 mg/kg dose of carrageenan-induced edema and 83.33% inhibition at 100 mg/kg dose. The ointment formulation F3 has showed maximum inhibition (78.57%) at 50 mg/kg dose of histamine persuade edema and 83.33% inhibition at 100 mg/kg dose. F3 ointment formulation is better than the F2 and F1 formulation in inhibition and in all phases showing its reserve of kinins as well as arachidonic acid. Conclusion: Quantitative and pharmacological evaluation indicated that ointment formulations of AH, MK, and PGhave exploit for anti-inflammatory activity. The normal extract has shown the least activity but ointment formulations have shown the better result. The ointment formulations containing plant extracts in 10% amount have better wound healing potential.

15.
Int J Pharm Pharm Sci ; 2020 Jan; 12(1): 54-58
Article | IMSEAR | ID: sea-205988

ABSTRACT

Objective: Phytochemicals as phenol and flavonoid have a powerful biological activity. So, this study aimed to carry out phytochemical screening, total phenol and flavonoid content in two plant species i.e. M. rubicaulis and R. indica. Methods: The extraction of different parts of two plant species was done by maceration using ethanol. Phytochemical screening was done to confirm the presence of phytochemicals. Total phenol content was done by Folin ciocalteu method and total flavonoid content was done by Aluminium chloride colorimetric method. Results: Phytochemical analysis revealed the presence of flavonoid, phenol, terpenoids in both plant species. The highest concentration of phenol content was observed in the root and stem of an extract of M. rubicaulis i.e. 281.83±1.98 mg GAE/g dry extract weight and 225.37±0.60 mg GAE/g dry extract weight. The highest concentration of flavonoid contents was observed in the leaves of R. indica i.e. 462.21±4.67 mg QE/g dry extract weight followed by stem and root of M. rubicaulis i.e. 381.06±5.23 mg QE/g dry extract weight and 337.43±1.39 mg QE/g dry extract weight. Conclusion: Phytochemical analysis concluded the presence of biologically important phytoconstituents like flavonoid and phenol in both plant species. Further studies, should be carried out to isolate specific chemical constituents and should be used in different studies to explore their biological effects.

16.
Braz. arch. biol. technol ; 63: e20200131, 2020. tab, graf
Article in English | LILACS | ID: biblio-1132247

ABSTRACT

Abstract Gallic acid (GA), as a strong antioxidant, was selected in this study to investigate its possible nephroprotective effects against gentamicin (GM)-induced nephrotoxicity. Twenty-four rats were separated into three groups (n=8): group 1 (control group) received saline (0.5 mL/day), group 2 (GM group) received GM (100 mg/kg/day), and group 3 (treated group) received GM (100 mg/kg/day) and GA (100mg/kg/day). All treatments were performed intraperitoneally for 12 days. After 12 days, the rats were euthanized, and kidneys were removed immediately. For serum preparation, blood samples were collected before killing. Kidney paraffin sections were prepared from one of the kidneys and stained by the periodic acid-Schiff process. GA significantly decreased GM-induced renal histopathological injuries, including tubular necrosis, tubular cast, and leucocyte infiltration compared with the GM group. Additionally, GA significantly improved proteinuria, serum levels of urea and creatinine, and serum activities of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) compared with nephrotoxic animals. Furthermore, GA caused a significant improvement in the levels of cholesterol (Chol), low-density lipoprotein (LDL), high-density lipoprotein (HDL), and cardiac risk ratios 1 and 2 in comparison with nephrotoxic animals. GA administration was observed to significantly improve the levels of lipid peroxidation, nitric oxide (NO), and glutathione (GSH) compared with the GM group. Finally, the activities and gene expression levels of catalase (CAT) and glutathione peroxidase (GPX) significantly increased following GA administration compared with the GM group. Our results indicated that GA has potential protective effects against GM nephrotoxicity by reducing oxidative stress in rats.


Subject(s)
Animals , Male , Rats , Gentamicins/adverse effects , Oxidative Stress/drug effects , Gallic Acid/therapeutic use , Kidney Diseases/drug therapy , Anti-Bacterial Agents/adverse effects , Antioxidants/therapeutic use , Biomarkers , Cholesterol , Rats, Wistar , Disease Models, Animal , Gallic Acid/chemistry , Kidney Diseases/chemically induced , Kidney Diseases/pathology , Lipoproteins, HDL , Lipoproteins, LDL
17.
Article in Chinese | WPRIM | ID: wpr-829953

ABSTRACT

Objective To design, synthesize and measure antifungal activities of galloyl piperazine derivatives. Methods Trimethoxyl gallic acid was used as starting material, reacted with piperazine in the presence of PyBOP/DIEA to afford the intermediates. The target compounds were obtained through the reaction with corresponding acids after deprotection gave. The antifungal activities of the target compounds were evaluated by FLC-resistant Candida albican isolated according to the CLSI recommended method. Results 11 target compounds were synthesized and six of them showed more potent antifungal activities than gallic acid. Conclusion Galloyl piperazine derivatives could enhance antifungal activities. Galloyl moiety was an important pharmacophore, which could improve antifungal activities with the introduction of cinnamic acid and 2,3-dichlorobenzoic acid.

18.
China Pharmacy ; (12): 963-968, 2020.
Article in Chinese | WPRIM | ID: wpr-820845

ABSTRACT

OBJECTIVE:To establish a method for simultaneous determination of gallic acid ,protocatechuic acid ,mangiferin, homomangiferin,hyperoside and isoquercetin in Mangguo zhike tablets. METHODS :HPLC was adopted. The determination was performed on Phenomenex Gemini C 18 column with mobile phase consisted of 0.1% phosphoric acid water solution-acetonitrile (gradient elution )at the flow rate of 1.0 mL/min. The detection wavelength was set at 258 nm. The column temperature was set at 30 ℃,and sample size was 5 μL. Gallic acid was used as the internal substance,and the correction factors of gallic acid , protocatechuic acid ,mangiferin,homomangiferin,hyperoside and isoquercetin were calculated ;the results of quantitative analysis of multi-components by single marker method (QAMS) were compared with those of external standard method (ESM). RESULTS:The linear range of gallic acid ,protocatechuic acid ,mangiferin,homomangiferin,hyperoside and isoquercetin were 45.75-183 0 μg/mL(r=0.999 9),2.525-101.0 μg/mL(r=0.999 9),65.33-261 3 μg/mL(r=0.999 6),9.058-362.3 μg/mL(r= 0.999 9),3.885-155.4 μg/mL(r=0.999 9),1.870-74.8 μg/mL(r=0.999 9),respectively. The limits of quantification were 0.571, 0.643,1.053,0.854,0.830,1.500 μg/mL,respectively. The limits of detection were 0.171,0.193,0.316,0.256,0.249,0.450 μg/mL, respectively. RSDs of precision ,stability and reproducibility tests were all lower than 3% . The average recoveries were 98.8%-101.9%(RSD=1.3% ,n=6),94.3%-101.5%(RSD=3.3%,n=6),97.9%-100.5%(RSD=0.9%,n=6),98.2%- 101.6% (RSD=1.2%,n=6),102.3%-106.1%(RSD=1.3%,n=6), 96.6% -99.3%(RSD=1.0% ,n=6),respectively. RCFs of 73) protocate-chuic acid , mangiferin, homomangiferin,hyperoside and isoquercetin were 0.568 3,0.500 3,0.687 6, 0.939 1 and 0.826 3,using gallic acid as internal substance . The content ranges of protocatechuic acid and other 4 com- ponents measured by QAMS were 0.197-0.440,3.262-11.250, 0.201-1.196,0.168-0.381,0.115-0.293 mg/tablet,respectively. The content ranges measured by ESM were 0.198-0.441,3.239-11.570,0.206-1.194,0.171-0.380,0.119-0.298 mg/tablet, respectively. By comparing the content determination results by QAMS and ESM ,the relative errors were -3.80%-0.74%,and there was no statistical significance (P>0.05). CONCLUSIONS :The established QAMS method is accurate ,reliable and repeatable,and can be used for content determination of 6 medicinal components in Mangguo zhike tablets.

19.
Article in Chinese | WPRIM | ID: wpr-846655

ABSTRACT

Objective: To provide references for optimizing adjuvants with Polygoni Multiflori Radix (PMR), we compared the effects of detoxification by different adjuvants processing according to Chinese medicine’s records of past dynasties. Methods: The chemical information of all samples including crude and processed PMR with different adjuvants was characterized by UPLC-Q-TOF-MS, and the normal human hepatocytes (L02 cell line) was cultured in vitro to evaluate the cytotoxicity, then we gave synthetic analyses on effects of processed PMR with different adjuvants for toxicity-decreasing and variations of chemical contents. The difference of toxicity reducing effect and the rule of composition change of PMR processed with different adjuvants were compared comprehensively. Results: Different adjuvants had different level of effects on chemical fingerprint, index component and cytotoxicity of PMR under the same conditions of pressure and time. More specifically, black bean, jujube and rice-rinsing water had greater impact on PMR main components including gallic acid, catechins, cis-stilbene glycoside, trans-stilbene glycoside, emodin-8-O-β-D-glucoside, physcion and emodin as well as hepatotoxicity. The three adjuvants with the best toxicity-decreasing effects were in sequence of rice-rinsing water > jujube > black bean. Furthermore, comprehensive analysis of simple correlation and multiple correlation suggested that cis-stilbene glycoside might be the main chemical component contributed to hepatotoxicity of PMR, and emodin-8-O-β-D-glucoside might be the potential toxicity component. Conclusion: Different adjuvants traditionally recorded can attenuate the toxicity of PMR. In addition to black beans, rice-rinsing water and jujube can also be used as candidate adjuvants for the toxicity-decreasing of PMR.

20.
Article in Chinese | WPRIM | ID: wpr-846626

ABSTRACT

Objective: To establish chemical fingerprint and multi-components determination of 15 batches of Taohong Siwu Decoction (TSD), and provide reference for the improvement of its quality control. Methods: The separation was performed on Thermo Hypersil Gold C18 column (250 mm × 4.6 mm, 5 μm) for gradient elution with methanol-0.1% phosphoric acid aqueous solution, flow rate 1.0 mL/min, column temperature 30 ℃, and detection wavelength 225 nm. The HPLC fingerprint was established and evaluated by the similarity evaluation system of TCM (version 2012A), and the difference of chemical information between 15 batches of different samples was evaluated by cluster analysis. Furthermore, the content of the nine active components in the sample was determined by HPLC multi-component wavelength switching method, with the partial least squares-discriminant analysis (PLS- DA) by SIMCA 14.1 software to find significant components of the quality between the batches. Results: The HPLC fingerprint of 15 batches of TSD was established. The similarity was greater than 0.96, and 35 common peaks were identified as gallic acid, chlorogenic acid, amygdalin, albiflorin, hydroxysafflor yellow A, paeoniflorin, ferulic acid, senkyunolide I, benzoylpaeoniflorin and ligustilide (corresponding to peaks 2, 8, 9, 13, 14, 15, 16, 25, 31, and 32). The linearity relationships of gallic acid, 5-hydroxymethylfurfural, chlorogenic acid, albiflorin, hydroxysafflor yellow A, paeoniflorin, ferulic acid, verbascoside, and senkyunolide I (r ≥ 0.999 6) were good. The results of content determination respectively were 187.5-344.4, 6.2-154.8, 413.2-459.2, 507.5-923.5, 873.8-1 202.0, 2 122.3-2 782.9, 59.2-121.3, 6.4-26.9, and 38.9-79.6 μg/g, respectively, including higher content of paeoniflorin, hydroxysafflor yellow A, and albiflorin. Furthermore, 15 batches of samples from different origins were classified into three categories. Using PLS-DA analysis, the content determination result showed that paeoniflorin, albiflorin, hydroxysafflor yellow A, and 5-hydroxymethylfurfural were the four components that affected the quality of different batches of TSD. Conclusion: HPLC fingerprint combined with multi-components determination is suitable for quality control and evaluation of TSD preparation.

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