scholarly journals Pharmacokinetic properties of inhibitors to Histidine Decarboxylase isolated from fennel

2020 ◽  
Vol 11 (4) ◽  
pp. 6707-6714
Author(s):  
Sneha Bhatt ◽  
Gletta Anjaly C.T ◽  
Shlini P
Keyword(s):  
Mast Cell ◽  
Thin Layer ◽  
Ellagic Acid ◽  
Inhibitory Activity ◽  
Histidine Decarboxylase ◽  
Methanolic Extract ◽  
Mast Cell Degranulation ◽  
Pharmacokinetic Properties ◽  
Phytochemical Constituents ◽  
Layer Chromatography

Histamine release is involved in developing wakefulness and activation of cortex. The purpose of the study was to find an alternative to these antihistamines by inhibiting the enzyme histidine decarboxylase which is responsible for the production of histamine. Histamine brings about the allergic response due to mast cell degranulation. It is also necessary that the enzyme is not completely inhibited as it plays a role as a neurotransmitter and also regulates gastric acid secretion. In the present study, the methanolic extract of commercially available fennel seeds were examined for its inhibitory activity on the purified extract of bacterial histidine decarboxylase. The methanolic extract of fennel was analyzed to check the presence of various phytochemical constituents. The spice extract was quantified to estimate the presence of flavonoids. The extract was subjected to purification by thin layer chromatography and HPLC in order to isolate and identify the flavonoids present in spice extract. The HPLC results with reference to the standard indicated the presence of ellagic acid and quercetin. The spice extracts were subjected to inhibitory studies at increasing concentrations. The fennel extract at concentration of 0.625 moles was found to be inhibiting histidine decarboxylase which was determined using the Dixon plot. The identified flavonoids were then subjected to software’s like Molinspiration and Swiss ADME in order to study the molecular properties, drug likeliness and pharmacokinetics.

scholarly journals High Performance Thin Layer Chromatography Fingerprinting Analysis of Piper betle L. Leaves

2021 ◽  
pp. 8-15
Author(s):  
Ramdas N. Kale ◽  
Ravindra Y. Patil
Keyword(s):  
Thin Layer ◽  
Thin Layer Chromatography ◽  
High Performance ◽  
Methanolic Extract ◽  
Chemical Constituents ◽  
Piper Betle ◽  
Soxhlet Apparatus ◽  
Rf Values ◽  
Pharmacologically Active ◽  
Layer Chromatography

Introduction: Many modern medicines used today based on plants and plant products. Piper betle is generally known as the betle vine, it is an important medicinal and recreational plant. High performance thin layer chromatography (HPTLC) is an advanced powerful analytical method with more separation power, high performance and superior reproducibility than classic thin layer chromatography (TLC). A chromatographic fingerprint of a plant extract is a chromatographic pattern of some common chemical constituents of pharmacologically active and/or chemical characteristics. Chromatographic fingerprints are useful in authentication and identification of plant. Objectives:  Objectives of present research was to establish HPTLC fingerprinting of methanolic extract of Piper betle L. leaves. Materials and Methods: Methanolic extract of Piper betle leaves was prepared using soxhlet apparatus. HPTLC studies were performed using a CAMAG HPTLC system equipped with automatic TLC sampler-4 (ATS 4), TLC scanner 4, and vision CATS 3.0 software. Results: The study revealed the presence of alkaloids with Rf value 0.65, flavonoids with Rf values 0.19, 0.29, 0.72, 0.95., and phenolic compound with Rf value 0.7. Conclusion: The HPTLC fingerprinting profile developed for the methanolic extract of Piper betle L. leaves will help in proper identification of the plant.Piper betle

scholarly journals High-Performance Thin-Layer Chromatography Densitometric Method for Simultaneous Quantitation of Phyllanthin, Hypophyllanthin, Gallic Acid, and Ellagic Acid in Phyllanthus amarus

2006 ◽  
Vol 89 (3) ◽  
pp. 619-623 ◽  
Author(s):  
Kamlesh Dhalwal ◽  
Yogesh S Biradar ◽  
Mandapati Rajani
Keyword(s):  
Thin Layer ◽  
Gallic Acid ◽  
Thin Layer Chromatography ◽  
Ellagic Acid ◽  
High Performance ◽  
Raw Material ◽  
Phyllanthus Amarus ◽  
Whole Plant ◽  
Recovery Study ◽  
Layer Chromatography

Abstract Whole plant of Phyllanthus amarus Linn. is a reputed drug of the Indian systems of medicine that is used as hepatoprotective agent. A simple high-performance thin-layer chromatography (HPTLC) densitometric method has been developed for the simultaneous quantitation of phyllanthin, hypophyllanthin, gallic acid, and ellagic acid in the whole plant of P. amarus. They were found at levels of 0.37, 1.16, 0.36, and 0.17% (w/w), respectively. The method was validated for precision, repeatability, and accuracy. Instrumental precision was found to be 0.54, 0.93, 0.08, and 0.78% (coefficient of variation, CV); repeatability of the method was 1.01, 0.79, 0.98, and 1.06% (CV) for phyllanthin, hypophyllanthin, gallic acid, and ellagic acid, respectively. Accuracy of the method was determined by a recovery study conducted at 3 different levels, and the average recovery was found to be 99.09% for phyllanthin, 99.27% for hypophyllanthin, 98.69% for gallic acid, and 100.49% for ellagic acid. The proposed HPTLC method was found to be simple, precise, specific, sensitive, and accurate and can be used for routine quality control of raw material of P. amarus and formulations containing P. amarus. It also has the applicability in quantitating any of these marker compounds in other drugs.

scholarly journals PRELIMINARY SCREENING OF PHYTOCHEMICAL CONSTITUENTS, ANTIOXIDANT AND ANTIMICROBICIDAL ACTIVITIES IN THE METHANOLIC LEAF EXTRACT OF COUROUPITA GUIANENSIS

2021 ◽  
pp. 203-206
Author(s):  
SUJATHA ILANGOVAN ◽  
THAVASUMANI P
Keyword(s):  
Inhibitory Activity ◽  
Leaf Extract ◽  
Methanolic Extract ◽  
Radical Scavenging ◽  
Preliminary Screening ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Couroupita Guianensis ◽  
Phytochemical Constituents ◽  
Antibacterial And Antifungal

Objective: The objective of the study was the preliminary screening of the methanolic leaf extract of Couroupita guianensis for various phytochemical constituents, its antioxidant, antibacterial, and antifungal activities. Methods: Phytochemical screening of 18 qualitative, 6 quantitative constituents, antioxidant activity, alpha-amylase inhibitory activity, and alpha-glucosidase inhibitory activity of the methanolic extract of the leaf of C. guianensis was performed adopting the standard protocols. The disk diffusion methods were used for assessing the antibacterial and antifungal activities of the extract. Results: The preliminary studies revealed the presence of alkaloids, saponin, flavonoids, phenol, tannin, and terpenoids in the methanolic extract of the leaf of C. guianensis. Potent antioxidant, free radical scavenging activity, and inhibitory activity against α-amylase and α-glucosidase activity of the methanolic extract were also evident. Conclusions: The preliminary studies in the methanolic extract of the leaf of C. guianensis are suggestive of the therapeutic potentials of the methanolic extract of leaves of C. guianensis.

scholarly journals HEPATOPROTECTIVE ACTIVITY OF THE WHOLE PLANT OF NEPTUNIA PROSTRATA L. IN CARBON TETRACHLORIDE INDUCED RATS

2021 ◽  
pp. 56-59
Author(s):  
HONEY JAJO ◽  
RAJAT GHOSH
Keyword(s):  
Thin Layer ◽  
Petroleum Ether ◽  
Thin Layer Chromatography ◽  
Methanolic Extract ◽  
Hepatoprotective Activity ◽  
Phytochemical Screening ◽  
Standard Drug ◽  
Whole Plant ◽  
Layer Chromatography ◽  
Serum Glutamate

Objective: The aim of this study is to investigate the hepatoprotective activity of the whole plant of Neptunia Prostrata L. Methods: The whole plant was collected and identified as Neptunia Prostrata L. The collected plants were shade dried and pulverized to fine powdered of particle size (#) 40. It was then defatted with petroleum ether for 24 hour and soaked with methanol and ethanol, respectively. The extracts was filtered and distilled off using a rotary evaporator. The phytochemical screening of the extracts was carried out and thin layer chromatography study was also done. Acute toxicity study and in vivo hepatoprotective activity of the methanolic extract using CCL4 (carbon tetra chloride) induced model was investigated. Results: The phytochemical screening revealed the presence of alkaloids, glycosides (saponins), flavonoids, tannins, carbohydrates, proteins, phenolic, steroids and terpenoids. Thin-layer chromatography of the methanolic and ethanolic extracts with their fractions using different solvents were performed by taking petroleum ether and ethyl acetate (2:8) as mobile phase system and were able to observe the presence of many spots. Oral administration of methanolic extract of Neptunia prostrata at doses till 2000 mg/kg was found safe and shows good hepatoprotective activity by showing decreased levels of serum SGOT (serum glutamate oxaloacetate transaminase), SGPT (serum glutamate pyruvate transaminase) and ALP (alkaline phosphatase) when compared with the standard drug silymarin. Conclusion: The preliminary phytochemical screening of the methanol and ethanolic extract shows phytoconstituents such as flavonoids, triterpenoids, tannins, saponins, alkaloids and chromatographic studies indicates the presence of several components in varying abundance. The decrease of serum bilirubin level by the methanolic extract of the plant shows hepatoprotective activity. It has confirmed the traditional claim for its use in the treatment of jaundice.

scholarly journals Phytochemical Investigation and Anti-angiogenic Examination of Iraqi Vigna radiata L. Seeds and Sprouts

2020 ◽  
Vol 29 (2) ◽  
pp. 37-47
Author(s):  
Rabab H. Qassim ◽  
Enas J. Kadhem
Keyword(s):  
High Performance Liquid Chromatography ◽  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Vigna Radiata ◽  
High Performance ◽  
Bioactive Constituents ◽  
Angiogenic Activity ◽  
Butanol Fraction ◽  
Phytochemical Constituents ◽  
Layer Chromatography

Abstract   The objective of this study was to investigate the phytochemical constituents of two different parts of Vigna radiata (seeds and sprouts), and identify their  anti angiogenic activity .the goal was achieved by Preliminary qualitative phytochemical screening for crude ethanolic extract of two parts of plant  ; rat aorta anti-angiogenesis assay had been conducted for both extracts .   isolation , separation and purification of some phytochemical constituents that belong to important groups (flavonoids) from  n-butanol fraction extract of Vigna radiata plant had been done in pure form by using preparative thin layer chromatography ( PTLC ) and then subjected to different spectral  analytical and physicochemical  techniques to identify their chemical structure : melting point ( M. P) , thin layer chromatography ( TLC ) high performance liquid chromatography ( HPLC ) , Fourier transforms infrared spectra ( FTIR ) . and high performance thin layer chromatography ( HPTLC ).the result  showed that  the existence of coumarin , alkaloids, phenols, flavonoids , terpenoids, phytosterol and saponin.Vitexin and isovitexin  were isolated in pure form .n-butanol fraction of sprouts  showed highest percentage of blood vessels inhibition ( 88%) in comparison to n-butanol fraction of seeds which showed (56%). There IC50 were 58.8µg/ml and 56.6 µg/ml respectively. The difference of anti angiogenic activity may be  related to the variation of concentration of the bioactive constituents or appearance of new bioactive constituents during germination.  Keywords: Vigna radiata, vitexin, isovitexin ,high performance thin layer chromatography  HPTLC , high performance liquid chromatography  HPLC

Synthesis and Biological Evaluation of Flavonoids as Antiacetyl- cholinesterase Agent

2014 ◽  
Vol 69 (1) ◽  
Author(s):  
Saleh Nazifi Ibrahim ◽  
Farediah Ahmad
Keyword(s):  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Microplate Assay ◽  
Synthetic Compounds ◽  
Ache Inhibitory Activity ◽  
Weak Activity ◽  
Layer Chromatography ◽  
Synthesis And Biological Evaluation

A series of chalcones, a flavone and one flavanone were synthesized and elucidated structurally by IR and 1H NMR spectroscopies. The synthetic compounds were then screened for acetylcholinesterase inhibitory activity using thin layer chromatography (TLC) and microplate assays. In the TLC assay, only 2′-hydroxy-4-methoxychalcone and 2′-hydroxy-4′-O-prenyl-2,6-dichlorochalcone were found to show moderate and weak activity respectively against acetylcholinesterase (AchE) at 0.1 mM concentration compared to the control galanthamine. 4′-Hydroxy-2,6-dichlorochalcone, 2′-hydroxy-4-nitrochalcone, 2′-hydroxy-4-(dimethyl)aminochalcone and 2′-hydroxy-4-methoxychalcone showed moderate AchE inhibitory activity with percentage inhibition of 54.24, 46.14 and 49.32 % respectively in the microplate assay.

Mast Cell Stabilizing, Antianaphylactic and Bronchodilatory activity of Methanolic extract of Averrhoa carambola Fruit

2021 ◽  
pp. 5258-5263
Author(s):  
Ravindra Babu Sajja ◽  
Prasad Konduri ◽  
Eswar Kumar Kilari
Keyword(s):  
Mast Cell ◽  
Methanolic Extract ◽  
Mast Cell Degranulation ◽  
Dependent Manner ◽  
Averrhoa Carambola ◽  
Peritoneal Mast Cells ◽  
Antianaphylactic Activity ◽  
Phytochemical Studies ◽  
Dose Dependent ◽  
Mast Cell Stabilization

This work was mainly aimed to study the mast cell stabilizing, anti-anaphylactic and bronchodilatory activities of methanolic extract of Averrhoa carambola (ACME). Mast cell stabilization activity was investigated by Compound 48/80 induced mast cell degranulation in rats and antianaphylactic activity was performed by determining the mortality rate of mice upon exposure to compound 48/80. The bronchodilatory effect of ACME was studied on histamine aerosol-induced bronchospasm using guinea pigs, in which occurrence of preconvulsive dyspnea (PCD) was noted as end point. Treatment with ACME (100, 200 and 400mg/kg) showed significant (p<0.05) protection of rat peritoneal mast cells and significantly (p<0.05) reduced the mortality of mice in a dose dependent manner. ACME significantly (p<0.05) increased the time of preconvulsive dyspnea (PCD) in a dose dependent manner that suggestive of bronchodilating activity. Phytochemical studies observed presence of saponins, tannins, steroids, alkaloids, flavonoids and glycosides. From these finding, we concluded that ACME possesses mast cell stabilizing; anti anaphylactic and bronchodilatory activity which might be used in treatment of asthma.

Estimation of Phenolic acid and Flavonoids in leaves of Amaranthus viridis and Amaranthus spinosus

2021 ◽  
pp. 3889-3895
Author(s):  
Swarnakumari S ◽  
Sasikala M ◽  
Mohan S ◽  
Divyanand Maharaj U ◽  
Kavipriya G
Keyword(s):  
Phenolic Compounds ◽  
Thin Layer ◽  
Gallic Acid ◽  
Phenolic Acid ◽  
Methanolic Extract ◽  
Solvent System ◽  
Who Guidelines ◽  
Phytochemical Screening ◽  
Amaranthus Spinosus ◽  
Layer Chromatography

Objective: To explore physiochemical and phytochemical standardization of leaves of Amaranthus viridis and Amaranthus spinosus. Method: As per WHO guidelines, physical standardization parameters with various solvents system were evaluated. The preliminary phytochemical screenings were adopted for disclosing the existence of phytochemicals in the discrete extracts. Thin layer chromatography and HPTLC were employed for methanolic extract of leaves of Amaranthus viridis and Amaranthus spinosus. Result: Preliminary phytochemical screening with various extracts reveals phytoconstituents. HPTLC fingerprint were executed for leaves of Amaranthus viridis and Amaranthus spinosus using selected solvent system. HPTLC analysis implies the presence of phenolic compounds and flavonoids in both the plant Amaranthus viridis and Amaranthus spinosus. Conclusion: Quercetin and Gallic acid was raise to be more in Amaranthus viridis compared to Amaranthus spinosus, however rutin was reported only in Amaranthus spinosus. The outcome of the research leads for isolation, purification and utilization in herbal industries.

scholarly journals Discovery of a Natural Syk Inhibitor from Chinese Medicine through a Docking-Based Virtual Screening and Biological Assay Study

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3114
Author(s):  
Xing Wang ◽  
Junfang Guo ◽  
Zhongqi Ning ◽  
Xia Wu
Keyword(s):  
Mast Cell ◽  
Chinese Medicine ◽  
Virtual Screening ◽  
Inhibitory Activity ◽  
Docking Studies ◽  
Mast Cell Degranulation ◽  
Amino Acid Residues ◽  
Tanshinone I ◽  
Syk Inhibitor

Spleen tyrosine kinase (Syk) is a critical target protein for treating immunoreceptor signalling-mediated allergies. In this study, a virtual screening of an in-house Chinese medicine database followed by biological assays was carried out to identify novel Syk inhibitors. A molecular docking method was employed to screen for compounds with potential Syk inhibitory activity. Then, an in vitro kinase inhibition assay was performed to verify the Syk inhibitory activity of the virtual screening hits. Subsequently, a β-hexosaminidase release assay was conducted to evaluate the anti-mast cell degranulation activity of the active compounds. Finally, tanshinone I was confirmed as a Syk inhibitor (IC50 = 1.64 μM) and exhibited anti-mast cell degranulation activity in vitro (IC50 = 2.76 μM). Docking studies showed that Pro455, Gln462, Leu377, and Lys458 were key amino acid residues for Syk inhibitory activity. This study demonstrated that tanshinone I is a Syk inhibitor with mast cell degranulation inhibitory activity. Tanshinone I may be a potential lead compound for developing effective and safe Syk-inhibiting drugs.

scholarly journals EXTRACTION, ISOLATION AND STRUCTURAL ELUCIDATION OF FLAVONOID FROM CHROZOPHORA PLICATA LEAVES AND EVALUATION OF ITS ANTIOXIDATIVE POTENTIALS

2017 ◽  
Vol 10 (4) ◽  
pp. 460
Author(s):  
Kadiri Sunil Kumar ◽  
Avanapu Srinivasa Rao
Keyword(s):  
Thin Layer ◽  
Superoxide Anion ◽  
Methanolic Extract ◽  
Reducing Power ◽  
Reducing Power Assay ◽  
Isolated Compound ◽  
Layer Chromatography ◽  
Column Chromatographic

Objective: This investigation involves the extraction, isolation, and characterization of flavonoid from a Euphorbiaceae family plant Chrozophoraplicata followed by evaluation of its antioxidant principles.Methods: The dried leaves were subjected to sequential soxhlation with polar and nonpolar solvents. Methanolic extract reveals the presence of largeamount of flavonoids. Methanolic extract was subjected to isolation using column chromatographic analysis with solvents such as petroleum ether,chloroform, hexane, ethyl acetate, methanol, and water. Further, the isolated compound was subjected to thin layer chromatography technique andspectral analysis such as infrared, 1HNMR, 13CNMR, mass spectroscopy, and high performance thin layer chromatography (HPTLC) finger printingtechniques. The compound was evaluated for in vitro antioxidant studies using 2,2-diphenyl-1-picrylhydrazyl (DPPH), NO assay, reducing power assay,H2O2 scavenging assay, superoxide anion scavenging assay and β-Carotene linoleate system and in vivo antioxidative studies using carbon tetrachloride(CCl4), and acetaminophen intoxicated rats.Results: The compound was isolated in methanol:water in the ratio of 80:20 using column chromatographic technique. On the basis of phytochemical,chromatographic, and spectral analysis, the isolated compound was identified as kaempferol and finally with HPTLC finger printing technique it wasfound that the Rf value of the isolated compound was found to be 0.58 which is nearly similar to the Rf value of standard kaempferol (0.55). Hence,the isolated compound was confirmed as kaempferol and is structurally elucidated as 3,5,7-trihydroxy-2-(4-hydroxyphenyl)chromen-4-one. Thiscompound was isolated for the first time from the C. plicata leaves. The in vitro antioxidant assay of isolated flavonoid has shown a dose-dependentincrease in free radical scavenging activity using DPPH, no assay, reducing power assay, H2O2 scavenging assay, superoxide anion scavenging assay, andβ-carotene linoleate system. Further, the methanolic extract of C. plicata (MECP) leaves was subjected to single dose acute toxicity study for 14 days infemale rats on the basis of OECD guidelines 423 and the therapeutically selected doses were 200 mg/kg and 400 mg/kg. In vivo antioxidant studies inCCl4 and acetaminophen intoxicated rats indicated that the MECP leaves have significantly decreased lipid peroxidation in a dose-dependent mannerand increased the levels of catalase, superoxide dismutase, and glutathione.Conclusions: By the above results, it was concluded that the isolated compound from C. plicata leaves was confirmed as kaempferol and it possessessignificant antioxidative potentials.Keywords: Chrozophora plicata leaves, Flavonoids, Extraction, Isolation, Characterization, Methanolic extract, Antioxidant activity, Carbontetrachloride, Acetaminophen.

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