Enzyme inhibitory assessment of the isolated constituents from Plantago holosteum Scop.

2020 ◽  
Vol 75 (3-4) ◽  
pp. 121-128
Author(s):  
F. Tugce Guragac Dereli ◽  
Yasin Genc ◽  
Iclal Saracoglu ◽  
Esra Kupeli Akkol
Keyword(s):  
Experimental Data ◽  
Enzyme Inhibition ◽  
Aqueous Extract ◽  
Inhibitory Activity ◽  
Folk Medicine ◽  
Inhibition Test ◽  
Phenylethanoid Glycosides ◽  
First Report ◽  
Aerial Parts

AbstractPlants of the Plantago genus are widely used in Turkish folk medicine especially for the treatment of wound, abscess, and inflammation. The aqueous extract and five phenylethanoid glycosides acteoside (1), arenarioside (2), echinacoside (3), isoacteoside (4), and leucosceptoside A (5) isolated from the aerial parts and roots of Plantago holosteum Scop. (Plantaginaceae) were tested for their possible inhibitory activity against hyaluronidase, elastase, and collagenase, related to wound pathogenesis. Even though the aqueous extract prepared from the aerial parts (36.26%) and roots (47.01%) and the isolated compounds acteoside (29.13%), echinacoside (28.73%), and isoacteoside (31.69%) exerted a notable inhibition, arenarioside and leucosceptoside A were found inactive in the hyaluronidase enzyme inhibition test. Similar results were obtained from the collagenase enzyme inhibition test. The aqueous extract prepared from the aerial parts (31.09%) and roots (35.17%), echinacoside (25.13%), and isoacteoside (23.85%) exerted a notable inhibition in this test. However, none of the extracts and isolated compounds displayed elastase enzyme inhibitory activity. The experimental data demonstrated that P. holosteum displayed a remarkable enzyme inhibitory activity against hyaluronidase and collagenase. This paper is the first report regarding the in vitro enzyme inhibitory activity of P. holosteum.

scholarly journals The Physical Adsorption of Gelatinized Starch with Tannic Acid Decreases the Inhibitory Activity of the Polyphenol against α-Amylase

Foods ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 1233
Author(s):  
Yueyi Wang ◽  
Shuangshuang Li ◽  
Fangting Bai ◽  
Junwei Cao ◽  
Lijun Sun
Keyword(s):  
Enzyme Inhibition ◽  
Tannic Acid ◽  
Inhibitory Activity ◽  
Adsorption Property ◽  
Physical Adsorption ◽  
Enzyme Active Site ◽  
Opposite Trend ◽  
Gelatinized Starch ◽  
The Difference

The effects of mixing orders of tannic acid (TA), starch, and α-amylase on the enzyme inhibition of TA were studied, including mixing TA with α-amylase before starch addition (order 1), mixing TA with pre-gelatinized starch before α-amylase addition (order 2) and co-gelatinizing TA with starch before α-amylase addition (order 3). It was found that the enzyme inhibition was always highest for order 1 because TA could bind with the enzyme active site thoroughly before digestion occurred. Both order 2 and 3 reduced α-amylase inhibition through decreasing binding of TA with the enzyme, which resulted from the non-covalent physical adsorption of TA with gelatinized starch. Interestingly, at low TA concentration, α-amylase inhibition for order 2 was higher than order 3, while at high TA concentration, the inhibition was shown with the opposite trend, which arose from the difference in the adsorption property between the pre-gelatinized and co-gelatinized starch at the corresponding TA concentrations. Moreover, both the crystalline structures and apparent morphology of starch were not significantly altered by TA addition for order 2 and 3. Conclusively, although a polyphenol has an acceptable inhibitory activity in vitro, the actual effect may not reach the expected one when taking processing procedures into account.

scholarly journals In Vitro α-Amylase and Protein Glycation Inhibitory Activity of the Aqueous Extract of Flueggea leucopyrus Willd

2018 ◽  
Vol 2018 ◽  
pp. 1-7 ◽  
Author(s):  
Vishmi Sachindra Thrikawala ◽  
Srianthie A. Deraniyagala ◽  
Chamira Dilanka Fernando ◽  
Dinusha Nishani Udukala
Keyword(s):  
Aqueous Extract ◽  
Diabetic Complications ◽  
Inhibitory Activity ◽  
Radical Scavenging ◽  
Vital Role ◽  
Protein Glycation ◽  
Total Phenolic ◽  
Chronic Hyperglycemia ◽  
Body Tissues

There is much interest in plant-based medicine with antidiabetic and antiglycation properties. Chronic hyperglycemia plays a vital role in the development of long-term diabetic complications by inducing protein glycation and the gradual formation of advanced glycation end products (AGEs) in various body tissues. The main objectives of this study were to investigate the aqueous extract of the whole plant of Flueggea leucopyrus Willd (FLAE), a medicinal plant used in traditional medicine in Sri Lanka for its in vitro α-amylase inhibitory activity and its inhibitory potential on the formation of AGEs. α-Amylase inhibitory activity determined by 3,5-dinitrosalicylic acid method revealed that FLAE possesses 29%–91% inhibitory activity at a concentration range of 2.5–400 μg/mL, respectively. Nonenzymatic protein glycation inhibitory capacity assessed by bovine serum albumin-fructose fluorescence spectrometric assay showed that FLAE at 15.6–250.0 μg/mL inhibited AGE formation by 0.9%–98%, respectively. Radical scavenging ability of FLAE using 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay and total phenolic and flavonoid contents of FLAE were also determined. This study shows that Flueggea leucopyrus Willd not only inhibits α-amylase enzyme, which is known to break starch to glucose, but also inhibits the formation of AGEs, which occur due to chronic hyperglycemia that leads to the onset of diabetic complications.

THEVETIA PERUVIANA ROOTS EXTRACT MEDICATED GOLD NANOPARTICLES AND ITS UREASE INHIBITORY ACTIVITY

2021 ◽  
pp. 79-82
Author(s):  
SAUD BAWAZEER
Keyword(s):  
Gold Nanoparticles ◽  
Aqueous Extract ◽  
Inhibitory Activity ◽  
Enzyme Inhibitor ◽  
Research Work ◽  
Thevetia Peruviana ◽  
Urease Enzyme ◽  
Urease Inhibitory ◽  
Microscopy Techniques

Objective: The main objective of the current research work was synthesized of gold nanoparticles (AuNPs) of Thevetia peruviana aqueous extract,characterization, and screening for urease enzyme inhibitory activity.Methods: AuNPs were synthesized by mixing 1 mM gold salt solution with T. peruviana aqueous extract without any reducing agents. The preparedAuNPs were characterized using UV–visible spectroscopy, Fourier transform infrared spectroscopy, and scanning electron microscopy techniques. Thesynthesized AuNPs were assessed for in vitro urease enzyme inhibitory activity at 0.2 μg in comparison with the aqueous extract.Results: In this finding, we synthesized the AuNPs of T. peruviana aqueous extract for the 1st time. The AuNPs exhibited significant stability atroom temperature. The AuNPs showed significant urease inhibitory activity with IC50 67.56±1.67 at 0.2 μg as compared to aqueous extract whichexhibited good activity with IC50 39.21±1.32 μ at 0.2 mg, against standard thiourea (IC50=21.00±1.16). The formation of AuNPs correlates due to activephytochemical present in extract which is responsible for synthesizing NPs.Conclusion: T. peruviana extract and prepared AuNPs are an outstanding urease enzyme inhibitor and are capable of making fine NPs. Application:The synthesized AuNPs of T. peruviana aqueous extract which significant urease inhibitory activity may allow us to discover NPs for potentiallyeffective and safe nanoherbal therapy.

scholarly journals Immunomodulatory Activity and Phytochemical Profile of Infusions from Cleavers Herb

Molecules ◽  
2020 ◽  
Vol 25 (16) ◽  
pp. 3721 ◽  
Author(s):  
Tetiana Ilina ◽  
Weronika Skowrońska ◽  
Natalia Kashpur ◽  
Sebastian Granica ◽  
Agnieszka Bazylko ◽  
...  
Keyword(s):  
Skin Diseases ◽  
Herbal Remedy ◽  
Folk Medicine ◽  
Immunomodulatory Activity ◽  
Blast Transformation ◽  
Immunostimulatory Activity ◽  
Traditional Use ◽  
Aerial Parts ◽  
Lymphocyte Blast Transformation

Extracts from aerial parts of G. aparine (cleavers) constitute a herbal remedy with monography in British Herbal Pharmacopeia. On the European market, there are several drugs and food supplements consisting of Galium extracts. In folk medicine, cleavers was used topically in Europe, Asia, and the Americas to treat skin diseases. In several remedies, cleavers is also listed as an immunomodulatory active herb influencing the defense response of the human body. The aim of this study was to investigate the immunostimulatory activity and antioxidant potential in vitro of a raw infusion of cleavers and bioactive fractions. The functional activity of lymphocytes in the reaction of the lymphocyte blast transformation (RLBT) method was used for immunomodulatory activity assays and direct scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO), and hydrogen peroxide (H2O2) was chosen for the examination of antioxidant activity. It was shown that both the raw extract and fractions show significant immunostimulatory and scavenging activities. The obtained data partially justify the traditional use of cleavers as topical remedy for skin infections and for wounds.

scholarly journals Flavonoids from Anoectochilus annamensis and their Anti-inflammatory Activity

2016 ◽  
Vol 11 (5) ◽  
pp. 1934578X1601100 ◽  
Author(s):  
Tran Minh Hoi ◽  
Tran Van Thai ◽  
Chu Thi Thu Ha ◽  
Ha Thi Van Anh ◽  
Phan Xuan Binh Minh ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Biological Activity ◽  
Chemical Composition ◽  
Inhibitory Activity ◽  
Inflammatory Mediator ◽  
Methanol Extract ◽  
Inflammatory Activity ◽  
Raw264.7 Cells ◽  
First Report ◽  
Aerial Parts

One new flavonol diglycoside, 4′,5-dihydroxy-3,3′,7-trimethoxyflavone 4′- O-α-L-rhamnopyranosyl-(1→6)-β-D-glucopyranoside (1), and two known compounds (2–3) were isolated from the methanol extract of Anoectochilus annamensis Aver. aerial parts. The effects were evaluated of all isolated compounds (1–3) on LPS-induced production of the inflammatory mediator nitric oxide (NO) by RAW264.7 cells. 4′,5-Dihydroxy-3,3′,7-trimethoxyflavone (2) was the most active while the addition of a rutinoside at C-4′ (compound 1) decreased the inhibitory activity. This is the first report on the chemical composition and biological activity of A annamensis.

scholarly journals Antioxidant Properties and Digestive Enzyme Inhibitory Activity of the Aqueous Extract from Leafy Stems of Cissus polyantha

2019 ◽  
Vol 2019 ◽  
pp. 1-7
Author(s):  
Mahamad Abba Talba ◽  
David Miaffo ◽  
Sylviane Laure Poualeu Kamani ◽  
Albert Kamanyi ◽  
Sylvie Léa Wansi
Keyword(s):  
Traditional Medicine ◽  
Aqueous Extract ◽  
Inhibitory Activity ◽  
Antiradical Activity ◽  
Digestive Enzyme ◽  
Antioxidant Properties ◽  
Antioxidant Potential ◽  
Antioxidant Power ◽  
Treatment Of Diabetes

Cissus polyantha (Vitaceae) is a plant used in Cameroonian traditional medicine for the treatment of diabetes. The aims of this study were to evaluate the in vitro antioxidant and antidiabetic activities of the aqueous extract of Cissus polyantha leafy stems. The enzyme inhibitory activity was determined in vitro on α-amylase and α-glucosidase enzymes, followed by confirmative study in vivo on normal rats (oral starch and sucrose tolerance tests at doses of 111, 222, and 444 mg/kg). The ferric reducing antioxidant power and the 2,2-diphenyl-1-picrylhydrazyl (DPPH) antiradical activity of the extract were examined to evaluate the antioxidant potential of the extract. The total content of phenols, flavonoids, and tannins of the extract were also determined. The results showed an inhibitory effect of the extract on the α-amylase and α-glucosidase activities with IC50 values of 216.14 and 182.40 μg/mL, respectively. The extract at doses of 222 and 444 mg/kg induced a significant decrease in postprandial glycaemia during the starch and sucrose tolerance tests. A remarkable antiradical activity of the extract was obtained although lower than that of the standard product. The aqueous extract of leafy stems of Cissus polyantha has an interesting inhibitory activity on the α-amylase and α-glucosidase enzymes, as well as an antioxidant potential, thus validating its use in traditional medicine for the treatment of diabetes mellitus and its complications.

scholarly journals GC-MS Investigation of Amaryllidaceae Alkaloids in Galanthus xvalentinei nothosubsp. subplicatus

2013 ◽  
Vol 8 (3) ◽  
pp. 1934578X1300800
Author(s):  
Buket Bozkurt Sarikaya ◽  
Strahil Berkov ◽  
Jaume Bastida ◽  
Gulen Irem Kaya ◽  
Mustafa Ali Onur ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Anticholinesterase Activity ◽  
Amaryllidaceae Alkaloids ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Aerial Parts ◽  
Ms Analysis ◽  
Ellman’S Method ◽  
First Time

A GC-MS analysis of alkaloids in the aerial parts and bulbs of Galanthus x valentinei nothosubsp. subplicatus was performed for the first time. Totally, twenty-six alkaloids were identified, of which tazettine and galanthindole were the major ones. Acetylcholinesterase inhibitory activity of the alkaloidal extracts was determined using modified in vitro Ellman's method. Significant anticholinesterase activity was observed in the tested samples (bulbs: IC50 = 21.3 μg/mL, aerial parts: IC50 = 16.3 μg/mL).

scholarly journals Hypoglycemic potential of Trixis angustifolia aqueous extract in alloxan-induced diabetic mice

2019 ◽  
Vol 14 (2) ◽  
pp. 74-79 ◽  
Author(s):  
Anuar Salazar-Gómez ◽  
María Elena Vargas-Díaz ◽  
Leticia Garduño-Siciliano
Keyword(s):  
Aqueous Extract ◽  
Reducing Sugars ◽  
Low Density Lipoprotein ◽  
Folk Medicine ◽  
Density Lipoprotein ◽  
Diabetic Mice ◽  
Glucose Levels ◽  
Hypoglycemic Agent ◽  
Aerial Parts ◽  
Blood Glucose Levels

The aim of the present study was to evaluate the hypoglycemic potential of Trixis angustifolia in alloxan-induced diabetic mice. An intragastric adminis-tration of the aqueous extract (50, 100 and 200 mg/kg) prepared from the aerial parts of T. angustifolia was evaluated. The treatment with the extract at 100 mg/kg produced a significant lowered (30.5%) of the blood glucose levels in diabetic mice after 15 days of daily oral administration. In addition, the extract induced a significant decrease in serum total cholesterol, low density lipoprotein whereas increased the high-density lipoprotein level. Additionally, the presence of alkaloids, cumarins, saponins, flavonoids and reducing sugars were identified in the extract. These findings provide a basis explain-ing the traditional folk medicine use of this plant as a hypoglycemic agent by the Mexican people.

scholarly journals UFLC-MS-IT-TOF and Bioassay Guided Isolation of Flavonoids as Xanthine Oxidase Inhibitors from Diospyros dumetorum

2017 ◽  
Vol 12 (11) ◽  
pp. 1934578X1701201
Author(s):  
Zhen-Tao Deng ◽  
Tong-Hua Yang ◽  
Xiao-Yan Huang ◽  
Xing-Long Chen ◽  
Jian-Gang Zhang ◽  
...  
Keyword(s):  
Xanthine Oxidase ◽  
Inhibitory Activity ◽  
Folk Medicine ◽  
Hydroxyl Groups ◽  
Active Constituents ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Pulmonary Abscess ◽  
Xanthine Oxidase Inhibitors

Diospyros dumetorum is an important folk medicine for treating pulmonary abscess and inflammation. The leaves of D. dumetorum revealed xanthine oxidase (XOD) inhibitory activity. With the guidance of UFLC-MS-IT-TOF analyses combined with bioassay in vitro, 15 flavonoids were isolated from the active parts of D. dumetorum. Except for 11 (IC50 > 200μM), all compounds showed obvious XOD inhibitory activity with IC50 values of 32.5 ± 0.7 ~ 145.0 ± 3.3 μM. The preliminary structure-activity relationships study suggested that glycosylation on C-3 was unfavorable for XOD inhibitory activity; hydroxyl groups on ring B were essential for maintaining activity; the activity was closely related with the position of galloylation. This is the first recognition of the XOD inhibitory activity and active constituents of D. dumetorum, and will provide valuable information for this plant as a new resource for treating hyperuricemia and gout.

Halimium halimifolium: From the Chemical and Functional Characterization to a Nutraceutical Ingredient Design

Planta Medica ◽  
2019 ◽  
Vol 85 (11/12) ◽  
pp. 1024-1033 ◽  
Author(s):  
Khawla Kerbab ◽  
Francesca Sansone ◽  
Lahcene Zaiter ◽  
Tiziana Esposito ◽  
Rita Celano ◽  
...  
Keyword(s):  
Functional Characterization ◽  
Folk Medicine ◽  
Oral Intake ◽  
In Vitro Dissolution ◽  
Bioactive Components ◽  
Ph Change ◽  
Laser Scattering ◽  
Aerial Parts ◽  
Derivatives Of

Abstract Halimium halimifolium (Hh) is a shrub used in Algerian folk medicine to treat gastrointestinal pain. An UHPLC-PDA-ESI/MSn method was developed to identify the metabolic profile of the traditionally used infusion (Hh-A) from the aerial parts. The structures of flavanols were confirmed by NMR analysis after the isolation procedure from a hydrohalcolic extract (Hh-B) that also allowed for the identification of phenolic acids, an aryl butanol glucoside, and different derivatives of quercetin, myricetin, and kaempferol. Tiliroside isomers were the chemical markers of Hh-A and Hh-B (54.33 and 36.00 mg/g, respectively). Hh-A showed a significant scavenging activity both against the radicals 1,1-diphenyl-2-picrylhydrazyl and 2,2′-Azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (EC50 = 10.49 µg/mL and TEAC value = 1.98 mM Trolox/mg infusion) and the lipopolysaccharide-induced reactive oxygen species release in A375 and HeLa cells. Moreover, the antihyperglycemic properties, by inhibiting the α-amylase and α-glucosidase enzymes (IC50 = 0.82 mg/mL and 25.01 µg/mL, respectively), were demonstrated. To upgrade the therapeutic effect, a microencapsulation process is proposed as a strategy to optimize stability, handling, and delivery of bioactive components, avoiding the degradation and loss of the biological efficacy after oral intake. Hh-loaded microparticles were designed using cellulose acetate phthalate as the enteric coating material and spray drying as a production process. The results showed a satisfactory process yield (67.9%), encapsulation efficiency (96.7%), and micrometric characteristics of microparticles (laser-scattering, fluorescent, and scanning electron microscopy). In vitro dissolution studies (USPII-pH change method) showed that Hh-loaded microparticles are able to prevent the release and degradation of the bioactive components in the gastric tract, releasing them into the intestinal environment.

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