STUDY ON BOTANICAL CHARACTERISTICS AND ACETYLCHOLINESTERASE INHIBITORY ACTIVITY OF TWO SPECIES LEEA SP. - LEEACEAE

2019 ◽  
pp. 22-29
Author(s):  
Thi Bich Hien Le ◽  
Thi Minh Quy Le
Keyword(s):  
Inhibitory Activity ◽  
Antibacterial Effects ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Osteoarthritis Pain ◽  
Microbiological Characteristics ◽  
Ic50 Values ◽  
Powder Characteristics ◽  
Botanical Characteristics ◽  
Inhibitory Activities ◽  
Dyeing Method

Background: The species belonging to the genus Leea, Leeaceae are reported to have anti-inflammatory, antioxidant, analgesic, antibacterial effects, and have been used to treat osteoarthritis pain, rheumatism, digestive and cancer diseases. The project aims to study botanical characteristics and Acetylcholinesterase inhibitory activity of two species of genus Leea. Materials and method: Two species Leea rubra Blume ex Spreng. and Leea curtisii King., Leeaceae were identified the powder characteristics, microsurgical characteristics by double dyeing method, determined Acetylcholinesterase inhibitory activity by the method of Ellman. Results: Identified characteristics of microsurgery and powder of 2 studied species; total extracts and fractional extracts of 2 studied species shown the average Acetylcholinesterase inhibitory activities with the IC50 values in the range of 42.44 to 97.96 µg/ml. Conclusion: The project contributed to standardize microbiological characteristics and determined Acetylcholinesterase inhibitory activity of two species belonging to the genus Leea. Key words: Acetylcholinesterase, Leea rubra, Leea curtisii, microsurgery, powder characteristics

Synthesis, in vitro Acetylcholinesterase Inhibitory Activity Evaluation and Docking Investigation of Some Aromatic Chalcones

MedPharmRes ◽  
2017 ◽  
Vol 1 (1) ◽  
pp. 15-25
Author(s):  
Dao Tran ◽  
Son Tran ◽  
Vi Nguyen ◽  
Tri Le ◽  
Minh Thai ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Condensation Reaction ◽  
Acetylcholinesterase Inhibitors ◽  
Docking Studies ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Ellman’S Method

In this study, a total of twenty chalcones were synthesized via Claisen-Schmidt condensation reaction and evaluated for their in vitro acetylcholinesterase inhibitory activities using Ellman’s method. Molecular docking studies on acetylcholinesterase were performed to elucidate the interactions between these chalcone derivatives and acetylcholinesterase active site at the molecular level. From the series, six compounds (S1-5 and S17) exhibited strong acetylcholinesterase inhibitory activities with IC50 values below 100 µM compared to the parent unsubstituted chalcone. Compound S17 (4’-amino-2-chlorochalcone) showed the strongest acetylcholinesterase inhibitory activity in the investigated group with IC50 value of 36.10 µM. Molecular modeling studies were consistent with the results of in vitro acetylcholinesterase inhibitory activities, and chalcone S17 could be considered as a potential lead compound for the development of new acetylcholinesterase inhibitors.

GC-MS Investigation and Acetylcholinesterase Inhibitory Activity of Galanthus rizehensis

2013 ◽  
Vol 68 (3-4) ◽  
pp. 118-124 ◽  
Author(s):  
Buket Bozkurt Sarikaya ◽  
Nehir Unver Somer ◽  
Gulen Irem Kaya ◽  
Mustafa Ali Onur ◽  
Jaume Bastida ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Gas Chromatography ◽  
Inhibitory Activity ◽  
Gas Chromatography Mass Spectrometry ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Aerial Parts ◽  
Chromatography Mass Spectrometry ◽  
Inhibitory Activities ◽  
Alkaloid Extracts ◽  
Potent Inhibitory Activity

GC-MS (gas chromatography-mass spectrometry) analyses of alkaloids in the aerial parts and bulbs of Galanthus rizehensis Stern (Amaryllidaceae), collected during two different vegetation periods, was performed. Twenty three alkaloids were identified in four different alkaloid extracts. Acetylcholinesterase (AChE) inhibitory activities of the alkaloid extracts were tested. Both the highest alkaloid diversity and the most potent inhibitory activity (IC50 12.94 μg/ml) were obtained in extracts from the bulbs of G. rizehensis collected during the fruiting period.

Alkaloids and lignans with acetylcholinesterase inhibitory activity from the flower buds of Magnolia biondii Pamp

2020 ◽  
Vol 44 (25) ◽  
pp. 10309-10316
Author(s):  
Yangang Cao ◽  
Hongwei Li ◽  
Yanli Zhang ◽  
Jianchao Wang ◽  
Yingjie Ren ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Flower Buds ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Inhibitory Activities

Sixteen compounds, including two new alkaloids and three new lignans, were isolated and their AChE inhibitory activities were evaluated.

Salazinic Acid-Derived Depsidones and Diphenylethers with α-Glucosidase Inhibitory Activity from the Lichen Parmotrema dilatatum

Planta Medica ◽  
2020 ◽  
Vol 86 (16) ◽  
pp. 1216-1224
Author(s):  
Asshaima Paramita Devi ◽  
Thuc-Huy Duong ◽  
Solenn Ferron ◽  
Mehdi A. Beniddir ◽  
Minh-Hiep Dinh ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Positive Control ◽  
Spectroscopic Analyses ◽  
Ic50 Values ◽  
Inhibitory Activities

AbstractThree new depsidones, parmosidones F – G (1 – 2), and 8′-O-methylsalazinic acid (3), and 3 new diphenylethers, parmetherines A – C (4 – 6), together with 2 known congeners were isolated from the whole thalli of Parmotrema dilatatum, a foliose chlorolichen. Their structures were unambiguously determined by extensive spectroscopic analyses and comparison with literature data. The isolated polyphenolics were assayed for their α-glucosidase inhibitory activities. Newly reported benzylated depsidones 1 and 2 in particular inhibited α-glucosidase with IC50 values of 2.2 and 4.3 µM, respectively, and are thus more potent than the positive control, acarbose.

α-Glucosidase Inhibitory Activity of the Extracts and Major Phytochemical Components of Smilax glabra Roxb

2020 ◽  
Vol 10 (1) ◽  
pp. 26-32
Author(s):  
Phuong T.M. Nguyen ◽  
Quang V. Ngo ◽  
Minh T.H. Nguyen ◽  
Alan T. Maccarone ◽  
Stephen G. Pyne
Keyword(s):  
Inhibitory Activity ◽  
In Vitro Cytotoxicity ◽  
Antidiabetic Activity ◽  
Ca 125 ◽  
Chemical Structures ◽  
Glucosidase Inhibitors ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Phytochemical Components

Background: A therapeutic approach to treat diabetes is to decrease postprandial hyperglycemia. α-Glucosidase inhibitors from plant sources offer an attractive strategy for the control of hyperglycemia. Smilax glabra Roxb is a medicinal plant found in Asia, including Vietnam, which is used in the treatment of chronic diseases. However, the antidiabetic activity and the identification of α-glucosidase inhibitors from this plant have not been intensively investigated. This research was carried out to determine the α-glucosidase inhibitory activity of the extracts and that of the major phytochemical components of Smilax glabra Roxb. This could lead to further studies on the role of these compounds in hyperglycemia control, as well as identify their potential future applications. Methods: Column chromatography combined with crystallization procedures were used to isolate active fractions and two major compounds. The chemical structures of these compounds were determined by analysis of their NMR spectroscopic data, as well as MS data and comparisons made with the literature data. The α-glucosidase inhibitory activity was determined spectrophotometrically using p-nitrophenyl α-D-glucopyranoside as a substrate. The in vitro cytotoxicity of the isolated compounds and fractions was determined using the MTT assay. Results: The two major compounds, astilbin and 5-O-caffeoylshikimic acid together with two very active fractions, F7 and F8, were isolated from the rhizome. The two major compounds had α- glucosidase inhibitory activities with IC50 values of ca. 125 µg/mL and 38 µg/mL, respectively which are about 4 and 13 folds higher activity than the reference compound acarbose (IC50 of ca. 525 µg/mL). Fractions F7 and F8 showed very promising inhibitory activities towards α-glucosidase with IC50 values of 5.5 and 5.8 µg/mL, respectively. Cytotoxicity data on mouse fibroblast NIH3T3 cells indicated that the active compounds and fractions were not toxic at concentrations that are greater than their respective IC50 values. The α-glucosidase inhibitory activity of 5-Ocaffeoylshikimic acid and that of the two active fractions are reported here for the first time. Conclusion: The two major isolated compounds and fractions, F7 and F8, significantly contribute to the α-glucosidase inhibitory activity of S. glabra Roxb extract. Further work is needed to clarify their modes of action and potential application.

Alkaloid profiles and acetylcholinesterase inhibitory activities of Fumaria species from Bulgaria

2016 ◽  
Vol 71 (1-2) ◽  
pp. 9-14 ◽  
Author(s):  
Radka Z. Vrancheva ◽  
Ivan G. Ivanov ◽  
Ina Y. Aneva ◽  
Ivayla N. Dincheva ◽  
Ilian K. Badjakov ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Hplc Analysis ◽  
Acetylcholinesterase Activity ◽  
Isoquinoline Alkaloids ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Ms Analysis ◽  
Inhibitory Activities ◽  
Alkaloid Extracts ◽  
Alkaloid Profiles

Abstract GC-MS analysis of alkaloid profiles of five Fumaria species, naturally grown in Bulgaria (F. officinalis, F. thuretii, F. kralikii, F. rostellata and F. schrammii) and analysis of acetylcholinesterase inhibitory activity of alkaloid extracts were performed. Fourteen isoquinoline alkaloids were identified, with the principle ones being protopine, cryptopine, sinactine, parfumine, fumariline, fumarophycine, and fumaritine. Protopine contents, defined by HPLC analysis varied between 210.6 ± 8.8 μg/g DW (F. schrammii) and 334.5 ± 7.1 μg/g DW. (F. rostellata). While all of the investigated alkaloid extracts significantly inhibited acetylcholinesterase activity, the F. kralikii demonstrated the highest level of inhibition (IC50 0.13 ± 0.01 mg extract/mL).

Design and Synthesis of arylnaphthalene lignan lactones derivatives as Potent Topoisomerase Inhibitors

2020 ◽  
Vol 16 ◽  
Author(s):  
Wang Chen ◽  
Zili Feng ◽  
Daihua Hu ◽  
Jin Meng
Keyword(s):  
Inhibitory Activity ◽  
Topoisomerase I ◽  
Antitumor Agents ◽  
Chemotherapeutic Agents ◽  
Dna Breaks ◽  
Dna Relaxation ◽  
Design And Synthesis ◽  
Ic50 Values ◽  
Inhibitory Activities

Background: Arylnaphthalene lignan lactones are a class of natural products containing the phenyl-naphthyl skeleton. Some arylnaphthalene lignan lactones have been used in clinical as antitumor agents, due to their cytotoxicity and inhibitory activities against DNA topoisomerase I (Topo I) and topoisomerase II (Topo II). Objective: We present the design and synthesis of arylnaphthalene lignan lactones derivatives. The inhibitory activities against Topo I and Topo IIα and antitumor activities of these compounds were assayed. Method: A series of arylnaphthalene lignan lactones derivatives have been designed and synthesized, using Diels-Alder reaction and Suzuki reaction as the key steps. Their antiproliferation activities were evaluated by sulforhodamine B assay on human breast cancer MDAMB-231, MDA-MB-435 and human cervical cancer HeLa cells. DNA relaxation assays were employed to examine the inhibitory activity of compounds 1-22 on Topo I and Topo IIα in vitro. Flow cytometry analysis was performed to study the drug effects on cell cycle progression. Results: Seven compounds exhibited modest anti-proliferation activity with IC50 values between 1.36 and 20 µM. Compounds 3, 19 and 22 showed potent inhibitory activities with IC50 values less than 1 µM. DNA relaxation assay revealed that compound 22 showed potent inhibitory activity against Topo IIα in vitro. Compound 22 also induced DNA breaks in MDA-MB-435 cells evidenced by comet tails and the accumulation of γ-H2AX foci. The ability of 22 in inducing DNA breaks mediated by Topo IIα resulted in G2/M phase arrest and apoptosis. Conclusion: This work indicates that arylnaphthalene lignan lactones derivatives represent a novel type of Topo IIα inhibitory scaffold for developing new antitumor chemotherapeutic agents.

scholarly journals Five New Pregnane Glycosides from Gymnema sylvestre and Their α-Glucosidase and α-Amylase Inhibitory Activities

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2525 ◽  
Author(s):  
Phan Van Kiem ◽  
Duong Thi Hai Yen ◽  
Nguyen Van Hung ◽  
Nguyen Xuan Nhiem ◽  
Bui Huu Tai ◽  
...  
Keyword(s):  
Medicinal Plant ◽  
Traditional Medicine ◽  
Oleanolic Acid ◽  
Inhibitory Activity ◽  
Gymnema Sylvestre ◽  
Spectroscopic Evidence ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
Treatment Of Diabetes ◽  
Inhibitory Activities

Gymnema sylvestre, a medicinal plant, has been used in Indian ayurvedic traditional medicine for the treatment of diabetes. Phytochemical investigation of Gymnema sylvestre led to the isolation of five new pregnane glycosides, gymsylosides A–E (1–5) and four known oleanane saponins, 3β-O-β-D-glucopyranosyl (1→6)-β-D-glucopyranosyl oleanolic acid 28-O-β-D-glucopyranosyl ester (6), gymnemoside-W1 (7), 3β-O-β-D-xylopyranosyl-(1→6)-β-D- glucopyranosyl-(1→6)-β-D-glucopyranosyl oleanolic acid 28-O-β-D-glucopyranosyl ester (8), and alternoside XIX (9). Their structures were identified based on spectroscopic evidence and comparison with those reported in the literature. All compounds were evaluated for their α-glucosidase and α-amylase inhibitory activities. Compounds 2–4 showed significant α-amylase inhibitory activity, with IC50 values ranging from 113.0 to 176.2 µM.

scholarly journals Alpha-Glucosidase and Alpha-Amylase Inhibitory Activities, Molecular Docking, and Antioxidant Capacities of Salvia aurita Constituents

Antioxidants ◽  
2020 ◽  
Vol 9 (11) ◽  
pp. 1149
Author(s):  
Ninon G. E. R. Etsassala ◽  
Jelili A. Badmus ◽  
Jeanine L. Marnewick ◽  
Emmanuel I. Iwuoha ◽  
Felix Nchu ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Antidiabetic Drugs ◽  
Alpha Amylase ◽  
Ic50 Values ◽  
Trolox Equivalent ◽  
Inhibitory Activities ◽  
Abietane Diterpenes ◽  
Alpha Glucosidase

Diabetes mellitus (DM) is one of the most dangerous metabolic diseases with a high rate of mortality worldwide. It is well known that insulin resistance and deficiency in insulin production from pancreatic β-cells are the main characteristics of DM. Due to the detrimental side effects of the current treatment, there is a considerable need to develop new effective antidiabetic drugs, especially alpha-glucosidase and alpha-amylase inhibitors with lesser adverse effects. These inhibitors are known to be directly involved in the delay of carbohydrate digestion, resulting in a reduction of glucose absorption rate and, consequently, reducing the postprandial rise of plasma glucose, which can reduce the risk of long-term diabetes complications. Furthermore, natural products are well-known sources for the discovery of new bioactive compounds that can serve as scaffolds for drug discovery, including that of new antidiabetic drugs. The phytochemical investigation of Salvia aurita collected from Hogobach Pass, Eastern Cape Province, South Africa (SA), yielded four known abietane diterpenes namely carnosol (1), rosmanol (2), 7-methoxyrosmanol (3), 12-methoxycarnosic acid (4), and one flavonoid named 4,7-dimethylapigenin (5). Structural characterization of these isolated compounds was conducted using 1 and 2D NMR, in comparison with reported spectroscopic data. These compounds are reported for the first time from S. aurita. The biological evaluation of the isolated compound against alpha-glucosidase exhibited strong inhibitory activities for 3 and 2 with the half maximal inhibitory concentration (IC50) values of 4.2 ± 0.7 and 16.4 ± 1.1 µg/mL respectively, while 4 and 1 demonstrated strong alpha-amylase inhibitory activity amongst the isolated compounds with IC50 values of 16.2 ± 0.3 and 19.8 ± 1.4 µg/mL. Molecular docking analysis confirms the strong inhibitory activity of 3 against alpha-glucosidase. Additionally, excellent antioxidant capacities were displayed by 2, 1, and 3, respectively, with oxygen radical absorbance capacity (ORAC) (25.79 ± 0.01; 23.96 ± 0.01; 23.94 ± 0.02) mM Trolox equivalent (TE)/g; 1 and 2 as ferric-ion reducing antioxidant power (FRAP) (3.92 ± 0.002; 1.52 ± 0.002) mM ascorbic acid equivalent (AAE)/g; 5 and 2 as Trolox equivalent absorbance capacity (TEAC) (3.19 ± 0.003; 2.06 ± 0.003) mM TE/g. The methanolic extract of S. aurita is a rich source of abietane diterpenes with excellent antioxidant and antidiabetic activities that can be useful to modulate oxidative stress and might possibly be excellent candidates for the management of diabetes. This is the first scientific report on the phytochemical isolation and biological evaluation of the alpha-glucosidase and alpha-amylase inhibitory activities of Salvia aurita.

scholarly journals Triterpenoids from Alisma orientale and their NF-кB Inhibitory Activity

2021 ◽  
Vol 8 (03) ◽  
pp. e114-e121
Author(s):  
Qian Yang ◽  
Yinqing Li ◽  
Xizi Liu ◽  
Shiyi Han ◽  
Siyang Fan
Keyword(s):  
Inhibitory Activity ◽  
Nuclear Factor ◽  
Human Embryonic Kidney ◽  
Electronic Circular Dichroism ◽  
Nuclear Factor Kappa ◽  
293 Cells ◽  
Alisma Orientale ◽  
Ic50 Values ◽  
Inhibitory Activities ◽  
Circular Dichroïsm

AbstractThe rhizome of Alisma orientale (sam.) Juz. is used in clinics for eliminating dampness, reducing edema, and promoting diuresis. This study aimed to elucidate the compounds and investigate their nuclear factor-kappa inhibitory activities in human embryonic kidney 293 cells. A new triterpene, alismaketone B (1); a new natural nortriterpene, noralisolic acid A (2); and 13 known protostane-type triterpenes were isolated from the rhizome of A. orientale. The new structures and their absolute configurations were established using HRESIMS, NMR, and electronic circular dichroism experiments. All isolated compounds were evaluated for their inhibitory activity on NF-κB. The compounds 8, 9, 10, and 14 showed moderate NF-κB inhibitory activities with their IC50 values being 64.7, 32.3, 47.3, and 37.3 μM, respectively.

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