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Anti-diabetic and anti-Alzheimer’s disease activities of Angelica decursiva
Md. Yousof Ali,최재수,정현아 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.12
Diabetes mellitus (DM) and Alzheimer’s disease (AD) constitute two global health issues. DM is an ever-increasing epidemic affecting millions of elderly people worldwide, causing major repercussions on patients’ daily lives, mostly due to chronic complications. Complications from DM can affect the brain, thereby characterizing DM as a risk factor for AD. In the present study, we examined the inhibitory activity of methanol extracts of different parts of 12 Angelica species against aglucosidase, protein tyrosine phosphatase 1B (PTP1B), acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). The methanol extract of Angelica decursiva exhibited the highest inhibitory activities against a-glucosidase, PTP1B, AChE, and BChE and so was selected for further investigation. Repeated column chromatography based on bioactivity-guided fractionation yielded seven compounds (1–7). Among these compounds, nodakenin (1), nodakenetin (2), umbelliferone (3), cis-30-acetyl-40- angeloylkhellactone (4), 30(R)-O-acetyl-40(S)-Otigloylkhellactone (5), isorutarine (6), and para-hydroxybenzoic acid (7) exhibited potent inhibitory activities against a-glucosidase, PTP1B, rat lens aldose reductase (RLAR), AChE, BChE, and b-site amyloid precursor protein cleaving enzyme 1 (BACE1). Our results clearly indicate the potential inhibition of a-glucosidase, PTP1B, RLAR, AChE, BChE, and BACE1 by A. decursiva as well as its isolated constituents, which could be further explored to develop therapeutic modalities for the treatment of DM and AD.
Md. Yousof Ali,정현아,Susoma Jannat,최재수 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.2
The formation of advanced glycation end-products(AGE) and aldose reductase activity have beenimplicated in the development of diabetic complications. The present study was aimed to evaluate human recombinantaldose reductase (HRAR) and AGE inhibitory activityof seven natural dihydroxanthyletin-type coumarins,4-hydroxy Pd-C-III (1), 40-methoxy Pd-C-I (2), Pd-C-I (3),Pd-C-II (4), Pd-C-III (5), decursidin (6), and (?)-transdecursidinol(7) from Angelica decursiva. Coumarins 1–7showed potent HRAR and AGE inhibitory activities withranges of IC50 values of 1.03–21.31 and 0.41–5.56 lM,respectively. In the kinetic study for HRAR enzyme inhibition,coumarins 1, 3, 4, and 7 were competitive-typeinhibitors, 6 was a mixed-type inhibitor, whereas 2 and 5were noncompetitive-type inhibitors. Furthermore, we alsopredicted the docking interactions of HRAR with coumarins1–7 using AutoDock Vina, and as a result, thesimulated enzyme-inhibitor complexes exhibited negativebinding energies (Autodock Vina = - 9.6 to- 8.1 kcal/mol for HRAR), indicating a high affinity andtight binding capacity for the HRAR active site. Our resultsclearly indicate the potential HRAR and AGE formationinhibitory activities of dihydroxanthyletin-type coumarins,which could be further explored to develop therapeuticmodalities for the treatment of diabetes and relatedcomplications.
Md. Yousof Ali,성수희,정현아,Susoma Jannat,최재수 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.7
In the present study, we investigated the anti-Alzheimer’s disease (AD) potential of six dihydroxanthyletin-type coumarins, 40-hydroxy Pd–C-III (1), decursidin(2), Pd–C-I (3), 40-methoxy Pd–C-I (4), Pd–C-II (5),and Pd–C-III (6) from Angelica decursiva by evaluatingtheir ability to inhibit acetylcholinesterase (AChE),butyrylcholinesterase (BChE) and b-site amyloid precursorprotein cleaving enzyme 1 (BACE1). Coumarins 1–6exhibited dose-dependent inhibition of AChE, BChE, andBACE1. IC50 values were 1.0–4.01 lM for AChE,5.78–13.91 lM for BChE, and 1.99–17.34 lM for BACE1. Kinetic studies revealed that 1 was noncompetitive inhibitorfor AChE, while 2–6 were mixed-type inhibitors ofAChE. Compounds 1, 5 and 6 had mixed-type inhibitoryeffects against BChE; 2 was a competitive inhibitor; and 3and 4 were noncompetitive inhibitors. Against BACE1,compounds 1, 2, 3, 5 showed mixed-type inhibition and 4,6 were noncompetitive inhibitors. Molecular dockingsimulation of the compounds demonstrated negative-bindingenergies indicating high proximity to the active site andtight binding to the enzyme. These data suggested that thecompounds inhibited AChE, BChE, and BACE1, providinga preventive and therapeutic strategy for AD treatment.
Ethnobotany, Phytochemistry, and Pharmacology of Angelica decursiva Fr. et Sav.
Md. Yousof Ali,성수희,Susoma Jannat,정현아,최재수 한국생약학회 2019 Natural Product Sciences Vol.25 No.3
Angelica decursiva Fr. et Sav. (Umbelliferae) has traditionally been used to treat different diseases due to its antitussive, analgesic, and antipyretic activities. It is also a remedy for thick phlegm, asthma, and upper respiratory infections. Recently, the leaf of A. decursiva has been consumed as salad without showing any toxicity. This plant is a rich in different types of coumarin derivatives, including dihydroxanthyletin, psoralen, dihydropsoralen, hydroxycoumarin, and dihydropyran. Its crude extracts and pure constituents possess anti-inflammatory, anti-diabetic, anti-Alzheimer disease, anti-hypertension, anti-cancer, antioxidant, anthelmintic, preventing cerebral stroke, and neuroprotective activities. This valuable herb needs to be further studied and developed not only to treat these human diseases, but also to improve human health. This review provides an overview of current knowledge of A. decursiva metabolites and their biological activities to prioritize future studies.
정현아,Md. Yousof Ali,Himanshu Kumar Bhakta,민병선,최재수 대한약학회 2017 Archives of Pharmacal Research Vol.40 No.1
Prunin is the main flavonoid in Prunus davidianastems and improves hyperglycemia and hyperlipidemiain streptozotocin-induced diabetic rats. The aim ofthis study was to investigate the in vitro anti-diabeticpotential of prunin via the inhibition of protein tyrosinephosphatase 1B (PTP1B), a-glucosidase, peroxynitrite(ONOO-)-mediated tyrosine nitration, and stimulation ofglucose uptake in insulin-resistant hepatocytes. In addition,a molecular docking simulation was performed to predictspecific prunin binding modes during PTP1B inhibition. Prunin showed strong inhibitory activity against PTP1B,with an IC50 value of 5.5 ± 0.29 lM, and significantinhibitory activity against a-glucosidase, with an IC50value of 317 ± 2.12 lM. Moreover, a kinetics studyrevealed that prunin inhibited PTP1B (Ki = 8.66) and aglucosidase(Ki = 189.56) with characteristics typical ofcompetitive and mixed type inhibitors, respectively. Docking simulations showed that prunin selectivelyinhibited PTP1B by targeting its active site and exhibitedgood binding affinity, with a docking score of -9 kcal/-mol. Furthermore, prunin exhibited dose-dependent inhibitoryactivity against ONOO--mediated tyrosine nitrationand stimulated glucose uptake by decreasing PTP1Bexpression level in insulin-resistant HepG2 cells. Theseresults indicate that prunin has significant potential as aselective PTP1B inhibitor and may possess anti-diabeticproperties by improving insulin resistance.
최재수,Md. Nurul Islam,Md. Yousof Ali,김영명,박혜진,손희숙,정현아 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.10
To investigate the effect of C-glycosylation atdifferent positions of luteolin, the structure–activity relationshipsof luteolin and a pair of isomeric C-glycosylatedderivatives orientin and isoorientin, were evaluated. Weinvestigated the effects of C-glycosylation on the antioxidant,anti-Alzheimer’s disease (AD), anti-diabetic and antiinflammatoryeffects of luteolin and its two C-glycosides viain vitro assays of peroxynitrite (ONOO-), total reactiveoxygen species (ROS), nitric oxide (NO), 1,1-diphenyl-2-picrylhydraxyl (DPPH), aldose reductase, protein tyrosinephosphatase 1B (PTP1B), acetylcholinesterase (AChE),butyrylcholinesterase (BChE), and b-site amyloid precursorcleaving enzyme 1 (BACE1), and cellular assays of NOproduction and inducible nitric oxide synthase (iNOS)/cyclooxygenase-2 expression in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. Of the three compounds, isoorientinshowed the highest scavenging activity againstDPPH, NO, and ONOO-, while luteolin was the most potentinhibitor of ROS generation. In addition, luteolin showed the most potent anti-AD activity as determined by its inhibitionof AChE, BChE, and BACE1. With respect to anti-diabeticeffects, luteolin exerted the strongest inhibitory activityagainst PTP1B and rat lens aldose reductase. Luteolin alsoinhibited NO production and iNOS protein expression inLPS-stimulated macrophages, while orientin and isoorientinwere inactive at the same concentrations. The effects of Cglycosylationat different positions of luteolin may be closelylinked to the intensity and modulation of antioxidant, anti-AD, anti-diabetic, and anti-inflammatory effects of luteolinand its C-glycosylated derivatives.