Last update 01 Nov 2024

AChE x COX-2

Last update 01 Nov 2024

Basic Info

Related Targets

AChECOX-2

Drugs associated with AChE x COX-2

NDH-4338

Target

AChE x COX-2

Mechanism

AChE inhibitors [+1]

Active Org.

Rutgers State University of New Jersey [+1]

Originator Org.

Rutgers State University of New Jersey

Active Indication

Skin injury

Inactive Indication-

Drug Highest PhasePreclinical

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with AChE x COX-2

100 Translational Medicine associated with AChE x COX-2

0 Patents (Medical) associated with AChE x COX-2

142

Literatures (Medical) associated with AChE x COX-2

01 Dec 2024·Bioprocess and Biosystems Engineering

Biosynthesis and biological activities of magnesium hydroxide nanoparticles using Tinospora cordifolia leaf extract

Article

Author: Althobaiti, Norah A ; Albalawi, Aishah E ; Gomathi, Thandapani ; Kirubakaran, Dharmalingam ; Alfaifi, Mohammad Y ; Menaa, Farid ; Elbehairi, Serag Eldin I ; Meenambigai, Krishnan ; Rajkumar, Manickam ; Presley, S I Davis ; Govindaraj, Prabha ; Shati, Ali A

The synthesis of magnesium hydroxide nanoparticles (Mg(OH)₂ NPs) using plant extracts are known to be a practical, economical, and an environmentally friendly approach. In this work, Mg(OH)₂ NPs were synthesized using aqueous leaf extract of Tinospora cordifolia, a medicinal plant commonly found in India. The synthesized Mg(OH)₂ NPs were characterized using various spectroscopic techniques. The ultraviolet-visible (UV-Vis) absorption peak of the Mg(OH)₂ NPs was detected at 289 nm, Fourier transform infrared (FTIR) analysis confirmed the presence of various functional groups, and X-ray diffraction (XRD) patterns revealed the well-crystallized structure of the Mg(OH)₂ NPs. High-resolution transmission electron microscopy (HR-TEM) and scanning electron microscopy (SEM) analyses depicted spherical morphology and an average particle size (PS) of 27.71 nm. The energy-dispersive X-ray (EDX) analysis confirmed the presence of C, O, and Mg elements, and the X-ray photoelectron spectroscopy (XPS) survey spectrum confirmed the elements for the Su 1 s peak at 280.2 eV. The dynamic light scattering (DLS) analysis displayed an average PS of 54.3 nm, and the Zeta potential (ZP) was of 9.89 mV. The fabricated Mg(OH)₂ NPs displayed notable antibacterial activity against S. epidermidis, E. coli, and S. aureus. In addition, these NPs exhibited strong antioxidant properties (> 75%) based on DPPH, ABTS, and hydrogen peroxide (H₂O₂) assays. Further, the same NPs exerted a potent anti-inflammatory activity (> 65%) based on COX-1 and COX-2 evaluations. The anti-Alzheimer' disease (AD) potential of Mg(OH)₂ NPs was assessed through effective inhibition (> 70%) of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activities. Molecular docking (MD) studies confirmed that caryophyllene has higher binding affinity with AChE (-5.3 kcal/mol) and BuChE (-6.4 kcal/mol) enzymes. This study emphasizes the green synthesis of Mg(OH)₂ NPs using T. cordifolia as a plant source and highlights their potential for biomedical applications.

01 Dec 2024·Natural Products and Bioprospecting

5α-Epoxyalantolactone from Inula macrophylla attenuates cognitive deficits in scopolamine-induced Alzheimer’s disease mice model

Article

Author: Ma, Rui ; Ha, Wei ; Tang, Jiang-Jiang ; Feng, Xu-Yao ; Shi, Yan-Ping

AbstractAlzheimer’s disease (AD) is a complex neurodegenerative condition. 5α-epoxyalantolactone (5α-EAL), a eudesmane-type sesquiterpene isolated from the herb of Inula macrophylla, has various pharmacological effects. This work supposed to investigate the improved impact of 5α-EAL on cognitive impairment. 5α-EAL inhibited the generation of nitric oxide (NO) in BV-2 cells stimulated with lipopolysaccharide (LPS) with an EC50 of 6.2 μM. 5α-EAL significantly reduced the production of prostaglandin E2 (PGE2) and tumor necrosis factor-α (TNF-α), while also inhibiting the production of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) proteins. The ability of 5α-EAL to penetrate the blood–brain barrier (BBB) was confirmed via a parallel artificial membrane permeation assay. Scopolamine (SCOP)-induced AD mice model was employed to assess the improved impacts of 5α-EAL on cognitive impairment in vivo. After the mice were pretreated with 5α-EAL (10 and 30 mg/kg per day, i.p.) for 21 days, the behavioral experiments indicated that the administration of the 5α-EAL could alleviate the cognitive and memory impairments. 5α-EAL significantly reduced the AChE activity in the brain of SCOP-induced AD mice. In summary, these findings highlight the beneficial effects of the natural product 5α-EAL as a potential bioactive compound for attenuating cognitive deficits in AD due to its pharmacological profile.Graphical Abstract

01 Oct 2024·Biomedicine & Pharmacotherapy

Evaluation of terpenes rich Hura crepitans extract on glucose regulation and diabetic complications in STZ-induced diabetic rats

Article

Author: Wu, Alexander T.H. ; De Waard, Michel ; Lawal, Bashir ; Onikanni, Sunday A. ; Olawale, Femi ; Wu, Alexander T H ; Onikanni, Sunday A ; Sabiu, Saheed ; Ajenifujah, Olabode T. ; Lukman, Halimat Yusuf ; Ajenifujah, Olabode T ; Chen, Lung-Ching ; Fouad, Dalia ; Huang, Hsu-Shan ; Fadaka, Adewale O. ; Sani, Saidu ; Batiha, Gaber El-Saber ; Kuo, Yucheng ; Owolabi, Mayowa Solomon ; Fadaka, Adewale O

The continual increase in global diabetic statistics portends decreased productivity and life spans, thus making it a disease of concern requiring more effective and safe therapeutic options. While several reports on antidiabetic plants, including Hura crepitans, are available, there is still a dearth of information on the holistic antidiabetic properties of H. crepitans and its associated complications. This study evaluated the antidiabetic potential of methanolic extract of Hura crepitans using in vitro, in vivo, and in silico approaches. The extract revealed a dose-dependent in vitro effect, with a 47.97 % and 65.34 % decrease in the fasting blood sugar levels of streptozotocin (STZ) induced diabetic rats at 150 and 300 mg/kg BW, respectively. Likewise, the extract increased serum and pancreatic insulin levels, and significantly ameliorated neuronal oxidative stress and inflammation by reducing the expression levels of cholinesterase, NF-κB, and COX-2 in the brain of hyperglycemic rats. Serum dyslipidemia, liver, and kidney biomarker indices, and hematological alterations in diabetic rats were also significantly attenuated by the extract. Several constituents, mainly terpenes, were identified in the extract. To further predict the drug-likeness, pharmacokinetics, and binding properties of the compounds, in silico analysis was conducted. Ergosta-2,24-dien-26-oicacid,18-(acetyloxy)-5,6-epoxy-4, 22-dihydroxy-1-oxo-,delta.-lactone-4.beta., displayed the highest docking scores for acetylcholinesterase, butyrylcholinesterases, alpha-amylase, and nuclear factor-kB with values of -12.4, -10.9, -10.3, and -9.4 kcal/mol, while ergost-25-ene-6,12-dione,3,5-dihydroxy-, (3.beta.,5.alpha.) topped for cyclooxygenase-2 (-9.0 kcal/mol). The top-ranked compounds also presented significant oral drug-likeness, pharmacokinetics, and safety properties. Altogether, our data provide preclinical evidence of the potential of Hura crepitans in ameliorating diabetes and its associated complications.

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