scholarly journals Antihypertensive Effect of Ethanolic Extract from Acanthopanax sessiliflorus Fruits and Quality Control of Active Compounds

2018 ◽  
Vol 2018 ◽  
pp. 1-14 ◽  
Author(s):  
In Ho Jung ◽  
Sung Eun Kim ◽  
Yeong-Geun Lee ◽  
Dae Hyun Kim ◽  
Haneul Kim ◽  
...  
Keyword(s):  
Quality Control ◽  
Antihypertensive Effect ◽  
Ex Vivo ◽  
Radical Scavenging ◽  
Ethanolic Extract ◽  
No Production ◽  
Active Compounds ◽  
Acanthopanax Sessiliflorus

Acanthopanax sessiliflorus (Rupr. & Maxim.) Seem., which belongs to the Araliaceae family, mainly inhabits Korea, China, and Japan. Traditionally, Acanthopanax species have been used as treatment for several diseases such as diabetes, tumors, and rheumatoid arthritis. Especially, its fruits have many biological functions including antitumor, immunostimulating, antithrombosis, and antiplatelet activities. Recently, the extract of A. sessiliflorus fruit has been reported to have antithrombotic and antiplatelet activities related to the alleviation of hypertension. Therefore, we investigated the antihypertensive effect of ethanolic extract from A. sessiliflorus fruits (DHP1501) through in vivo, ex vivo, and in vitro studies. In this study, DHP1501 demonstrated free radical scavenging capacity, enhanced endothelial nitric oxide (NO) production, and inhibited angiotensin-converting enzyme (ACE) activity in spontaneously hypertensive rats (SHRs), resulting in the improvement of vascular relaxation and decrease in blood pressure in the hypertensive animal model. These results suggest that A. sessiliflorus fruit extract may be a promising functional material for the prevention and treatment of hypertension. Furthermore, this study demonstrated the utility of MS-based active compounds for the quality control of DHP1501.

2,5-disubstituted-4-thiazolidinones: Synthesis, anti-inflammatory, free radical scavenging potentials and structural insights through molecular docking

2021 ◽  
Vol 18 ◽  
Author(s):  
Jagseer Singh ◽  
Pooja A Chawla ◽  
Rohit Bhatia ◽  
Shamsher Singh
Keyword(s):  
Free Radicals ◽  
Antioxidant Activities ◽  
Radical Scavenging ◽  
Assay Method ◽  
Acidic Group ◽  
Active Compounds ◽  
Cox 2 ◽  
Anti Inflammatory

: The present work reports synthesis and screening of fifteen 2,5-disubstituted-4-thiazolidinones with different substitutions of varied arylidene groups at imino. The structures of the compounds were confirmed by spectral characterization. The compounds were subjected to in vivo anti-inflammatory and in vitro antioxidant activities. The derivatives possessed remarkable activities quite close to standard drugs used. Unlike conventional non-selective NSAIDs, the synthesized compounds did not contain any acidic group, thereby ensuring a complete cure from ulcers. To further substantiate the claim for safer derivatives, the active compounds were docked against the cyclooxygenase (COX)-2 enzyme. It was found that 4-fluorophenylimino substituent at 2- position and 3-nitro moiety on a 5-benzylidene nucleus of the 4-thiazolidinone derivative fitted in the COX-2 binding pocket. The compounds exhibited remarkable activity in scavenging free radicals, as depicted by the DPPH assay method. The structure-activity relationship was also established in the present work with respect to the nature and position of the substituents. The active compounds were evaluated for drug-like nature under Lipinski’s rule of five, and the toxicity behaviour of active compounds was predicted using ADMETlab software. The compounds have the potential to target degenerative disorders associated with inflammation and the generation of free radicals.

scholarly journals In vivo Neurological, Analgesic and In vitro Antioxidant and Cytotoxic Activities of Ethanolic Extract of Leaf and Stem Bark of Wedelia chinensis

2019 ◽  
Vol 22 (1) ◽  
pp. 18-26
Author(s):  
Sayema Khanum ◽  
Md Shahid Sarwar ◽  
Mohammad Safiqul Islam
Keyword(s):  
Body Weight ◽  
Oral Administration ◽  
Radical Scavenging ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
Pharmaceutical Journal ◽  
Stem Bark ◽  
Cytotoxic Activities

Wedelia chinensis is a widely used anti-inflammatory and hepatoprotective medicinal plant in Bangladesh. In this study, analgesic, neurological, antioxidant and cytotoxic activities of the ethanolic extract of leaf and stem bark of W. chinensis were investigated. Oral administration of the ethanolic extract of W. chinensis (200- and 300-mg/kg body weight) was investigated on animal model for neurological activity using open field test and hole cross test. Acetic acid induced writhing method was used to assess the analgesic activity. DPPH (1,1-diphenyl, 2-picryl hydrazyl) radical scavenging assay was used for determining the antioxidant activity, while brine shrimp lethality bioassay was used for investigating cytotoxicity. The ethanol extract of the plant produced significant reduction (P<0.05) of locomotion in both doses (200- and 300-mg/kg body weight) indicating pronounced neurological activity. Oral administration of alcoholic leaves and stem extracts significantly (p < 0.05) inhibited writhing response in mice. The percentage of scavenging of DPPH free radical was found to be concentration dependent with IC50 value of 44.10 ± 0.65 and 38.96 ± 0.50 μg/ml for leaves and stem extracts, respectively. Our findings indicate that W. chinensis may be a source of natural antioxidant with potent analgesic, neurological and cytotoxic activities. Bangladesh Pharmaceutical Journal 22(1): 18-26, 2019

scholarly journals Current Trends in the Pharmacotherapy of Cataracts

2020 ◽  
Vol 13 (1) ◽  
pp. 15 ◽  
Author(s):  
Segewkal H. Heruye ◽  
Leonce N. Maffofou Nkenyi ◽  
Neetu U. Singh ◽  
Dariush Yalzadeh ◽  
Kalu K. Ngele ◽  
...  
Keyword(s):  
Low Income ◽  
Ex Vivo ◽  
Radical Scavenging ◽  
Antioxidant Defense System ◽  
Enzymatic Antioxidants ◽  
Repair Mechanisms ◽  
Blurry Vision ◽  
Experimentally Induced

Cataracts, one of the leading causes of preventable blindness worldwide, refers to lens degradation that is characterized by clouding, with consequent blurry vision. As life expectancies improve, the number of people affected with cataracts is predicted to increase worldwide, especially in low-income nations with limited access to surgery. Although cataract surgery is considered safe, it is associated with some complications such as retinal detachment, warranting a search for cheap, pharmacological alternatives to the management of this ocular disease. The lens is richly endowed with a complex system of non-enzymatic and enzymatic antioxidants which scavenge reactive oxygen species to preserve lens proteins. Depletion and/or failure in this primary antioxidant defense system contributes to the damage observed in lenticular molecules and their repair mechanisms, ultimately causing cataracts. Several attempts have been made to counteract experimentally induced cataract using in vitro, ex vivo, and in vivo techniques. The majority of the anti-cataract compounds tested, including plant extracts and naturally-occurring compounds, lies in their antioxidant and/or free radical scavenging and/or anti-inflammatory propensity. In addition to providing an overview of the pathophysiology of cataracts, this review focuses on the role of various categories of natural and synthetic compounds on experimentally-induced cataracts.

scholarly journals Identifying of Anti-Thrombin Active Components From Curcumae Rhizoma by Affinity-Ultrafiltration Coupled With UPLC-Q-Exactive Orbitrap/MS

2021 ◽  
Vol 12 ◽  
Author(s):  
Zhenwei Lan ◽  
Ying Zhang ◽  
Yue Sun ◽  
Lvhong Wang ◽  
Yuting Huang ◽  
...  
Keyword(s):  
Quality Control ◽  
Molecular Docking ◽  
Targeted Therapy ◽  
Screening Method ◽  
Active Ingredients ◽  
Active Compounds ◽  
Q Exactive ◽  
Orbitrap Ms

Recent studies concerning products that originate from natural plants have sought to clarify active ingredients, which both explains the mechanisms of the function and aids in quality control during production. As a traditional functional plant, Curcumae Rhizoma (CR) has been proven to be effective in promoting blood circulation and removing blood stasis. However, the components that play a role in its huge compound library are still unclear. The present study aimed to develop a high-throughput screening method to identify thrombin inhibitors in CR and validate them by in vitro and in vivo experiments. The effect of CR on thrombin in HUVECs cells was determined by ELISA, then an affinity-ultrafiltration-UPLC-Q-Exactive Orbitrap/MS approach was applied. Agatroban and adenosine were used as positive and negative drugs respectively to verify the reliability of the established method. The in vitro activity of the compounds was determined by specific substrate S-2238. The in vivo effect of the active ingredients was determined using zebrafish. Molecular docking was used to understand the internal interactions between compounds and enzymes. ELISA results showed that CR had an inhibitory effect on thrombin. The screening method established in this paper is reliable, by which a total of 15 active compounds were successfully identified. This study is the first to report that C7, 8, and 11 have in vitro thrombin-inhibitory activity and significantly inhibit thrombosis in zebrafish models at a safe dose. Molecular docking studies were employed to analyze the possible active binding sites, with the results suggesting that compound 16 is likely a better thrombin inhibitor compared with the other compounds. Based on the affinity-ultrafiltration-UPLC-Q-Exactive Orbitrap/MS approach, a precisely targeted therapy method using bio-active compounds from CR might be successfully established, which also provides a valuable reference for targeted therapy, mechanism exploration, and the quality control of traditional herbal medicine.

scholarly journals Antioxidant and Hypoglycemic Properties of Seeds of Cucurbitaceae Family from Western Nepal

2019 ◽  
Vol 9 (2) ◽  
pp. 1-5
Author(s):  
Atisammodavardhana Kaundinnyayana ◽  
Anita G.C ◽  
Asmita Banstola ◽  
Kishwor Poudel ◽  
Nirmal Acharya ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Radical Scavenging ◽  
Ethanolic Extract ◽  
Positive Control ◽  
Lagenaria Siceraria ◽  
Benincasa Hispida ◽  
Ic50 Values ◽  
In Vitro Antioxidant Activity

Introduction: Diabetes mellitus is an endocrine and metabolic disorder characterized by the defect in insulin secretion or insulin action or both. The association between diabetes mellitus and oxidative stress is well established. Cucurbitaceae is the largest family containing 120 genera mostly grown for its sweet and juicy fruit in warm climates all over the world. In the present work ethanolic extracts of the seeds of Trichosanthes cucumerina Linn (Chichinno), Lagenaria siceraria (Lauka), Cucurbita pepo (Pharsi), Luffa aegiptiaca (Ghiraula), and Benincasa hispida (Kubindo) collected from Western Nepal has been evaluated for their in vitro antioxidant activity and in vivo hypoglycemic effects. Methods: In vitro antioxidant activity was assessed by using DPPH free radical scavenging activities and their IC50 values were calculated. In vivo hypoglycemic effect was examined on normoglycemic rats. The clinical significance of ethanolic extract at the doses of 250 and 500 mg/kg body weight was investigated in 0, 30, 60, 120 and 180 minutes of oral administration. Metformin treated group was used as the positive control. Results: For DPPH radical scavenging action, the IC50 values of Trichosanthes cucumerina, Luffa aegiptiaca, Benincasa  hispida, Cucurbita pepo, Lagenaria siceraria were found to be 60.72, 127.73, 49.63, 98.16 and 52.46 µg/ml respectively which were compared to the IC50 value of ascorbic acid (Positive control) which was found to be 38.11 µg/ml. The extracts of Benincasa hispida, and were having higher antioxidant activity and tested for in vivo hypoglycemic activity.In vivo administration of two doses of ethanolic extract of Lagenaria siceraria reduced the level of blood glucose while the best result was obtained at 250 mg/kg. Conclusions: Present study revealed promising antioxidant and hypoglycemic activity of ethanolic extract of Lagenaria siceraria. The further exploration of Lagenaria siceraria for its effective use in the traditional medicinal system is essential.

scholarly journals Sorbaria kirilowii Ethanol Extract Exerts Anti-Inflammatory Effects In Vitro and In Vivo by Targeting Src/Nuclear Factor (NF)-κB

Biomolecules ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 741 ◽  
Author(s):  
Jiwon Jang ◽  
Jong Sub Lee ◽  
Young-Jin Jang ◽  
Eui Su Choung ◽  
Wan Yi Li ◽  
...  
Keyword(s):  
Signaling Pathways ◽  
Ex Vivo ◽  
Ethanol Extract ◽  
Inflammatory Activity ◽  
No Production ◽  
Nuclear Factor ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Inflammation is a fundamental process for defending against foreign antigens that involves various transcriptional regulatory processes as well as molecular signaling pathways. Despite its protective roles in the human body, the activation of inflammation may also convey various diseases including autoimmune disease and cancer. Sorbaria kirilowii is a plant originating from Asia, with no anti-inflammatory activity reported. In this paper, we discovered an anti-inflammatory effect of S. kirilowii ethanol extract (Sk-EE) both in vivo and in vitro. In vitro effects of Sk-EE were determined with lipopolysaccharide (LPS)-stimulated RAW264.7 cells, while ex vivo analysis was performed using peritoneal macrophages of thioglycollate (TG)-induced mice. Sk-EE significantly reduced the nitric oxide (NO) production of induced macrophages and inhibited the expression of inflammation-related cytokines and the activation of transcription factors. Moreover, treatment with Sk-EE also decreased the activation of proteins involved in nuclear factor (NF)-κB signaling cascade; among them, Src was a prime target of Sk-EE. For in vivo assessment of the anti-inflammatory effect of Sk-EE, HCl/EtOH was given by the oral route to mice for gastritis induction. Sk-EE injection dose-dependently reduced the inflammatory lesion area of the stomach in gastritis-induced mice. Taking these results together, Sk-EE exerts its anti-inflammatory activity by regulating intracellular NF-κB signaling pathways and also shows an authentic effect on reducing gastric inflammation.

IN VITRO ANTIOXIDANT AND IN VIVO HEPATOPROTECTIVE ACTIVITY OF ETHANOLIC EXTRACT OF ZIZIPHUS RUGOSA LAM. LEAVES

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (07) ◽  
pp. 69-75
Author(s):  
S Parashar ◽  
V. Uplanchiwar ◽  
R. K. Gautam ◽  
S. Goyal ◽  
Keyword(s):  
Free Radical ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Ethanolic Extract ◽  
Hepatoprotective Activity ◽  
Free Radical Scavenging ◽  
Scavenging Activity ◽  
Ic50 Value

Ziziphus rugosa Lam. belongs to the family Rhamnaceae and is found chiefly in deciduous and semi evergreen forest of Western Ghats. The present research was undertaken to establish in vitro antioxidant and in vivo hepatoprotective activity of ethanolic extract of Z.rugosa Lam. leaves. The powdered leaves of Z. rugosa were extracted with ethanol and preliminary phytochemical screening was performed for the presence of various phytoconstituents. DPPH assay and β-glucuronidase inhibition assay were selected for the free radical scavenging activity. For the assessment of hepatoprotective activity, alcohol and CCl4 induced hepatotoxicity model were used. The phytochemical analysis of ethanolic extract showed the presence of alkaloids, saponins and flavonoids. The extract exhibited concentration dependent radical scavenging activity with an IC50 value of 61.88 μg/ml and β –glucoronidase inhibition activity with an IC50 value of 70.61 μg/ml. It was speculated that the Z. rugosa Lam. ethanolic extract shows dosedependent hepatoprotective activity which is equivalent with the standard drug Silymarin. The inhibition of free radicals or free radical scavenging activity is significant in the protection against CCl4 and alcohol induced hepatopathy. Hence, it is likely that the antioxidant activity of ethanolic extract of Z. rugosa Lam. might contribute to the hepatoprotective action.

scholarly journals Functional spreading of hyperexcitability induced by human and synthetic intracellular Aβ oligomers

2020 ◽  
Author(s):  
Eduardo Javier Fernandez-Perez ◽  
Braulio Muñoz ◽  
Denisse Andrea Bascuñan ◽  
Christian Peters ◽  
Nicolas Osiel Riffo-Lepe ◽  
...  
Keyword(s):  
Hippocampal Neurons ◽  
Neuronal Excitability ◽  
Ex Vivo ◽  
Synaptic Activity ◽  
No Production ◽  
Synaptic Currents ◽  
Aβ Oligomers ◽  
Brain Hyperexcitability

Abstract Background: Intracellular amyloid-beta oligomers (iAβo) accumulation and neuronal hyperexcitability are two crucial events at early stages of Alzheimer’s disease (AD). However, to date, no mechanism linking them has been reported. Methods: Here, the effects of human AD brain-derived (h-iAβo) and synthetic (iAβo) peptides on synaptic currents and action potential (AP) firing were investigated in hippocampal neurons in vitro , ex vivo and in vivo. Results: Starting from 500 pM, iAβo rapidly increased the frequency of synaptic currents and higher concentrations potentiated the AMPA receptor-mediated current. Both effects were PKC-dependent. Parallel recordings of synaptic currents and nitric oxide (NO)-related fluorescence changes indicated that the increased frequency, related to pre-synaptic release, was dependent on a NO-mediated retrograde signaling. Moreover, increased synchronization in NO production was also observed in neurons neighboring those dialyzed with iAβo, indicating that iAβo can increase network excitability at a distance. Current-clamp recordings suggested that iAβo increased neuronal excitability via AMPA-driven synaptic activity without altering membrane intrinsic properties. Conclusion: These results strongly indicate that iAβo causes functional spreading of hyperexcitability through a synaptic-driven mechanism and offer an important neuropathological significance to intracellular species in the initial stages of AD, which include brain hyperexcitability and seizures.

scholarly journals Standardization of Diploid Codonopsis laceolata Root Extract as an Anti-Hyperuricemic Source

Processes ◽  
2021 ◽  
Vol 9 (11) ◽  
pp. 2065
Author(s):  
Seung-Yub Song ◽  
So-Hyeon Bok ◽  
Sung-Ho Lee ◽  
Min-Hee Kim ◽  
Hee-Ock Boo ◽  
...  
Keyword(s):  
Quality Control ◽  
Xanthine Oxidase ◽  
Ethanolic Extract ◽  
Functional Materials ◽  
Extraction Methods ◽  
Oxidase Inhibitor ◽  
Root Extract ◽  
Xanthine Oxidase Inhibitor

Codonopsis lanceolate exerts various medicinal effects and has been used as a traditional medicine for inflammation, asthma, gastritis, and liver disease. Recently, we reported the xanthine oxidase inhibitory activity of C. lanceolata extract and that lobetyolin, one of the key components, was a xanthine oxidase inhibitor. Lobetyolin showed anti-hyperuricemic activity in vitro and in vivo. In this study, we prepared various types of C. lanceolata extracts for the development of functional materials and natural drugs. We present the optimal analytical approach for the quality control and extraction optimization of C. lanceolata preparations. We established and validated a HPLC analysis for easy separation and quantification of the lobetyolin biomarker. Solvent extracts of C. lanceolata root were prepared and the profiles of the active marker and the optimal extraction methods were evaluated. The 100% ethanolic extract demonstrated the highest lobetyolin content. The validated HPLC method confirmed that lobetyolin was present in C. lanceolata root extracts. We suggest that the anti-hyperuricemic activities of C. lanceolata extract could be attributed to this marker compound. The results proposed that the 100% ethanolic extract could be used for the prevention of hyperurecemia, and that this analytical method and biomarker could be useful for the quality control of C. lanceolata preparations.

scholarly journals Antioxidant Activity of the Ethanol Extract of Manilkara zapota Leaf

2011 ◽  
Vol 4 (1) ◽  
pp. 193 ◽  
Author(s):  
M. E. Islam ◽  
M. S. Parvin ◽  
M. R. Islam ◽  
M. S. Islam ◽  
S. M. R. Hasan
Keyword(s):  
Antioxidant Activity ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Ethanolic Extract ◽  
Serum Marker ◽  
Control Group ◽  
Marker Enzymes ◽  
Manilkara Zapota

The present study evaluated the antioxidant activity of cold ethanolic extract of Manilkara zapota (Sapotaceae) leaves. In vitro antioxidant activity was determined using 1, 1-diphenyl-2-picrylhydrazyl radical, reducing power capacity, total phenol and flavonoid content. The extract demonstrated significant dose dependent antioxidant activity in vitro methods. In DPPH radical scavenging assay IC50 values of Manilkara zapota leaves (MZL) and ascorbic acid (standard) were found to be 68.27 and 16.17 μg/ml, respectively. In vivo, the extract was evaluated by carbon tetrachloride (CCl4) induced liver damage rats in hepatoprotective model. CCl4 produced significant alteration of serum marker enzymes, total bilirubin, total protein and liver weight. Restoration of these values towards normal, which is comparable to control group, indicated hepatoprotective activity, which reflects the antioxidant potential of the extract. Results presented here indicate that MZL possess strong antioxidant activity and they can therefore be used as a good natural source of antioxidant.Keywords: MZL; DPPH; Scavenging activity; Serum marker enzymes.© 2012 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.doi: http://dx.doi.org/10.3329/jsr.v4i1.7148J. Sci. Res. 4 (1), 193-202 (2012)

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