The combination of sesamol and clofibric acid moieties leads to a novel potent hypolipidemic agent with antioxidant, anti-inflammatory and hepatoprotective activity

Dipterocarpus tuberculatus Roxb. has been used traditionally as a remedy for many diseases, especially inflammation. Therefore, we analyzed and explored the mechanism of the anti-inflammatory effect of a Dipterocarpus tuberculatus Roxb. ethanol extract (Dt-EE). Dt-EE clearly and dose-dependently inhibited the expression of pro-inflammatory cytokines such as IL-6, TNF-α, and IL-1β in lipopolysaccharide (LPS)-treated RAW264.7 cells. Also, Dt-EE suppressed the activation of the MyD88/TRIF-mediated AP-1 pathway and the AP-1 pathway related proteins JNK2, MKK4/7, and TAK1, which occurred as a result of inhibiting the kinase activity of IRAK1 and IRAK4, the most upstream factors of the AP-1 pathway. Finally, Dt-EE displayed hepatoprotective activity in a mouse model of hepatitis induced with LPS/D-galactosamine (D-GalN) through decreasing the serum levels of alanine aminotransferase and suppressing the activation of JNK and IRAK1. Therefore, our results strongly suggest that Dt-EE could be a candidate anti-inflammatory herbal medicine with IRAK1/AP-1 inhibitory and hepatoprotective properties.

Download Full-text

Secondary Metabolite Profiling, Anti-Inflammatory and Hepatoprotective Activity of Neptunia triquetra (Vahl) Benth

Molecules ◽

10.3390/molecules26237353 ◽

2021 ◽

Vol 26 (23) ◽

pp. 7353

Author(s):

Nasir Aziz Wagay ◽

Shah Rafiq ◽

Mohammad Aslam Rather ◽

Younas Rasheed Tantray ◽

Feng Lin ◽

...

Keyword(s):

Total Protein ◽

Ethanolic Extract ◽

Liver Weight ◽

Hepatoprotective Activity ◽

Experimental Models ◽

Inflammatory Activity ◽

Albino Rats ◽

Total Lipids ◽

Anti Inflammatory

The present study aimed to analyze the phytoconstituents of Neptunia triquetra (Vahl) Benth. Anti-inflammatory and hepatoprotective activities of ethanol (EE), chloroform (CE) and dichloromethane (DCME) of stem extracts were evaluated using in vivo experimental models. The extracts were analyzed for phytoconstituents using GC-HRMS. Anti-inflammatory activity of CE, EE and DCME was accessed using carrageenan-induced paw oedema, cotton pellet-induced granuloma and the carrageenan-induced air-pouch model in Wistar albino rats. The hepatotoxicity-induced animal models were investigated for the biochemical markers in serum (AST, ALT, ALP, GGT, total lipids and total protein) and liver (total protein, total lipids, GSH and wet liver weight). In the in vivo study, animals were divided into different groups (six in each group) for accessing the anti-inflammatory and hepatoprotective activity, respectively. GC-HRMS analysis revealed the presence of 102 compounds, among which 24 were active secondary metabolites. In vivo anti-inflammatory activity of stem extracts was found in the order: indomethacin > chloroform extract (CE) > dichloromethane extract (DCME) > ethanolic extract (EE), and hepatoprotective activity of stem extracts in the order: CE > silymarin > EE > DCME. The results indicate that N. triquetra stem has a higher hepatoprotective effect than silymarin, however the anti-inflammatory response was in accordance with or lower than indomethacin.

Download Full-text

FLAVONOID COMPOUNDS FROM ARTEMISIA GLABELLA KAR. ET. KIR., SYNTHESIS ON THEIR BASIS AND BIOLOGICAL ACTIVITY

chemistry of plant raw material ◽

10.14258/jcprm.2018033766 ◽

2018 ◽

pp. 215-222

Author(s):

Габиден (Gabiden) Маратович (Maratovich) Байсаров (Baysarov) ◽

Айдана (Аjdana) Рахманиякызы (Rakhmaniyakyzy) Жуматаева (Zhumatayeva) ◽

Гулим (Gulim) Кенесбековна (Kenesbekovna) Мукушева (Mukusheva) ◽

Эльвира (El'vira) Эдуардовна (Eduardovna) Шульц (Shul'ts) ◽

Роза (Roza) Батталовна (Battalovna) Сейдахметова (Seydakhmetova) ◽

...

Keyword(s):

Biological Activity ◽

Raw Materials ◽

Hepatoprotective Activity ◽

Biologically Active ◽

Secondary Amines ◽

Moderate Activity ◽

Amino Derivatives ◽

Anti Inflammatory ◽

Derivatives Of

As a result of complex chemical processing of medicinal raw materials of Artemisia glabella Kar. et Kir., including CO2 extraction and lactones isolation, we have investigated the chemical composition of flavonoids to select the biologically active ones and carry out modifications on their basis. Two flavonoids pectolinaringenin and cirsilineol have been isolated by partition chromatography from the secondary raw materials of Artemisia glabella Kar. et. Kir. and identified. To obtain new biologically active compounds, we have synthesized new amino derivatives of cirsilineol by the Mannich reaction with secondary amines (piperidine and N-methylpiperazine) in isopropanol with the presence of dimethylaminopyridine. In proton NMR spectrum of the synthesized compounds there are proton signals of the initial cirsilineol fragment; however, there is no N-8 proton signal, besides other signals typical for amines’ benzene ring have been observed at 1.53–3.90 ppm. It means that reaction occurred at the C-8 position of carbon in ring A. The synthesized compounds have been studied for various types of biological activity typical for this class, including hepatoprotective and anti-inflammatory activities. Amino derivatives of cirsilineol exhibit a moderate activity against HepG2 cell line, while cirsilineol at a dose of 5 mg/ml expresses a pronounced hepatoprotective activity. Moreover, all samples at a dose of 25 mg/kg show poor anti-inflammatory effects on the model of acute exudative reaction in vivo.

Download Full-text

Boronated Pyrimidines and Purines as Cytotoxic, Hypolipidemic and Anti-Inflammatory Agents

Metal-Based Drugs ◽

10.1155/mbd.1996.155 ◽

1996 ◽

Vol 3 (3) ◽

pp. 155-160 ◽

Cited By ~ 6

Author(s):

Iris H. Hall ◽

Bruce S. Burnham ◽

Amy Elkins ◽

Anup Sood ◽

Walda Powell ◽

...

Keyword(s):

Pharmacological Activity ◽

Inflammatory Activity ◽

Analgesic Effects ◽

Hypolipidemic Agent ◽

Anti Inflammatory ◽

Adenine Derivatives

The simple boronated bases, e.g. cytosine, adenine and guanine, containing no sugar residues retained good pharmacological activity as hypolipidemic, anti-neoplastic and anti-inflammatory agents in mice at 8 mg/kg. Their activities were generally identical to their respective nucleoside derivatives. Interestingly the boronated acyclovir derivative was a very potent hypolipidemic agent achieving better activity than clofibrate and lovastatin. The boronated adenine derivatives appeared to have the best anti-inflammatory activity in reducing local edema and analgesic effects. The agents were active against the growth of murine and human leukemias and human HeLa-S3 suspended uterine carcinoma. Only the boronated adenine derivatives were effective in blocking the growth of human SW480 adenocarcinoma and the KB nasopharynx.

Download Full-text

An Appraisal of Current Pharmacological Perspectives of Sesamol: A Review

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557520666200313120419 ◽

2020 ◽

Vol 20 (11) ◽

pp. 988-1000 ◽

Cited By ~ 1

Author(s):

Bellamkonda Bosebabu ◽

Sri Pragnya Cheruku ◽

Mallikarjuna Rao Chamallamudi ◽

Madhavan Nampoothiri ◽

Rekha R. Shenoy ◽

...

Keyword(s):

Molecular Mechanisms ◽

Biological Effects ◽

Hepatoprotective Activity ◽

In Vivo Studies ◽

Therapeutic Effects ◽

Pharmacological Effects ◽

Bioactive Constituents ◽

Anti Inflammatory

Sesame (Sesamum indicum L.) seeds have been authenticated for its medicinal value in both Chinese and Indian systems of medicine. Its numerous potential nutritional benefits are attributed to its main bioactive constituents, sesamol. As a result of those studies, several molecular mechanisms are emerging describing the pleiotropic biological effects of sesamol. This review summarized the most interesting in vitro and in vivo studies on the biological effects of sesamol. The present work summarises data available from Pubmed and Scopus database. Several molecular mechanisms have been elucidated describing the pleiotropic biological effects of sesamol. Its major therapeutic effects have been elicited in managing oxidative and inflammatory conditions, metabolic syndrome and mood disorders. Further, compelling evidence reflected the ability of sesamol in inhibiting proliferation of the inflammatory cell, prevention of invasion and angiogenesis via affecting multiple molecular targets and downstream mechanisms. Sesamol is a safe, non‐toxic chemical that mediates anti‐inflammatory effects by down‐regulating the transcription of inflammatory markers such as cytokines, redox status, protein kinases, and enzymes that promote inflammation. In addition, sesamol also induces apoptosis in cancer cells via mitochondrial and receptor‐mediated pathways, as well as activation of caspase cascades. In the present review, several pharmacological effects of sesamol are summarised namely, antioxidant, anti-cancer, neuroprotective, cardioprotective, anti-inflammatory, hypolipidemic, radioprotective, anti-aging, anti-ulcer, anti-dementia, anti-depressant, antiplatelet, anticonvulsant, anti-anxiolytic, wound healing, cosmetic (skin whitening), anti-microbial, matrix metalloproteinase (MMPs) inhibition, hepatoprotective activity and other biological effects. Here we have summarized the proposed mechanism behind these pharmacological effects.

Download Full-text

Oligonol Ameliorates CCl4-Induced Liver Injury in Rats via the NF-Kappa B and MAPK Signaling Pathways

Oxidative Medicine and Cellular Longevity ◽

10.1155/2016/3935841 ◽

2016 ◽

Vol 2016 ◽

pp. 1-12 ◽

Cited By ~ 23

Author(s):

Jeonghyeon Bak ◽

Nam Kyung Je ◽

Hae Young Chung ◽

Takako Yokozawa ◽

Sik Yoon ◽

...

Keyword(s):

Oxidative Stress ◽

Mapk Signaling ◽

Hepatoprotective Activity ◽

Inos Mrna ◽

Mrna Levels ◽

Hepatic Diseases ◽

Mitogen Activated Protein ◽

Anti Inflammatory

Oxidative stress is thought to be a key risk factor in the development of hepatic diseases. Blocking or retarding the reactions of oxidation and the inflammatory process by antioxidants could be a promising therapeutic intervention for prevention or treatment of liver injuries. Oligonol is a low molecular weight polyphenol containing catechin-type monomers and oligomers derived from lychee fruit. In this study, we investigated the anti-inflammatory effect of oligonol on carbon tetrachloride- (CCl4-) induced acute hepatic injury in rats. Oral administration of oligonol (10 or 50 mg/kg) reduced CCl4-induced abnormalities in liver histology and serum AST and serum ALT levels. Oligonol treatment attenuated the CCl4-induced production of inflammatory mediators, including TNF-α, IL-1β, cyclooxygenase-2 (COX-2), and inducible nitric oxide synthase (iNOS) mRNA levels. Western blot analysis showed that oligonol suppressed proinflammatory nuclear factor-kappa B (NF-κB) p65 activation, phosphorylation of extracellular signal-regulated kinase (ERK), c-Jun NH2-terminal kinase (JNK), and p38 mitogen-activated protein kinases (MAPKs) as well as Akt. Oligonol exhibited strong antioxidative activityin vitroandin vivo, and hepatoprotective activity againstt-butyl hydroperoxide-induced HepG2 cells. Taken together, oligonol showed antioxidative and anti-inflammatory effects in CCl4-intoxicated rats by inhibiting oxidative stress and NF-κB activation via blockade of the activation of upstream kinases including MAPKs and Akt.

Download Full-text

Hepatoprotective and Anti-inflammatory Activities of Hydro-alcoholic Extract of Oxalis debilis Kunth. Leaves

Letters in Applied NanoBioScience ◽

10.33263/lianbs113.36263633 ◽

2021 ◽

Vol 11 (3) ◽

pp. 3626-3633

Keyword(s):

Body Weight ◽

Folk Medicine ◽

Hepatoprotective Activity ◽

Control Group ◽

Alcoholic Extract ◽

Paw Edema ◽

Oral Toxicity ◽

Significant Difference ◽

Anti Inflammatory ◽

Oral Doses

This study aimed to investigate hepatoprotective and anti-inflammatory activities of the hydro-alcoholic extract of Oxalis debilis (ODHE) leaves. Acute oral toxicity evaluated ODHE in graded oral doses (100, 500, 1000, 3000, and 5000 mg/kg body weight) in rats. The hepatoprotective activity was evaluated in CCl4 intoxicated rats at 200 and 400 mg/kg body weight doses of ODHE, while anti-inflammatory activity was determined by carrageenan-induced paw edema in rats at 200, 400, 800 mg/kg body weight doses of ODHE. The ODHE was safe at the highest dose of 5000 mg/kg in experimental rats. In hepatoprotective activity, ODHE significantly reduced the serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), and total bilirubin (TB) levels as compared to the CCl4control group. On the other hand, ODHE showed an anti-inflammatory effect similar to that of the control group in the carrageenan-induced paw edema model. The histopathological findings showed a significant difference between the ODHE (400 mg/kg) and CCl4 groups. The present experiment showed that ODHE has significant hepatoprotective and anti-inflammatory activities. Results confirm the use of O. debilis in folk medicine in the treatment of hepatotoxicity and inflammation.

Download Full-text

STUDIES ON HEPATOPROTECTIVE AND ANTI-INFLAMMATORY ACTIVITY OF COIX LACRYMA–JOBI (LINN)

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i11.26307 ◽

2018 ◽

Vol 11 (11) ◽

pp. 290

Author(s):

Geetha S ◽

Jannathul Firdous ◽

Karpagam T ◽

Varalakshmi B ◽

Shanmuga Priya ◽

...

Keyword(s):

Serum Cholesterol Level ◽

Hepatoprotective Activity ◽

Seed Extract ◽

Inflammatory Activity ◽

Control Groups ◽

Egg Albumin ◽

Plant Seeds ◽

Test And Evaluation ◽

Study Evaluation ◽

Anti Inflammatory

Objective: In the present study, evaluation of hepatoprotective activity of Coix lacryma-jobi by CCl4-induced hepatotoxicity test, and evaluation of anti-inflammatory activity of by egg albumin-induced paw edema, and complete Freund’s adjuvant-induced arthritis model were done.Methods: Plant extract was prepared by mixing ethanol with powdered plant seeds and experiment was done as per the procedures of above-mentioned three models.Results: C. lacryma-jobi test extracts out of two doses, 400 mg/kg exhibited a significant reduction in serum cholesterol level as 33 mg/dl when compared to control groups. C. lacryma-jobi seed extract has restored various serological alterations following CCl4-induced hepatotoxicity and was capable of reversing the toxic effects of CCl4 on liver cells. Considerable reduction in the paw volume of exudates observed with C. lacryma-jobi extract, indicating significant anti-inflammatory activity.Conclusion: Therefore, this study shows that C. lacryma-jobs seed extract have anti-inflammatory activity in the models studied.

Download Full-text