scholarly journals Cytotoxic, analgesic and anti-inflammatory activity of colchicine and its C-10 sulfur containing derivatives

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Joanna Kurek ◽  
Krzysztof Myszkowski ◽  
Irena Okulicz-Kozaryn ◽  
Agnieszka Kurant ◽  
Ewa Kamińska ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Natural Product ◽  
Biological Activities ◽  
Cyclin B1 ◽  
Spectroscopic Methods ◽  
Ovarian Cell ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Sulfur Containing ◽  
Inflammatory Effect

Abstract10-Alkylthiocolchicines have been obtained and characterized by spectroscopic methods and their biological activities as: cytotoxic, anti-inflammatory and analgesic activities have been tested. Cytotoxic activity against SKOV-3 ovarian cell line for 10-alkylthiocolchicine analogues was reported and tested compounds showed to be more active than commonly used doxorubicin. Some of tested C-10 alkylthiolated colchicines have been found to exhibit cytotoxicity at levels comparable to that of the natural product—colchicine. 10-Methylthiocolchicine has IC50 = 8 nM and 10-ethylthiocolchicine has IC50 = 47 nM in comparison to colchicine IC50 = 37 nM. Moreover for 10-alkylthioderivatives apoptosis test, cyclin B1 and cell cycle tests were performed. 10-n-Butylthiocolchicine was tested for anti-inflammatory and analgesic activities it showed to produce analgesic rather than anti-inflammatory effect.

Synthesis of Limonin Derivatives with Improved Anti-inflammatory and Analgesic Properties

2020 ◽  
Vol 17 (3) ◽  
pp. 285-299 ◽  
Author(s):  
Chengshu Jia ◽  
Bin Hu ◽  
Yingying Ji ◽  
Yourui Su ◽  
Guoqing Gong ◽  
...  
Keyword(s):  
Furan Ring ◽  
Biological Activities ◽  
Aqueous Solubility ◽  
Structural Modifications ◽  
Pharmacological Studies ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Ld50 Value ◽  
Inflammatory Effect

Background: Limonoids represent an important class of natural products which possess a broad range of biological activities. Albeit their enormous potentials as therapeutic candidates, they usually suffer from low bioavailability, poor aqueous solubility and relatively weak biological activities which result in significant challenges in the clinic applications. Therefore, the exploration and development of novel limonin derivatives with improved drug-like properties through the structural modifications recently have attracted great attention in the biological and medicinal chemistry field. Methods: Based on the structural modifications of C17-furan ring in limonin, a series of limonin derivatives was designed, synthesized and screened for their anti-inflammatory and analgesic activities in vivo. Results and Conclusion: Preliminary pharmacological studies revealed that most tested compounds exhibited more potent anti-inflammatory and analgesic efficacies than lead molecule limonin. Especially, for compound 3f, it exhibited a stronger anti-inflammatory effect than that of naproxen and comparable analgesic potency with aspirin. In the formalin test, 3f showed an obviously attenuated phase-II pain response which indicated that it may produce an anti-inflammatory effect in the periphery. Furthermore, the significantly low hERG inhibition (IC50 >100 μM) and high LD50 value of target molecule 3f further demonstrated it as a promising analgesic/anti-inflammatory candidate with excellent drug-like profiles.

scholarly journals Retrofractamide C Derived from Piper longum Alleviates Xylene-Induced Mouse Ear Edema and Inhibits Phosphorylation of ERK and NF-κB in LPS-Induced J774A.1

Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4058 ◽  
Author(s):  
Hyung Jin Lim ◽  
Seon Gyeong Bak ◽  
Eun Jae Park ◽  
Sae-Kwang Ku ◽  
Soyoung Lee ◽  
...  
Keyword(s):  
Biological Activities ◽  
Edema Formation ◽  
Ear Edema ◽  
Extracellular Signal ◽  
Edema Model ◽  
Mouse Ear ◽  
Anti Inflammatory ◽  
Factor Α ◽  
Mouse Ear Edema ◽  
Inflammatory Effect

Many studies have reported the biological activities of retrofractamide C (RAC). However, few studies have investigated the anti-inflammatory effect of RAC. In the present study, we investigated the anti-inflammatory effect of RAC using lipopolysaccharide (LPS)-induced J774A.1 cells and a xylene-induced mouse ear edema model. Treatment with RAC decreased LPS-induced nitric oxide (NO) and prostaglandin E2 (PGE2) secretion and inducible NO synthase (iNOS) and cyclooxygenase 2 (COX2) protein expression. It also downregulated the LPS-induced production of interleukin-1β (IL-1β) and interleukin-6 (IL-6) but not tumor necrosis factor α (TNF-α). In the LPS-induced signaling pathway, RAC inhibited the phosphorylation of extracellular signal-regulated kinase (ERK) and nuclear factor kappa light chain enhancer of activated B cells (NF-κB) but not c-Jun N-terminal kinase (JNK) or p38. In a xylene-induced mouse ear edema model, RAC treatment alleviated edema formation and inflammatory cell infiltration. In conclusion, the present study indicates that RAC has the potential to have anti-inflammatory effects and could be a prospective functional food.

scholarly journals MiR-155/GSK-3β mediates anti-inflammatory effect of Chikusetsusaponin IVa by inhibiting NF-κB signaling pathway in LPS-induced RAW264.7 cell

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Yi Xin ◽  
Qin Yuan ◽  
Chaoqi Liu ◽  
Changcheng Zhang ◽  
Ding Yuan
Keyword(s):  
Signaling Pathway ◽  
Mouse Liver ◽  
Inflammatory Responses ◽  
Biological Activities ◽  
Raw264.7 Cells ◽  
Inflammation Model ◽  
Raw264.7 Cell ◽  
Anti Inflammatory ◽  
Gsk 3Β ◽  
Inflammatory Effect

Abstract It has been demonstrated that Chikusetsusaponin IVa (CsIVa) possesses abundant biological activities. Herein, using LPS to establish acute inflammation model of mouse liver and cell line inflammation model, we investigated whether miR-155/GSK-3β regulated NF-κB signaling pathway, and CsIVa exerted anti-inflammatory effects by regulating miR-155/GSK-3β signaling pathway. Our results showed that LPS induced high expression of miR-155 and miR-155 promoted macrophage activation through GSK-3β. In addition, CsIVa inhibited inflammatory responses in LPS-induced mouse liver and RAW264.7 cells. Furthermore, we demonstrated that CsIVa improved the inflammatory response in LPS-induced RAW264.7 cells by inhibiting miR-155, increasing GSK-3β expression, and inhibiting NF-κB signaling pathway. In conclusion, our study reveals that CsIVa suppresses LPS-triggered immune response by miR-155/GSK-3β-NF-κB signaling pathway.

scholarly journals Sesquiterpenoids and Their Anti-Inflammatory Activity: Evaluation of Ainsliaea yunnanensis

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1701
Author(s):  
Jinjie Li ◽  
Xiuting Li ◽  
Xin Wang ◽  
Xiangjian Zhong ◽  
Linlin Ji ◽  
...  
Keyword(s):  
Nlrp3 Inflammasome ◽  
Ethanolic Extract ◽  
The Self ◽  
Inflammatory Activity ◽  
Spectroscopic Methods ◽  
Activity Evaluation ◽  
Caspase 1 ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Four new sesquiterpenoids (1–4) and six known sesquiterpenoids (5–10), were isolated from the EtOAc phase of the ethanolic extract of Ainsliaea yunnanensis. Their structures were established by spectroscopic methods, including 1-D, 2-D NMR and HPLC-MS. All compounds were tested for their anti-inflammatory effect by the inhibition of the activity of NLRP3 inflammasome by blocking the self-slicing of pro-caspase-1, which is induced by nigericin, then the secretion of mature IL-1β, mediated by caspase-1, was suppressed. Unfortunately none of the compounds showed an anti-inflammatory effect.

scholarly journals Anti-Inflammatory and Antinociceptive Activity of Pollen Extract Collected by Stingless Bee Melipona fasciculata

2019 ◽  
Vol 20 (18) ◽  
pp. 4512 ◽  
Author(s):  
Alberto Jorge Oliveira Lopes ◽  
Cleydlenne Costa Vasconcelos ◽  
Francisco Assis Nascimento Pereira ◽  
Rosa Helena Moraes Silva ◽  
Pedro Felipe dos Santos Queiroz ◽  
...  
Keyword(s):  
Native Species ◽  
Biological Activities ◽  
Stingless Bee ◽  
In Vitro Assays ◽  
Pollen Extract ◽  
Biological Potential ◽  
Anti Inflammatory ◽  
Analgesic Activities

The stingless bee, Melipona fasciculata Smith (Apidae, Meliponini), is a native species from Brazil. Their products have high biotechnological potential, however there are no studies about the biological activities of pollen collected by M. fasciculata. In this context, the present study investigated the chemical composition, anti-oxidant, anti-inflammatory, and analgesic activities of hydroethanolic pollen extracts collected by M. fasciculata in three cities in Maranhão State, Brazil. We verified the antioxidant activity of the extracts and inhibitory activity against the cyclooxygenase enzyme using in vitro assays and in allowed to select the extract with higher efficiency to be used on in vivo assays. In these trials, the selected extract showed high anti-inflammatory activity as well as nociceptive effects at central and peripheral level, suggesting that this extract acts on inhibition of histamine release and decreased synthesis of prostaglandins and the in-silico study suggested that polyphenols and acids fatty acids in the extract may be associated with these activities. The results of the present study report the high biological potential of pollen extract and we conclude that the pollen collected by M. fasciculata can be considered as the object of research for new pharmacological alternatives.

Antiproliferative effect of catechin in GRX cells

2012 ◽  
Vol 90 (4) ◽  
pp. 575-584 ◽  
Author(s):  
Cristina Machado Bragança de Moraes ◽  
Denizar Alberto da Silva Melo ◽  
Roberto Christ Vianna Santos ◽  
Shanna Bitencourt ◽  
Fernanda Cristina Mesquita ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cell Growth ◽  
Caspase 3 ◽  
Stellate Cell ◽  
Chronic Liver Injury ◽  
Cycle Arrest ◽  
Wound Healing Response ◽  
Anti Inflammatory ◽  
Almost All ◽  
Inflammatory Effect

The phenolic compounds present in cocoa seeds have been studied regarding health benefits, such as antioxidant and anti-inflammatory activities. Fibrosis is a wound healing response that occurs in almost all patients with chronic liver injury. A large number of cytokines and soluble intercellular mediators are related to changes in the behavior and phenotype of the hepatic stellate cell (HSC) that develop a fibrogenic and contractile phenotype leading to the development of fibrosis. The objective of this study was to assess the catechin effect in GRX liver cells in activities such as cell growth and inflammation. The GRX cells treatment with catechin induced a significant decrease in cell growth. This mechanism does not occur by apoptosis or even by autophagy because there were no alterations in expression of caspase 3 and PARP (apoptosis), and LC3 (autophagy). The expression of p27 and p53 proteins, regulators of the cell cycle, showed increased expression, while COX-2 and IL-6 mRNA showed a significant decrease in expression. This study shows that catechin decreases cell growth in GRX cells and, probably, this decrease does not occur by apoptosis or autophagy but through an anti-inflammatory effect and cell cycle arrest. Catechin also significantly decreased the production of TGF-β by GRX cells, showing a significant antifibrotic effect.

scholarly journals A Review on the Anti-Inflammatory Activity of Pomegranate in the Gastrointestinal Tract

2013 ◽  
Vol 2013 ◽  
pp. 1-11 ◽  
Author(s):  
Elisa Colombo ◽  
Enrico Sangiovanni ◽  
Mario Dell'Agli
Keyword(s):  
Gastrointestinal Tract ◽  
Clinical Studies ◽  
Intestinal Tract ◽  
Biological Activities ◽  
Inflammatory Activity ◽  
Beneficial Effects ◽  
Anti Inflammatory ◽  
Gastro Intestinal Tract ◽  
Inflammatory Effect

Several biological activities of pomegranate have been widely described in the literature, but the anti-inflammatory effect in the gastrointestinal tract has not been reviewed till now. The aim of the present paper is to summarize the evidence for or against the efficacy of pomegranate for coping with inflammatory conditions of the gastro-intestinal tract. The paper has been organized in three parts: (1) the first one is devoted to the modifications of pomegranate active compounds in the gastro-intestinal tract; (2) the second one considering the literature regarding the anti-inflammatory effect of pomegranate at gastric level; (3) the third part considers the anti-inflammatory effect of pomegranate in the gut.In vivostudies performed on the whole fruit or juice, peel, and flowers demonstrate antiulcer effect in a variety of animal models. Ellagic acid was the main responsible for this effect, although other individual ellagitannins could contribute to the biological activity of the mixture. Different preparations of pomegranate, including extracts from peels, flowers, seeds, and juice, show a significant anti-inflammatory activity in the gut. No clinical studies have been found, thus suggesting that future clinical studies are necessary to clarify the beneficial effects of pomegranate in the gastrointestinal tract.

scholarly journals Synthesis, Characterization and evaluation of Anti-inflammatory and Analgesic activity of Benzothiazole derivatives

2014 ◽  
Vol 2 (03) ◽  
pp. 84-89 ◽  
Author(s):  
Abhay Kumar Verma ◽  
Alex Martin ◽  
Arun Kumar Singh
Keyword(s):  
Benzoic Acid ◽  
1H Nmr ◽  
Mass Spectroscopy ◽  
Analgesic Activity ◽  
Aromatic Aldehydes ◽  
Spectroscopic Methods ◽  
Schiff’S Bases ◽  
Benzothiazole Derivatives ◽  
Anti Inflammatory ◽  
Analgesic Activities

A parent benzothiazole nucleus was synthesized by para amino acetanilide, then it is subjected to treatment with various substituted aromatic aldehydes to get the corresponding Schiff’s bases followed by treatment with pthalic anhydride to form 2-(6- acetamidobenzo[d]thiazol-2-ylcarbamoyl)benzoic acid. The structures of synthesized compounds were confirmed by various spectroscopic methods such as IR, 1H NMR and mass spectroscopy. The products were evaluated for their anti-inflammatory and analgesic activities. Some of the compounds exhibited potent activities when compared with the standards.

scholarly journals Buckwheat and buckwheat enriched products exert an anti-inflammatory effect on the myofibroblasts of colon CCD-18Co

2018 ◽  
Vol 9 (6) ◽  
pp. 3387-3397 ◽  
Author(s):  
J. A. Giménez-Bastida ◽  
J. M. Laparra-Llopis ◽  
N. Baczek ◽  
H. Zielinski
Keyword(s):  
Cell Cycle ◽  
Cell Migration ◽  
Tnf Α ◽  
Anti Inflammatory ◽  
Cell Cycle Alteration ◽  
Inflammatory Effect

Buckwheat products ameliorated cell migration and cell cycle alteration of colon myofibroblasts in the presence of TNF-α.

Synthesis and Biological Evaluation of Polyfluoroalkylated Antipyrines and their Isomeric O-Methylpyrazoles

2019 ◽  
Vol 15 (5) ◽  
pp. 521-536 ◽  
Author(s):  
Natalya Agafonova ◽  
Evgeny Shchegolkov ◽  
Yanina Burgart ◽  
Victor Saloutin ◽  
Alexandra Trefilova ◽  
...  
Keyword(s):  
Biological Activities ◽  
Biological Evaluation ◽  
Antipyretic Activity ◽  
Starting Point ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Synthesis And Biological Evaluation ◽  
Cox 1

Background: Formally belonging to the non-steroidal anti-inflammatory drug class pyrazolones have long been used in medical practices. Objective: Our goal is to synthesize N-methylated 1-aryl-3-polyfluoroalkylpyrazolones as fluorinated analogs of antipyrine, their isomeric O-methylated derivatives resembling celecoxib structure and evaluate biological activities of obtained compounds. Methods: In vitro (permeability) and in vivo (anti-inflammatory and analgesic activities, acute toxicity, hyperalgesia, antipyretic activity, “open field” test) experiments. To suggest the mechanism of biological activity, molecular docking of the synthesized compounds was carried out into the tyrosine site of COX-1/2. Conclusion: The trifluoromethyl antipyrine represents a valuable starting point in design of the lead series for discovery new antipyretic analgesics with anti-inflammatory properties.

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