scholarly journals Anti-Inflammatory and Cytostatic Activities of a Parthenolide-Like Sesquiterpene Lactone fromCota palaestinasubsp.syriaca

2015 ◽  
Vol 2015 ◽  
pp. 1-13 ◽  
Author(s):  
Rabih S. Talhouk ◽  
Bilal Nasr ◽  
Mohamed-Bilal Fares ◽  
Bushra Ajeeb ◽  
Rana Nahhas ◽  
...  
Keyword(s):  
Sesquiterpene Lactone ◽  
Eastern Mediterranean ◽  
Breast Adenocarcinoma ◽  
Binding Affinities ◽  
Cellular Motility ◽  
Endemic Plant ◽  
Analogous Structure ◽  
Bioassay Guided Fractionation ◽  
Anti Inflammatory ◽  
Anticancer Compound

A sesquiterpene lactone 1-β,10-Epoxy-6-hydroxy-1,10H-inunolide (K100) was isolated through “bioassay-guided fractionation” fromCota palaestinasubsp.syriaca, an Eastern Mediterranean endemic plant. K100 inhibited endotoxin- (ET-) induced proinflammatory markers: IL-6, MMP-9, and NO in normal mouse mammary SCp2 Cells. Molecular dockingin silicosuggested that K100, having highly analogous structure as parthenolide (PTL), an anticancer compound, could bind PTL target proteins at similar positions and with comparable binding affinities. Both compounds, K100 and PTL, inhibited the proliferation and prolonged the S-phase of the cell cycle of breast adenocarcinoma MDA-MB-231 cells grown in 2D cultures. Noncytotoxic concentrations of K100 and PTL decreased the proliferation rate of MDA-MB-231 and shifted their morphology from stellate to spherical colonies in 3D cultures. This was accompanied with a significant increase in the amount of small colonies and a decrease in the amount of large colonies. Moreover, K100 and PTL decreased cellular motility and invasiveness of MDA-MB-231 cells. In summary, these results suggest that K100 exhibits PTL-analogous anti-inflammatory, cytostatic, and antimetastatic effects.

Anticancer Potential of Aguerin B, a Sesquiterpene Lactone Isolated from Centaurea behen in Metastatic Breast Cancer Cells

2020 ◽  
Vol 15 (2) ◽  
pp. 165-173
Author(s):  
Elaheh Amini ◽  
Mohammad Nabiuni ◽  
Seyed Bahram Behzad ◽  
Danial Seyfi ◽  
Farhad Eisvand ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cell Growth ◽  
Tumor Cell ◽  
Sesquiterpene Lactone ◽  
Sesquiterpene Lactones ◽  
Metastatic Breast ◽  
Breast Adenocarcinoma ◽  
Human Breast ◽  
Skin Malignancy

Background: Breast carcinoma is a malignant disease that represents the most common non-skin malignancy and a chief reason of cancer death in women. Large interest is growing in the use of natural products for cancer treatment, especially with goal of suppression angiogenesis, tumor cell growth, motility, as well as invasion and metastasis with low/no toxicity. It is evident from recent patents on the anticancer properties of sesquiterpene lactones such as parthenolide. Objective: In this study, using MDA-MB-231 cells of a human breast adenocarcinoma, the effects of aguerin B, as a natural sesquiterpene lactone, has been evaluated, in terms of the expression of metastatic-related genes (Pak-1, Rac-1 and HIF-1α). Methods: Cytotoxicity of aguerin B was tested toward MDA-MB-231 breast tumor cells using MTT. Scratch assay was accomplished to evaluate the tumor cell invasion. To understand the underlying molecular basis, the mRNA expressions were evaluated by real time PCR. Results: It was found that aguerin B significantly inhibited human breast cancer cell growth in vitro (IC50 = 2μg/mL) and this effect was accompanied with a persuasive suppression on metastasis. Our results showed that aguerin B in IC50 concentration down-regulated Rac-1, Pak-1, Hif-1α and Zeb-1 transcriptional levels. Conclusion: Taken together, this study demonstrated that aguerin B possessed potential anti-metastatic effect, suggesting that it may consider as a potential multi target bio compound for treatment of breast metastatic carcinoma.

Anti-inflammatory activity of the sesquiterpene lactone diacethylpiptocarphol in dextransulfate sodium-induced colitis in mice

2019 ◽  
Vol 245 ◽  
pp. 112186 ◽  
Author(s):  
R. Sabel ◽  
A.S. Fronza ◽  
L.Z.B. Carrenho ◽  
A. Maes ◽  
M.L. Barros ◽  
...  
Keyword(s):  
Sesquiterpene Lactone ◽  
Inflammatory Activity ◽  
Anti Inflammatory

scholarly journals 3-{[(2,3-Dichlorophenyl)amino]methyl}-5-(furan-2-ylmethylidene)-1,3-thiazolidine-2,4-dione

Molbank ◽  
10.3390/m1083 ◽  
2019 ◽  
Vol 2019 (4) ◽  
pp. M1083
Author(s):  
Uwabagira ◽  
Sarojini
Keyword(s):  
Breast Adenocarcinoma ◽  
Cyclin Dependent Kinase ◽  
Human Breast ◽  
Hemolysis Assay ◽  
Human Breast Adenocarcinoma ◽  
Inflammatory Agent ◽  
Human Blood Cell ◽  
Anti Inflammatory ◽  
Mcf 7

The compound 3-{[(2,3-Dichlorophenyl)amino]methyl}-5-(furan-2-ylmethylidene)-1,3-thiazolidine-2,4-dione has been designed, synthesized, and screened for its in vitro antibreast cancer activity, using human breast adenocarcinoma cell lines (MCF-7) and in vitro anti-inflammatory activity. By hemolysis assay, it showed that it has a nonhemolytic and nontoxic effect on human blood cell. The title compound 5, subjected to in vitro activities, showed that it is cytotoxic with an IC50 of 42.30 µM and a good anti-inflammatory agent. The docking results against cyclin dependent kinase 2 (CDK2) (PDB ID: 3QQK) gave insights on its inhibitory activity.

scholarly journals 2α-Acetoxy-15-acetylartemisiifolin, a new Anti-trypanosomal Sesquiterpene Lactone from Mikania guaco

2017 ◽  
Vol 12 (5) ◽  
pp. 1934578X1701200
Author(s):  
Ahmed A. Hussein ◽  
Luz Romero ◽  
Jose Luis López-Pérez ◽  
Mahabir P. Gupta
Keyword(s):  
Mass Spectrometry ◽  
Trypanosoma Cruzi ◽  
Sesquiterpene Lactone ◽  
Chemical Structure ◽  
Methanol Extract ◽  
Amastigote Form ◽  
Bioassay Guided Fractionation ◽  
Nmr Techniques

Mikania guaco Bonpl. methanol extract showed an interesting activity against Trypanosoma cruzi with an IC50 of 4 μg/mL. Bioassay-guided fractionation of the methanol extract resulted in the isolation of a new sesquiterpene lactone, 2α-acetoxy, 15-acetylartemisiifolin (1), which was shown to be active (IC50 = 25 μM) against the amastigote form of T. cruzi,. The chemical structure of 1 was elucidated using 2-D NMR techniques and mass spectrometry.

scholarly journals Synthesis of Novel Diclofenac Hydrazones: Molecular Docking, Anti-Inflammatory, Analgesic, and Ulcerogenic Activity

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Nawaf A. Alsaif ◽  
Mashooq A. Bhat ◽  
Mohamed A. Al-Omar ◽  
Hanaa M. Al-Tuwajiri ◽  
Ahmed M. Naglah ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Analgesic Activity ◽  
Binding Affinities ◽  
Standard Drug ◽  
Reference Drug ◽  
Ulcerogenic Activity ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Sparing Effect ◽  
Cox 1

This study was aimed to design novel diclofenac hydrazones having anti-inflammatory and analgesic activity with gastric sparing effect. A new series of 2-[2-(2,6-dichloroanilino)phenyl]-N’-[(substituted phenyl) methylidene] acetohydrazide derivatives (1−14) were synthesized and evaluated for their anti-inflammatory, analgesic, and ulcerogenic activity. The compounds were identified and confirmed by elemental analysis and spectral data. During anti-inflammatory activity by carrageenan-induced paw edema method, compounds (2, 3, 7, 8, 11, and 13) were found to be most promising. Compounds 3, 8, and 13 have been found to have significant analgesic activity compared to the reference drug diclofenac in analgesic activity by both the hot plate method and acetic acid-induced writhing method. The compounds which presented highly significant anti-inflammatory and analgesic activity were further tested for their ulcerogenic activity. Compounds 3 and 8 showed maximum ulcerogenic reduction activities. Compound 8 was found to have LD50 of 168 mg/kg. Compound 8 with 3,5-dimethoxy-4-hydroxyphenyl substitution was found to be the most promising anti-inflammatory and analgesic agent with gastric sparing activity. Molecular docking of compounds was performed for COX−1/COX−2 binding site. Lead compound 8 showed better binding affinities of −9.4 kJ/mol with both COX-1 and COX-2 as compared to the standard drug, diclofenac with binding affinities of −6.6 kJ/mol and −8.1 kJ/mol for COX−1 and COX−2, respectively.

scholarly journals Dectin-2 mediates phagocytosis of Lactobacillus paracasei KW3110 and IL-10 production by macrophages

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Mia Yoshikawa ◽  
Sayuri Yamada ◽  
Miho Sugamata ◽  
Osamu Kanauchi ◽  
Yuji Morita
Keyword(s):  
Lactic Acid ◽  
Lactic Acid Bacteria ◽  
Interleukin 10 ◽  
Lactobacillus Paracasei ◽  
Binding Affinities ◽  
Antibody Treatment ◽  
Lectin Array ◽  
Specific Strain ◽  
Anti Inflammatory ◽  
Carbohydrate Chains

AbstractLactic acid bacteria (LAB) are most generally used as probiotics and some strains of LAB are known to have anti-inflammatory effects. A specific strain of lactic acid bacteria, Lactobacillus paracasei KW3110 (KW3110), activates macrophages to produce interleukin-10 (IL-10), an anti-inflammatory cytokine; however, the biological mechanism remains unclear. In this study, we showed that the amount of incorporated KW3110 into a macrophage cell line, RAW 264.7, was higher than other genetically related strains using fluorescence microscopy. RNA-seq analysis indicated that treatment of macrophages with KW3110 induced Dectin-2 gene expression, which is a pattern recognition receptor, recognizing α-mannose. In addition, antibody treatment and knock down of Dectin-2, or factors downstream in the signaling pathway, decreased the amount of incorporated KW3110 and IL-10 production. Substantial lectin array analysis also revealed that KW3110 had higher binding affinities to lectins, which recognize the carbohydrate chains comprised of α-mannose, than two other LAB. In conclusion, KW3110 is readily incorporated into macrophages, leading to IL-10 production. Dectin-2 mediated the phagocytosis of KW3110 into macrophages and this may be involved with the characteristic carbohydrate chains of KW3110.

Tricarabrols A–C, three anti-inflammatory sesquiterpene lactone trimers featuring a methylene-tethered linkage from Carpesium faberi

2020 ◽  
Vol 7 (11) ◽  
pp. 1374-1382
Author(s):  
Jie Yuan ◽  
Xuelan Wen ◽  
Chang-Qiang Ke ◽  
Tian Zhang ◽  
Ligen Lin ◽  
...  
Keyword(s):  
Sesquiterpene Lactone ◽  
Anti Inflammatory

Three anti-inflammatory trimeric compounds constructed from carabrol-type sesquiterpenoids through a methylene-tethered linkage were characterized from Carpesium faberi.

New Sesquiterpene Lactone and Neolignan Glycosides with Antioxidant and Anti-Inflammatory Activities from the Fruits of Illicium oligandrum

Planta Medica ◽  
2007 ◽  
Vol 73 (5) ◽  
pp. 484-490 ◽  
Author(s):  
Wen-Zhao Tang ◽  
Yun-Bao Liu ◽  
Shi-Shan Yu ◽  
Jing Qu ◽  
Dong-Min Su
Keyword(s):  
Sesquiterpene Lactone ◽  
Anti Inflammatory
Sign in / Sign up

Export Citation Format

Share Document