scholarly journals Thymol derivatives with antibacterial and cytotoxic activity from the aerial parts of Ageratina adenophora

RSC Advances ◽  
2021 ◽  
Vol 11 (10) ◽  
pp. 5755-5761
Author(s):  
Mei Zhang ◽  
Jin-Kui Ouyang ◽  
Qiao-Lin Xu ◽  
Shao-Bo Liu ◽  
Tao Qian ◽  
...  

Eight thymol derivatives including three new ones (1–3) were obtained from the aerial parts of Ageratina adenophora, with most of them, in particular 1 and 5, showing notable in vitro antimicrobial and cytotoxic activity.

2021 ◽  
Vol 11 (2) ◽  
pp. 3480-3487

The present study is intended to reveal the biochemical profile and assess the toxicity and cytotoxic activity of aerial and underground parts of Eragrostis amabilis (L.) Wight. Arn. and Eragrostis pilosa (L.) Beauv. extracts using Brine shrimp lethality bioassay and Dalton’s lymphoma ascites cell (DLA). The maximum amount of protein 31.2 mg/g, amino acid 50.5 mg/g, glucose 62.8 mg/g and Indole acetic acid 29.5 mg/g were found in E. amabilis aerial parts. The maximum amount of total phenolics (218.21 mg/g) and tannins (88.5 mg/g) was observed in ethanolic extracts of E. amabilis aerial parts. The highest value of flavonoids was stated in chloroform extracts of E. amabilis underground parts (544 mg/g). The maximum amount of total phenolics and total tannin was observed in ethyl acetate extracts of E. pilosa aerial parts. The highest amount of flavonoids was found in ethyl acetate extracts of E. pilosa underground parts. The toxicity (LC50 values) of E. amabilis aerial and underground parts were ranged from 0.48 - 1.52 mg/ mL and 0.012 - 1.154 mg/ mL respectively. The LC50 value of E. pilosa aerial and underground parts extract was ranged from 1.089 - 1.904 mg/ mL and 0.038 -1.726 mg/ mL. The high cytotoxicity (ICT50) was observed in ethyl acetate extracts of E. amabilis and E. pilosa.


2021 ◽  
Vol 10 (3) ◽  
pp. 344-350
Author(s):  
Seyed Ahmad Hossiniyan ◽  
Farideh ghalamfarsa ◽  
Shaghayegh Rostami yasuj ◽  
Zeynab salehpour ◽  
Mohsen Latifpour ◽  
...  

Introduction: Herbal products are beneficial compounds with many applications in human life. In this study the chemical composition and cytotoxic activity of the essential oil of the aerial parts of Dorema aucheri were assessed. Methods: The essential oil was extracted by hydrodistillation after drying the aerial parts of D. aucheri, collected from the mountains around Yasuj city in the South-West of Iran. The oil composition was determined by GC/MS. To evaluate in vitro cytotoxic activity, the apoptotic effects of the essential oil were investigated against SW48 and SW1116 colorectal cancer cell lines by (3-[4, 5-dimethylthiazol-2-yl]-2, 5 diphenyl tetrazolium) bromide (MTT) assay and flow cytometry. Results: The essential oil yield was obtained 0.02% (W/W). Twenty-five compounds were identified in the oil, and the main constituents were caryophyllene (E) (31.29%), Phytol (14.92%), gurjunene (β-) (9.84%), 3,7,11,15-tetramethyl-2-hexadecen-1-ol (8.7%), and n-hexadecanoic acid (8.09%). The MTT assay showed that the IC50 values of the essential oil for SW48 and SW1116 cell lines were 1.4 and 1.2 mg/mL, respectively. The results of flow cytometry showed that the essential oil significantly increased the apoptosis in SW48 cell line compared with the vincristine (P < 0.05). It also increased the apoptosis in SW1116 cells compared with the vincristine, but this difference is not significant. Conclusion: The essential oil of D. aucheri consisted of high amounts of caryophyllene and showed significant cytotoxic effects against SW48 and SW1116 cancerous cell lines.


2017 ◽  
Vol 5 (2) ◽  
Author(s):  
Marina Letícia Do Carmo Caxito ◽  
Cerli Rocha Gattass ◽  
Ricardo Machado Kuster ◽  
Cristiane Pimentel Victório

Many studies have reported on the use of Euphorbia species against cancer. Tinctures of Euphorbia tirucalli L., popularly known as aveloz, have been widely used in Brazilian traditional medicine to treat cancer. However, the influence of seasonal variations on the cytotoxic activity of E. tirucalli ethanolic extracts (tinctures) has not been investigated. To accomplish this in the present work, aerial parts of E. tirucalli were collected each month in an experimental garden in Rio de Janeiro City. Effects of seasonality on the in vitro cytotoxic activity of E. tirucalli were evaluated. Tinctures were prepared by maceration in ethanol 70%, and qualitative phytochemical analyses were carried out using high-performance liquid chromatography (HPLC/UV/DAD). Cytotoxicity was evaluated in vitro against human lymphoma cells (Daudi) by MTT assay. The presence of triterpenes, hydrolysable tannins and flavonoids was detected in the tinctures. Tinctures prepared from plants collected seasonally showed concentration-dependent cytotoxicity against the analyzed cell line. Therefore, it can be concluded that environmental conditions based on seasonal changes did induce variability in phenolic compounds content and, hence, cytotoxic activity of aveloz on tumor cells.


2019 ◽  
Vol 23 (17) ◽  
pp. 1857-1866
Author(s):  
Munawar Hussain ◽  
Zaheer Ahmed ◽  
Shamsun N. Khan ◽  
Syed A. A. Shah ◽  
Rizwana Razi ◽  
...  

Three new 5-deoxyflavonoid and dihydroflavonoids 2, 3 and 4 have been isolated from the methanolic extract of Abutioln pakistanicum aerial parts, for which structures were elucidated explicitly by extensive MS- and NMR-experiments. In addition to these, 3,7,4′-trihydroxy-3′-methoxy flavonol (1) is reported for the first time from Abutioln pakistanicum. Compound 2 and 4 are p-coumaric acid esters while compounds 2–4 exhibited α-glucosidase inhibitory activity. Docking studies indicated that the ability of flavonoids 2, 3 and 4 to form multiple hydrogen bonds with catalytically important residues is decisive hence is responsible for the inhibition activity. The docking results signified the observed in-vitro activity quite well which is in accordance with previously obtained conclusion that phenol moiety and hydroxyl group are critical for the inhibition of α-glucosidase enzyme.


2019 ◽  
Vol 19 (2) ◽  
pp. 265-275 ◽  
Author(s):  
Faeze Khalili ◽  
Sara Akrami ◽  
Malihe Safavi ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Mina Saeedi ◽  
...  

Background: This paper reports synthesis, cytotoxic activity, and apoptosis inducing effect of a novel series of styrylimidazo[1,2-a]pyridine derivatives. Objective: In this study, anti-cancer activity of novel styrylimidazo[1,2-a]pyridines was evaluated. Methods: Styrylimidazo[1,2-a]pyridine derivatives 4a-o were synthesized through a one-pot three-component reaction of 2-aminopyridines, cinnamaldehydes, and isocyanides in high yield. All synthesized compounds 4a-o were evaluated against breast cancer cell lines including MDA-MB-231, MCF-7, and T-47D using MTT assay. Apoptosis was evaluated by acridine orange/ethidium bromide staining, cell cycle analysis, and TUNEL assay as the mechanism of cell death. Results: Most of the synthesized compounds exhibited more potent cytotoxicity than standard drug, etoposide. Induction of apoptosis by the most cytotoxic compounds 4f, 4g, 4j, 4n, and 4m was confirmed through mentioned methods. Conclusion: In conclusion, these results confirmed the potency of styrylimidazo[1,2-a]pyridines for further drug discovery developments in the field of anti-cancer agents.


Foods ◽  
2020 ◽  
Vol 9 (2) ◽  
pp. 144
Author(s):  
Immacolata Faraone ◽  
Daniela Russo ◽  
Lucia Chiummiento ◽  
Eloy Fernandez ◽  
Alka Choudhary ◽  
...  

The genus Minthostachys belonging to the Lamiaceae family, and is an important South American mint genus used commonly in folk medicine as an aroma in cooking. The phytochemical-rich samples of the aerial parts of Minthostachys diffusa Epling. were tested for pharmacological and health-promoting bioactivities using in vitro chemical and enzymatic assays. A range of radical scavenging activities of the samples against biological radicals such as nitric oxide and superoxide anion and against synthetic 2,2-diphenyl-1-picrylhydrazyl and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radicals, the ferric reducing antioxidant power and the lipid peroxidation inhibition were determined and ranked using the ‘relative antioxidant capacity index’ (RACI). The ethyl acetate fraction showed the highest RACI of +1.12. Analysis of the various fractions’ inhibitory ability against enzymes involved in diabetes (α-amylase and α-glucosidase), and against enzymes associated with Parkinson’s or Alzheimer’s diseases (acetylcholinesterase and butyrylcholinesterase) also suggested that the ethyl acetate fraction was the most active. Liquid chromatography–tandem mass spectrometry analysis of the ethyl acetate fraction showed more than 30 polyphenolic compounds, including triterpenes. The inhibitory cholinesterase effects of the triterpenes identified from M. diffusa were further analysed by in silico docking of these compounds into 3D-structures of acetylcholinesterase and butyrylcholinesterase. This is the first study on pharmacological activities and phytochemical profiling of the aerial parts of M. diffusa, showing that this plant, normally used as food in South America, is also rich in health-promoting phytochemicals.


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