scholarly journals In vitro antimicrobial, anticancer, and apoptosis-inducing effects of the methanolic extract of Launaea mucronata

2021 ◽  
Vol 49 (4) ◽  
pp. 12556
Author(s):  
Amr S. ABOUZIED ◽  
Mohammed K.B. BREAK ◽  
Kareem YOUNES ◽  
Essam N. ADS ◽  
Rahamat U. SYED ◽  
...  

Traditional medicine is widely used in the treatment and management of various ailments due to its low toxicity, low number of side effects and low cost. Many components of common fruits and vegetables play crucial roles as chemopreventive or chemotherapeutic agents. This study aimed to evaluate in vitro the antioxidant, cytotoxic and antimicrobial activities of Launaea mucronata’s methanolic stems and leaves extract. In this screening study, Launaea mucronata’s methanolic extracts showed remarkably antifungal activity against Candida albicans. The maximum zone of inhibition of the methanolic extract of Launaea mucronata leaves was detected against Proteus vulgaris with inhibition zones of 17.8 mm and 14.6 mm, respectively. 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay results showed high antioxidant activity for the extract almost comparable to that of ascorbic acid at 30 µg/ml, which indicates that it might potentially be developed into a successful antioxidant agent. Meanwhile, 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay was performed by screening the extract against HepG2 (Hepatocellular), A549 (Lung), HCT116 (Colon) and MCF7 (Breast) cancer cells and it was found that the extract exerted its highest activity against A549 cells with an IC50 value of 14.9 µg/ml. The extracts also shown lower cytotoxic activity against normal, healthy MRC-5 cells, with IC50 values of 204.83 g/ml for the stem extract and 412.4 g/ml for the leaves extract, respectively. This suggests that the extract is safe for normal, healthy cells, which is an important characteristic of any possible anticancer treatment. The antiproliferative and apoptosis activities of our selected plant showed that the extracts induced S-phase arrest and apoptosis in A549 cells. This high cytotoxic activity of the extract indicates that highly bioactive pure compounds could potentially be isolated from the extract in future studies and further developed into an anticancer agent specifically against lung cancer. Therefore, the current study has proven the potential of Launaea mucronata’s methanolic extract as a source of potent antioxidant and anticancer agent.

Author(s):  
Olubukola H. Oyeniran ◽  
Adedayo O. Ademiluyi ◽  
Ganiyu Oboh

AbstractObjectivesRauvolfia vomitoria is a medicinal plant used traditionally in Africa in the management of several human diseases including psychosis. However, there is inadequate scientific information on the potency of the phenolic constituents of R. vomitoria leaf in the management of neurodegeneration. Therefore, this study characterized the phenolic constituents and investigated the effects of aqueous and methanolic extracts of R. vomitoria leaf on free radicals, Fe2+-induced lipid peroxidation, and critical enzymes linked to neurodegeneration in rat’s brain in vitro.MethodsThe polyphenols were evaluated by characterizing phenolic constituents using high-performance liquid chromatography coupled with diode array detector (HPLC-DAD). The antioxidant properties were assessed through the extracts ability to reduce Fe3+ to Fe2+; inhibit ABTS, DPPH, and OH radicals and Fe2+-induced lipid peroxidation. The effects of the extracts on AChE and MAO were also evaluated.ResultsThe phenolic characterization of R. vomitoria leaf revealed that there were more flavonoids present. Both aqueous and methanolic extracts of R. vomitoria leaf had inhibitory effects with the methanolic extract having higher significant (p≤0.05) free radicals scavenging ability coupled with inhibition of monoamine oxidases. However, there was no significant (p≤0.05) difference obtained in the inhibition of lipid peroxidation and cholinesterases.ConclusionThis study suggests that the rich phenolic constituents of R. vomitoria leaf might contribute to the observed antioxidative and neuroprotective effects. The methanolic extract was more potent than the aqueous extract; therefore, extraction of R. vomitoria leaf with methanol could offer better health-promoting effects in neurodegenerative condition.


Polymers ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1515
Author(s):  
Xiukun Xue ◽  
Yanjuan Wu ◽  
Xiao Xu ◽  
Ben Xu ◽  
Zhaowei Chen ◽  
...  

Polymeric prodrugs, synthesized by conjugating chemotherapeutic agents to functional polymers, have been extensively investigated and employed for safer and more efficacious cancer therapy. By rational design, a pH and reduction dual-sensitive dextran-di-drugs conjugate (oDex-g-Pt+DOX) was synthesized by the covalent conjugation of Pt (IV) prodrug and doxorubicin (DOX) to an oxidized dextran (oDex). Pt (IV) prodrug and DOX were linked by the versatile efficient esterification reactions and Schiff base reaction, respectively. oDex-g-Pt+DOX could self-assemble into nanoparticles with an average diameter at around 180 nm. The acidic and reductive (GSH) environment induced degradation and drug release behavior of the resulting nanoparticles (oDex-g-Pt+DOX NPs) were systematically investigated by optical experiment, DLS analysis, TEM measurement, and in vitro drugs release experiment. Effective cellular uptake of the oDex-g-Pt+DOX NPs was identified by the human cervical carcinoma HeLa cells via confocal laser scanning microscopy. Furthermore, oDex-g-Pt+DOX NPs displayed a comparable antiproliferative activity than the simple combination of free cisplatin and DOX (Cis+DOX) as the extension of time. More importantly, oDex-g-Pt+DOX NPs exhibited remarkable reversal ability of tumor resistance compared to the cisplatin in cisplatin-resistant lung carcinoma A549 cells. Take advantage of the acidic and reductive microenvironment of tumors, this smart polymer-dual-drugs conjugate could serve as a promising and effective nanomedicine for combination chemotherapy.


Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1694
Author(s):  
Kamel Arraki ◽  
Perle Totoson ◽  
Alain Decendit ◽  
Andy Zedet ◽  
Justine Maroilley ◽  
...  

Polyphenolic enriched extracts from two species of Cyperus, Cyperus glomeratus and Cyperus thunbergii, possess mammalian arginase inhibitory capacities, with the percentage inhibition ranging from 80% to 95% at 100 µg/mL and 40% to 64% at 10 µg/mL. Phytochemical investigation of these species led to the isolation and identification of two new natural stilbene oligomers named thunbergin A-B (1–2), together with three other stilbenes, trans-resveratrol (3), trans-scirpusin A (4), trans-cyperusphenol A (6), and two flavonoids, aureusidin (5) and luteolin (7), which were isolated for the first time from C.thunbergii and C. glomeratus. Structures were established on the basis of the spectroscopic data from MS and NMR experiments. The arginase inhibitory activity of compounds 1–7 was evaluated through an in vitro arginase inhibitory assay using purified liver bovine arginase. As a result, five compounds (1, 4–7) showed significant inhibition of arginase, with IC50 values between 17.6 and 60.6 µM, in the range of those of the natural arginase inhibitor piceatannol (12.6 µM). In addition, methanolic extract from Cyperus thunbergii exhibited an endothelium and NO-dependent vasorelaxant effect on thoracic aortic rings from rats and improved endothelial dysfunction in an adjuvant-induced arthritis rat model.


Author(s):  
A. Renjith Alex ◽  
K. Ilango

Objective: The main aim of the study was to screen the isolated compounds of Viburnum Punctatum for its in vitro anticancer activity and its percentage viability against HCT 15 (Human Colon Cancer Cells) Cell lines.Methods: Pet ether, Chloroform, Methanol and Aqueous extracts was prepared and assayed for the presence of phytochemicals. Two compounds were isolated from the methanol extract of Viburnum Punctatum by column chromatography such as ME1 (Quercetin) and ME2 (Kaemferol-3-glycoside) characterised by UV, IR, MS, 1H NMR and 13C NMR. The above isolated compounds were subjected to in vitro anticancer activity on HCT 15 cell lines was evaluated by Micro culture Tetrazolium (MTT) assay.Results: ME1 showed significant cytotoxic activity than the ME2 on HCT 15 cells with a percentage viability of 54.60 and 67.18 in the concentration of 10µg/ml and 50µg/ml respectively.Conclusion: On the basis of obtained results, ME1 and ME2 isolated from a methanolic extract of Viburnum Punctatum represent a new group of cytotoxic against HCT 15 Cell lines.


2018 ◽  
Vol 87 (2) ◽  
Author(s):  
Anita Agnieszka Śliwińska ◽  
Katarzyna Sykłowska-Baranek ◽  
Anita Kośmider ◽  
Sebastian Granica ◽  
Karolina Miszczak ◽  
...  

<p>In this study, an efficient method to enhance phenolic compound production in the in vitro cultured shoots of <em>Polyscias filicifolia</em> was developed. The phenolic compound content in <em>P. filicifolia</em> has not yet been reported. Shoots were treated with methyl jasmonate (JM) or salicylic acid (SA) at doses of 50, 100, or 200 µM. HPLC-UV-VIS and LC-MS techniques were used for the determination of chlorogenic, caffeic, and ferulic acids. The total phenolics and flavonoids were quantified, and the antioxidant capacity of plant extracts was determined using DPPH and ABTS methods. Finally, the cytotoxic activity of <em>P. filicifolia</em> extracts in normal (HaCaT) and cancer (A549) cells was investigated. Further, the effect of the extracts on cisplatin cytotoxicity was assessed.</p><p>The elicitors significantly enhanced phenolic production compared to that in untreated shoots and leaves of intact plants. Chlorogenic acid was the most abundant compound with the highest yield of 5.03 ±0.25 mg/g DW after treatment with 50 µM SA. The total flavonoid and phenolic content was significantly and dose-dependently influenced by JM. The highest antioxidant capacity was noted in extracts derived from shoots grown on media supplemented with 50 µM SA and 200 µM JM; these doses were used for further cytotoxic activity investigations. The extracts from JM or SA treatments reduced cancer cell viability and increased their mortality, whereas the extract from JM treatment exhibited protective effect on normal cells. Moreover, the comparison of cytotoxic properties of plant extracts and cisplatin indicated that plant phenolic compounds in combination with anticancer drugs could reduce the detrimental effect of the latter on human cells.</p>


2021 ◽  
Vol 33 ◽  
pp. 03001
Author(s):  
Annise Proboningrat ◽  
Amaq Fadholly ◽  
Sri Agus Sudjarwo ◽  
Fedik Abdul Rantam ◽  
Agung Budianto Achmad

Several efforts have been made to discover new anticancer agents based on natural ingredients. Meanwhile, previous studies have shown that different Pine genus species exhibit cytotoxic activity against various types of cancer cells. This plant is rich in phenolic compounds, especially procyanidins, flavonoids, and phenolic acids. Therefore, this study aims to investigate the in vitro cytotoxicity of Pinus merkusii needles extract on HeLa cancer cell lines. The cytotoxicity assessment was measured using MTT assay and expressed as IC50 value. The results showed that the ethanolic extract poses a dose and time-dependent cytotoxic activity with an IC50 value of 542.5 µg/ml at 48 hours of incubation. Based on this result, Pinus merkusii needles’ ethanolic extract has the potential of a novel candidate for an anticancer agent.


Author(s):  
Md. Abdur Rahman ◽  
Md. Saddam Hussain ◽  
Md. Shalahuddin Millat ◽  
Md. Mizanur Rahman Moghal

Excoecaria agallocha plant (Leaves) was analyzed to explore In Vitro antimicrobial and membrane stabilizing activities as a crude methanolic extract. Antimicrobial activity was performed against a wide range of Gram positive(+Ve) and Gram negative(-Ve) bacteria by using disc diffusion method and various methanolic extracts of leaves of E.agallocha was tested for determining membrane stabilizing activity at hypotonic solution and heat induce condition and standard acetyl salicylic acid (0.10 mg/mL) was employed as standard. the zones of inhibition created was found to be 1.3 cm at a concentration of 100 µL/ disc in case of Gram negative(-Ve) bacteria Salmonella typhi. The results obtained were compared with that of a standard Ampicillin (10 µL) and imipenem (10µL), penicillin (10µl), cefoxitine(30µl). Crude methanolic extract of 10mg/ml concentration showed maximum value of 17.67±0.0102 and 18.92±0.086% respectively under hypotonic solution and heat induced condition. Thus the result suggest that, crude methanolic extracts of E.agallocha possessed slight to moderate antimicrobial and membrane stabilizing properties.


2020 ◽  
Vol 11 (1) ◽  
pp. 25-38
Author(s):  
Nadia I. Zakhary ◽  
Emad E.H. El Gemeie ◽  
Adel K. Youssef ◽  
Marwa Abdel-salam Ibrahim Metwaly

Erucaria pinnata (Viv.) is a wild annual plant growing in North-Western Coastal Region in Egypt. This study reports for the first time the cytotoxic activity of different extracts of Erucaria pinnata plant against HEP-G2 cell line. The 70% methanolic extract (E1) recorded the best potent cytotoxic activity (IC50=13.6 µg/ml), so we analysis the flavonoids constituent of this extract using HPLC, which show that our extract is rich with important flavonoids compounds (rutin, quercetin, leutolin, etc.). We evaluated its antitumor activity against hepatocellular carcinoma (HCC) induced by diethylnitrosamine (DEN) (200mg/Kg. b.wt., i.p, single dose) after two weeks, animals received carbontetrachloride (CCl4) (3ml/Kg. b.wt., SC, once a week for 6 weeks) and the experiment continued for 44 weeks in rats. After the experimental period, the administration of DEN/CCl4 showed significant increase in the levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase (ALP), total bilirubin, gamma-glutamyl transferase (γGT) and significant decrease in the levels of total proteins and albumin content in the serum with reduction in the liver antioxidants, including superoxide dismutase (SOD) and catalase (CAT). This was accompanied by increases in serum specific tumor markers (AFP). The 70% methanolic plant extract (E1) was orally administrated (400mg/kg/day respectively) for the whole study period, and it showed a significant improvement at the different biological liver functions, remodeled the antioxidant enzymes activity and down-regulated the serum AFP. All these findings were confirmed by histopathological studies of the liver samples obtained from all groups. In addition, we evaluated its antiangeogenic activity by docking study against VEGFR-2 tyrosine kinase after it showed an ability to inhibit the VEGFR-2 expression in vitro and inhibit the concentration of VEGF-A in vivo. The hepatoprotective effect of our extract was attributed to its antioxidant and antiangeogenic activity.


Author(s):  
José Fernando Araújo Neto ◽  
Erika Maria de Oliveira Ribeiro ◽  
Ademir Evangelista do Vale ◽  
Jorge Maurício David ◽  
Juceni Pereira de Lima David

: Erythroxylaceae is a family composed of four genera being Erythroxylum the only one represented in the Neotropical region. Chemical studies indicate the presence of alkaloids, terpenes, flavonoids and phenolic compounds as main compounds. The incorporation of cytotoxic activity assays of natural products using cell cultures assists in the selection of potential chemotherapeutic agents. In this work we describe a revision of the cytotoxicity evaluation studies performed with extracts and/or pure substances obtained from Erythroxylum species through an integrative review. We have found studies that evaluated the cytotoxic activity of 21 species of Erythroxylum against 45 different cell lines, the analysis of the chemical composition of these species shows that the metabolites present in each species influence the cytotoxic potential of them, especially the presence of disubstituted tropane alkaloids species with the highest cytotoxic potential. MTT and Sulforrodamine B assays were the main in vitro tests used for the evaluation of the cytotoxic activities. From the total of species, less than 10% of the Erythroxylum species have already been evaluated for the cytotoxic activity, four of them showed high cytotoxic activity according to with the criteria of the NCI plant screening program. Thus, this genus represents a potential source of natural products with antitumor activity.


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