scholarly journals Isolation and Evaluation of Bioactive Compounds from Rheum emodi and their Anti-Inflammatory and Anticancer Properties

2021 ◽  
Vol 25 (06) ◽  
pp. 1161-1172
Author(s):  
Sang Koo Park

Rheum emodi Wall. ex Meissn is a popular medicinal herb having wide application in traditional medicine for treating of several diseases. The present study was aimed to identify and isolate phytochemicals present in ethyl acetate extract fraction of R. emodi and to evaluate the anticancer and anti-inflammatory activities of water/organic solvent fractions and isolated compounds of R. emodi rhizome extracts. Based on the structure, flavonoid compound i.e., Myricitrin (sym. Myricetin 3- rhamnoside), myricetin 3-galloylrhamnoside and myricetin were identified to be present in ethyl acetate extract. The molecular weight of compound 1 cannot be identified; while compound 5 remained unknown as there was not enough evidence to propose its structure. The isolated compounds and different solvent fractions were tested for their anticancer and antiinflammatory activities. Among Myricetins derivatives, particularly unknown compounds significantly induced the apoptosis and restrained the proliferation of cancer cell lines (A549 and MCF-7) and inhibited the LPS induced NO production (proinflammatory mediator), IL-6 activity, IL-1β and TNF-α (cytokines) activity in RAW 264.7 macrophages in a dose dependent manner and was effective even at lower concentration (50 µg/mL). Similarly, the higher concentration of aqueous and solvent fractions exhibited strong cytotoxic and anti-inflammatory activities. However, water and dichloromethane fractions were most effective in inhibiting the anticancer activities in A549 and MCF-7 cancer cell lines, respectively. At lower concentration (50 and 100 µg/mL), highest inhibition activity for NO, IL-6 and IL-1β was noted with ethyl acetate fractions and n-Hexane fractions; while water and n-Butanol (fractions) strongly inhibited the TNF-α activity at lower (100 µg/mL) and high (200 µg/mL) concentration, respectively. In conclusion, the isolated compounds from R. emodi rhizome extracts and its rhizome solvent fractions exhibit strong anti-cancer and anti-inflammatory activities and can be used to develop chemotherapeutics and anti-inflammation drugs. © 2021 Friends Science Publishers

2011 ◽  
Vol 2011 ◽  
pp. 1-9 ◽  
Author(s):  
Zahra Tayarani-Najaran ◽  
Seyed Ahmad Emami ◽  
Javad Asili ◽  
Alireza Mirzaei ◽  
Seyed Hadi Mousavi

TheScutellariaspecies (Lamiaceae) is used as a source of flavonoids to treat a variety of diseases in traditional medicine. In spite of many reports about the cytotoxic and antitumor effects of some species of this genus, anticancer researches on one of the Iranian speciesS. litwinowiihave not yet been conducted.The cytotoxic properties of total methanol extract ofS. litwinowiiand its fractions were investigated on different cancer cell lines including AGS, HeLa, MCF-7, PC12 and NIH 3T3. Meanwhile, the role of apoptosis in this toxicity was explored. The cells were cultured in DMEM medium and incubated with different concentrations of herb plant extracts. Cell viability was quantitated by MTT assay. Apoptotic cells were determined using propidium iodide staining of DNA fragmentation by flow cytometry (sub-G1 peak).Scutellaria litwinowiiinhibited the growth of malignant cells in a dose-dependent manner. Among solvent fractions ofS. litwinowii, the methylene chloride fraction was found to be more toxic compared to other fractions. The IC50values of this fraction against AGS, HeLa, MCF-7 and PC12 cell lines after 24 h were determined, 121.2 ± 3.1, 40.9 ± 2.5, 115.9 ± 3.5 and 64.5 ± 3.4μg/ml, respectively.Scutellaria litwinowiiinduced a sub-G1 peak in the flow cytometry histogram of treated cells compared to control cells indicating that apoptotic cell death is involved inS. litwinowiitoxicity.Scutellaria litwinowiiexerts cytotoxic and proapototic effects in a variety of malignant cell lines and could be considered as a potential chemotherapeutic agent in cancer treatment.


Author(s):  
Manikandan Alagumuthu ◽  
Vanshika Srivastava ◽  
Manisha Shah ◽  
Sivakumar Arumugam ◽  
Mohandoss Sonaimuthu ◽  
...  

Background: Macrophages play a serious part in the instigation, upkeep, and resolution of inflammation. They are activated or deactivated during inflammation progression. Activation signals include cytokines (IF-γ, granulocyte-monocyte colonystimulating factor (GM-CSF), and TNF-α), extracellular matrix proteins, and other chemical mediators. Activated macrophages are deactivated by anti-inflammatory cytokines (IL- 10 and TGF-β (transforming growth factor-beta) and cytokine antagonists that are mainly produced by macrophages. Based on this, the present study aimed to develop novel (E)- Benzylidene-indazolpyridin methanones (Cpd-1-10) as effective anti-inflammatory agents by analyzing pro- and anti-inflammatory cytokine levels in macrophages. Objectives: To determine the anti-inflammatory effect of indazolpyridin-methanones by examining pro- and anti-inflammatory interleukin levels in J77A.1 macrophages. Methods: Expression of cytokines such as TNF-α, IL-1β, IL-6 and IL-10 serum levels measured by ELISA method. Anti-cancer and cytotoxicity studies were carried out by MTT assay. COX-2 seems to be associated with cancers and atypical developments in the duodenal tract. So, a competitive ELISA based COX-2 inhibition assay was done. To validate the inhibitory potentials and to get more insight into the interaction of COX-2 with Cpd1-10, molecular docking was performed. Results: Briefly, the COX-2 inhibitory relative activity was found to be in between the range of 80-92% (Diclofenac showed 84%, IC50 0.95 μM). Conclusion: Cytotoxicity effect of the compounds against breast cancer cell lines found excellent and an extended anticancer study ensured that these compounds are also alternative therapeutic agents against breast cancer. Among all the tested cancer cell lines, the anti- cancer effect on breast cancer was exceptional for the most active compounds Cpd5 and Cpd9.


2020 ◽  
Vol 10 ◽  
Author(s):  
Zaynab Al-Eisawi ◽  
Salim M. Abderrahman ◽  
Yasmin M. S. Abdelrahim ◽  
Reem Al-Abbassi ◽  
Yasser K. Bustanji

Background: Medicinal plants have been used for many centuries for their significant phytochemical reservoir, forming a foundation for many medicinal drugs. Conventional cancer therapy possesses a number of undesired problems including poor selectivity, severe side effects and resistance of cancer. Objective: There is a need for new anticancer drugs possibly from natural sources such as medicinal plants. A. Hierochuntica L. is rich with phytochemicals and is widely used in traditional medicine. Method: The antiproliferative activities of A. hierochuntica whole plant extracts (ethanol, methanol, ethyl acetate, chloroform and water) were determined against a panel of cancer cells and normal primary dermal fibroblasts. The genotoxic effect of A. hierochuntica ethyl acetate on mice bone marrow cells was also evaluated. Genotoxic parameters included Chromosomal aberration, Mitodepression, Micronuclei formation and sister chromatid exchange. Results: A. hierochuntica exhibited antiproliferative activity against leukemia (K-562) and melanoma (A-375) cells. This is the first study to demonstrate the effect of A. hierochuntica ethyl acetate extract on cancer cell lines, found to be the most cytotoxic of all extracts. Furthermore, the chloroform extract showed notable anti-proliferative effects against most cancer cell lines tested. The extracts proved to be highly safe on human normal skin fibroblasts. Furthermore, A. hierochuntica ethyl acetate extract was also found to have limited genotoxic effects, with these changes seen at very high doses only. Conclusion: The results indicate that A. hierochuntica extracts have significant selective anticancer activity and that genotoxicity is only observed at very high concentrations.


2019 ◽  
Vol 8 (2) ◽  
pp. 101-106
Author(s):  
Amin Mohammadi ◽  
Ali Mostafaie ◽  
Ahmad Bagheri ◽  
Sarah Kiani ◽  
Maryam Chalabi

Background: Breast cancer is the most common cause of cancer-related death in women worldwide. Therefore, there is an urget need to identify and develop therapeutic strategies against this deadly disease. This study is the first to investigate the effects of Hemolymph Serum of Potamon persicum Crab (HSPPC) on MCF-7 and MDA-231 breast cancer cell lines. Materials and Methods: LDH and MTT assays were performed on MCF-7 and MDA-231 breast cancer cell lines as well as human umbilical vein endothelial cells (HUVEC) to determine the cytotoxic and antiproliferative activity of the HSPPC at different concentrations. Further, the apoptosis inducing action of the hemolymph serum was determined by TUNEL (terminal deoxynucleotidyl transferasemediated dUTP nick end labeling) and cell death assay. Results: The IC50 values of HSPPC for MCF-7 and MDA-231 cell lines were 960±0.369 and 850±1.422 μg/mL, respectively. The growth of both MCF-7 and MDA-231 cell lines were significantly (P<0.001) inhibited by HSPPC as compared with untreated controls at 48 hours. The results showed that HSPPC had no cytotoxic effects but significantly inhibited cell growth in a dose and time dependent manner. In addition, DNA fragmentation analysis (TUNEL) and cell death assay indicated induction of apoptosis by HSPPC in MCF-7 and MDA-231 cell lines. Conclusion: The results suggest that HSPPC contains bioactive compound(s) with potentials for the treatment of breast cancer.


2021 ◽  
Vol 53 (1) ◽  
pp. 109-117
Author(s):  
Ratna Asmah Susidarti ◽  
Edy Meiyanto ◽  
Muthi' Ikawati ◽  
Normaidah Normaidah ◽  
Nurramadhani A. Sida

Isolation and identification of compounds and pharmacological activity of the Micromelum minutum grown in some countries has been done, but the Indonesian M. minutum has not been studied, either phytochemically or pharmacologically. This study aimed to determine the cytotoxic activity of Indonesian M. minutum leave extracts toward MCF-7 and 4T1 breast cancer cell lines. The leaves were obtained from M. minutum grow in Bantimurung National Park, Bulusaraung, South Sulawesi, and then were macerated gradually in hexane, ethyl acetate, and methanol. The cytotoxic activity of obtained extracts was determined by MTT assay. The extraction yielded hexane (HEM), ethyl acetate (EEM), and methanol (MEM) extracts of 2.65, 6.12, and 6.49%, respectively. HEM was the most potent extract with IC50 values of 148 and 87 µg/mL on MCF-7 and 4T1 cells, respectively, followed by EEM (185 and 170 µg/mL). MEM possessed a weak potency with an IC50 value of 384 µg/mL on MCF-7 cells and was not toxic toward 4T1 cells. Therefore, HEM is important to be further investigated for its active constituents.


Pharmacia ◽  
2021 ◽  
Vol 68 (4) ◽  
pp. 779-787
Author(s):  
Sahar M. AlMotwaa

The anticancer effects of chemotherapeutic agents may be accentuated, and their side effects minimized by combining them with essential oils in nanocarrier systems. This study aimed to incorporate ifosfamide (IF) into nanoemulsion-based clove oil (IF-CLV). The nano-emulsion (NE) formulas were characterized with Zetasizer. The cytotoxicity of the formulated NEs against cervical (HeLa) and breast (MCF-7) cancer cell lines was determined using MTT assay, light microscopy, and DAPI staining. The z – average diameters of NE-CLV and IF-CLV were 63.1±1.00 and 89.4±2.64 nm, while Zeta potential values were – 4.39±0.4 and – 11.65±1.1mV, respectively. Cytotoxicity studies revealed that relative to free IF, NE-CLV and IF-CLV were highly toxic on HeLa and MCF-7cells, in a dose-dependent manner. The half-maximal inhibitory concentration (IC50) values of NE-CLV against HeLa and MCF-7 have decreased 38 and 27 folds, while the corresponding IC50 values of IF-CLV have decreased 57 and 35 folds, respectively. These results suggest that the incorporation of IF into NE-based clove oil produces potent therapeutic effects against cancer cell lines.


2019 ◽  
Author(s):  
Manal Abdel-Fattah ◽  
Hesham Saeed ◽  
Lamiaa El-Shennawy ◽  
Manal Shalaby ◽  
Amira M. Embaby ◽  
...  

AbstractThe current study highlights for the first time cloning, overexpression, purification, and assessing the cytotxcity of the novel interferon epsilon (IFNε), from the Arabian camelCamelus dromedarius, against two human breast cancer cell lines MDA-MB-231 and MCF-7. Full-length cDNA encoding interferon epsilon (IFNε) was isolated and cloned from the liver of the Arabian camel,C. dromedariususing reverse transcription-polymerase chain reaction. The sequence analysis of the camel IFNε cDNA showed a 582-bp open reading frame encoding a protein of 193 amino acids with an estimated molecular weight of 22.953 kDa. A BLAST search analysis revealed that theC. dromedariusIFNε shared high sequence identity with the IFN genes of other species, such asCamelus ferus,Vicugna pacos, andHomo sapiens. Expression of the camel IFNε cDNA inEscherichia coligave a fusion protein band of 22.73 kDa after induction with either isopropyl β-D-1-thiogalactopyranoside or lactose for 5 h. Recombinant IFNε protein was overexpressed in the form of inclusion bodies that were easily solubilized and refolded using SDS and KCl. The solubilized inclusion bodies were purified to apparent homogeneity using nickel affinity chromatography. We examined the effect of IFNε on two breast cancer cell lines MDA-MB-231 and MCF-7. In both cell lines, IFNε inhibited cell survival in a dose dependent manner as observed by MTT assay, morphological changes and apoptosis assay. Caspase-3 expression level was found to be increased in MDA-MB-231 treated cells as compared to untreated cells.


Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 4009
Author(s):  
Ahmed S. Abu Zaid ◽  
Ahmed E. Aleissawy ◽  
Ibrahim S. Yahia ◽  
Mahmoud A. Yassien ◽  
Nadia A. Hassouna ◽  
...  

Background: This study aimed to produce, purify, structurally elucidate, and explore the biological activities of metabolites produced by Streptomyces (S.) griseus isolate KJ623766, a recovered soil bacterium previously screened in our lab that showed promising cytotoxic activities against various cancer cell lines. Methods: Production of cytotoxic metabolites from S. griseus isolate KJ623766 was carried out in a 14L laboratory fermenter under specified optimum conditions. Using a 3-(4,5-dimethylthazol-2-yl)-2,5-diphenyl tetrazolium-bromide assay, the cytotoxic activity of the ethyl acetate extract against Caco2 and Hela cancer cell lines was determined. Bioassay-guided fractionation of the ethyl acetate extract using different chromatographic techniques was used for cytotoxic metabolite purification. Chemical structures of the purified metabolites were identified using mass, 1D, and 2D NMR spectroscopic analysis. Results: Bioassay-guided fractionation of the ethyl acetate extract led to the purification of two cytotoxic metabolites, R1 and R2, of reproducible amounts of 5 and 1.5 mg/L, respectively. The structures of R1 and R2 metabolites were identified as β- and γ-rhodomycinone with CD50 of 6.3, 9.45, 64.8 and 9.11, 9.35, 67.3 µg/mL against Caco2, Hela and Vero cell lines, respectively. Values were comparable to those of the positive control doxorubicin. Conclusions: This is the first report about the production of β- and γ-rhodomycinone, two important scaffolds for synthesis of anticancer drugs, from S. griseus.


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