scholarly journals Cytotoxic sesquiterpene lactones from the aerial parts of Inula aucheriana.

2015 ◽  
Vol 87 (2) ◽  
pp. 777-785 ◽  
Author(s):  
Ahmad Reza Gohari ◽  
Mahmoud Mosaddegh ◽  
Farzaneh Naghibi ◽  
Bahara Eslami-Tehrani ◽  
Atefeh Pirani ◽  
...  
Keyword(s):  
Cancer Research ◽  
Secondary Metabolites ◽  
Cytotoxic Activity ◽  
Sesquiterpene Lactones ◽  
Tetrazolium Bromide ◽  
Aerial Parts ◽  
The Family ◽  
Ic50 Values ◽  
Diphenyl Tetrazolium Bromide ◽  
Mcf 7

Inula aucheriana DC is a member of the family Asteraceae which is known to produce cytotoxic secondary metabolites noted as sesquiterpene lactones. In the present study, sesquiterpene lactones inuchinenolide B, 6-deoxychamissonolide (stevin) and 14-acetoxy-1β,5α,7αH-4β-hydroxy-guai-9(10),11(13)-dien-12,8α-olide were isolated from I. aucheriana. Inuchinenolide B and 14-acetoxy-1β,5α,7αH-4β-hydroxy-guai-9(10),11(13)-dien-12,8α-olide were further evaluated by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide) assay to demonstrate cytotoxic activity with IC50 values of (56.6, 19.0), (39.0, 11.8), and (55.7, 15.3) μg/mL against HepG-2, MCF-7 and A-549 cells, respectively. The cytotoxic activity of the two evaluated sesquiterpene lactones partly explains the cytotoxic activity that was previously observed for the extracts of Inula aucheriana. The isolated compounds could be further investigated in cancer research studies.

Cytotoxic Constituents from the Bark of Erythrina poeppigiana Against the MCF-7 Breast Cancer Cell Lines

2020 ◽  
Vol 10 (3) ◽  
pp. 257-261
Author(s):  
Tati Herlina ◽  
Merlin ◽  
Mohd. Azlan ◽  
Unang Supratman
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Chemical Structure ◽  
Breast Cancer Cell Lines ◽  
Erythrina Poeppigiana ◽  
Structure Activity ◽  
Cancer Line ◽  
Cytotoxic Compounds ◽  
Ic50 Values ◽  
Mcf 7

Background: Erythrina poeppigiana (Leguminosae) is a high-growing plant with an orange flower that is widely distributed in tropical and subtropical countries. This particular plant is widely used in traditional medicine for gynecological complications and the treatment of various diseases. There exists no previous information regarding cytotoxic compounds from this plant. Objective: This research is to isolate cytotoxic compounds from E. poeppigiana. Methods: The isolation step was carried out using a combination of chromatographic techniques to obtain isolated three compounds (1, 2, and 3). Results: The chemical structure of isolated compounds was elucidated by spectroscopic methods and identified as β-erythroidine (1), 8-oxo-β-erythroidine (2), and 8-oxo-α-erythroidine (3). Compounds (1-3) showed cytotoxic activity against MCF-7 breast cancer line with IC50 values of 36.8, 60.8 and 875.4 μM, respectively. Conclusion: Three compounds have been successfully isolated from Erythrina poeppigiana (Leguminosae), showing cytotoxic properties against MCF-7 breast cancer line. Structure-activity relationship studies showed that the presence of enone moiety on compound 1 can reduce its cytotoxic activity towards MCF-7 breast cancer line.

scholarly journals ISOLATION OF CYTOTOXIC CONSTITUENT FROM BIOACTIVITY GUIDED FRACTION OF ALYSICARPUS MONILIFER L. (DC.)

2019 ◽  
pp. 69-77
Author(s):  
PURVI HARISHKUMAR KAKRANI ◽  
HARISH KAKRANI ◽  
MANAN RAVAL
Keyword(s):  
Growth Inhibition ◽  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Betulinic Acid ◽  
Breast Cancer Cells ◽  
Methanolic Extract ◽  
Chloroform Fraction ◽  
Tumor Removal ◽  
Aerial Parts ◽  
Mcf 7

Objective: Alysicarpus monilifer (Family Papilionaceae) has been used in the Indigenous system of medicine in tumor removal. The present study was designed to isolate and identify the constituent responsible for cytotoxic (anti-tumor) effects of the plant Alysicarpus monilifer. Methods: The plant was powdered and extracted to give a methanolic extract. Initially, Hexane, chloroform, ethyl acetate and methanolic fractions of the methanolic extract of the plant were subjected to cytotoxic screening using cell line based assay (MTT assay and NRU assay). The chloroform fraction showed significant cytotoxicity, so it was further subjected to column chromatography, to separate the cytotoxic phytoconstituent. The cell lines selected were breast cancer cells (MCF-7 and MDA-MB-468) and Liver cancer cells (HepG2 and HLE cell). Results were calculated as percentage growth inhibition with respect to untreated (control) cells versus treated cells. Result: A triterpene, Betulinic acid, was isolated from the aerial parts of Alysicarpus monilifer. The cytotoxic activity of the identified compound against MCF-7, MDA-MB-231, HLE and HepG2 cells was also found to be highly significant with 90% growth inhibition. Conclusion: The triterpene was identified to be betulinic acid, to which the cytotoxic activity can be attributed. It is a first report of isolation of betulinic acid from the Alysicarpus species.

scholarly journals Cytotoxic Activity of Essential Oils of Aerial Parts and Ripe Fruits of Echinophora spinosa (Apiaceae)

2013 ◽  
Vol 8 (11) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Daniele Fraternale ◽  
Donata Ricci ◽  
Cinzia Calcabrini ◽  
Michele Guescini ◽  
Chiara Martinelli ◽  
...  
Keyword(s):  
Linear Regression ◽  
Essential Oils ◽  
Cytotoxic Activity ◽  
Central Italy ◽  
U937 Cells ◽  
Cytotoxic Effects ◽  
Regression Curves ◽  
Aerial Parts ◽  
Ic50 Values ◽  
Per Se

The cytotoxic effects of the essential oils obtained from the flowering aerial parts (APO) and ripe fruits (RFO) of Echinophora spinosa L. (Apiaceae) from central Italy toward human U937 promonocytoid cells were studied; the contribution of each of the major constituents to the whole cytotoxic activity of either APO or RFO was also characterized. The major components of APO were β-phellandrene (34.7%), myristicin (16.5%), p-cymene (16.3%), δ3-carene (12.6%), α-pinene (6.7%) and α-phellandrene (6.2%); those of RFO p-cymene (50.2%), myristicin (15.3%), α-pinene (15.1%) and α-phellandrene (8.1%). Both oils tested were toxic to U937 cells, but RFO was much more cytotoxic: indeed, the IC50 values calculated from the linear regression curves of RFO and APO were 14.5 ± 0.85 and 43.4 ± 2.81 μg/mL, respectively. α-Pinene and α-phellandrene were identified as the most toxically relevant constituents: however, they did not completely account for the toxic effects of genuine APO and RFO. Interestingly, we found that p-cymene, although per se devoid of toxicity within the tested range of concentrations, was capable of significantly sensitizing U937 cells to the cytotoxic activity of α-pinene and α-phellandrene, and that specific mixtures of these three terpenes were as toxic as genuine APO and RFO.

scholarly journals LC-MS/MS and Cytotoxic Activity Analysis of Extract and Fraction of Calophyllum soulattri Stembark

2021 ◽  
pp. 356-364
Author(s):  
Muhamad Salman Fareza ◽  
Nur Amalia Choironi ◽  
Sri Sutji Susilowati ◽  
Melina Puspita Rini ◽  
Vyola Festihawa ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Cytotoxic Activity ◽  
Cancer Cell ◽  
Breast Cancer Cell ◽  
Stem Bark ◽  
Positive Control ◽  
Bark Extract ◽  
Ic50 Values ◽  
Stem Bark Extract ◽  
Mcf 7

Calophyllum soulattri (Sulatri), a plant from Clusiaceae family, has been empirically used as traditional medicine. In the present study, C. soulattri stem bark extract and fractions were evaluated for their toxicity against MCF-7 breast cancer cell. The extract and fraction’s chemical content was analyzed using the combination of liquid chromatography with mass spectrometry (LC-MS/MS). The results showed that methanol extract and n-hexane fractions have strong cytotoxic activity with IC50 values 93.6 and 36 µg/mL, respectively. Meanwhile, as the positive control, ethyl acetate and cisplatin fractions have IC50 values 233 and 16.2 µg/mL, respectively. The LC-MS/MS analysis showed that the extract and fractions contained polyporusterone A, poricoic acid D, polyporusterone F, esulentagenin, and 1-acetyl-3-(methoxy-carbonyl)-β-carboline. Therefore, C. soulattri stem bark extract and fractions have potential activity as an anticancer agent that was able to inhibit MCF-7 breast cancer cell growth.  

scholarly journals Encapsulation of Variabilin in Stearic Acid Solid Lipid Nanoparticles Enhances Its Anticancer Activity in Vitro

Molecules ◽  
2020 ◽  
Vol 25 (4) ◽  
pp. 830
Author(s):  
Mookho S. Lerata ◽  
Sarah D’Souza ◽  
Nicole R.S. Sibuyi ◽  
Admire Dube ◽  
Mervin Meyer ◽  
...  
Keyword(s):  
Natural Products ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Lipid Nanoparticles ◽  
Structural Assignment ◽  
Ic50 Values ◽  
Ht 29 ◽  
Mcf 7

The use of natural products as chemotherapeutic agents is well established; however, many of these are associated with undesirable side effects, including high toxicity and instability. Furthermore, the development of drug resistant cancers makes the search for new anticancer lead compounds a priority. In this study, the extraction of an Ircinia sp. sponge resulted in the isolation of an inseparable mixture of (7E,12E,20Z)-variabilin (1) and (7E,12Z,20Z)-variabilin (2) and structural assignment was established using standard 1D and 2D NMR experiments. The cytotoxic activity of the compound against three solid tumour cell lines displayed moderate anti-cancer activity through apoptosis, together with a general lack of selectivity among the cancer cell lines studied. Structural assignment and cytotoxic evaluation of variabilin was complicated and further aggravated by its inherent instability. Variabilin was therefore incorporated into solid lipid nanoparticles (SLNs) and the stability and cytotoxic activity evaluated. Encapsulation of variabilin into SLNs led to a marked improvement in stability of the natural product coupled with enhanced cytotoxic activity, particularly against the prostate (PC-3) cancer cell line, with IC50 values of 87.74 μM vs. 8.94 μM for the variabilin alone and Var-SLN, respectively. Both variabilin and Var-SLN revealed comparable activity to Ceramide against the MCF-7 breast cancer cell line, revealing IC50 values of 34.8, 38.1 and 33.6 μM for variabilin, Var-SLN and Ceramide, respectively. These samples revealed no activity (>100 μM for all) against HT-29 (colon) cell lines and MCF-12 (normal breast) cell lines. Var-SLNs induced 47, 48 and 59% of apoptosis in HT-29, MCF-7 and PC-3 cells, respectively, while variabilin alone revealed 38, 29 and 29% apoptotic cells for HT-29, MCF-7 and PC-3 cell lines, respectively. The encapsulation of natural products into SLNs may provide a promising approach to overcome some of the issues hindering the development of new anticancer drugs from natural products.

scholarly journals Antiprotozoal Germacranolide Sesquiterpene Lactones from Tanacetum sonbolii

Planta Medica ◽  
2019 ◽  
Vol 85 (05) ◽  
pp. 424-430 ◽  
Author(s):  
Sahar Mofidi Tabatabaei ◽  
Samad Nejad Ebrahimi ◽  
Peyman Salehi ◽  
Ali Sonboli ◽  
Marzieh Tabefam ◽  
...  
Keyword(s):  
Trypanosoma Brucei ◽  
High Resolution Mass Spectrometry ◽  
Sesquiterpene Lactones ◽  
Resonance Spectroscopy ◽  
Trypanosoma Brucei Rhodesiense ◽  
L6 Cells ◽  
Aerial Parts ◽  
Phytochemical Investigation ◽  
Ic50 Values

AbstractA phytochemical investigation of extracts from flowers and aerial parts of Tanacetum sonbolii afforded 7 new germacranolide sesquiterpene lactones. The structures were established by a combination of 1- and 2-dimensional nuclear magnetic resonance spectroscopy, high-resolution mass spectrometry, and electronic circular dichroism. The in vitro antiprotozoal activity of the compounds against Trypanosoma brucei rhodesiense and cytotoxicity against rat myoblast (L6) cells were determined. Compounds 4 and 5 showed IC50 values of 5.1 and 10.2 µM and selectivity indices of 3.9 and 4.0, respectively.

Antioxidant, cytotoxic activity and pharmacokinetic studies by SwissAdme, Molinspiration, Osiris and DFT of PhTAD-substituted dihydropyrrole derivatives

2021 ◽  
Vol 17 ◽  
Author(s):  
Arif Ayar ◽  
Masuk Aksahin ◽  
Seda Mesci ◽  
Burak Yazgan ◽  
Melek Gül ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cell Lines ◽  
Heterocyclic Compounds ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Molecular Structures ◽  
Biologically Active ◽  
Pharmacokinetic Studies ◽  
Ic50 Values ◽  
Mcf 7

Background: Pyrrole compounds having a heterocyclic structure are the most researched and biological activities such as antioxidant and anticancer. Objective: Herein is a first effort to study the significance of heterocyclic compounds to include pyrrole and triazolidine-3,5-dion moiety, on the pharmacokinetic, antioxidant activity and cytotoxic activity on MCF-7 and MCF-12A cell lines. Method: The molecular structures of compounds I-XIV were simulated by the theoretical B3LYP/DFT method. Pharmacokinetic studies of PhTAD-substituted heterocyclic compounds (I-XIV) were analyzed to show Lipinski's rules via in-silico methods of Swiss-ADME. The drug likeness calculations were carried out Molinspiration analyses. The some toxicity risk parameter can be quantified using Osiris. Antioxidant activities determined by DPPH, Fe+2 ions chelating and reducing. Cytotoxic activity measured by MTT and RTCA. Results: Compared with the DPPH activity, the metal chelating activity exhibited serious similar antioxidant effects by PhTAD substituted pyrrole compounds. The same compounds showed the highest activity among the two antioxidant activities. The IC50 values of the compounds are in the range of 12 and 290 µM in MCF-7 cell line. In the MTT and RTCA assays, All compounds showed cytotoxic activity, but about half of the fourteen compounds showed high cytotoxicity. IC50 values of the compounds are in the range of 5 and 54 µM for MTT and range of 1.5 and 44 µM for RTCA. Conclusion: Data of the antioxidant and cytotoxic activity of PhTAD-substituted dihydropyrrole-derived compounds in MCF-7 and MCF-12A cell lines confirmed that the compounds are a biologically active compound and is notable for anti-cancer researches.

Three New Cytotoxic Monoterpenoid Bisindole Alkaloids from Tabernaemontana bufalina

Planta Medica ◽  
2018 ◽  
Vol 84 (15) ◽  
pp. 1127-1133 ◽  
Author(s):  
Si-Yuan Zhou ◽  
Ting-Lan Zhou ◽  
Guofu Qiu ◽  
Xiajuan Huan ◽  
Ze-Hong Miao ◽  
...  
Keyword(s):  
Human Cancer ◽  
Spectroscopic Methods ◽  
Human Cancer Cell ◽  
Inhibitory Effects ◽  
Human Cancer Cell Lines ◽  
Human Cancer Cells ◽  
Aerial Parts ◽  
Ic50 Values ◽  
Circular Dichroic ◽  
Mcf 7

AbstractThree new bisindole alkaloids, 3′-(2-oxopropyl)-19,20-dihydrotabernamine (1), 3′-(2-oxopropyl)-ervahanine B (2), 19,20-dihydrovobparicine (3), and 20 known compounds were isolated from the aerial parts of Tabernaemontana bufalina. The structures of these alkaloids were elucidated using spectroscopic methods. The absolute configurations of 1–3 were determined by the circular dichroic exciton chirality method. Compounds 1–23 were screened for their cytotoxicity against two human cancer cell lines, A-549 and MCF-7. Ten compounds (1–3, 10, 14, 16, 17, 19, 22, and 23) exhibited inhibitory effects against the two human cancer cells with IC50 values of 1.19 ~ 6.13 µM.

scholarly journals Cytotoxic Sesquiterpene Lactones of Egyptian Tanacetum santolinoides

2007 ◽  
Vol 2 (8) ◽  
pp. 1934578X0700200 ◽  
Author(s):  
Diaa T. A. Youssef ◽  
Mahmoud A. Ramadan ◽  
Sabrin R. M. Ibrahim ◽  
Jihan M. Badr
Keyword(s):  
Cytotoxic Activity ◽  
Brine Shrimp ◽  
Nmr Spectra ◽  
Methanolic Extract ◽  
Soluble Fraction ◽  
Sesquiterpene Lactones ◽  
Natural Source ◽  
Mass Spectral ◽  
Aerial Parts ◽  
First Time

The chloroform soluble fraction of the methanolic extract of the aerial parts of Tanacetum santolinoides afforded six sesquiterpene lactones. Tanacetolide A (1) was isolated for the first time from a natural source, in addition to five known sesquiterpene lactones. The structures were established on the basis of extensive studies of their 1D and 2D (1H-1H COSY, HMQC, HMBC, HOHAHA and NOESY) NMR spectra and FAB mass spectral determinations. The compounds showed good cytotoxic activity when tested using the brine shrimp bioassay.

scholarly journals Six New Coumarin Glycosides from the Aerial Parts of Gendarussa vulgaris

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1456 ◽  
Author(s):  
Yanjun Sun ◽  
Meiling Gao ◽  
Haojie Chen ◽  
Ruijie Han ◽  
Hui Chen ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Hepg2 Cell ◽  
Mtt Assay ◽  
Spectroscopic Data ◽  
Hplc Analysis ◽  
Cytotoxic Activities ◽  
Aerial Parts ◽  
Structure Activity ◽  
Hepg2 Cell Lines ◽  
Mcf 7

Six new coumarin glycosides, genglycoside A–F (1–6), were isolated from the aerial parts of Gendarussa vulgaris, along with ten known analogues (7–16). Their structures were unambiguously established on the basis of extensive spectroscopic data and HPLC analysis. The cytotoxic activities of all isolated compounds were evaluated by MTT assay. Compound 12 showed the most potent cytotoxicity in Eca-109, MCF-7, and HepG2 cell lines. By the preliminary structure–activity relationships, it was firstly discovered that the glycosylation or esterification at 7,8-dihydroxy or 7-hydroxy drastically reduced the cytotoxic activity of the parent coumarin.

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