scholarly journals Mitocanic Di- and Triterpenoid Rhodamine B Conjugates

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5443
Author(s):  
Sophie Hoenke ◽  
Immo Serbian ◽  
Hans-Peter Deigner ◽  
René Csuk
Keyword(s):  
Cytotoxic Activity ◽  
Rhodamine B ◽  
Secondary Amines ◽  
Promising Candidate ◽  
Maslinic Acid ◽  
Biological Studies ◽  
First Results ◽  
Cytotoxic Compounds ◽  
Tumor Selectivity ◽  
Tormentic Acid

The combination of the “correct” triterpenoid, the “correct” spacer and rhodamine B (RhoB) seems to be decisive for the ability of the conjugate to accumulate in mitochondria. So far, several triterpenoid rhodamine B conjugates have been prepared and screened for their cytotoxic activity. To obtain cytotoxic compounds with EC50 values in a low nano-molar range combined with good tumor/non-tumor selectivity, the Rho B unit has to be attached via an amine spacer to the terpenoid skeleton. To avoid spirolactamization, secondary amines have to be used. First results indicate that a homopiperazinyl spacer is superior to a piperazinyl spacer. Hybrids derived from maslinic acid or tormentic acid are superior to those from oleanolic, ursolic, glycyrrhetinic or euscaphic acid. Thus, a tormentic acid-derived RhoB conjugate 32, holding a homopiperazinyl spacer can be regarded, at present, as the most promising candidate for further biological 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 Profil Fraksi Sitotoksik terhadap Sel Murine Leukemia P-388 dari Ekstrak Biji Honje (Etlingera elatior)

2017 ◽  
Vol 3 (1) ◽  
pp. 79-87
Author(s):  
Alfindah Rusanti ◽  
Dede Sukandar ◽  
Tarso Rudiana ◽  
Adawiah Adawiah
Keyword(s):  
Ethyl Acetate ◽  
Cytotoxic Activity ◽  
Mtt Assay ◽  
Chemical Structure ◽  
Ethyl Acetate Extract ◽  
Artemia Salina ◽  
Cytotoxic Compounds ◽  
Murine Leukemia ◽  
Etlingera Elatior

The research characterization of cytotoxic fraction against P-388 leukemia murine cells from the extract honje (Etlingera elatior) seed have been reported. This research lead to isolated and characterization of cytotoxic compounds against P-388 leukemia murine cells from the extract E. elantior seed. The extract of E. elantior seed was maserated by methanol, n-hexane, and ethyl acetate, respectively and estimated their cytotoxic activity against P-388 leukemia murine cell with 3- (4, 5-dimetiltiazol-2-yl) -2,5-difeniltetrazolium bromide (MTT) assay guided toxicity test against of shrimp Artemia salina Leach. Brine shirmp Lethality Test (BSLT) method. The active extracts will be separated by fractionation using column chromatography, radial chromatography, and for analyzing the purity of isolate will estimate by HPLC. The chemical structure of pure isolate will be identified by spectroscopies data UV Vis, FTIR, NMR and MS. The ethyl acetate extract from honje seed have cytotoxic activity by leukemia P-388 cell  with IC50 19.21 µg/mL. The compound toxic as cytotoxicagainst P-388 leukemia murine cells is flavonoid compouds their is resveratrol, lapachol, apigenin, methylated chrysin, 6,2’-dihydroxyflavanone, 3-hydroxy-3,4’-dymethoxyflavone and 4’-hydroxy-5,7-dimethoxyflavanone.DOI: http://dx.doi.org/10.15408/jkv.v0i0.3640

scholarly journals Cytotoxic Activity of Dihydrochalcones Isolated from Corema Album Leaves against HT-29 Colon Cancer Cells

2013 ◽  
Vol 8 (9) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Antonio J. León-González ◽  
Miguel López-Lázaro ◽  
José L. Espartero ◽  
Carmen Martín-Cordero
Keyword(s):  
Cytotoxic Activity ◽  
Reactive Oxygen Species Generation ◽  
Colon Adenocarcinoma ◽  
Human Colon ◽  
2D Nmr ◽  
Positive Control ◽  
H Nmr ◽  
Cytotoxic Compounds ◽  
Ht 29 ◽  
Human Colon Adenocarcinoma

During our search for cytotoxic compounds from Andalusian vascular plants, the ethyl acetate extract from the leaves of Corema album (L.) D. Don (Ericaceae) was selected for its cytotoxic activity against the HT-29 human colon adenocarcinoma cell line. Two dihydrochalcones, 2′,4′-dihydroxydihydrochalcone (1) and 2′-methoxy-4′-hydroxydihydrochalcone (2), have been isolated from the leaves of C. album. Their structural identification was based on 1H NMR and 13C NMR data, including 2D NMR, and mass spectrometry. These compounds were subjected to the sulfhorhodamine B (SRB) cytotoxic assay against human colon adenocarcinoma cells (HT-29). Compounds 1 and 2 showed higher cytotoxicity than the positive control 5-fluorouracil (5-FU); the IC50 values (μM ± SEM) were 1.8 ± 0.4 for compound 1, 8.5 ± 2.1 μM for compound 2, and 8.7 ± 4.0 for 5-FU. The cytotoxic activity of 1 and 2 was reduced in the presence of the antioxidants N-acetylcysteine (NAC) and Mn(III) Tetrakis(1-methyl-4-pyridyl) porphyrin pentachloride (MnTMPyP), therefore suggesting that reactive oxygen species generation participates in the cytotoxic activity of these dihydrochalcones.

scholarly journals A REVIEW ON CYTOTOXIC ACTIVITY OF (GARCINIA COWA ROXB.): POTENTIAL AS AN ANTICANCER

2020 ◽  
Vol 11 (12) ◽  
pp. 1-6
Author(s):  
Nur Syakila ◽  
Aried Eriadi ◽  
Dwi Dinni Aulia Bakhtra ◽  
Ridho Asra
Keyword(s):  
Cancer Therapy ◽  
Cytotoxic Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Death Rate ◽  
Prevention And Treatment ◽  
Cytotoxic Compounds ◽  
Garcinia Cowa ◽  
Made In

Cancer is a disease of abnormal body tissue cells that turn malignant. From the data, it can be seen that new cases and the death rate from cancer continues to increase every year so that efforts are made in the search for new anticancer agents for the prevention and treatment of cancer. There are many natural ingredients that can be used for its benefits, one of which is the Asam Kandis plant (Garcinia cowa Roxb.) This plant is rich in phytochemicals. It can be an important source of natural cytotoxic compounds and has potential as an anticancer. The analysis showed that the extract or compound from the roots, bark, twigs, leaves, and fruit rind of Asam Kandis (Garcinia cowa Roxb.) has good cytotoxic activity and is active against cancer cell lines so that it can help in the development of cancer therapy.

scholarly journals Active Cytotoxic Compounds and Essential Oil from Bougainvillea Alba

2015 ◽  
Vol 15 (1) ◽  
pp. 49
Author(s):  
AbdEl-nabi E. EL-Deeb ◽  
Ibrahim M. Abdel-Aleem ◽  
Samir M. El-Amin ◽  
Laila A. Refahy ◽  
Maha A. El-Shazly
Keyword(s):  
Cytotoxic Activity ◽  
Methyl Palmitate ◽  
Methanol Extract ◽  
Human Tumor ◽  
Tumor Cell Line ◽  
Srb Assay ◽  
Human Tumor Cell ◽  
Oil Fraction ◽  
Oil Fractions ◽  
Cytotoxic Compounds

Chemical analysis of methanol extract of flowers and leaves of Bougainvillea alba led to isolation of four compounds identified as 3’, 4’, 6 - trimethoxy, 5 – hydroxyl 7-prenyl 3-O- (feruloyl (1→2) - rhamnpyranosyl) flavone[1], 3-O β-D-glucopyranosyl oleanolic acid 28-O-β-D-glucopyranosyl (1→3”) β-D-glucopyranosyl (1→3”’) α-L–xylopyrenoside [2], Lepidolide [3], E feruloyl 3-O- Coumaroyl α-L Rhamnopyranoside [4]. In addition, two oil fractions, the major identified components of oil are Elemene, Lanceol , Nerolidol , Methyl palmitate and Abietatriene. Cytotoxic activity of methanol extract of both leaves and flowers of <em>Bougainvillea alba</em>, isolated compounds and oil fractions were determined using the SRB Assay on human tumor cell line (Hepatocyte generation 2, HepG2). The isolated compounds showed cytotoxic activity at LC50 15.2, 17.2, 15.6 and 2.82 μg/ml for compound 1,2, 3 and 4 respectively, while the two oil fraction showed activity at 2.67 μg/ml.

scholarly journals UPLC-ESI-MS/MS Profile and Antioxidant, Cytotoxic, Antidiabetic, and Antiobesity Activities of the Aqueous Extracts of Three Different Hibiscus Species

2020 ◽  
Vol 2020 ◽  
pp. 1-17
Author(s):  
Hanan M. Al-Yousef ◽  
Wafaa H. B. Hassan ◽  
Sahar Abdelaziz ◽  
Musarat Amina ◽  
Rasha Adel ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Aqueous Extract ◽  
Biological Activities ◽  
Biological Effects ◽  
Aqueous Extracts ◽  
Potent Effect ◽  
Esi Ms ◽  
Biological Studies ◽  
Hct 116

The aqueous extracts of Hibiscus calyphyllus (HcA), Hibiscus micranthus (HmA), and Hibiscus deflersii (HdA) growing in Saudi Arabia did not receive enough attention in phytochemical and biological studies. This inspired the authors to investigate the phytochemicals of these extracts for the first time using UPLC-ESI-MS/MS in negative and positive ionization modes. The analysis afforded the tentative identification of 103 compounds including phenolic compounds, flavonoids, and anthocyanins. Moreover, in vitro evaluations of their cytotoxic, antioxidant, antidiabetic, and antiobesity activities were carried out. The results showed that aqueous extract of Hibiscus calyphyllus had the highest activity as an antioxidant agent (SC50 = 111 ± 1.5 μg/mL) compared with ascorbic acid (SC50 = 14.2 ± 0.5 μg/mL). MTT assay was used to evaluate cytotoxic activity compared to cisplatin. Hibiscus deflersii showed the most potent cytotoxic effect against A-549 (human lung carcinoma) with IC50 = 50 ± 5.1 μg/mL, and Hibiscus micranthus showed a close effect with IC50 = 60.4 ± 1.7 μg/mL. Hibiscus micranthus showed the most potent effect on HCT-116 (human colon carcinoma) with IC50 = 56 ± 1.9 μg/mL compared with cisplatin (IC50 = 7.53 ± 3.8 μg/mL). HcA and HdA extracts showed weak cytotoxic activity against A-549 and HCT-116 cell lines compared to the other extracts. Eventually, Hibiscus deflersii showed astonishing antidiabetic (IC50 = 56 ± 1.9 μg/mL) and antiobesity (IC50 = 95.45 ± 1.9 μg/mL) activities using in vitro α-amylase inhibitory assay (compared with acarbose (IC50 = 34.71 ± 0.7 μg/mL)) and pancreatic lipase inhibitory assay (compared with orlistat (IC50 = 23.8 ± 0.7 μg/mL)), respectively. In conclusion, these findings are regarded as the first vision of the phytochemical constituents and biological activities of different Hibiscus aqueous extracts. Hibiscus deflersii aqueous extract might be a hopeful origin of functional constituents with anticancer (on A-549 cell line), antidiabetic, and antiobesity activities. It might be a natural alternative remedy and nutritional policy for diabetes and obesity treatment without negative side effects. Isolation of the bioactive phytochemicals from the aqueous extracts of aerial parts of Hibiscus calyphyllus, Hibiscus micranthus, and Hibiscus deflersii and estimation of their biological effects are recommended in further studies.

scholarly journals Synthesis, Cytotoxic Activity Evaluation and Quantitative Structure-ActivityAnalysis of Substituted 5,8-Dihydroxy-1,4-naphthoquinones and Their O- and S-Glycoside Derivatives Tested against Neuro-2a Cancer Cells

Marine Drugs ◽  
2020 ◽  
Vol 18 (12) ◽  
pp. 602
Author(s):  
Sergey Polonik ◽  
Galina Likhatskaya ◽  
Yuri Sabutski ◽  
Dmitry Pelageev ◽  
Vladimir Denisenko ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Sea Urchins ◽  
Neuroblastoma Cells ◽  
Qsar Model ◽  
Quantitative Structure Activity Relationship ◽  
Quantitative Structure ◽  
Mtt Method ◽  
Structure Activity ◽  
Cytotoxic Compounds ◽  
Qsar Models

Based on 6,7-substituted 2,5,8-trihydroxy-1,4-naphtoquinones (1,4-NQs) derived from sea urchins, five new acetyl-O-glucosides of NQs were prepared. A new method of conjugation of per-O-acetylated 1-mercaptosaccharides with 2-hydroxy-1,4-NQs through a methylene spacer was developed. Methylation of 2-hydroxy group of quinone core of acetylthiomethylglycosides by diazomethane and deacetylation of sugar moiety led to 28 new thiomethylglycosidesof 2-hydroxy- and 2-methoxy-1,4-NQs. The cytotoxic activity of starting 1,4-NQs (13 compounds) and their O- and S-glycoside derivatives (37 compounds) was determined by the MTT method against Neuro-2a mouse neuroblastoma cells. Cytotoxic compounds with EC50 = 2.7–87.0 μM and nontoxic compounds with EC50 > 100 μM were found. Acetylated O- and S-glycosides 1,4-NQs were the most potent, with EC50 = 2.7–16.4 μM. Methylation of the 2-OH group innaphthoquinone core led to a sharp increase in the cytotoxic activity of acetylated thioglycosidesof NQs, which was partially retained for their deacetylated derivatives. Thiomethylglycosides of 2-hydroxy-1,4-NQs with OH and MeO groups in quinone core at positions 6 and 7, resprectively formed a nontoxic set of compounds with EC50 > 100 μM. A quantitative structure-activity relationship (QSAR) model of cytotoxic activity of 22 1,4-NQ derivatives was constructed and tested. Descriptors related to the cytotoxic activity of new 1,4-NQ derivatives were determined. The QSAR model is good at predicting the activity of 1,4-NQ derivatives which are unused for QSAR models and nontoxic derivatives.

Pump/Probe Spectroscopy by Asynchronous Optical Sampling

1987 ◽  
Vol 41 (1) ◽  
pp. 2-4 ◽  
Author(s):  
Paul A. Elzinga ◽  
Fred E. Lytle ◽  
Yanan Jian ◽  
Galen B. King ◽  
Normand M. Laurendeau
Keyword(s):  
Rhodamine B ◽  
Repetition Rate ◽  
Beat Frequency ◽  
Laser System ◽  
Probe Laser ◽  
Optical Delay Line ◽  
Pump Probe ◽  
Optical Sampling ◽  
First Results ◽  
Probe Spectroscopy

We report the first results from a new pump/probe technique called asynchronous optical sampling (ASOPS). The method employs a mode-locked, frequency-doubled Nd:YAG laser operating at a repetition rate of 81.5970000 MHz as the pump laser, and a synchronously pumped dye laser (R6G) operating at a repetition rate of 81.5870000 MHz as the probe laser system. The 10-kHz beat frequency produces a repetitive relative phase walk-out of the pump and probe pulses which replaces the optical delay line used in conventional instruments. Studies of rhodamine B in methanol demonstrate that the instrument response is proportional to pump power, probe power, and sample absorptance. The fluorescence lifetime of 4 × 10−5 M rhodamine B is determined to be 2.3 ns.

scholarly journals Benzo[c]phenanthrene derivatives: Synthesis, optical properties and cytotoxic activity

2016 ◽  
Vol 12 (9) ◽  
pp. 4404-4412 ◽  
Author(s):  
Habiba Guédouar ◽  
Faouzi Aloui ◽  
Bechir Ben hassine
Keyword(s):  
Optical Properties ◽  
Cytotoxic Activity ◽  
Visible Region ◽  
Secondary Amines ◽  
Primary Amines ◽  
Resonance Spectroscopy ◽  
Heck Coupling ◽  
Visible Absorption ◽  
Tetracyclic System ◽  
New Compounds

A new benzo[c]phenanthrene ketone has been synthesized through Heck coupling and oxidative photocyclization. The optical properties of the target tetracyclic system were also investigated by UV-visible absorption and photoluminescence spectroscopy and an emission in the visible region was observed. The tetracyclic ketone has been reacted with primary amines in the presence of Lewis acid followed by NaBH4 reduction to provide new polyaromatic secondary amines in good yields and purity. All the synthesized new compounds were identified and characterized through a combination of nuclear magnetic resonance spectroscopy and mass spectrometric methods. The cytotoxic activity of all pure benzo[c]phenanthrene derivatives has been evaluated against Hep-2 cell line using (MTT) colori­metric assay.

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