scholarly journals Novel Efficient Bioprocessing of Marine Chitins into Active Anticancer Prodigiosin

Marine Drugs ◽  
2019 ◽  
Vol 18 (1) ◽  
pp. 15 ◽  
Author(s):  
Van Bon Nguyen ◽  
Shan-Ping Chen ◽  
Thi Hanh Nguyen ◽  
Minh Trung Nguyen ◽  
Thi Thanh Thao Tran ◽  
...  
Keyword(s):  
Serratia Marcescens ◽  
Bioactive Compound ◽  
Potential Candidate ◽  
Hep G2 ◽  
Anticancer Activities ◽  
Anti Cancer ◽  
Initial Ph ◽  
Ic50 Values ◽  
First Time ◽  
Mcf 7

Marine chitins (MC) have been utilized for the production of vast array of bioactive products, including chitooligomers, chitinase, chitosanase, antioxidants, anti-NO, and antidiabetic compounds. The aim of this study is the bioprocessing of MC into a potent anticancer compound, prodigiosin (PG), via microbial fermentation. This bioactive compound was produced by Serratia marcescens TKU011 with the highest yield of 4.62 mg/mL at the optimal conditions of liquid medium with initial pH of 5.65–6.15 containing 1% α-chitin, 0.6% casein, 0.05% K2HPO4, and 0.1% CaSO4. Fermentation was kept at 25 °C for 2 d. Notably, α-chitin was newly investigated as the major potential material for PG production via fermentation; the salt CaSO4 was also found to play the key role in the enhancement of PG yield of Serratia marcescens fermentation for the first time. PG was qualified and identified based on specific UV, MALDI-TOF MS analysis. In the biological activity tests, purified PG demonstrated potent anticancer activities against A549, Hep G2, MCF-7, and WiDr with the IC50 values of 0.06, 0.04, 0.04, and 0.2 µg/mL, respectively. Mytomycin C, a commercial anti-cancer compound was also tested for comparison purpose, showing weaker activity with the IC50 values of 0.11, 0.1, 0.14, and 0.15 µg/mL, respectively. As such, purified PG displayed higher 2.75-fold, 1.67-fold, and 3.25-fold efficacy than Mytomycin C against MCF-7, A549, and Hep G2, respectively. The results suggest that marine chitins are valuable sources for production of prodigiosin, a potential candidate for cancer drugs.

scholarly journals Anticancer Activities of Chemical Constituents from Leaves and Twigs of Mitrephora winitii

2021 ◽  
Vol 21 (3) ◽  
pp. 699
Author(s):  
Sukee Sukdee ◽  
Puttinan Meepowpan ◽  
Narong Nantasaen ◽  
Siriporn Jungsuttiwong ◽  
Sarinya Hadsadee ◽  
...  
Keyword(s):  
Cancer Cell ◽  
Chemical Constituents ◽  
Cancer Cell Line ◽  
2D Nmr ◽  
Anticancer Activities ◽  
Chromatographic Separations ◽  
Chemical Structures ◽  
Anti Cancer ◽  
First Time ◽  
Mcf 7

The genus Mitrephora has been investigated and its anti-inflammatory, anti-bacterial and anti-parasitical activities were examined along with its potential as an anti-cancer cell line and inhibitor for platelet aggregation. In this work, air-dried leaves and twigs of M. winitii were grounded and extracted with n-hexane, ethyl acetate and methanol, respectively. Chromatographic separations of these extracts led to the isolation of three known compounds and one new compound (compound 2). The chemical structures of these were identified using spectroscopic investigation of 1D- and 2D-NMR and the resulting data confirmed these as stigmasterol (1), (3,4-dimethoxyphenyl)(5-(3,4-dimethoxyphenyl)-4-(hydroxymethyl)tetrahydrofuran-3-yl)methanol (2), diayangambin (3), and methyl-L-inositol (4). The chemical constituents were reported the first time in M. winitii. Compound 2 showed anti-cancer cell lines with ED50 13.07 µg/mL against KB cells and then was tested for cytotoxicity against MCF-7 cells with ED50 11.77 µg/mL.

scholarly journals Cytotoxic and Anti-Inflammatory Activities of Dihydroisocoumarin and Xanthone Derivatives from Garcinia picrorhiza

Molecules ◽  
2021 ◽  
Vol 26 (21) ◽  
pp. 6626
Author(s):  
Edwin R. Sukandar ◽  
Sutin Kaennakam ◽  
Pia Raab ◽  
Xuehong Nöst ◽  
Kitiya Rassamee ◽  
...  
Keyword(s):  
2D Nmr ◽  
Stem Bark ◽  
No Production ◽  
Hep G2 ◽  
Pharmacological Studies ◽  
Ic50 Values ◽  
Hela S3 ◽  
Anti Inflammatory ◽  
First Time ◽  
Mcf 7

Garcinia picrorhiza, a woody plant native to Sulawesi and Maluku Islands, Indonesia, has been traditionally used as a wound healing ointment. In our continuous search for bioactive compounds from this plant, 15 phenolic compounds were isolated from its stem bark, including a previously undescribed dihydroisocoumarin, 2′-hydroxyannulatomarin, and two undescribed furanoxanthones, gerontoxanthone C hydrate and 3′-hydroxycalothorexanthone. The structures of the new metabolites were elucidated on the basis of spectroscopic analysis, including 1D and 2D NMR and HRESIMS. Gerontoxanthone C hydrate possessed cytotoxicity against four cancer cells (KB, HeLa S3, MCF-7, and Hep G2) with IC50 values ranging from 5.6 to 7.5 µM. Investigation on the anti-inflammatory activities showed that 3′-hydroxycalothorexanthone inhibited NO production in RAW 264.7 and BV-2 cell lines with IC50 values of 16.4 and 13.8 µM, respectively, whereas only (−)-annulatomarin possessed inhibition activity on COX-2 enzyme over 10% at 20 µM. This work describes the presence of 3,4-dihydroisocoumarin structures with a phenyl ring substituent at C-3, which are reported the first time in genus Garcinia. These findings also suggest the potential of furanxanthone derivatives as cytotoxic and anti-inflammatory agents for further pharmacological studies.

scholarly journals Synthesis, Characterization and Cytotoxic Activity of New 2,9-BIS(2-Fluorobenzyl)-β-Carbolinium Bromide as a potential compound for anti-cancer agents

2019 ◽  
Vol 10 (SPL1) ◽  
Author(s):  
Mazlin Mohideen ◽  
Wan Mohamad Hafiz Wan Hamid ◽  
Nur Damia Zaidi ◽  
Adibah Akmal ◽  
Nuramanina Othman ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Synthesis Method ◽  
Positive Control ◽  
Crystallographic Analysis ◽  
Hep G2 ◽  
Anticancer Activities ◽  
One Pot ◽  
Recent Emergence ◽  
Anti Cancer ◽  
Ic50 Values

β-carbolines constitute a vast group of indole alkaloids and exhibit various biochemical effects and pharmacological properties. With the recent emergence of β-carboline in the field of cancer, this study investigated the synthesis, characterization, and potential anticancer activity of β-carboline derivative. An efficient method was described for the synthesis of new 2,9-bis(2-fluorobenzyl)-β-carbolinium bromide from L-tryptophan through the Pictet-Spengler reaction and oxidation of K2Cr2O7 by a sequential one-pot synthesis method then followed by N2, N9-benzylated using 2-fluorobezyl with good yield (92%). The structure of the compound was established by 1H-, 13C-NMR, and mass spectroscopy (ESI-MS) as well as single-crystal X-ray crystallographic analysis. The compound was tested for anticancer activity against Hela, HT-29, Hep-G2, and K562 cell lines by using MTT assay. 2,9-bis(2-fluorobenzyl)-β-carbolinium bromide exerted promising anticancer activities with IC50 values ranging between 0.97 to 6.00 μM as compared to doxorubicin which was employed as the positive control (0.77 μM). The results suggested that new, 2,9-bis(2-fluorobenzyl)-β-carbolinium bromide could potentially be developed as a novel anticancer agent.

scholarly journals Synthesis, DFT Calculations, Antiproliferative, Bactericidal Activity and Molecular Docking of Novel Mixed-Ligand Salen/8-Hydroxyquinoline Metal Complexes

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4725
Author(s):  
Badriah Saad Al-Farhan ◽  
Maram T. Basha ◽  
Laila H. Abdel Rahman ◽  
Ahmed M. M. El-Saghier ◽  
Doaa Abou El-Ezz ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Molecular Docking ◽  
Metal Complexes ◽  
Wide Spectrum ◽  
Mixed Ligand ◽  
Molecular Formula ◽  
Hep G2 ◽  
Anticancer Activities ◽  
Azomethine Group ◽  
Ic50 Values

Despite the common use of salens and hydroxyquinolines as therapeutic and bioactive agents, their metal complexes are still under development. Here, we report the synthesis of novel mixed-ligand metal complexes (MSQ) comprising salen (S), derived from (2,2′-{1,2-ethanediylbis[nitrilo(E) methylylidene]}diphenol, and 8-hydroxyquinoline (Q) with Co(II), Ni(II), Cd(II), Al(III), and La(III). The structures and properties of these MSQ metal complexes were investigated using molar conductivity, melting point, FTIR, 1H NMR, 13C NMR, UV–VIS, mass spectra, and thermal analysis. Quantum calculation, analytical, and experimental measurements seem to suggest the proposed structure of the compounds and its uncommon monobasic tridentate binding mode of salen via phenolic oxygen, azomethine group, and the NH group. The general molecular formula of MSQ metal complexes is [M(S)(Q)(H2O)] for M (II) = Co, Ni, and Cd or [M(S)(Q)(Cl)] and [M(S)(Q)(H2O)]Cl for M(III) = La and Al, respectively. Importantly, all prepared metal complexes were evaluated for their antimicrobial and anticancer activities. The metal complexes exhibited high cytotoxic potency against human breast cancer (MDA-MB231) and liver cancer (Hep-G2) cell lines. Among all MSQ metal complexes, CoSQ and LaSQ produced IC50 values (1.49 and 1.95 µM, respectively) that were comparable to that of cisplatin (1.55 µM) against Hep-G2 cells, whereas CdSQ and LaSQ had best potency against MDA-MB231 with IC50 values of 1.95 and 1.43 µM, respectively. Furthermore, the metal complexes exhibited significant antimicrobial activities against a wide spectrum of both Gram-positive and -negative bacterial and fungal strains. The antibacterial and antifungal efficacies for the MSQ metal complexes, the free S and Q ligands, and the standard drugs gentamycin and ketoconazole decreased in the order AlSQ > LaSQ > CdSQ > gentamycin > NiSQ > CoSQ > Q > S for antibacterial activity, and for antifungal activity followed the trend of LaSQ > AlSQ > CdSQ > ketoconazole > NiSQ > CoSQ > Q > S. Molecular docking studies were performed to investigate the binding of the synthesized compounds with breast cancer oxidoreductase (PDB ID: 3HB5). According to the data obtained, the most probable coordination geometry is octahedral for all the metal complexes. The molecular and electronic structures of the metal complexes were optimized theoretically, and their quantum chemical parameters were calculated. PXRD results for the Cd(II) and La(III) metal complexes indicated that they were crystalline in nature.

scholarly journals Labdane and Abietane Diterpenoids from Juniperus oblonga and Their Cytotoxic Activity

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1561 ◽  
Author(s):  
Qiao ◽  
Khutsishvili ◽  
Alizade ◽  
Atha ◽  
Borris
Keyword(s):  
Cell Lines ◽  
Human Tumor ◽  
2D Nmr ◽  
Human Tumor Cell Lines ◽  
Abietane Diterpenoids ◽  
Whole Plant ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
First Time ◽  
Mcf 7

A phytochemical investigation of the whole plant of Juniperus oblonga led to the isolationof one previously undescribed labdane diterpenoid, (4R,5S,9S,10R)‐13‐des‐ethyl‐13‐oxolabda‐8(17),11E‐dien‐19‐oic acid (1), together with nine known diterpenoids (2–3, 6–12), two lignans (4, 5),and a coumarin (13). The structures of all the compounds were elucidated on the basis ofspectrometric data, primarily one‐dimensional (1D)‐ and two‐dimensional (2D)‐NMR and massspectrometry. Electronic circular dichroism (ECD) calculations determined the absoluteconfiguration of 1. In addition, the isolated compounds were evaluated for their cytotoxic activityagainst three human tumor cell lines (HepG2, MCF‐7, and HeLa). 6,12‐Dihydroxyabieta‐5,8,11,13‐tetraen‐7‐one (6) showed moderate cytotoxicity against all three cell lines with IC50 values rangingfrom 24.41 μM to 58.39 μM and trilobinone (10) showed weaker activity with IC50 values rangingfrom 56.93 μM to 79.98 μM. None of the isolated diterpenoids have been previously reported fromJuniperus oblonga, and five compounds are here reported from the genus Juniperus for the first time.

Do herbal drinks augment the cytotoxic effect against different cancer cells? Are they potent stimulators of innate and acquired immunity?

2020 ◽  
Vol 38 (15_suppl) ◽  
pp. e21657-e21657 ◽  
Author(s):  
Israa Adnan ◽  
Wamidh Talib
Keyword(s):  
Middle East ◽  
Cell Lines ◽  
Biological Activities ◽  
Neutral Red ◽  
Acquired Immunity ◽  
Anticancer Activities ◽  
Anti Cancer ◽  
Wild Thyme ◽  
Phagocytosis Activity ◽  
Mcf 7

e21657 Background: The herbal drinks are highly prevalent in the Middle East and are consumed in large quantities as daily drinks. Few studies have evaluated the biological activities of the herbal drinks produced from some plants.The current study aims to evaluate the anticancer and immunomodulatory activities of five herbal drinks consumed in the Middle East. These drinks are Palestinian Zhourat, Lebanese Zhourat, Lemon and Ginger combination, Wild Thyme, and Marjoram. Methods: The selected herbal drinks as concentrated water extracts were tested separately for: A. Anti-cancer effect on the cell lines (MCF-7, MDA-MB231, HCT-116, A549, and Vero-normal cells) by assessing: - Antiproliferation activities using MTT assay. Apoptosis (using the caspase-3 assay) and vascular endothelial growth factor (VEGF) expression (using ELISA kit) for the most potent antiproliferative extract. B. Immunomodulatory effect by evaluating: - Splenocytes proliferation using the mitogen proliferation assay. Phagocytosis activity using the nitro blue tetrazolium assay. - Pinocytosis function using the neutral red method. Results: The Lemon and Ginger combination was the most potent against MDA-MB231, MCF-7 and A549l cell lines with IC50 3.5,4, 6.5mg/ml, respectively. Lemon and Ginger combination and Wild thyme separately showed high apoptosis induction and angiogenesis suppression on the MDA-MB231cell line at concentrations 3.5 and 4.4 mg/ml for both extracts, respectively. Wild thyme was the most potent stimulant lymphocyte proliferation (with index 4.7), and Marjoram has the highest percentage (314.4%) in phagocytosis activity, while moderate stimulation by Zhourat was noted. Lemon and Ginger combination, Wild thyme, Marjoram, and the Lebanese herbal drink "Zhourat" were the most active extracts in stimulating pinocytosis with absorbance value 0.5745,0.4645,0.461,0.4575 nm, respectively. Meanwhile, the Palestinian herbal drink "Zhourat" had a moderate effect. Conclusions: The consumption ofthe mentioned herbal drinks has various Anti-cancer and immunomodulatory effects. Lemon and ginger combination exhibits the most potent anticancer activities. Wild thyme and marjoram are potent stimulators of innate and acquired immunity. The result achieved in this study is very optimistic and encouraging to be considered for further clinical trials.

scholarly journals Chemical constituents and cytotoxicity of Aspidistra letreae

2020 ◽  
Vol 129 (1B) ◽  
pp. 31-39
Author(s):  
Duc Viet Ho ◽  
Hanh Nhu Thi Hoang ◽  
Khue Minh Vo ◽  
Anh Tuan Le ◽  
Hoai Thi Nguyen
Keyword(s):  
Human Cancer ◽  
Chemical Constituents ◽  
Hep G2 ◽  
Human Cancer Cell Lines ◽  
Phytochemical Investigation ◽  
Ic50 Values ◽  
Reported Data ◽  
Whole Plants ◽  
First Time

A phytochemical investigation of whole Aspidistra letreae plants led to the isolation of 2H-chromen-2-one (1), α-tocopherol (2), (E)-phytol (3), asparenydiol (4) and (25S)-spirost-1β,3α,5β-triol (5). Their structures were determined on the basis of NMR spectral evidences and in comparison with the reported data. Of these, asparenydiol (4) was isolated from the genus Aspidistra for the first time. This is also the first report on the separation and structural determination of (25S)-spirost-1β,3α,5β-triol (5) as a pure compound. The methanol extract from the whole plants of Aspidistra letreae exhibits moderate cytotoxicity against the LU-1, HeLa, MDA-MB-231, Hep-G2, and MKN-7 human cancer cell lines with IC50 values ranging from 52.58 ± 3.65 to 64.78 ± 4.89 μg/mL.

SYNTHESIS, CHARACTERISATION, ANTIOXIDANT AND ANTICANCER EVALUATION OF NOVEL FLAVONE-4-OXIMES

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (11) ◽  
pp. 7-14
Author(s):  
B. S Jayashree ◽  
◽  
Gurushyam Sri ◽  
A Pai
Keyword(s):  
Antioxidant Activity ◽  
Cell Lines ◽  
Scavenging Activity ◽  
Hep G2 ◽  
Dpph Method ◽  
Anti Cancer ◽  
Aldehyde Derivative ◽  
Cancer Activity ◽  
Better Than ◽  
Mcf 7

A series of novel flavone-4-oximes were synthesized by the oximation of substituted flavones. The synthesized compounds were characterized by various spectrochemical methods including IR, MS and NMR spectroscopy. Out of the 14 test compounds screened for their antioxidant activity, compounds such as JGS-VI (a N,N dimethyl benzaldehyde derivative) and JGS-VII (a 3,4 dimethoxy benzaldehyde derivative) exhibited antioxidant activity comparable to that of ascorbic acid and quercetin as standards following DPPH method. Compounds such as JGS-II (a p-fluoro benzaldehyde derivative), JGS-IV (a p-methyl benzaldehyde derivative) and JGS-V (a thiophene-2-aldehyde derivative) exhibited antioxidant activity among all the test compounds screened against ABTS. However, none of them showed any significant scavenging activity against nitric oxide scavenging assay in the concentration range of 200 μM-25μM. Further, anti-cancer potency for all the test compounds were evaluated by MTT assay against two different cell lines namely MCF-7 and Hep-G2. Compounds such as JGS-I (a p-chloro benzaldehyde derivative), JGS-II (a p-fluoro benzaldehyde derivative), JGS-IV, JGS-V (a thiophene -2-aldehyde derivative), JGS-VI and JGS-IX (a 3,4 chloro benzaldehyde derivative) exhibited activity better than the rest of the test compounds tested against MCF-7 cell lines. Compounds such as JGS-VI, JGS-VII, JGS-VIII (a p-bromo benzaldehyde derivative) and JGS-IX exhibited anti-cancer activity better than other test compounds tested against Hep-G2 cell lines. Thus, a few of the synthesized test compounds could become promising anti-cancer agents.

scholarly journals Lensoside Aβ as an Adjuvant to the Anti-Glioma Potential of Sorafenib

Cancers ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 2637
Author(s):  
Aleksandra Maciejczyk ◽  
Justyna Kapral-Piotrowska ◽  
Joanna Sumorek-Wiadro ◽  
Adrian Zając ◽  
Ewa Grela ◽  
...  
Keyword(s):  
Cell Death ◽  
Caspase 3 ◽  
Kinase Inhibitor ◽  
Morphological Changes ◽  
Potential Candidate ◽  
Membrane Structures ◽  
Raf Kinase ◽  
Programmed Death ◽  
Anti Cancer ◽  
First Time

Aim: The anti-glioma effect of lensoside Aβ alone and in combination with sorafenib (pro-survival Raf kinase inhibitor) was evaluated for the first time in terms of programmed cell death induction in anaplastic astrocytoma and glioblastoma multiforme cell lines as an experimental model. Apoptosis, autophagy, and necrosis were identified microscopically (fluorescence and scanning microscopes) and confirmed by flow cytometry (mitochondrial membrane potential MMP and cell death). The expression of apoptotic (caspase 3) and autophagic markers (beclin 1) as well as Raf kinase were estimated by immunoblotting. The FTIR method was used to determine the interaction of the studied drugs with lipid and protein groups within cells, while the modes of drug action within the cells were assessed with the FLIM technique. Results: Lensoside Aβ itself does not exhibit anti-glioma activity but significantly enhances the anti-cancer potential of sorafenib, initiating mainly apoptosis of up to 90% of cells. It was correlated with an increased level of active caspase 3, a reduced MMP value, and a lower level of Raf kinase. The interaction with membrane structures led to morphological changes typical of programmed death. Conclusions: Our results indicate that lensoside Aβ plays an important role as an adjuvant in chemotherapy with sorafenib and may be a potential candidate in anti-glioma combination therapy.

scholarly journals Chemical and biological characterization of sulfated chitosan oligomer as heparin mimics

2021 ◽  
pp. 096739112110350
Author(s):  
Samet Kocabay ◽  
Mehmet Refik Bahar ◽  
Suat Tekin ◽  
Recep Akkaya ◽  
Birnur Akkaya
Keyword(s):  
Potential Candidate ◽  
Biological Characterization ◽  
Scanning Calorimetry ◽  
Chitosan Oligomer ◽  
Bond Stretching ◽  
Ft Ir ◽  
Spectrum Band ◽  
First Time ◽  
Mcf 7

In the present study, chitosan oligomer was modified to sulfated chitosan oligomer (ShCsO) to mimic heparin. Its chemical structure was determined by infrared spectroscopy (FT-IR), X-ray diffractometry (XRD), differential scanning calorimetry (DSC), and thermogravimetric analysis. The results showed that the FT-IR spectrum band at 799 cm−1 corresponds to C–O–S and that at 1212 cm−1 corresponds to S=O bond stretching, which prove that the sulfate groups are incorporated into chitosan oligomer successfully. The antimicrobial activity of ShCsO against to Bacillus subtilis in 1% concentration was 89.1 ± 1.7% . The IC50 (μg/ml) of ShCsO was 67.75, 56.07, 85.47, and 84.68 for A2780, MCF-7, DU-145, and HepG2, respectively. The results show that this newly synthesized material is a potential candidate to heparin-like chitosan derivatives. According to the literature, it was the first time that chitosan oligomer was modified to mimic heparin.

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