scholarly journals New Cytotoxic Cytochalasans from a Plant-Associated Fungus Chaetomium globosum kz-19

Marine Drugs ◽  
2021 ◽  
Vol 19 (8) ◽  
pp. 438
Author(s):  
Tantan Li ◽  
Yun Wang ◽  
Li Li ◽  
Mengyue Tang ◽  
Qinghong Meng ◽  
...  
Keyword(s):  
Hela Cell ◽  
Cell Lines ◽  
Absolute Configuration ◽  
2D Nmr ◽  
Chaetomium Globosum ◽  
Electronic Circular Dichroism ◽  
Spectroscopic Analyses ◽  
Hela Cell Lines ◽  
Ic50 Values ◽  
The Absolute

Four new cytochalasans, phychaetoglobins A–D (1–4), together with twelve known cytochalasans (5–16), were isolated from a mangrove-associated fungus Chaetomium globosum kz-19. The new structures were elucidated on the basis of extensive 1D and 2D NMR, HR ESIMS spectroscopic analyses, and electronic circular dichroism (ECD) calculations. The absolute configuration of 2 was established by application of Mosher’s method. Compounds 4–8 exhibited moderate cytotoxicities against A549 and HeLa cell lines with the IC50 values less than 20 μM.

scholarly journals A New Diterpenoid with a Rearranged Skeleton from Salvia prattii

2017 ◽  
Vol 12 (8) ◽  
pp. 1934578X1701200
Author(s):  
Hiroshi Kawabe ◽  
Riyo Suzuki ◽  
Hiroshi Hirota ◽  
Keiichi Matsuzaki ◽  
Xun Gong ◽  
...  
Keyword(s):  
Circular Dichroism ◽  
Hela Cell ◽  
Cell Lines ◽  
Absolute Configuration ◽  
Electronic Circular Dichroism ◽  
Methyl Group ◽  
Spectroscopic Analyses ◽  
Hela Cell Lines ◽  
The Absolute ◽  
Circular Dichroïsm

A new diterpenoid with a rearranged skeleton, prattinin A (1), was isolated along with five known compounds (2–6) from the roots of Salvia prattii. The structure of 1 bearing a methyl group at the C-5 position was established by extensive spectroscopic analyses and the absolute configuration of 1 was elucidated by comparing the calculated and experimental electronic circular dichroism (ECD) spectra. Compounds 1, 3, 4, and 5 exhibited moderate or weak cytotoxicity against HL-60 and HeLa cell lines.

scholarly journals In-vitro Cytotoxicity and In-silico Insights of the Multi-target Anticancer Candidates from Haplophyllum tuberculatum

2021 ◽  
Vol 4 (3) ◽  
pp. 192-201
Author(s):  
Mosab Yahya Al-Nour ◽  
Ahmed H Arbab ◽  
Mohammad Khalid Parvez ◽  
Arwa Y Mohamed ◽  
Mohammed S Al-Dosari
Keyword(s):  
Hela Cell ◽  
Anticancer Activity ◽  
Cell Lines ◽  
In Vitro Cytotoxicity ◽  
Binding Modes ◽  
Web Servers ◽  
Hela Cell Lines ◽  
Ic50 Values ◽  
Haplophyllum Tuberculatum

This study aimed to investigate the anticancer activity of Haplophyllum tuberculatum(Forsk.) aerial parts ethanol extract and fractions and reveal the potential anticancer targets, binding modes, pharmacokinetics, and toxicity properties of its phytoconstituents. MTT assay was used to investigate the anticancer activity. TargetNet, ChemProt version 2.0, and CLC-Pred web servers were used for virtual screening, and Cresset Flare software was used for molecular docking with the 26 predicted targets. Moreover, pkCSM, swiss ADME, and eMolTox web servers were used to predict pharmacokinetics and safety. Ethanolic extracts of H. tuberculatum on HepG2 and HeLa cell lines showed promising activities with IC50 values 54.12 and 48.1 µg/mL, respectively. Further, ethyl acetate fraction showed the highest cytotoxicity on HepG2 and HeLa cell lines with IC50 values 41.7 and 52.31 µg/mL. Of 70 compounds screened virtually, polygamain, justicidin A, justicidin B, haplotubine, kusunokinin, and flindersine were predicted as safe anticancer drugs candidates. They showed the highest binding scores with targets involved in cell growth, proliferation, survival, migration, tumor suppression, induction of apoptosis, metastasis, and drug resistance. Our findings revealed the potency of H. tuberculatum as a source of anticancer candidates that further studies should support.

scholarly journals Synthesis and HPLC-ECD Study of Cytostatic Condensed O,N-Heterocycles Obtained from 3-Aminoflavanones

Biomolecules ◽  
2020 ◽  
Vol 10 (10) ◽  
pp. 1462
Author(s):  
Ádám Szappanos ◽  
Attila Mándi ◽  
Katalin Gulácsi ◽  
Erika Lisztes ◽  
Balázs István Tóth ◽  
...  
Keyword(s):  
Cell Lines ◽  
Absolute Configuration ◽  
Major Product ◽  
Acid Ceramidase ◽  
Substitution Pattern ◽  
Aryl Group ◽  
Ic50 Values ◽  
The Absolute ◽  
Cis And Trans ◽  
Condensed Heterocycles

Racemic chiral O,N-heterocycles containing 2-arylchroman or 2-aryl-2H-chromene subunit condensed with morpholine, thiazole, or pyrrole moieties at the C-3-C-4 bond were synthesized with various substitution patterns of the aryl group by the cyclization of cis- or trans-3-aminoflavanone analogues. The 3-aminoflavanone precursors were obtained in a Neber rearrangement of oxime tosylates of flavanones, which provided the trans diastereomer as the major product and enabled the isolation of both the cis- and trans-diastereomers. The cis- and trans-aminoflavanones were utilized to prepare three diastereomers of 5-aryl-chromeno[4,3-b][1,4]oxazines. Antiproliferative activity of the condensed heterocycles and precursors was evaluated against A2780 and WM35 cancer cell lines. For a 3-(N-chloroacetylamino)-flavan-4-ol derivative, showing structural analogy with acyclic acid ceramidase inhibitors, 0.15 μM, 3.50 μM, and 6.06 μM IC50 values were measured against A2780, WM35, and HaCat cell lines, and apoptotic mechanism was confirmed. Low micromolar IC50 values down to 2.14 μM were identified for the thiazole- and pyrrole-condensed 2H-chromene derivatives. Enantiomers of the condensed heterocycles were separated by HPLC using chiral stationary phase, HPLC-ECD spectra were recorded and TDDFT-ECD calculations were performed to determine the absolute configuration and solution conformation. Characteristic ECD transitions of the separated enantiomers were correlated with the absolute configuration and effect of substitution pattern on the HPLC elution order was determined.

scholarly journals Chemical Constituents of Tibetan Herbal Medicine Pulicaria insignis and Their in vitro Cytotoxic Activities

2020 ◽  
Vol 15 (2) ◽  
pp. 91-102
Author(s):  
Xinzhu Wang ◽  
Peilei Hou ◽  
Yanbo Qu ◽  
Rizhen Huang ◽  
Yan Feng ◽  
...  
Keyword(s):  
Herbal Medicine ◽  
Cell Lines ◽  
Hepg2 Cells ◽  
Chemical Constituents ◽  
2D Nmr ◽  
Cytotoxic Activities ◽  
Hela Cell Lines ◽  
Ic50 Values ◽  
Hepg2 Cell Lines

One new phenolic derivative, 1-(4',5'-dihydroxy-2'-methylphenyl)-pentane-1,4-dione (1), along with eighteen known compounds including eight sesquiterpenoids (2–9), one triterpenoid (10), one bisdpoxylignan (11), one coumarin (12), and seven flavonoids (13–19) were isolated from the dried inflorescence of Tibetan herbal medicine Pulicaria insignis. The structure of 1 was established by spectroscopic methods, including HRESIMS, IR, 1D, and 2D NMR. All isolates were assessed for the cytotoxic activities against MGC-803, T24, HepG2, and HeLa cell lines using the MTT assay. The results showed that compound 1 displayed moderate cytotoxicity against Hela and HepG2, and compounds 3, 4, 5, 6, and 13 exhibited potential cytotoxic activities against the four cell lines with IC50 values ranging from 3.05 to 14.37 μM. Notably, compound 5 exhibited significant anti-proliferative activities against HepG2 cell lines with the IC50 values of 3.05 ± 0.36 μM. Further bioactivity investigation showed that compound 5 could block HepG2 cells in the G1 phase of the cell cycle, thereby inhibiting the growth of HepG2 cells and inducing apoptosis in HepG2 cells.

scholarly journals A New Peptide Isolated from a Marine Derived Streptomyces bacillaris

2012 ◽  
Vol 7 (2) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Youcai Hu ◽  
John B. MacMillan
Keyword(s):  
Lactic Acid ◽  
Absolute Configuration ◽  
Marine Sediment ◽  
2D Nmr ◽  
Hplc Method ◽  
Base Hydrolysis ◽  
Hydroxy Acids ◽  
Spectroscopic Analyses ◽  
Acid And Base ◽  
The Absolute

A new peptide, L- O-Lac-L-Val-D- O-Hiv-D-Val (1), consisting of D-valine, L-valine, L-lactic acid, and 3-D-hydroxyisovaleric acid, was isolated from the culture of the marine sediment derived Streptomyces bacillaris. The planar structure of compound 1 was assigned by 1D, 2D NMR and mass spectroscopic analyses. Following acid and base hydrolysis, the absolute configuration of the valine residues in 1 were determined by application of the advanced Marfey's method and the absolute configurations of hydroxy acids units were determined by a HPLC method based on Mosher's reagents.

Chemical Constituents, Antioxidant, Anticholinesterase and Antiproliferative Effects of Algerian Pistacia atlantica Desf. Extracts

2020 ◽  
Vol 11 (3) ◽  
pp. 249-256
Author(s):  
Imene Achili ◽  
Amel Amrani ◽  
Chaouki Bensouici ◽  
Fatih Gül ◽  
Muhammed Altun ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Hela Cell ◽  
Cell Lines ◽  
Reducing Power ◽  
Butylated Hydroxytoluene ◽  
Pistacia Atlantica ◽  
Ms Analysis ◽  
Hela Cell Lines ◽  
Ic50 Values ◽  
Tof Ms

Background: Pistacia atlantica Desf. (Anacardiaceae) has various applications for dietetic and medicinal purposes. Objective: The aim of the present study was to evaluate antioxidant, antiproliferative and anticholinesterase activities of different extracts from leaf and stem of Pistacia atlantica Desf. Methods: The antioxidant activity was performed by four methods: DPPH, ABTS, CUPRAC and reducing power assays. Anti-cholinesterase activity was performed against acetylcholinesterase (AChE) and Butyrylcholinesterase (BuChE) enzymes. Antiproliferative assays were investigated against HeLa cell lines using xCELLigence RTCA instrument. The secondary metabolites composition was established by HPLC-TOF/MS analysis. Results: In DPPH, reducing power and in ABTS .+ scavenging activity, all the extracts showed strong inhibitory activity compared to synthetic antioxidants such as butylated hydroxytoluene (BHT) and butylated hydroxyanisole (BHA), in which the activities were almost equal to the two standards. The results were less significant in CUPRAC assay. The ethyl acetate (EtOAc) extracts exhibited the best antioxidant activity in all tests. Moreover, P. atlantica extracts inhibited AChE and BChE activities in a dose-dependent manner. The strongest AChE and BuChE inhibition activities were obtained for EtOAc extract of the stem (IC50 values 15.14±0.74 and 24.01±0.21 μg/mL, respectively) compared to galantamine (IC50 values 6.27±1.15 and 34.75±1.99 μg/mL, respectively). P. atlantica extracts also showed significant antiproleferative activity against HeLa cell lines, the best antiproleferative activity was obtained for the methanol and EtOAc extracts. The observed biological activities can be attributed to the presence of phenolic compounds and flavonoids in the extracts. The HPLC-TOF/MS analysis identified the presence of 22 phytochemicals. Gallic acid and rutin were the main compounds detected. Cichoric, gentisic, vanillic, protocatechuic and rosmarinic acids as well as catechin and quercetin were also present. Conclusion: This study demonstrated good antioxidant, anticholinesterase and antiproliferative activities of P. atlantica extracts, which opens up new possibilities for pharmaceutical and food industries.

scholarly journals Aspidoptoids A–D: Four New Diterpenoids from Aspidopterys obcordata Vine

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 529
Author(s):  
Sun ◽  
Cao ◽  
Xiao ◽  
Zhang ◽  
Wang ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Circular Dichroism ◽  
Absolute Configuration ◽  
2D Nmr ◽  
Cytotoxic Activities ◽  
No Production ◽  
Inhibitory Effects ◽  
Electronic Circular Dichroism ◽  
Spectroscopic Analyses ◽  
Circular Dichroïsm

Four new diterpenoids, named aspidoptoids A–D (1–4), together with two known analogues (5–6) were isolated from Aspidopterys obcordata vine. Aspidoptoids A–B (1–2) are the first examples of phenylethylene-bearing 20-nor-diterpenoids of which aspidoptoid B (2) possesses a rare 3,10-oxybridge. Their structures and absolute configuration were determined by extensive spectroscopic analyses (IR, HRESIMS, 1D and 2D NMR) and electronic circular dichroism (ECD) calculation. In addition, all the isolates were evaluated for their cytotoxic activities and inhibitory effects on the nitric oxide (NO) production.

scholarly journals Absolute Structure Determination and Kv1.5 Ion Channel Inhibition Activities of New Debromoaplysiatoxin Analogues

Marine Drugs ◽  
2021 ◽  
Vol 19 (11) ◽  
pp. 630
Author(s):  
Sicheng Shen ◽  
Weiping Wang ◽  
Zijun Chen ◽  
Huihui Zhang ◽  
Yuchun Yang ◽  
...  
Keyword(s):  
Absolute Configuration ◽  
2D Nmr ◽  
Ring System ◽  
X Ray Diffraction ◽  
Planar Structures ◽  
Channel Inhibition ◽  
Ic50 Values ◽  
The Absolute ◽  
New Treatments ◽  
Fused Ring System

Potassium channel Kv1.5 has been considered a key target for new treatments of atrial tachyarrhythmias, with few side effects. Four new debromoaplysiatoxin analogues with a 6/6/12 fused ring system were isolated from marine cyanobacterium Lyngbya sp. Their planar structures were elucidated by HRESIMS, 1D and 2D NMR. The absolute configuration of oscillatoxin J (1) was determined by single-crystal X-ray diffraction, and the absolute configurations of oscillatoxin K (2), oscillatoxin L (3) and oscillatoxin M (4) were confirmed on the basis of GIAO NMR shift calculation followed by DP4 analysis. The current study confirmed the absolute configuration of the pivotal chiral positions (7S, 9S, 10S, 11R, 12S, 15S, 29R and 30R) at traditional ATXs with 6/12/6 tricyclic ring system. Compound 1, 2 and 4 exhibited blocking activities against Kv1.5 with IC50 values of 2.61 ± 0.91 µM, 3.86 ± 1.03 µM and 3.79 ± 1.01 µM, respectively. However, compound 3 exhibited a minimum effect on Kv1.5 at 10 µM. Furthermore, all of these new debromoaplysiatoxin analogs displayed no apparent activity in a brine shrimp toxicity assay.

Evaluation of Antioxidant, Antimicrobial and Anticancer activity of Thiazole Tagged Isatin Hydrazones

2016 ◽  
Vol 3 (2) ◽  
pp. 4-9 ◽  
Author(s):  
Venkateshwarlu Eggadi ◽  
Umasankar Kulandaivelu ◽  
Sharvana Bhava Bandaru Sheshagiri ◽  
Venkateshwar Rao Jupalli
Keyword(s):  
Antioxidant Activity ◽  
Hela Cell ◽  
Cytotoxic Activity ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Wide Spectrum ◽  
Zone Of Inhibition ◽  
Hela Cell Lines ◽  
Ic50 Values ◽  
Isatin Derivatives

Isatin and its derivatives is versatile lead molecule for potential bioactive agents and shows wide spectrum of activities. In this study, we evaluated antioxidant, antimicrobial and cytotoxic activity of isatin-3-[N2-(2-benzalaminothiazol-4-yl)] hydrazone derivatives using well defined models. Antioxidant activity of the isatin derivatives (Va-Vj) was evaluated by using the 1, 1-diphenyl-2-picryl hydrazine radicals scavenging assay. The antimicrobial activity is evaluated by cup plate method and anticancer activity is evaluated by MTT assay against HBL-100 & HeLa cell lines. Compound Vh (R = 5-Cl, R1 = OH & R2 = OCH3) showed good antioxidant activity with the IC50 of 8.09 M. In addition Ve and Vi have showned most active antibacterial activity against Bacillus subtilis, Staphylococcus aureus and Escherichia coli with a Zone of Inhibition (mm) 20, 16, 18 and 14, 12, 15 on respective organism at 100 g/disc. The compound Vi have produced a good antifungal activity against Aspergillus niger and Clostridium vericulata with the zone of inhibition values of 9 and 8 mm respectively. These isatin derivatives also among the test compounds, compound Vd (R = 5-Cl, R1 = OH & R2 = OCH3) and compound Vh (R = 5-Cl, R1 = OH & R2 = OCH3) have shown nearly equal cytotoxic activity with IC50 values of 246.53 mM and 247.29 mM against HBL-100 cell lines and HeLa cell lines respectively. From the results, isatin derivatives showed powerful antioxidant activity, antimicrobial and anticancer activity may be due to the halogens substituted at 5th position of isatin. The standard drugs used were ampicillin, clotrimazole, cisplatin and ascorbic acid for antibacterial, antifungal, anticancer and antioxidant respectively.

scholarly journals Strepsiamide A-C, New Ceramides from the Marine Sponge Strepsichordaia Lendenfeldi

2008 ◽  
Vol 3 (2) ◽  
pp. 1934578X0800300 ◽  
Author(s):  
Sabrin R. M. Ibrahim ◽  
Gamal A. Mohamed ◽  
Ehab S. Elkhayat ◽  
Yaser G. Gouda ◽  
Peter Proksch
Keyword(s):  
Hela Cell ◽  
Cell Lines ◽  
Marine Sponge ◽  
2D Nmr ◽  
Cytotoxic Activities ◽  
Lipophilic Extract ◽  
Spectrometric Data ◽  
Hela Cell Lines

Investigation of the lipophilic extract of the Indonesian sponge Strepsichordaia lendenfeldi afforded three new ceramides, given the names strepsiamides A–C (1–3). The compounds showed cytotoxic activities against L5187Y and Hela cell lines. All structures were unambiguously established by 1D and 2D NMR spectroscopic and mass (EI-, APCI- and GC-MS) spectrometric data.

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