scholarly journals Acorenone C: A New Spiro-Sesquiterpene from a Mangrove-Associated Fungus, Pseudofusicoccum sp. J003

2021 ◽  
Vol 9 ◽  
Author(s):  
Shujie Jia ◽  
Xiangdong Su ◽  
Wensi Yan ◽  
Meifang Wu ◽  
Yichuang Wu ◽  
...  
Keyword(s):  
Biological Activities ◽  
Human Tumor ◽  
Antimicrobial Activities ◽  
Culture Broth ◽  
Cytotoxic Activities ◽  
No Production ◽  
Inhibition Rate ◽  
2D Nmr Spectroscopy ◽  
Mangrove Species

Mangrove-derived endophytes are rich in bioactive secondary metabolites with a variety of biological activities. Recently, a fungus Pseudofusicoccum sp. J003 was first isolated by our research group from mangrove species Sonneratia apetala Buch.-Ham. The subsequent chemical investigation of the methanol extract of the culture broth of this strain has led to the isolation of a new sesquiterpenoid named acorenone C (1), two alkaloids (2–3), four phenolic compounds (4–7), and four steroid derivatives (8–11). The new structure of 1 was established by extensive spectroscopic analysis, including 1D, 2D NMR spectroscopy, and HRESIMS. Its absolute configuration was elucidated by experimental ECD and ECD calculation. The in vitro AChE inhibitory, anti-inflammatory, and cytotoxic activities of the selected compounds were evaluated. The results showed that compound 1 showed mild AChE inhibitory activity, with an inhibition rate of 23.34% at the concentration of 50 μM. Compound 9 exerted a significant inhibitory effect against nitric oxide (NO) production in LPS-stimulated RAW 264.7 mouse macrophages, with an inhibition rate of 72.89% at the concentration of 25 μM, better than that of positive control L-NMMA. Compound 9 also displayed obvious inhibition effects on the growth of two human tumor cell lines, HL-60 and SW480 (inhibition rates 98.68 ± 0.97% and 60.40 ± 4.51%, respectively). The antimicrobial activities of the compounds (1–11) against Escherichia coli, Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa were also tested; however, none of them showed antimicrobial activities.

scholarly journals Cytotoxic Activity-Guided Isolation from Achillea monocephala, and Biological Activities of its Different Extracts

2020 ◽  
Vol 8 (1) ◽  
pp. 7-14
Author(s):  
Turgut Taşkın ◽  
Eray M. Güler ◽  
Şeyda Şentürk ◽  
Damla D. Çelik ◽  
Turan Arabacı ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Cytotoxic Activity ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Cytotoxic Activities ◽  
Active Compounds ◽  
Antioxidant Power ◽  
Biological Potential

Background: The genus Achillea is one of the most important genus of the Asteraceae family and many species of Achillea are used in traditional medicine to treat several ailments. Aim: The aim of the current research was to evaluate in vitro cytotoxic activities of n-hexan, chloroform, ethyl acetate and methanol extracts and to isolate the active compounds from the extract showing the strongest cytotoxic activity. In addition to this, it was aimed to evaluate the biological activities (cytotoxic, antioxidant, anti-urease, anticholinesterase, antimicrobial) of different extracts and active compounds from Achillea monocephala. Methods and Materials: The in vitro antioxidant, cytotoxic, anti-urease, anticholinesterase and antimicrobial activities of different extracts from A. monocephala aerial parts were examined. The structures of the active compounds were determined by NMR techniques, UV, IR and LC-MS/MS analysis and their biological potential was examined. Results: The chloroform extract showed strong and selective cytotoxic activity on the cancer cell lines (MDA-MB-231, MCF-7). Besides, this extract exhibited stronger antimicrobial activity than other extracts. Therefore, through activity-guided procedures, luteolin, naringenin and 8-hydroxy-salvigenin compounds were isolated from this extract. The methanol extract showed stronger antioxidant (DPPH, ABTS, CUPRAC) and anticholinesterase activity than other extracts. The n-hexan extract exhibited the highest anti-urease activity. In this study, it was determined that the isolated compounds had a strong biological activity. Naringenin compound had stronger ABTS radical cation scavenging and ferric reducing/antioxidant power, cytotoxic and antimicrobial activity than other compounds. 8-hydroxy-salvigenin compound showed the highest urease and acetylcholinestease enzyme inhibition. Conclusion: The results of this study suggest that the extracts and isolated compounds from the A. monocephala may be used as antioxidant, cytotoxic, anti-urease, anticholinesterase and antimicrobial agents in the future.

Synthesis and Cytotoxicity of New Mannich Bases of 6-[3-(3,4,5-Trimetoxyphenyl)-2- propenoyl]-2(3H)-Benzoxazolone

2020 ◽  
Vol 17 (4) ◽  
pp. 512-517
Author(s):  
Ognyan Ivanov Petrov ◽  
Yordanka Borisova Ivanova ◽  
Mariana Stefanova Gerova ◽  
Georgi Tsvetanov Momekov
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Biological Activities ◽  
Human Tumor ◽  
Mannich Bases ◽  
In Vitro Cytotoxicity ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

Background: Chemotherapy is one of the mainstays of cancer treatment, despite the serious side effects of the clinically available anticancer drugs. In recent years increasing attention has been directed towards novel agents with improved efficacy and selectivity. Compounds with chalcone backbone have been reported to possess various biological activities such as anticancer, antimicrobial, anti-inflammatory, analgesic, antioxidant, etc. It was reported that aminomethylation of hydroxy chalcones to the corresponding Mannich bases increased their cytotoxicity. In this context, our interest has been focused on the design and synthesis of the so-called multi-target molecules, containing two or more pharmacophore fragments. Methods: A series of Mannich bases were synthesized by the reaction between 6-[3-(3,4,5- trimethoxyphenyl)-2-propenoyl]-2(3Н)-benzoxazolone, formaldehyde, and a secondary amine. The structures of the compounds were confirmed by elemental analysis, IR and NMR spectra. The new Mannich bases were evaluated for their in vitro cytotoxicity against a panel of human tumor cell lines, including BV-173, SKW-3, K-562, HL-60, HD-MY-Z and MDA-MB-231. The effects of selected compounds on the cellular levels of glutathione (GSH) were determined. Results: The new compounds 4a-e exhibited concentration-dependent cytotoxic effects at micromolar concentrations in MTT-dye reduction assay against a panel of human tumor cell lines, similar to those of starting chalcone 3. The tested agents led to concentration - dependent depletion of cellular GSH levels, whereby the effects of the chalcone prototype 3 and its Mannich base-derivatives were comparable. Conclusion: The highest chemosensitivity to the tested compounds was observed in BV- 173followed by SKW-3 and HL-60 cell lines.

Synthesis, Antimicrobial Evaluation and Docking Study of Novel Thiosemicarbazone clubbed with 1,2,3-Triazoles

2020 ◽  
Vol 16 ◽  
Author(s):  
Adinath D. Badar ◽  
Shubham M. Sulakhe ◽  
Mahesh B. Muluk ◽  
Naziya N. M. A. Rehman ◽  
Prashant P. Dixit ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Biological Activities ◽  
Dna Gyrase ◽  
Docking Study ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Molecular Docking Study ◽  
Triazole Derivatives ◽  
Antibacterial And Antifungal

Background: Thiosemicarbazone, 1,2,3-triazole and their derivatives received great pharmaceutical importance due to their prominent biological activities. In the present study, the molecular hybrid thiosemicarbazone-1,2,3-triazoles derivatives were synthesized and screened for their antimicrobial activities. Methods: A series of thiosemicarbazone clubbed with 1,2,3-triazole derivatives were synthesized via click chemistry approach in good yields. The structures of synthesized compounds were assigned by their spectral data. The in vitro antimicrobial activity was performed by the agar well diffusion method. A molecular docking study was performed to identify the possible mode of action of synthesized derivatives. Results: The compounds 5d, 5h, 5i and 5k have exhibited excellent antimicrobial activities against both antibacterial and antifungal pathogens. The active thiosemicarbazone-1,2,3-triazole derivatives have shown excellent binding affinity towards DNA gyrase. Conclusion: The molecular hybrid thiosemicarbazone-1,2,3-triazole derivatives were synthesized. The newly synthesized compounds were evaluated for their antimicrobial activities. Few of the thiosemicarbazone-1,2,3-triazoles derivatives have exhibited good antimicrobial activities. They have been shown excellent binding affinity towards DNA gyrase.

Influence of New Synthetic Xanthones on the Proliferation and Migration Potential of Cancer Cell Lines In Vitro

2020 ◽  
Vol 19 (16) ◽  
pp. 1949-1965 ◽  
Author(s):  
Natalia Szkaradek ◽  
Daniel Sypniewski ◽  
Dorota Żelaszczyk ◽  
Sabina Gałka ◽  
Paulina Borzdziłowska ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Higher Plants ◽  
Biological Activities ◽  
Human Tumor ◽  
Plant Metabolites ◽  
Xtt Assay ◽  
Treatment Protocols

Background: Natural plant metabolites and their semisynthetic derivatives have been used for years in cancer therapy. Xanthones are oxygenated heterocyclic compounds produced as secondary metabolites by higher plants, fungi or lichens. Xanthone core may serve as a template in the synthesis of many derivatives that have broad biological activities. Objective: This study synthesized a series of 17 new xanthones, and their anticancer potential was also evaluated. Methods: The anticancer potential was evaluated in vitro using a highly invasive T24 cancer cell line. Direct cytotoxic effects of the xanthones were established by IC50 estimation based on XTT assay. Results: 5 compounds of the total 17 showed significant cytotoxicity toward the studied cancer cultures and were submitted to further detailed analysis, including studies examining their influence on gelatinase A and B expression, as well as on the cancer cells migration and adhesion to an extracellular matrix. These analyses were carried out on five human tumor cell lines: A2780 (ovarian cancer), A549 (lung cancer), HeLa (cervical cancer), Hep G2 (liver cancer), and T24 (urinary bladder cancer). All the compounds, especially 4, showed promising anticancer activity: they exhibited significant cytotoxicity towards all the evaluated cell lines, including MCF-7 breast cancer, and hindered migration-motility activity of cancer cells demonstrating more potent activity than α-mangostin which served as a reference xanthone. Conclusion: These results suggest that our xanthone derivatives may be further analyzed in order to include them in cancer treatment protocols.

scholarly journals In Vitro Evaluation of the Potential Pharmacological Activity and Molecular Targets of New Benzimidazole-Based Schiff Base Metal Complexes

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 728
Author(s):  
Alberto Aragón-Muriel ◽  
Yamil Liscano ◽  
Yulieth Upegui ◽  
Sara M. Robledo ◽  
María Teresa Ramírez-Apan ◽  
...  
Keyword(s):  
Schiff Base ◽  
Molecular Docking ◽  
Lanthanide Complexes ◽  
Human Tumor ◽  
Model Membranes ◽  
Leishmania Braziliensis ◽  
Cytotoxic Activities ◽  
Schiff Base Ligands ◽  
Major Interest

Metal-based drugs, including lanthanide complexes, have been extremely effective in clinical treatments against various diseases and have raised major interest in recent decades. Hence, in this work, a series of lanthanum (III) and cerium (III) complexes, including Schiff base ligands derived from (1H-benzimidazol-2-yl)aniline, salicylaldehyde, and 2,4-dihydroxybenzaldehyde were synthesized and characterized using different spectroscopic methods. Besides their cytotoxic activities, they were examined in human U-937 cells, primate kidney non-cancerous COS-7, and six other, different human tumor cell lines: U251, PC-3, K562, HCT-15, MCF-7, and SK-LU-1. In addition, the synthesized compounds were screened for in vitro antiparasitic activity against Leishmania braziliensis, Plasmodium falciparum, and Trypanosoma cruzi. Additionally, antibacterial activities were examined against two Gram-positive strains (S. aureus ATCC® 25923, L. monocytogenes ATCC® 19115) and two Gram-negative strains (E. coli ATCC® 25922, P. aeruginosa ATCC® 27583) using the microdilution method. The lanthanide complexes generally exhibited increased biological activity compared with the free Schiff base ligands. Interactions between the tested compounds and model membranes were examined using differential scanning calorimetry (DSC), and interactions with calf thymus DNA (CT-DNA) were investigated by ultraviolet (UV) absorption. Molecular docking studies were performed using leishmanin (1LML), cruzain (4PI3), P. falciparum alpha-tubulin (GenBank sequence CAA34101 [453 aa]), and S.aureus penicillin-binding protein 2a (PBP2A; 5M18) as the protein receptors. The results lead to the conclusion that the synthesized compounds exhibited a notable effect on model membranes imitating mammalian and bacterial membranes and rolled along DNA strands through groove interactions. Interactions between the compounds and studied receptors depended primarily on ligand structures in the molecular docking study.

Synthesis and Characterization of New Palladium(II) Complexes with Ligands Derived from Furan-2-carbaldehyde and Benzaldehyde Thiosemicarbazone and their in vitro Cytotoxic Activities against Various Human Tumor Cell Lines

2010 ◽  
Vol 65 (10) ◽  
pp. 1271-1278 ◽  
Author(s):  
Wilfredo Hernández ◽  
Juan Paz ◽  
Fernando Carrasco ◽  
Abraham Vaisberg ◽  
Jorge Manzur ◽  
...  
Keyword(s):  
Tumor Cell ◽  
Cell Lines ◽  
Human Tumor ◽  
Myelogenous Leukemia ◽  
Cytotoxic Activities ◽  
Spectroscopic Techniques ◽  
Tumor Cell Lines ◽  
Human Tumor Cell ◽  
Human Tumor Cell Lines

With the ligands 4-phenyl-1-(furan-2-carbaldehyde)thiosemicarbazone, HTSC1, (1), 4-phenyl-1- (5´-phenyl-furan-2-carbaldehyde)thiosemicarbazone, HTSC2 (2), o-methoxy-benzaldehydethiosemicarbazone, HTSC3 (3), and o-cyano-benzaldehydethiosemicarbazone, HTSC4 (4), the corresponding palladium(II) complexes, Pd(TSC1)2 (5), Pd(TSC2)2 (6), Pd(TSC3)2 (7), and Pd(TSC4)2 (8) were synthesized and characterized by elemental analysis and spectroscopic techniques. The crystal structure of Pd(TSC3)2 (7) was determined by single-crystal X-ray diffraction. Complex 7 shows a squareplanar geometry, where two deprotonated ligands are coordinated to the PdII center through the nitrogen and sulfur atoms in a trans arrangement. In vitro antitumor studies against different human tumor cell lines have revealed that the palladium(II) complexes 5- 8 are more cytotoxic (IC50 values in the range of 0.21 - 3.79 μM) than their corresponding ligands (1 - 4) (> 60 μM). These results indicate that the antiproliferative activity is enhanced when thiosemicarbazone ligands are coordinated to the metal. Among the studied palladium(II) complexes, 8 exhibits high antitumor activity on K562 chronic myelogenous leukemia cells with a low value of the inhibitory concentration (IC50 = 0.21 μM).

scholarly journals Phytochemical Characterization and Evaluation of Biological Activities of Egyptian Carob Pods (Ceratonia siliqua L.) Aqueous Extract: In Vitro Study

Plants ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 2626
Author(s):  
Wael Sobhy Darwish ◽  
Abada El Sayed Khadr ◽  
Maher Abd El Naby Kamel ◽  
Mabrouk A. Abd Eldaim ◽  
Ibrahim El Tantawy El Sayed ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Phytochemical Analysis ◽  
Type I ◽  
Hypotonic Solution ◽  
Ceratonia Siliqua

Ceratonia siliqua (Carob) is an evergreen Mediterranean tree, and carob pods are potentially nutritive and have medicinal value. The present study was carried out to estimate the possible biological activities of phytochemical-characterized carob pod aqueous extract (CPAE). The phytochemical contents of CPAE were determined by using colorimetric methods and HPLC. In addition, the free radical scavenging properties and anti-diabetic, anti-hemolytic, and antimicrobial activities were estimated by using standardized in vitro protocols. The phytochemical analysis revealed that CPAE was rich in polyphenols, flavonoids, and alkaloids, where it contained a significant amount of gallic acid, catechin, and protocatechuic acid. Furthermore, CPAE exhibited strong antioxidant activity where it prevented the formation of 2, 2-Diphenyl-1-picryl hydrazyl, hydroxyl, and nitric oxide free radicals. Additionally, it had a potent inhibitory effect against digestive enzymes (amylase, maltase, sucrase, and lactase). Moreover, CPAE exhibited anti-Staph aureus, anti-Escherichia coli, anti-Candida albicans, and anti-herpes simplex type I virus (HSV-I). Finally, CPAE protected the erythrocyte membrane from hypotonic solution-induced hemolysis. Altogether, CPAE could be regarded as an interesting source of biologically active antioxidant, anti-diabetic, and antimicrobial preparation for a potential application in pharmaceutical and food supplement fields.

In Vitro Screening for Cytotoxic, Anti-bacterial, Anti-HIV1-RT Activities and Chemical Constituents of Croton fluviatilis, Croton acutifolius, and Croton thorelii

2021 ◽  
Vol 11 ◽  
Author(s):  
Charina Worarat ◽  
Wilart Pompimon ◽  
Phansuang Udomputtimekakul ◽  
Sukee Sukdee ◽  
Punchavee Sombutsiri ◽  
...  
Keyword(s):  
Ethyl Acetate ◽  
Ethyl Acetate Extract ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Bacterial Activity ◽  
Cytotoxic Activities ◽  
Separation And Purification ◽  
Crude Extracts ◽  
Cytotoxicity Activities

Background: Although the chemical constituents and biological activities of a large number of plants in the Croton genus have been studied, there are still recently discovered plants to be investigated. Objective: 1. To investigate the anti-bacterial, anti-HIV1-RT, and cytotoxicity activities of crude extracts from these plants. 2. To investigate the chemical constituents of Croton fluviatilis, Croton acutifolius, and Croton thorelii. Method: The anti-bacterial, anti-HIV1-RT, and cytotoxicity of the three plants were evaluated by standard techniques. Extraction, separation, and purification of extracts from the three plants were undertaken. Results: The ethyl acetate extract of C. fluviatilis showed low anti-bacterial activity against E. aerogenes, E. coli 0157: H7, and P. mirabilis, together with the ethyl acetate extract of C. acutifolius displayed low anti-bacterial activity against E. aerogenes, while all the crude extracts of C. thorelii were inactive. The ethyl acetate extracts of C. thorelii, and C. fluviatilis showed strong inhibited HIV1-RT, whereas the ethyl acetate extract of C. acutifolius, and the hexane extract of C. fluviatilis displayed moderate inhibited HIV1-RT. Cytotoxic properties of three Croton plants were specific to KKU-M213, MDA-MB-231, A-549, and MMNK-1. Especially, the ethyl acetate extract of C. acutifolius exhibited strong cytotoxic activities against MDA-MB-231, A-549, and MMNK-1. Furthermore, the ethyl acetate extract of C. thorelii showed high cytotoxic activities against KKU-M213, and MDA-MB-231. Compounds 1, and 4 were found in C. fluviatilis. Compounds 2 and 4 were also found in C. acutifolius. Moreover, compound 3 was only found in C. thorelii. Conclusion: The present study revealed that the three Croton species are good sources of flavonoid compounds and further investigation of the chemical constituents from these plants may prove to be fruitful to discover more active compounds to be tested as potential medicines.

scholarly journals Four New Pterosins from Pteris cretica and Their Cytotoxic Activities

Molecules ◽  
2019 ◽  
Vol 24 (15) ◽  
pp. 2767
Author(s):  
Jian Lu ◽  
Caiying Peng ◽  
Shuang Cheng ◽  
Jianqun Liu ◽  
Qinge Ma ◽  
...  
Keyword(s):  
Human Tumor ◽  
2D Nmr ◽  
Cytotoxic Activities ◽  
Aerial Parts ◽  
Pteris Cretica ◽  
Phytochemical Investigation ◽  
Hct 116 ◽  
Hct 116 Cells ◽  
New Compounds

Phytochemical investigation of the aerial parts of Pteris cretica led to the isolation and elucidation of nine pterosins, including four new pterosins, creticolacton A (1), 13-hydroxy-2(R),3(R)-pterosin L (2), creticoside A (3), and spelosin 3-O-β-d-glucopyranoside (4), together with five known pterosins 5–9. Their structures were identified mainly on the basis of 1D and 2D NMR spectral data, ESI-MS and literature comparisons. Compounds 1 and 3 were new type of petrosins with a six membered ring between C-14 and C-15. The new compounds were tested in vitro for their cytotoxic activities against four human tumor cell lines (SH-SY5Y, SGC-7901, HCT-116, Lovo). Results showed that compounds 1 and 2 exhibited cytotoxic activity against HCT-116 cells with IC50 value of 22.4 μM and 15.8 μM, respectively.

Essential Oil Composition, Antimicrobial and Cytotoxic Activities of Two Endemic Stachys Cretica Subspecies (Lamiaceae) from Turkey

2010 ◽  
Vol 5 (9) ◽  
pp. 1934578X1000500 ◽  
Author(s):  
Tuba Şerbetçi ◽  
Betül Demirci ◽  
Çağrla Bozkurt Güzel ◽  
Şükran Kültür ◽  
Mine Ergüven ◽  
...  
Keyword(s):  
Essential Oil ◽  
Cell Line ◽  
Human Tumor ◽  
Antimicrobial Activities ◽  
Light Petroleum ◽  
Cytotoxic Activities ◽  
Chemical Compositions ◽  
Oil Composition ◽  
Bacterial Strains ◽  
Ishikawa Cell

The chemical compositions of the water-distilled essential oil of Stachys cretica ssp. lesbiaca Rech. fil. and S. cretica ssp. trapezuntica Rech. fil. were determined by GC and GC–MS. Altogether 63 compounds were identified. The sesquiterpene hydrocarbon, germacrene D (20.3% and 12.9% respectively) was the main component identified in both oils. Furthermore, ethanol, light petroleum, dichloromethane, ethyl acetate and n-butanol extracts prepared from the aerial parts of the plants were tested for their antimicrobial activities against six bacterial strains and the yeast Candida albicans. The extracts exhibited no antibacterial activity, but the light petroleum and n-butanolic fractions showed low antifungal activities. Crude ethanolic extracts of the two subspecies were tested for their ability to inhibit the growth of HL-60 and Ishikawa human tumor cell lines. The IC50 values were 100 μg/mL for the HL-60 cell line and 200 μg/mL for the Ishikawa cell line.

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