scholarly journals Thyme as a perspective antioxidant agent with antidiabetic and antitumor potential

2021 ◽  
Author(s):  
Mariana Oalđe Pavlović ◽  
Tanja Lunić ◽  
Marija Mandić ◽  
Ana Alimpić Aradski ◽  
Katarina Šavikin ◽  
...  
2020 ◽  
Vol 44 (15) ◽  
pp. 5762-5773 ◽  
Author(s):  
Tatiyana V. Serebryanskaya ◽  
Mikhail A. Kinzhalov ◽  
Vladimir Bakulev ◽  
Georgii Alekseev ◽  
Anastasiya Andreeva ◽  
...  

Water soluble Pd(ii) and Pt(ii)–ADC species synthesized via the metal-mediated coupling of isocyanides and 1,2-diaminobenzene have demonstrated antitumor potential.


2020 ◽  
Vol 16 (5) ◽  
pp. 833-838
Author(s):  
Jalal Moludi ◽  
Mohammad Alizadeh ◽  
Godarz Chehri ◽  
Hamed Jafari-Vayghyan ◽  
Elaheh Foroumandi ◽  
...  

Background: Coronary artery bypass graft (CABG) is associated with oxidative stress and tissue damage. Vitamin C, as an antioxidant agent, has an important role in attenuating the oxidative stress damage and might have cardio-protective effects after CABG. We aimed to evaluate the probable roles of vitamin C supplementation in cardiac biomarkers after CABG. Methods:: In this randomized control trial, 122 patients undergoing CABG were randomly assigned to the intervention (n=54) and control group (n=68) and received vitamin C (2 g intravenously) or placebo, respectively. The surgical methods of the patients in the two groups were identical. The primary efficacy endpoint of this trial is the difference in the levels of CK-MB, Troponin and Total Antioxidant Capacity (TAC) were measured at study entry and 24 hrs after surgery between the two groups. Results:: The two groups were not significantly different in terms of basic variables. Within-group comparison showed significant rises in the level of troponin (P < 0.001) and CK-MB (P < 0.001) over time. However, between-group comparison showed no significant difference between the two groups in terms of CK-MB (P=0.826) and troponin (P=0.821). As a whole, the correlation between cardiac enzymes and surgical characteristic was not seen. Conclusion:: The results showed that pretreatment with vitamin C could not reduce cardiac marker following CABG. After the intervention, TAC did not differ between and within the intervention and the control groups. Pretreatment with vitamin C as an antioxidant agent could not reduce ischemicreperfusion resulting in CABG.


Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1764
Author(s):  
Anna Kaps ◽  
Paweł Gwiazdoń ◽  
Ewa Chodurek

The search for safe and effective anticancer therapies is one of the major challenges of the 21st century. The ineffective treatment of cancers, classified as civilization diseases, contributes to a decreased quality of life, health loss, and premature mortality in oncological patients. Many natural phytochemicals have anticancer potential. Pentacyclic triterpenoids, characterized by six- and five-membered ring structures, are one of the largest class of natural metabolites sourced from the plant kingdom. Among the known natural triterpenoids, we can distinguish lupane-, oleanane-, and ursane-types. Pentacyclic triterpenoids are known to have many biological activities, e.g., anti-inflammatory, antibacterial, hepatoprotective, immunomodulatory, antioxidant, and anticancer properties. Unfortunately, they are also characterized by poor water solubility and, hence, low bioavailability. These pharmacological properties may be improved by both introducing some modifications to their native structures and developing novel delivery systems based on the latest nanotechnological achievements. The development of nanocarrier-delivery systems is aimed at increasing the transport capacity of bioactive compounds by enhancing their solubility, bioavailability, stability in vivo and ensuring tumor-targeting while their toxicity and risk of side effects are significantly reduced. Nanocarriers may vary in sizes, constituents, shapes, and surface properties, all of which affect the ultimate efficacy and safety of a given anticancer therapy, as presented in this review. The presented results demonstrate the high antitumor potential of systems for delivery of pentacyclic triterpenoids.


Antioxidants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 875
Author(s):  
Katerina Spyridopoulou ◽  
Tamara Aravidou ◽  
Evangeli Lampri ◽  
Eleni Effraimidou ◽  
Aglaia Pappa ◽  
...  

Lippia citriodora is a flowering plant cultivated for its lemon-scented leaves and used in folk medicine for the preparation of tea for the alleviation of symptoms of gastrointestinal disorders, cold, and asthma. The oil extracted from the plant leaves was shown to possess antioxidant potential and to exert antiproliferative activity against breast cancer. The aim of this study was to further investigate potential antitumor effects of L. citriodora oil (LCO) on breast cancer. The in vitro antiproliferative activity of LCO was examined against murine DA3 breast cancer cells by the sulforhodamine B assay. We further explored the LCO’s pro-apoptotic potential with the Annexin-PI method. The LCO’s anti-migratory effect was assessed by the wound-healing assay. LCO was found to inhibit the growth of DA3 cells in vitro, attenuate their migration, and induce apoptosis. Finally, oral administration of LCO for 14 days in mice inhibited by 55% the size of developing tumors in the DA3 murine tumor model. Noteworthy, in the tumor tissue of LCO-treated mice the apoptotic marker cleaved caspase-3 was elevated, while a reduced protein expression of survivin was observed. These results indicate that LCO, as a source of bioactive compounds, has a very interesting nutraceutical potential.


Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3672
Author(s):  
Yulin Ren ◽  
Sijin Wu ◽  
Joanna E. Burdette ◽  
Xiaolin Cheng ◽  
A. Douglas Kinghorn

Digoxin is a cardiac glycoside long used to treat congestive heart failure and found recently to show antitumor potential. The hydroxy groups connected at the C-12, C-14, and C-3′a positions; the C-17 unsaturated lactone unit; the conformation of the steroid core; and the C-3 saccharide moiety have been demonstrated as being important for digoxin’s cytotoxicity and interactions with Na+/K+-ATPase. The docking profiles for digoxin and several derivatives and Na+/K+-ATPase were investigated; an additional small Asn130 side pocket was revealed, which could be useful in the design of novel digoxin-like antitumor agents. In addition, the docking scores for digoxin and its derivatives were found to correlate with their cytotoxicity, indicating a potential use of these values in the prediction of the cancer cell cytotoxicity of other cardiac glycosides. Moreover, in these docking studies, digoxin was found to bind to FIH-1 and NF-κB but not HDAC, IAP, and PI3K, suggesting that this cardiac glycoside directly targets FIH-1, Na+/K+-ATPase, and NF-κB to mediate its antitumor potential. Differentially, digoxigenin, the aglycon of digoxin, binds to HDAC and PI3K, but not FIH-1, IAP, Na+/K+-ATPase, and NF-κB, indicating that this compound may target tumor autophagy and metabolism to mediate its antitumor propensity.


2020 ◽  
Vol 32 (3) ◽  
pp. 580-586
Author(s):  
Ranjit V. Gadhave ◽  
Bhanudas S. Kuchekar

A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.


2021 ◽  
Author(s):  
Baoen He ◽  
Zuchang Zhu ◽  
Fenglian Chen ◽  
Rong Zhang ◽  
Weiqiang Chen ◽  
...  

2020 ◽  
Vol 18 (1) ◽  
pp. 175-184 ◽  
Author(s):  
Ramzi A. Mothana ◽  
Fahd A. Nasr ◽  
Jamal M. Khaled ◽  
Omar M. Noman ◽  
Nael Abutaha ◽  
...  

AbstractThe essential oil of Ducrosia ismaelis Asch. (Apiaceae) that grows wild in Saudi Arabia was investigated utilizing gas chromatography (GC), and gas chromatography-mass spectrometry. Fifty constituents were characterized, representing 96.1% of the total oil. The D. ismaelis essential oil (DIEO) was distinguished by a high composition of oxygenated monoterpenes (51.6%). Decanal (40.6%), α-pinene (15.1%) and dodecanal (13.7%) were the fundamental components. Additionally, DIEO was evaluated for its cytotoxic, antibacterial, antifungal and antioxidant activities. DIEO revealed a great cytotoxic effectiveness against the tested cancer cell lines with IC50 values between 66.2 and 137.3 μg/mL particularly against MCF-7 cancer cells. Furthermore, the induction of apoptosis against MCF-7 cells has been asserted using staining assay (annexin VFITC and/or propidium iodide (PI) dyes) and flow cytometry technique. The DIEO possessed a strong antimicrobial activity against Gram-positive bacterial and fungal strains with MIC-values between 0.07 and 0.31 mg/ml. The values of MBC or MFC were almost once higher than those of MIC’s. Moreover, the β-carotene-bleaching and DPPH free radical-scavenging tests showed that DIEO had a moderate activity (68%) as an antioxidant agent in decolouring of the β-carotene at 1.0 mg/mL and a moderate radical scavenging for DPPH (66 and 72%) at 0.50 and 1.0 mg/mL.


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