A biphosphinic ruthenium complex with potent anti-bacterial and anti-cancer activity

2017 ◽  
Vol 41 (21) ◽  
pp. 13085-13095 ◽  
Author(s):  
José Marcos da Silveira Carvalho ◽  
Andressa Hellen de Morais Batista ◽  
Nádia Accioly Pinto Nogueira ◽  
Alda Karine Medeiros Holanda ◽  
Jackson Rodrigues de Sousa ◽  
...  

Photorelease of CO and moderate binding to DNA did not seem to be essential features for potent biological activities.

2014 ◽  
pp. 98-101
Author(s):  
Thi Bich Hien Le ◽  
Viet Duc Ho ◽  
Thi Hoai Nguyen

Nowadays, cancer treatment has been a big challenge to healthcare systems. Most of clinical anti-cancer therapies are toxic and cause adverse effects to human body. Therefore, current trend in science is seeking and screening of natural compounds which possess antineoplastic activities to utilize in treatment. Uvaria L. - Annonaceae includes approximately 175 species spreading over tropical areas of Asia, Australia, Africa and America. Studies on chemical compositions and pharmacological effects of Uvaria showed that several compound classes in this genus such as alkaloid, flavonoid, cyclohexen derivaties, acetogenin, steroid, terpenoid, etc. indicate considerable biological activities, for example anti-tumor, anti-cancer, antibacterial, antifungal, antioxidant, etc. Specifically, anti-cancer activity of fractions of extract and pure isolated compounds stands out for cytotoxicity against many cancer cell lines. This study provides an overview of anti-cancer activity of Uvaria and suggests a potential for further studies on seeking and developing novel anti-cancer compounds. Key words: Anti-cancer, Uvaria.


Biomedicines ◽  
2019 ◽  
Vol 7 (4) ◽  
pp. 96 ◽  
Author(s):  
Subramani Paranthaman Balasubramani ◽  
Mohammad Atikur Rahman ◽  
Sheikh Mehboob Basha

Muscadine grape is rich in stilbenes, which include resveratrol, piceid, viniferin, pterostilbene, etc. Resveratrol has been extensively studied for its biological activities; however, the synergistic effect of stilbene compounds in berry extracts is poorly understood. The aim of this study was to evaluate the anti-cancer activity of stilbene-rich muscadine berry extract and pure resveratrol. Stilbenes were extracted from ripened berries of muscadine grape cultivars, Pineapple, and Southern Home. HPLC analysis was performed to determine quantity of stilbenes. The extracts were tested for their cytotoxic activity against A549 (lung carcinoma cells), triple negative breast cancer (HCC-1806) and HepG2 (human liver cancer) cells. The stilbene-rich extracts of the muscadine berry extracts showed cytotoxic activity against all of the cells tested. The extracts at 1 μg/mL induced death in 50–80% of cells by 72 h of treatment. About 50 μg/mL of resveratrol was required to induce a similar response in the cells. Further, modulation of genes involved in tumor progression and suppression was significantly (p < 0.0005) higher with the HepG2 cells treated with stilbene-rich berry extracts than the pure resveratrol. This shows that the synergistic activity of stilbenes present in muscadine grape berries have more potent anti-cancer activity than the resveratrol alone.


Author(s):  
Zang Li ◽  
Hao Xu ◽  
Chao Huang ◽  
Cunqin Wang ◽  
Rongbin Wang ◽  
...  

Background: Plants with triterpenoid compounds in nature have various biological activities and are reported in many scientific works of literature. Triterpenoids are compounds that draw the attention of scientists because of their wide source, wide variety, high medicinal value, and anti-tumor properties. However, a lack of approach to understand their chemical structures has limited the fundamental comprehension of these compounds in cancer cell therapy. Objective: To seek anti-cancer activity of the structures of triterpenoid compounds and their derivatives, we summarized a number of plants and their derivatives that are a source of potential novel therapeutic anti-cancer agents. Methods: This work focuses on relevant 1036 patents and references that detail the structure of organic compounds and derivatives for the treatment of tumors. Result: Compared to tetracyclic triterpenoid, pentacyclic triterpenoid has contributed more to improve the autophagic signaling pathways of cancer cells. Conclusion: The heterogenous skeleton structure of triterpenoids impaired the programmed cell death signaling pathway in various cancers


Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 577
Author(s):  
Hamdoon A. Mohammed ◽  
Riaz A. Khan ◽  
Atef A. Abdel-Hafez ◽  
Marwa Abdel-Aziz ◽  
Eman Ahmed ◽  
...  

Zygophyllum coccineum, an edible halophytic plant, is part of the traditional medicine chest in the Mediterranean region for symptomatic relief of diabetes, hypertension, wound healing, burns, infections, and rheumatoid arthritis pain. The current study aimed to characterize Z. coccineum phytoconstituents, and the evaluations of the anti-microbial-biofilm, and anti-cancers bioactivities of the plant’s mother liquor, i.e., aqueous-ethanolic extract, and its subsequent fractions. The in silico receptors interaction feasibility of Z. coccineum major constituents with Staph GyraseB, and human topoisomerase-IIβ (h-TOP-IIβ) were conducted to confirm the plant’s anti-microbial and anti-cancer biological activities. Thirty-eight secondary metabolites of flavonoids, stilbene, phenolic acids, alkaloids, and coumarin classes identified by LC-ESI-TOF-MS spectrometric analysis, and tiliroside (kaempferol-3-O-(6′′′′-p-coumaroyl)-glucoside, 19.8%), zygophyloside-F (12.78%), zygophyloside-G (9.67%), and isorhamnetin-3-O-glucoside (4.75%) were identified as the major constituents. A superior biofilm obliteration activity established the minimum biofilm eradication concentration (MBEC) for the chloroform fraction at 3.9–15.63 µg/mL, as compared to the positive controls (15.63–31.25 µg/mL) against all the microbial strains that produced the biofilm under study, except the Aspergillus fumigatus. The aqueous-ethanolic extract showed cytotoxic effects with IC50 values at 3.47, 3.19, and 2.27 µg/mL against MCF-7, HCT-116, and HepG2 cell-lines, respectively, together with the inhibition of h-TOP-IIβ with IC50 value at 45.05 ng/mL in comparison to its standard referral inhibitor (staurosporine, IC50, 135.33 ng/mL). This conclusively established the anti-cancer activity of the aqueous-ethanolic extract that also validated by in silico receptor-binding predicted energy levels and receptor-site docking feasibility of the major constituents of the plant’s extract. The study helped to authenticate some of the traditional phytomedicinal properties of the anti-infectious nature of the plant.


Plants ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 66
Author(s):  
Hany Ezzat Khalil ◽  
Hairul-Islam Mohamed Ibrahim ◽  
Hossam M. Darrag ◽  
Katsuyoshi Matsunami

Essential oils have been used in various traditional healing systems since ancient times worldwide, due to their diverse biological activities. Several studies have demonstrated their plethora of biological activities—including anti-cancer activity—in a number of cell lines. Anisosciadium lanatum Boiss. is a perennial aromatic herb. Traditionally, it is an edible safe herb with few studies exploring its importance. The current study aims to investigate the chemical composition of essential oil isolated from Anisosciadium lanatum using GC-MS, as well as report its anti-cancer potential and its mechanistic effect on HepG2 liver cancer cell lines, and conduct molecular docking studies. To achieve this, the essential oil was isolated using a Clevenger apparatus and analyzed using GC-MS. The cell viability of HepG2 liver cancer and normal fibroblast NIH-3T3 cell lines was assessed by MTT cytotoxicity assay. The effects of the essential oil on cell migration and invasion were assessed using wound healing and matrigel assays, respectively. The effect of the essential oil on migration and apoptotic-regulating mRNA and proteins was quantified using quantitative real-time PCR and Western blot techniques, respectively. Finally, computational docking tools were used to analyze in silico binding of major constituents from the essential oil against apoptotic and migration markers. A total of 38 components were identified and quantified. The essential oil demonstrated regulation of cell proliferation and cell viability in HepG2 liver cancer cells at a sub-lethal dose of 10 to 25 μg/mL, and expressed reductions of migration and invasion. The treatment with essential oil indicated mitigation of cancer activity by aborting the mRNA of pro-apoptotic markers such as BCL-2, CASPASE-3, CYP-1A1, and NFκB. The algorithm-based binding studies demonstrated that eucalyptol, nerol, camphor, and linalool have potent binding towards the anti-apoptotic protein BCL-2. On the other hand, camphor and eucalyptol showed potent binding towards the pro-apoptotic protein CASPASE-3. These findings highlight the effectiveness of the essential oil isolated from Anisosciadium lanatum to drive alleviation of HepG2 cancer cell progression by modulating apoptotic markers. Our findings suggest that Anisosciadium lanatum could be used as a phytotherapeutic anti-cancer agent, acting through the regulation of apoptotic markers. More well-designed in vivo trials are needed in order to verify the obtained results.


2021 ◽  
Vol 37 (1) ◽  
pp. 221-228
Author(s):  
Mavara Azmi ◽  
Imam Pasha Syed ◽  
Anupama Koneru

Thymoquinone, the active constituent of Nigella sativa has been reported to have various biological activities. Due to its significance, various analogues of it have been synthesized and reported for anti-cancer activity. In the present research, we have taken the analogs of thymoquinone and performed docking study with an objective to find the binding pattern of all the molecules. Apart from this, pharmacokinetic parameters were predicted along with their toxicological parameters. From the results, the molecule Thy09 was found to have the optimized structure and further modification on this could lead to more potent compounds.


2013 ◽  
Vol 683 ◽  
pp. 34-37
Author(s):  
Bin Zeng ◽  
Xiao Hua Zhu

Isatin, an endogenous compound existent in many organisms, shows a wide range of biological activities. In this paper, we like to report the design and synthesis of several isatin derivatives through the acetalization and N-Acylation. Six newly synthesized compounds were characterized on the basis of 1H NMR, and those compounds were determined using two different human cancer cell . Anti-cancer activity showed those compounds IC50<50 μm.


2020 ◽  
Vol 44 (16) ◽  
pp. 6610-6622
Author(s):  
Geângela de Fátima Sousa Oliveira ◽  
Florencio Sousa Gouveia ◽  
Aryane de Azevedo Pinheiro ◽  
Luiz Gonzaga do Nascimento Neto ◽  
Mayron Alves de Vasconcelos ◽  
...  

Efficient avidin binding and selective cancer cell response upon light irradiation of an enhanced ROS photogenerator biotinylated ruthenium complex.


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