Anti-lung Cancer Activity Research Articles

Kenaf (Hibiscus cannabinus L.) Leaves and Seed as a Potential Source of the Bioactive Compounds: Effects of Various Extraction Solvents on Biological Properties.

Hibiscus cannabinus (Kenaf) is a potential source of bioactive constituents and natural antioxidant. The current study determined the impact of various solvents on extraction yield, recovery of polyphenol and flavonoid, antioxidant, anticancer, and antibacterial properties of Kenaf leaves and seed. The powder of leaves and seed was separately extracted with n-hexane, ethyl acetate, ethanol, and water solvent. Among them, the ethanol extract of leaves and seed showed the highest extraction yield, and their GC-MS analysis revealed a total of 55 and 14 bioactive compounds, respectively. The total polyphenols (TP) and flavonoids (TF) content were quantified by a spectrophotometric technique where water extracts displayed a noteworthy amount of TP and TF content compared to other extracts. A similar demonstration was noticed in antioxidant activity, evaluated by DPPH (2,2-diphenyl-1-picrylhydrazyl) and hydrogen peroxide scavenging capacity. In addition, cytotoxicity and anti-lung cancer activity were identified against mouse embryonic fibroblast (NIH3T3) and human lung cancer (A549) cells. All extracts of leaves and seed were observed as non-toxic to the NIH3T3 cells, but slight toxicity was expressed by n-hexane extracts at the optimum dose (1000 µg/mL) of treatment. In parallel, n-hexane and ethanol extracts (leaves and seed) exposed promising anti-lung cancer activity at the same concentration. Furthermore, antibacterial activity was assessed using disc diffusion assay, and seed extracts exhibited a significant inhibition zone against Gram-positive and Gram-negative microorganisms. Overall, Kenaf seed extracted with polar solvents was found very potent in terms of important bioactive compounds and pharmacological aspects, which can be an excellent biological matrix of natural antioxidants.

Inhibition of glucuronomannan hexamer on the proliferation of lung cancer through binding with immunoglobulin G

The anti-lung cancer activity of oligosaccharides derived from glucuronomannan was investigated. The inhibition of A549 cell proliferation by glucuronomannan (Gn) and its oligomers (dimer (G2), tetramer (G4) and hexamer (G6)) were concentration dependent. In vivo activities on the A549-derived tumor xenografts showed the tumor inhibition of G2, G4 and G6 were 17 %, 40 % and 46 %, respectively. Organ coefficients in nude mice showed an increase in the kidney with G4, the brain with G6, and the spleen with G6. An advanced tandem mass tag labeled proteomics approach was performed. A significant differential expression was found in 59 out of the 4371 proteins, which involved the immune system. Surface plasmon resonance (SPR) studies revealed G6 was strongly bound to immunoglobulin G. This suggests that glucuronomannan hexamer inhibits the proliferation of lung cancer through its binding to immunoglobulin.

Structural analysis of a glucoglucuronan derived from laminarin and the mechanisms of its anti-lung cancer activity

Laminarin (LA), a storage glucan, was purified from the brown alga Sargassum thunbergii. After specific oxidation using the stable nitroxyl radical, 2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO), together with NaBr and NaClO, glucoglucuronan (LAO) was obtained. Compositional analysis of LAO showed a molar ratio of glucuronic acid (GlcA) to glucose (Glc) of 12.7: 1. Nuclear magnetic resonance (NMR) and mass spectroscopy (MS) showed LAO to have a backbone of (1 → 3)-linked β-D-GlcpA interspersed with (1 → 3, 1 → 6)-linked β-D-Glcp, that was terminated with β-D-GlcpA. LAO inhibited human lung cancer A549 cell proliferation in vitro. IC50 values at 12 h and 24 h were 2.70 mg/mL and 2.85 mg/mL, respectively. Western blotting showed that TSC2 was up-regulated at an LAO concentration of 3.80 mg/mL. FAK, PI3K, P-AKT and mTOR were down-regulated, indicating LAO inhibited cancer cell proliferation through the FAK/PI3K/AKT/mTOR pathway. Surface plasmon resonance (SPR) studies revealed that LAO showed an IC50 of 0.07 mg/mL inhibiting the binding of heparin to fibroblast growth factor 1 (FGF1) LAO inhibition of heparin binding to FGF2 fluctuated between 15% and 28%, suggesting that LAO inhibits A549 cell proliferation by selectively interacting with FGF1.

The complete chloroplast genome sequence of Populus simonii, a medicinal plant for anti-lung cancer activity

Lung cancer is one of the most common malignant tumors. It is clinically divided into two types: small cell lung cancer and non-small cell lung cancer. Populus simonii distributed in East Asia region including China used as traditional medicine, which is an important medicinal plant for anti-lung cancer activity. The complete chloroplast genome sequence of P. simonii was characterized from Illumina pair-end sequencing. The chloroplast genome of P. simonii was 156,559 bp in length, containing a large single-copy region (LSC) of 84,825 bp, a small single-copy region (SSC) of 47,561 bp, and two inverted repeat (IR) regions of 16,494 bp. The overall GC content is 36.70%, while the corresponding values of the LSC, SSC, and IR regions are 34.5%, 30.0%, and 42.0%, respectively. The genome contains 131 complete genes, including 86 protein-coding genes (68 protein-coding gene species), 37 tRNA genes (29 tRNA species), and 8 rRNA genes (4 rRNA species). The neighbour-joining phylogenetic analysis showed that P. simonii and P. qamdoensis clustered together as sisters to other Populus species.

Quinazolinone-Schiff's Base hybrids as Phosphodiesterase 4B inhibitors with dual activity against COPD and Lung Cancer

A series of thirty compounds of quinazolinone-Schiff's base hybrids were rationally designed, synthesized, and evaluated for their in vitro Phosphodiesterase 4B inhibition, anti-lung and anti-colon cancer activities. Compounds 9, 16, 23, 29, 30, 31, 32 and 33, each possessing a tri-hydroxy moiety, showed the highest inhibitory activity (56.05-89.07%) at 10 µM concentration if compared to rolipram. Compounds 16 and 23 showed good anti-lung cancer activity with IC50 1.55 and 1.30 µM, respectively. Moreover, compound 16 showed high anti-colon cancer activity with IC50 0.6 µM. Compound 33 showed good affinity and molecular binding modes towards the key amino acid Gln 443 and Phe 446 for inhibition of the target enzyme. Finally, active compounds showed good ADME calculations.

Production, characterization, and functions of sulfated polysaccharides from zinc sulfate enriched cultivation of Antrodia cinnamomea

This research utilized zinc sulfate enriched cultural conditions to produce sulfated polysaccharides from Antrodia cinnamomea (denoted as ZnFSPS) and physiochemically characterize functional and mechanical investigations of ZnFSPS. The maximum SPS yield reached a value of 6.68% when A. cinnamomea was fed zinc sulfate with 250 mM (denoted as Zn250). Zn250 had a maximal inhibitory effect on LPS-induced tumor necrosis factor (TNF-α) release in RAW264.7 macrophage. Zn250 contained the highest area percentage of molecular weight of 178.5, 105.1, and 1.56 kDa at values of 19.08, 15.09, and 5.04. Zn250 contained three times the sulfate content as compared with the control. Mechanism studies revealed a novel finding that Zn250 inhibited the LPS-induced RAW264.7 macrophage inflammation and selectively blocked pAKT, pERK and p38. Zn250 also attenuated the LPS-induced IkB-α degradation. In addition, ZnFSPS interfered with lung cancer cell H1975 TGFRI/FAK/Slug signaling. These results suggest ZnFSPS plays roles in regulating inflammatory and anti-lung cancer activity.

Recent advances in the antilung cancer activity of biosynthesized gold nanoparticles.

Gold nanoparticles (Au-NPs) have been widely used in biomedical fields such as imaging, diagnosis, and treatment because of their special characteristics. Au-NPs can be synthesized using several methods, including the biological method, also called green or eco-friendly synthesis. Recent studies have reported the anticancer activity of biosynthesized Au-NPs, especially in lung cancer. This review focused on the advances in the antilung cancer activity of biosynthesized Au-NPs and its potential mechanisms.

Compositional characterization ofPyrus ussuriensisMaxim and their antioxidant activities and induction of apoptosis in Bel‐7402 cell

In this work, a comparison study on active sites (the total phenolic, total flavonoids, and total triterpenes contents) and antioxidant activities (DPPH, ABTS, and FRAP assays) of different fractions from Pyrus ussuriensis Maxim was evaluated. Moreover, the inhibition capability on human hepatocarcinoma cells Bel-7402 cells and the mechanism was also discussed. Results showed that the ethyl acetate fraction significantly scavenged DPPH and ABTS+ radicals, exhibited ferric ion reducing antioxidant, and inhibited Bel-7402 cells proliferation. In addition, oleanolic acid was the dominant compound act on the Bel-7402 cells in the extract and it induced apoptosis by the caspase pathway and induced cell cycle arrest at the G0/G1 phase by inhibiting the cyclin D1/CDK4 pathway. The extracts of P. ussuriensis Maxim were confirmed to have anti-oxidative and antiproliferative effects against Bel-7402 cell in vitro. PRACTICAL APPLICATIONS: Fruits and vegetables which contain high levels of antioxidants can help to reduce the risk of chronic diseases such as cancer. Pyrus ussuriensis Maxim is a kind of edible and medical fruit with multiple bioactivities, whereas the capability to anti-lung cancer activity has not been investigated. The extracts of P. ussuriensis Maxim were revealed to have anti-oxidative and antiproliferative effects against Bel-7402 cell in vitro. Accordingly, it is the first time to verify that oleanolic acid was the main chemical components of P. ussuriensis with antitumor potential.

Quinonoids: Therapeutic Potential for Lung Cancer Treatment.

Lung cancer is the leading cause of cancer-related deaths worldwide. Owing to its high incidence and mortality, the development and discovery of novel anticancer drugs is of great importance. In recent years, many breakthroughs have been achieved in the search for effective anticancer substances from natural products. Many anticancer drugs used clinically and proven to be effective are derived from natural products. Quinonoids, including naphthoquinones, phenanthrenequinones, benzoquinones, and anthraquinones, constitute a large group of natural bioactive compounds that widely exist in higher and lower plant species. Given that most of these compounds possess anticancer effects, they are applied in many cancer studies, especially in lung cancer research. They can promote apoptosis, induce autophagy, and inhibit proliferation, angiogenesis, and cell invasion and migration. Some drugs can enhance anticancer effects when combined with other drugs. Thus, quinonoids have broad application prospects in the treatment of lung cancer. Here, we summarize the previous studies on the antilung cancer activities of quinonoids together with their underlying mechanisms and analyze the common research targets with different effects so as to provide references for the discovery of quinonoids against lung cancer.

Structural characterization and anti-lung cancer activity of a sulfated glucurono-xylo-rhamnan from Enteromorpha prolifera

A sulfated glucurono-xylo-rhamnan (EP-3-H) was purified from a green alga, Enteromorpha prolifera. EP-3-H and its oligomers were characterized by high performance liquid chromatography, mass spectrometry and one and two-dimensional nuclear magnetic resource spectroscopy. The structural analysis showed EP-3-H has a backbone of glucurono-xylo-rhamnan, branches with glucuronic acid and sulfated at C3 of rhamnose and/or C2 of xylose. The inhibition of EP-3-H on human lung cancer A549 cell proliferation in vitro and its therapeutic effects in BALB/c-nu mice in vivo were determined to evaluate the anti-lung cancer activity of EP-3-H. The tumor inhibition level was 59 %, suggesting that EP-3-H might be a good candidate for the treatment of lung cancer. Surface plasmon resonance (SPR) studies revealed the IC50 on the binding of fibroblast growth factors, (FGF1 and FGF2), to heparin were 0.85 and 1.47 mg/mL, respectively. These results suggest that EP-3-H inhibits cancer proliferation by interacting with these growth factors.

Construction of two coordination polymers based on imidazolyl and aromatic dicarboxylic acid ligands: structural diversity and anti-lung cancer activity study

Solvothermal reaction of 4,4′-bis(imidazol-1-yl)diphenyl ether (BIDPE) or 1,4-Bis(imidazole-1-ylmethyl)benzene (BiB) with 1,4-benzenedicarboxylic acid (H2bdc) or 4,4’-(thiobis(methylene))dibenzoic acid (H2tba) in the presence of Zn(NO3)2·6H2O or Co(NO3)2·6H2O in a mixed solvent of H2O/DMF yielded two new coordination polymers, namely, [Zn(bdc)(BIDPE)](DMF)2(H2O) (1) and [Co(tba)(BIB)](H2tba)(DMF)(H2O)2 (2). These complexes were characterized by elemental analysis and X-ray single-crystal diffraction, which revealed that complex 1 is a 2D layered network with hexagonal windows while complex 2 is a 1D chain-like structure containing the 0D Co2(BIB)2 loops. Furthermore, the anticancer activity of the two coordination complexes has been evaluated via the CCK-8 assay and western blot assay.

B36 Effects of Trifluoperazine and Its Analog on A549 Human Lung Cancer Cells

Although there have been great advances in technology, molecular diagnosis, and therapeutics, lung cancer is still the leading cause of cancer-related mortality all over the world. Recently, some antipsychotic drugs have been shown to possess anticancer activity. Thus, the present study was designed to evaluate the anticancer effects of trifluoperazine (TFP), a commonly used antipsychotic drug, and its synthetic analogs on human lung cancer cell lines. To this end, effects of TFP and its selected analog on A549 cells were investigated in in vitro as well as in vivo experiments. Synthetic TFP analogs were evaluated by the proliferation of A549 cells following drug treatment and compared to TFP. 3dc, a selected TFP analog, significantly inhibited the proliferation of A549 cells. Further experiment showed that TFP and 3dc had activities to inhibit the anchorage dependent/independent colony formation, and migration of A549 cells. Western blot analysis revealed that 3dc affected the gene expression levels related to apoptosis and cell cycle. Flow cytometric analysis showed that 3dc induced sub-G1 and G1 population and reduced cell population in S and G2/M phase. Additionally, Annexin V/PI staining showed that 3dc increased apoptotic cell population. Moreover, 3dc increased DNA fragmentation. 3dc showed stronger anticancer effects in all the experiments than TFP. In addition, in in vivo experimental models, 3dc also showed powerful anticancer effect in orthotropic lung cancer development than TFP. Thus, the present study demonstrates that a synthetic TFP analog has anti-lung cancer activity and provides a potential therapeutic candidate for lung cancer.

Structural analysis of a novel sulfated galacto-fuco-xylo-glucurono-mannan from Sargassum fusiforme and its anti-lung cancer activity

Polysaccharide (HFSGF) was purified from Sargassum fusiforme. Autohydrolysis and gel column chromatography were performed to fractionate HFSGF into three components (HFSGF-S, HFSGF-L and HFSGF-H). Compositional analysis, mass spectrometry and nuclear magnetic resonance spectroscopy were used to elucidate the structural features of HFSGF. HFSGF-S was a mixture of sulfated galacto-fuco-oligomers, from the branches terminal ends; in HFSGF-L, the branches of HFSGF, was a sulfated galactofucan, containing a backbone of 1,3-linked α-L-fucan sulfated at C2/4 and/or C4 and interspersed with galactose (Gal); and in HFSGF-H, the backbone of HFSGF, was composed of alternating 1,2-linked α-D-mannose (Man) and 1,4-linked β-D-glucuronic acid (GlcA), branched with sulfated galactofucan or sulfated fucan, 1,3-linked α-L-fucan sulfated at C2/4 and/or C4 and partly interspersed with Gal. Some fucose (Fuc) residues were also partially branched with xylose (Xyl). The anti-lung cancer activities of HFSGF-L and HFSGF-H against human lung cancer A549 cells in vitro and A549 xenograft tumor growth in vivo were determined. HFSGF-H had higher activity in vitro (IC50 ~12 mg/mL for 24 h) and in vivo (tumor inhibition ~51%.) than HFSGF-L, indicating that HFSGF-H might be a leading compound for a potential new therapeutics for the treatment of lung cancer.

Synthesis, characterization and anti-lung cancer activity of two transition metal coordination polymers based on the imidazole-containing ligands

This work presents the synthesis and characterization of two new transition metal coordination polymers [Co(tib)2](NO3)2 (1, tib = 1,3,5-tris(1-imidazolyl)benzene) and [Cd4(bib)5(HCOO)8](DMF)3 (2, bib = 4,4′-bisimidazolylbiphenyl) have been successfully prepared by using two imidazole-containing ligands with different geometers. All structures have been fully elucidated by single-crystal X-ray diffraction along with the elemental analysis. The structural solution and refinement results based on the crystal data collected at room temperature reveal that complex 1 shows a 2D layered structure with a binodal (3,6)-connected kgd topological net, while complex 2 also demonstrates a 2D framework but reflecting a 4-connected sql topological net. Furthermore, the anti-lung cancer activity of the two complexes has been studied via the Cell Counting Kit-8 (CCK-8) assay along with the corresponding action mechanism.

Bio-engineered TiO2 nanoparticles using Ledebouria revoluta extract: Larvicidal, histopathological, antibacterial and anticancer activity

ABSTRACT Titanium dioxide nanoparticles have been synthesised using bulb extract of Ledebouria revoluta. The prepared TiO2 nanoparticles were characterised by structural (XRD, FTIR), morphological (HRTEM) and optical (UV-Vis) analysis. XRD shows the bioengineered TiO2 nanoparticles exhibit an average crystalline size of 47 nm with tetragonal structure. In FTIR spectra, the peak 482 cm−1 is indicating the presence of Ti-O stretching vibration. The morphology of bioengineered TiO2 nanoparticles shows a spherical shape. Antibacterial activity of L. revoluta bulb aqueous extract and TiO2 nanoparticles were evaluated against human pathogens. The larvicidal activity of TiO2 nanoparticles showed LC50 (18.960 mg/mL) and LC90 (77.097 mg/mL) against Aedes aegypti. Anti-lung cancer activity of TiO2 nanoparticles was examined using MTT assay and it results in IC50 value of 53.65 µg/mL. Furthermore, bioengineered TiO2 nanoparticles will be applicable to pharmaceutical applications.

RETRACTED ARTICLE: Two new Bi(III) and Ce(III) chelates incorporating 1,10-phenanthroline-2,9-dicarboxylic acid: structure elucidation and anti-lung cancer activity study

We, the Editors and Publisher of the journal Inorganic and Nano-Metal Chemistry, have retracted the following article: Di Li, Li-Fei Li, Zhi-Fang Zhang, Wen-Bo Shi, Lei Pan & Yang Liu. Two new Bi(III) and Ce(III) chelates incorporating 1,10-phenanthroline-2,9-dicarboxylic acid: structure elucidation and anti-lung cancer activity study, Inorganic and Nano-Metal Chemistry, 2020, VOL. 50, NO. 4, 245–250. DOI: 10.1080/24701556.2019.1709505 Since publication, concerns have been raised about the integrity of the data in the article. When approached for an explanation, the authors have been unable to address the concerns raised and have not been able to provide sufficient supporting information. As verifying the validity of published work is core to the integrity of the scholarly record, we are therefore retracting the article. The corresponding author listed in this publication has been informed. The authors have agreed to the retraction. We have been informed in our decision-making by our policy on publishing ethics and integrity and the COPE guidelines on retractions. The retracted article will remain online to maintain the scholarly record, but it will be digitally watermarked on each page as ‘Retracted’.

Synthesis, Characterization and Biological Studies of Nickel ( Ii) and Zinc ( Ii) Complexes with Mono - and Di - Bromo Substituted Schiff Base Ligands

Transition metal complexes of nickel(II) and zinc(II) with 5-bromo- N -(8-quinolyl)salicylaldimine (HqsalBr, HL 1 ) and 3,5-dibromo- N -(8-quinolyl)salicylaldimine (HqsalBr 2 , HL 2 ) have been synthesized and successfully characterized using several techniques: IR, 1 H-NMR, mass spectrometry and thermogravimetric analysis (TGA). The molecular structures of nickel(II) and zinc(II) complexes with HL 2 were determined by single crystal X-Ray crystallography. Ligands HL 1 and HL 2 both act as a tridentate ligand and coordinate to metal ion center via deprotonated hydroxyl oxygen atom, nitrogen of azomethine functional group and nitrogen of quinoline substituent. The interaction of these complexes with DNA was investigated using calf thymus DNA (CT-DNA) in which the studies by electronic absorption and luminescence titrations reveal that DNA binding mode of the complexes is intercalation. All the synthesized complexes provide great values of binding constant (K b ) and these results are consistent with the quenching capability defined by quenching constant values (K q ). Amongst the synthesized complexes, zinc(II) with ligand HL 2 complex, [Zn(qsalBr) 2 ], exhibits the most superior ability in the interaction with CT-DNA and the verification mode of binding by the competitive reaction with ethidium bromide (EB) also indicates the strongest intercalation by such complex. Additionally, ligands and complexes were also examined in anti-lung cancer activity against A549 cell line and compared with standard compounds, Etoposide and Cisplatin.

RETRACTED ARTICLE: Structural diversity and anti-lung cancer activity evaluation of two Co(II) and Cu(II) containing mixed-ligand coordination polymers

We, the Editors and Publisher of the journal Inorganic and Nano-Metal Chemistry, have retracted the following article: Di Li, Li-Fei Li, Zhi-Fang Zhang, Fan Lin, Lei Pan & Yang Liu. Structural diversity and anti-lung cancer activity evaluation of two Co(II) and Cu(II) containing mixed-ligand coordination polymers, Inorganic and Nano-Metal Chemistry. 2020, 50:4, 229–237, DOI: 10.1080/24701556.2019.1706568 Since publication, concerns have been raised about the integrity of the data in the article. When approached for an explanation, the authors have been unable to address the concerns raised and have not been able to provide sufficient supporting information. As verifying the validity of published work is core to the integrity of the scholarly record, we are therefore retracting the article. The corresponding author listed in this publication has been informed. The authors have agreed to retract the article. We have been informed in our decision-making by our policy on publishing ethics and integrity and the COPE guidelines on retractions. The retracted article will remain online to maintain the scholarly record, but it will be digitally watermarked on each page as ‘Retracted’.

Synthesis, crystal structure, anti-lung cancer activity of 2-(4-fluorophenyl)-5-(5-iodo-2-methylbenzyl)thiophenee

New heterocycle compound 2-(4-fluorophenyl)-5-(5-iodo-2-methylbenzyl)thiophene (1), designed using 5-iodo-2-methylbenzoic acid (2) as the starting material is successfully obtained via the multiple synthesis route and finally characterized by IR, 1H NMR, and single crystal X-ray crystallography. In addition, the in vitro anticancer activity of compound 1 on three human lung cancer cells (H20, H2227, and H69) is further determined, which suggests that compound 1 may be a potential anticancer agent.

RETRACTED ARTICLE: A New Coordination Polymer for Effective 5-fluorouracil Loading and Anti-lung Cancer Activity Study

A new three-dimensional porous coordination polymer with the formula of [Ba(HTATB)-(H2O)](DMF)2 (I) has been solvothermally synthesized from 4,4′,4″-s-triazine-2,4,6-triyltribenzoic acid (H3TATB) and Ba(NO3)2 under DMF media and characterized by single crystal X-ray diffraction (CIF file CCDC no. 1856562) and elemental analysis. The efficient encapsulation of an anticancer drug 5-fluorouracil (5-FU) on the desolvated I (Ia) has been studied both experimentally and computationally. In addition, in vitro anti-lung cancer activity of compounds I and 5-FU loaded 1a have also been evaluated using MTT assay.