Cytotoxic Activity Research Articles

Potential therapeutic applications of Cistus laurifolius extract: Anti-proliferative, anti-cancer activity on MCF-7, and anti-microbial effects

Cistus laurifolius L. is commonly used in Turkish folk medicine for the treatment of ulcers and various types of pain. In this study, the cytotoxic and apoptotic activities of C. laurifolius extract on the MCF-7 breast cancer cell line, as well as its antimicrobial activity against eight microorganisms (Listeria monocytogenes, Enterococcus faecalis, Bacillus subtilis, Staphylococcus aureus, Escherichia coli, S. typhimurium, and Pediococcus acidilactici) were investigated. Different concentrations (100 µg/mL, 250 µg/mL, 500 µg/mL, and 1000 µg/mL) of the plant extract were applied for 24, 48, and 72 h, and its effects were determined using MTT, BrdU, and in situ apoptosis detection assays on human breast cancer cell MCF-7. Prolonged high-dose application of C. laurifolius extract led to decreased cell viability, inhibition of DNA synthesis, and induction of apoptosis. Its potential to induce cell death, which is the most desirable pathway for cancer treatment, is noteworthy alongside its cytotoxic activity. The antimicrobial effect of C. laurifolius extract varied depending on the Gram reaction of the microorganisms, with the extract being more effective against Gram-positive bacteria than Gram-negative bacteria. In conclusion, the C. laurifolius extract exhibits cytotoxic, anticancer, and antimicrobial properties.

Sesquiterpene coumarins with anti-vitiligo and cytotoxic activities from Ferula samarkandica

Two undescribed sesquiterpene coumarins (1–2) and eight known analogues (3–10) were isolated from the roots of Ferula samarkandica Korovin, growing in Uzbekistan. Their structures were established by comprehensive spectroscopic analysis including NMR, HRESIMS, UV and IR data. The absolute configurations were determined based on ECD calculations and confirmed by single-crystal X-ray diffraction analysis. Six compounds carrying 7′-carbonyl, 3′-carbonyl and 3′-acetoxy (4, 5, 6, 7, 9, 10) demonstrated anti-vitiligo potentials, in addition to five (4, 7, 8, 9, 10) with cytotoxic effects. Evaluation of anti-vitiligo activity in B16 cells revealed that compounds 4–7 and 9 exhibited promotion effects on melanin synthesis in B16 cells more potent than the positive control 8-methoxypsoralen (8-MOP), while 5, 7, 9 and 10 could also stimulate the tyrosinase activity superior to 8-MOP. Besides, compounds 4 and 7–10 also presented certain cytotoxic activities against HeLa, HT-29 and A549 cell lines, wherein 8 displayed a significant cytotoxicity against HT-29 cells with an IC50 value of 8.33 ± 0.34 μM.

Flavonoid-metal ion Complexes as Potent Anticancer metallodrugs: A comprehensive Review.

Flavonoids and their analogous are mainly found in pink lady apples, green and black tea (catechins), celery and red peppers, onions, broccoli and spinach, berries, cherries, soybean, citrus fruits, and fungi. The different derivatives of flavonoids belonging to polyphenolic compounds such as 3,4',5,7-Tetrahydroxyflavylium (pelargonidin), 2-(3,4-Dihydroxyphenyl)chromenylium-3,5,7-triol (cyanidin), 3,3',4',5,5',7-Hexahydroxyflavylium (delphinidin), 3,3',4',5,7-Pentahydroxy-5'-methoxyflavylium (petunidin), and 3,4',5,7-Tetrahydroxy-3',5'-dimethoxyflavylium (malvidin) can act as good chelating agents for metal-chelate complex formation. These flavonoid-metal complexes have been reported to have various biomedical and pharmacological activities. Flavonoid-metal ion complexes display a broad spectrum of biological properties such as antioxidant, anti-inflammatory, anti-allergic, antiviral, anticarcinogenic, and cytotoxic activity. The literature survey showed that flavonoid metal complexes have potential therapeutic properties against various cancerous cells. The objective is to gain insight into the current perspective and development of novel anticancer metallodrug drugs. The flavonoid-metal ion complexes can be prepared by reacting flavonoid ligand with appropriate metal salt in aqueous or alcoholic reaction medium under stirring or refluxing conditions. In this review article, the various reported methods for the synthesis of flavonoid-metal complexes have been included. The utility of synthetic methods for flavonoid-metal complexes will support the discovery of novel therapeutic drugs. In this review study, short libraries of flavonoid-metal ion complexes were studied as potential anticancer agents against various human cancer cell lines. The review report reveals that metal ions such as Fe, Co, Ni, Cu, Zn, Rh, Ru, Ga, Ba, Sn etc., when binding to flavonoid ligands, enhance the anticancer activity compared to free ligands. This review study covered some important literature surveys for the last two decades. It has been concluded that flavonoid metal complexes have been associated with a wide range of biological properties that could be noteworthy in the medicinal field. Therefore, to develop a new anticancer drug, it is essential to determine the primordial interaction drug with DNA under physiological or anatomical conditions. The study of numerous flavonoid metal complexes mentioned in this paper could be the future treatment against various cancerous diseases.

Bioactive metabolites from endophytes of African club moss- Selaginella kraussiana (Kunze) A. Braun exhibit broad-spectrum pharmaceutical utilities

The search for potent natural compounds from plant and microbial sources is increasing logarithmically to combat various types of health issues of which multidrug-resistant microbes and problems related to oxidative stress are the prime ones. Novel secondary metabolites from endophytes have always been potent alternatives to contemporary antimicrobials and antioxidants. The present study shows that two potent endophytic fungal isolates Ascochyta medicaginicola SK16 and Phomopsis sp. SK5 synthesises non-proteinaceous, thermostable secondary metabolites with broad-spectrum antimicrobial, antioxidative, and cytotoxic activity. Bioassay-guided fractionation revealed that the Ethyl acetate (EA) extract of the cell-free culture extract (CFCE) of SK5 and SK16 constitutes ten and eleven secondary metabolites of which 2,4, -di tert butyl phenol, aziridine- 1,2-amino ethyl, actinobolin, bactobolin, azulene, menthyl acetate, phenol, p-[2-(methylamino)ethyl], and imidazole components were significant. SK16 exhibited strong antimicrobial activity against seventeen pathogens including Methicillin-resistant Staphylococcus aureus (MRSA), and C. albicans with a minimum microbicidal concentration of 100- 400 µg mL−1. These metabolites disrupt the microbial cell membranes causing lethal leakage of biomacromolecules- nucleic acid, protein, and potassium ions. Enzymes involved in the EMP pathway, TCA cycle, and gluconeogenesis were also blocked. Both the biofilm formation and transition of Candida cells from the yeast-to-hyphal form were inhibited. SK5 metabolites are potent radical scavengers with an IC50 of 34.25 ± 0.87 – 195.21 ± 5.73 µg mL−1 against DPPH, ABTS, FRAP, and H2O2 free radical generators and significantly increased antioxidant parameters in treated peritoneal macrophage cells of male Wistar rats. Also, SK5 metabolites were cytotoxic against breast (T47D), pancreatic (MIA Paca-2), lung (A549) and colon (HCT-116) cancer cells. The present findings suggest that metabolites from endophytes of African club moss hold potent pharmaceutical utilities.

Heteroaromatization of Coumarin Part I: Design, Synthesis, Reactions, Antitumor Activities of Novel Pyridine and Naphthyridine Derivatives.

A novel series of chromen-3-yl-pyridine moieties were synthesized. IR, NMR, and MS spectroscopy were used to confirm the structure of these novel compounds and study antitumor activity of these compounds. The structure-activity relationship investigation demonstrated that 2,4-diamino- 5-(3-methoxyphenyl)-7-(2-oxo-2H-chromen-3-yl)-1,8-naphthyridine-3-carbonitrile (16), naphthyridine- 3-carbonitrile derivatives 17, 18 and pyrido[2,3-d]pyrimidine derivative 12 were found to be more effective, while compounds 5a,b, 9c, 11, 13 and 14 showed moderate activity for antitumor activities. The objective was to design a series of new chromen-3-yl-pyridine and pyrido[2,3-d]pyrimidine derivatives and study the antitumor of these compounds. The condensation reaction of 3-acetyl-2H-chromen-2-one with 3-methoxy benzaldehyde and malononitrile or ethyl cyanoacetate in the presence of ammonium acetate and acetic acid under reflux to give the corresponding chromen-3-yl pyridine-3-carbonitrile derivatives. In this study, the antitumor activity of the synthesized compounds chromen-3-yl-pyridine derivatives has been determined for the broad spectrum of cytotoxic activity toward the investigated three cell lines and 5-Fluorouracil, as reference drugs. A series of new chromen-3-yl-pyridine and pyrido[2,3-d]pyrimidine derivatives were synthesized in this work. All compounds were evaluated for cytotoxic activity.

Evaluation of the antibacterial, antibiofilm, and cytotoxic activities of Peltophorum africanum leaf methanolic extract

Evaluation of the antibacterial, antibiofilm, and cytotoxic activities of Peltophorum africanum leaf methanolic extract

1,3-Diaryl Triazenes Incorporating Disulfonamides Show Both Antiproliferative Activity and Effective Inhibition of Tumor-associated Carbonic Anhydrases IX and XII.

The aim of this study was to synthesize a library of novel di-sulfa drugs containing 1,3- diaryltriazene derivatives TS (1-13) by conjugation of diazonium salts of primary sulfonamides with sulfa drugs to investigate the cytotoxic effect of these new compounds in different cancer types and to determine their inhibitory activity against tumor-associated carbonic anhydrases IX and XII. A carbonic anhydrase inhibitory activity of the obtained compounds was evaluated against four selected human carbonic anhydrase isoforms (hCA I, hCA II, hCA IX and hCA XII) by a stoppedflow CO2 hydrase assay. In addition, in vitro, cytotoxicity studies were applied by using A549 (lung cancer), BEAS-2B (normal lung), MCF-7 (breast cancer), MDA-MB-231 (breast cancer), CRL-4010 (normal breast epithelium), HT-29 (colon cancer), and HCT -116 (colon cancer) cell lines. As a result of the inhibition data, the 4-aminobenzenesulfonamide derivatives were more active than their 3-aminobenzenesulfonamide counterparts. More specifically, compounds TS-1 and TS-2, both of which have primary sulfonamides on both sides of the triazene linker, showed the best inhibitory activity against hCA IX with Ki values of 19.5 and 13.7 nM and also against hCA XII with Ki values of 6.6 and 8.3 nM, respectively. In addition, in vitro cytotoxic activity on the human breast cancer cell line MCF-7 showed that some derivatives of di-sulfa triazenes, such as TS-5 and TS-13, were more active than SLC-0111. With the aim of developing more potent and isoform-selective CA inhibitors, these novel hybrid molecules containing sulfa drugs, triazene linkers, and the classical primary sulfonamide chemotype may be considered an interesting example of effective enzyme inhibitors and important anticancer agents.

An article reviews of anti-cataract activity of hydroalcoholic extract of Annona squamosa leaves

Other medicines and natural remedies have been used for the treatment and health of people since ancient times. Medicinal plants are considered useful and of the most important purpose. It can be applied to botanical medicines, nutraceuticals, medicines, food products, cosmetics, etc. There is an increasing demand for. Custard apples. It is a versatile tree whose fruit is edible and a source of medicine and products. It is used as antioxidant, antidiabetic, hepatoprotective, cytotoxic activity, genotoxicity, antitumor activity, anti-inflammatory drug. Cataract is nothing but visual impairment caused by a defect in the lens. It is one of the causes of blindness worldwide; It accounts for approximately 42% of all blindness. One significant risk factor for the development of posterior subcapsular cataracts is long-term glucocorticoid usage. The preventive and therapeutic effects of many herbs such as onion, Chinese cinnamon and ginkgo, which have protective properties against cataracts, have been reported. This review demonstrates the therapeutic potential of custard apple leaf extract as an anti-cataract effec

GEOGRAPHICAL DESCRIPTION AND PHARMACOLOGICAL PROPERTIES OF DICHANTHIUM ANNULATUM: A REVIEW

Dichanthium annulatum herb belongs to Poaceae family; also referred to as marvel grass. It grows to a height of about 25cm. Due to its straightforward and affordable development from seed, it is used as forage. The present review was based on the geographical description and pharmacological properties of dichanthium annulatum. It is indigenous to regions of Africa, the Middle East, and tropical Asia. It has been brought to many different regions of the world for cultivation, and in some, like Australia, it has established itself as a native species. This pasture grass is well-liked in various regions. It can be harvested for hay and silage and used in fields to graze livestock. It can grow in a wide range of soil types, including those with a lot of clay and sand, poor drainage, and a little saline and alkaline soil. It creates turf that can withstand pressure from grazing animals. It can bounce back from fire and drought, but it can't stand frost and shade as well. Although it doesn't need fertiliser, it does benefit from a little more nitrogen. It concluded that D. annulatum is versatile herb having diverse pharmacological activities including antioxidant, antioxidant activity index, DNA damage protection assay, antimicrobial assay, and cytotoxic activity. It also reported for protective effect against DNA damage. These biological properties are reported due to numerous phytochemicals present in the D. annulatum herb.

Isolation of flavonoids from Tagetes patula(French Marigold) flowers: Cytotoxic and oxidant activity in human cervical carcinoma cells

Isolation of flavonoids from Tagetes patula(French Marigold) flowers: Cytotoxic and oxidant activity in human cervical carcinoma cells

Isolation and identification of hyperin and naringenin from guava cultivated in Iraq and evaluation of cytotoxic activity of hyperin

The guava plant, Psidium guajava L., serves as proof of the abundant donations of nature, providing a delicious guava fruit; this plant is rich in groups of medicinal and nutritional benefits. Guava belonging to the Myrtaceae family, many previous studies reported many phytochemical constituents in its leaves that have many pharmacological activities and medicinal properties; this study focuses on the isolation, structural elucidation and calculation concentration of flavonoids, assessment of the cytotoxic activityof hyperin from Psidium guajava leaves newly cultivated in Iraq. The isolation process involved the use of thin-layer chromatography (TLC) and preparative high-performance liquid chromatography (PHPLC) and structural elucidation involved NMR (nuclear magnetic resonance spectroscopy) and FTIR (Fourier transform infrared spectrometer) for detailed structural insights into 2 isolated flavonoids. The isolation techniques proved effective in obtaining pure samples of hyperin and naringenin from the ethyl acetate and n.butanol fractions and structural elucidation techniques gives a good explanation for 2 isolated flavonoids. Evaluate cytotoxic activity of hyperin flavonoid against prostate cancer cell line (PC-3), human breast cancer cell line (MCF-7) and normal dermal fibroblast neonatal (HdFn), hyperin flavonoid exhibited a decrease in cell viability (%) with IC50 58.9 ?g /mL against the prostate cancer cell and IC50 90.58 ?g /mL against human breast cancer and noncytotoxic to HDFn, with an IC50 value substantially surpassing concentrations of 100 ?g/mL. These analytical approaches provided a comprehensive understanding of the chemical composition of the isolated flavonoids and interpreted that guava has cytotoxic activity against some cancers, depending on a concentration-dependent mode.

Novel binuclear copper(II) complexes with sulfanylpyrazole ligands: Synthesis, crystal structure, fungicidal, cytostatic and cytotoxic activity.

New binuclear Cu(II) tetraligand complexes (six examples) with sulfanylpyrazole ligands were synthesized. EPR Studies have shown that in solution the complexes are transformed to the mononuclear one. Fungicidal properties against Candida albicans were found for the Cu complexes with benzyl and phenyl substituents. An in vitro evaluation of the cytotoxic properties of copper chelates against Hek293, Jurkat, MCF-7, and THP-1 cells identified the copper complex with the cyclohexylsulfanyl substituent in the pyrazole core as the lead compound, whereas the copper complex without a sulfur atom in the pyrazole ligand had virtually no cytotoxic or fungicidal activity. The lead Cu(II) complex was more active than cisplatin. Effect of S-containing Cu complex on apoptosis and cell cycle distribution has been investigated as well.

Biogenic Synthesis, Characterization, Along with Investigation of Cytotoxicity and Antibacterial Activities of Silver Nanoparticles Using Twigs of Polyalthia sclerophylla

Biogenic Synthesis, Characterization, Along with Investigation of Cytotoxicity and Antibacterial Activities of Silver Nanoparticles Using Twigs of Polyalthia sclerophylla

Synthetic Colors in Food: A Warning for Children’s Health

This study addressed the harmful effects of artificial colors in pediatric populations, including children diagnosed with Autism Spectrum Disorder (ASD) and Attention Deficit Hyperactivity Disorder (ADHD), as well as those without behavioral disorders. There is a consensus that synthetic food colorings have several impacts on consumers, especially pediatrics, due to their influence on sensory appeal, which can encourage preference for certain foods. The results revealed that these color additives are directly linked to a series of health problems, with a greater impact on children, including a predisposition to pathological conditions such as carcinogenic, allergenic, mutagenic, cytotoxic, and clastogenic activities, as well as gastrointestinal and respiratory problems, in addition to behavioral changes in children with and without diagnosed disorders. The harms of synthetic dyes in children with or without comorbidities are worrying and require a careful and proactive approach from parents, caregivers and public authorities.

Non-clinical investigations about cytotoxic and anti-platelet activities of gamma-terpinene.

Gamma-terpinene (γ-TPN) is a cyclohexane monoterpene isolated from plant essential oils, such as tea tree (Melaleuca alternifolia), oregano (Origanum vulgare), rosemary (Rosmarinus officinalis L.), thyme (Thymus vulgaris Marchand), and eucalyptus (Eucalyptus sp.). Terpenes are widely studied molecules pharmacologically active on the cardiovascular system, hemostasis, and antioxidant actions. Herein, it was investigated the cytotoxic and antiplatelet activity of γ-TPN using different non-clinical laboratory models. For in silico evaluation, the PreADMET, SwissADME, and SwissTargetPrediction softwares were used. Molecular docking was performed using the AutoDockVina and BIOVIA Discovery Studio databases. The cytotoxicity of γ-TPN was analyzed by the MTT assay upon normal murine endothelial SVEC4-10 and fibroblast L-929 cells. Platelet aggregation was evaluated with platelet-rich (PRP) and platelet-poor (PPP) plasma from spontaneously hypertensive rats (SHR), in addition to SVEC4-10 cells pre-incubated with γ-TPN (50, 100, and 200 µM) for 24 h. SHR animals were pre-treated by gavage with γ-TPN for 7 days and divided into four groups (negative control, 25, 50, and 100 mg/kg). Blood samples were collected to measure nitrite using the Griess reagent. Gamma-TPN proved to be quite lipid-soluble (Log P = +4.50), with a qualified profile of similarity to the drug, good bioavailability, and adequate pharmacokinetics. It exhibited affinity mainly for the P2Y12 receptor (6.450 ± 0.232 Kcal/mol), moderate cytotoxicity for L-929 (CC50 = 333.3 µM) and SVEC 4-10 (CC50 = 366.7 µM)cells. The presence of γ-TPN in SVEC 4-10 cells was also able to reduce platelet aggregation by 51.57 and 44.20% at lower concentrations (50 and 100 µM, respectively). Then, γ-TPN has good affinity with purinergic receptors and an effect on the reversal of platelet aggregation and oxidative stress, being promising and safe for therapeutic targets and subsequent studies on the control of thromboembolic diseases.

Phytochemical and biological assessment of secondary metabolites isolated from a rhizosphere strain, Sphingomonas sanguinis DM of Datura metel

BackgroundThe plant roots excrete a large number of organic compounds into the soil. The rhizosphere, a thin soil zone around the roots, is a hotspot for microbial activity, making it a crucial component of the soil ecosystem. Secondary metabolites produced by rhizospheric Sphingomonas sanguinis DM have sparked significant curiosity in investigating their possible biological impacts.MethodsA bacterial strain has been isolated from the rhizosphere of Datura metel. The bacterium’s identification, fermentation, and working up have been outlined. The ethyl acetate fraction of the propagated culture media of Sphingomonas sanguinis DM was fractioned and purified using various chromatographic techniques. The characterization of the isolated compounds was accomplished through the utilization of various spectroscopic techniques, such as UV, MS, 1D, and 2D-NMR. Furthermore, the evaluation of their antimicrobial activity was conducted using the agar well diffusion method, while cytotoxicity was assessed using the MTT test.ResultsThe extract from Sphingomonas sanguinis DM provided two distinct compounds: n-dibutyl phthalic acid (1) and Bis (2-methyl heptyl) phthalate (2) within its ethyl acetate fraction. Furthermore, the 16S rRNA gene sequence of Sphingomonas sanguinis DM has been registered under the NCBI GenBank database with the accession number PP422198. The bacterial extract exhibited its effect against gram-positive bacteria, inhibiting Streptococcus mutans (12.6 ± 0.6 mm) and Staphylococcus aureus (10.6 ± 0.6 mm) compared to standard antibiotics. Conversely, compound 1 showed a considerable effect against phytopathogenic fungi such as Alternaria alternate (56.3 ± 10.6 mm) and Fusarium oxysporum (21.3 ± 1.5 mm) with a MIC value of 17.5 µg/mL. However, it was slightly active against Klebsiella pneumonia (11.0 ± 1.0 mm). Furthermore, compound 2 was the most active metabolite, having a significant antimicrobial efficacy against Rhizoctonia solani (63.6 ± 1.1 mm), Pseudomonas aeruginosa (16.7 ± 0.6 mm), and Alternaria alternate (20.3 ± 0.6 mm) with MIC value at 15 µg/mL. In addition, compound 2 exhibited the most potency against hepatocellular (HepG-2) and skin (A-431) carcinoma cell lines with IC50 values of 107.16 µg/mL and 111.36 µg/mL, respectively.ConclusionSphingomonas sanguinis DM, a rhizosphere bacterium of Datura metel, was studied for its phytochemical and biological characteristics, resulting in the identification of two compounds with moderate antimicrobial and cytotoxic activities.

Biomaterials in Cancer Therapy: Investigating the Interaction between Kaempferol and Zinc Ions through Computational, Spectroscopic and Biological Analyses

A complex of the natural flavonoid kaempferol with zinc (Kam-Zn) was synthesized, and its physicochemical properties were investigated using spectroscopic methods such as Fourier transform infrared spectroscopy (FT-IR), ultraviolet–visible (UV-Vis) spectroscopy and theoretical chemistry. Biological studies were conducted to evaluate the cytotoxic and antiproliferative effects of these complexes on MCF-7 breast cancer cells. Treatment with Kam 100 µM (84.86 ± 7.79%; 64.37 ± 8.24%) and Kam-Zn 100 µM (91.87 ± 3.80%; 87.04 ± 13.0%) showed no significant difference in proliferation between 16 h and 32 h, with the gap width remaining stable. Both Kam-Zn 100 μM and 200 μM demonstrated effective antiproliferative and cytotoxic activity, significantly decreasing cell viability and causing cell death and morphology changes. Antioxidant assays revealed that Kam (IC50 = 5.63 ± 0.06) exhibited higher antioxidant potential compared to Kam-Zn (IC50 = 6.80 ± 0.075), suggesting that zinc coordination impacts the flavonoid’s radical scavenging activity by the coordination of metal ion to hydroxyl groups. Computational studies revealed significant modifications in the electronic structure and properties of Kam upon forming 1:1 complexes with Zn2+ ions. Spectroscopy analyses confirmed structural changes, highlighting shifts in absorption peaks and alterations in functional group vibrations indicative of metal–ligand interactions. FT-IR and UV-Vis spectra analysis suggested that Zn coordinates with the 3-OH and 4C=O groups of ligand. These findings suggest that the Kam-Zn complex exhibits interesting antiproliferative, cytotoxic and modified antioxidant effects on MCF-7 cells, providing valuable insights into their structural and anticancer properties.

Trimeric and Tetrameric Cationic Styryl Dyes as Novel Fluorescence and CD Probes for ds-DNA and ds-RNA

The wide use of mono- or bis-styryl fluorophores in biomedical applications prompted the presented design and study of a series of trimeric and tetrameric homo-analogues, styryl moieties arranged around a central aromatic core. The interactions with the most common biorelevant targets, ds-DNA and ds-RNA, were studied by a set of spectrophotometric methods (UV-VIS, fluorescence, circular dichroism, thermal denaturation). All studied dyes showed strong light absorption in the 350–420 nm range and strongly Stokes-shifted (+100–160 nm) emission with quantum yields (Φf) up to 0.57, whereby the mentioned properties were finely tuned by the type of the terminal cationic substituent and number of styryl components (tetramers being red-shifted in respect to trimers). All studied dyes strongly interacted with ds-DNA and ds-RNA with 1–10 nM−1 affinity, with dye emission being strongly quenched. The tetrameric analogues did not show any particular selectivity between ds-DNA or ds-RNA due to large size and consequent partial, non-selective insertion into DNA/RNA grooves. However, smaller trimeric styryl series showed size-dependent selective stabilization of ds-DNA vs. ds-RNA against thermal denaturation and highly selective or even specific recognition of several particular ds-DNA or ds-RNA structures by induced circular dichroism (ICD) bands. The chiral (ICD) selectivity was controlled by the size of a terminal cationic substituent. All dyes entered efficiently live human cells with negligible cytotoxic activity. Further prospects in the transfer of ICD-based selectivity into fluorescence-chiral methods (FDCD and CPL) is proposed, along with the development of new analogues with red-shifted absorbance properties.

Cymbopogon proximus phytochemicals induce S-phase arrest in A549 lung cancer cell lines via CDK2/cyclin A2 inhibition: gas chromatography-mass spectrometry and molecular docking analyses.

Cymbopogon proximus comprises several phytoconstituent classes that are reported to possess anticancer activity; however, studies on the anticancer potentials of theplant are lacking. C.proximus was extracted using solvents with increasing polarity. In-vitro cytotoxic activity of C.proximus extracts was examined against liver (HepG2), lung (A549), prostate (PC3), and bone (MG63) cell lines using MTT assay in comparison to doxorubicin. Flow cytometry was used to analyze the cell cycle for identification of the phase of inhibition. Chemical composition of the most active fraction was examined using the GC/MS technique. Molecular docking was used to explore the mechanism of cytotoxicity against A549, and the results were confirmed by Western blot analysis. Petroleum ether fraction was the highly effective fraction against A549 with IC50=14.02±2.79. GC/MS analysis of Pet.Eth led to the identification of nine compounds in unsaponifiable matter and 27 components in the saponifiable fraction. Di-N-octyl phthalate, 3-β-hydroxylean-11.13(18)-dien-30-oic acid methyl ester, elemol hydrocarbons, linoelaidic acid and linoleic acid demonstrated the lowest docking binding scores and similar binding modes against CDK2 as compared to that attained by the native ligand R-Roscovitine "CDK2 ATP inhibitor". Western blot analysis demonstrated that CDK2/cyclinA2 protein expression has been suppressed in A549 cell lines by Pet.Eth fraction.

Exploring the Composition and Bioactivity of Hedychium flavum Leaf and Stem Essential Oil: In Vitro Assessment of Antibacterial, Antioxidant, Cytotoxicity, and Enzyme Inhibitory Activities

Hedychium flavum is an edible, medicinal, and aromatic plant widely cultivated for its essential oil. So far, little studies have been done on its phytoconstituents and bioactivities. Hence, the research aimed to determine the chemical constituents of leaf essential oil (L-EO) and stem essential oil (S-EO) of H. flavum and first estimate their antibacterial, antioxidant, cytotoxic, and enzyme inhibitory activities. According to gas chromatography-flame ionization detector/mass spectrometer (GC-FID/MS) assay, L-EO was mainly composed of β-pinene (33.4%), α-pinene (10.4%), humulene (6.8%), β-caryophyllene (6.0%), eucalyptol (6.0%), caryophyllene oxide (5.5%), endo-borneol (3.8%), humulene epoxide II (3.7%), and D-limonene (3.2%). The predominant components of S-EO were β-pinene (17.2%), eucalyptol (9.7%), nerolidol (7.8%), α-phellandrene (6.7%), α-pinene (5.8%), β-caryophyllene (5.4%), terpinen-4-ol (4.5%), D-limonene (4.4%), p-cymene (3.7%), endo-borneol (3.5%), and α-terpineol (3.5%). For the bioactivities, L-EO and S-EO showed strong antibacterial activity against Escherichia coli, Enterococcus faecalis, and Bacillus subtilis with the minimum inhibitory concentration (MIC) of 9.77–625.00 µg/mL and the minimum bactericidal concentration (MBC) of 9.77–1250.00 µg/mL. Both L-EO and S-EO exhibited moderate antioxidant activity in the DPPH (14.52 ± 0.93 mg/mL and 4.73 ± 0.15 mg/mL, respectively) and ABTS (4.05 ± 0.75 mg/mL and 2.38 ± 0.14 mg/mL, respectively) free radical scavenging capacity. S-EO showed selective cytotoxicity on human leukemic K562 cell line (IC50 = 93.94 ± 0.91 µg/mL), which was nearly three times that of noncancer L929 cell line (IC50 = 294.49 ± 9.40 µg/mL). In enzyme inhibitory properties, L-EO exerted a potent inhibition on α-glucosidase (IC50 = 1.03 ± 0.02 mg/mL), and both essential oils had weak inhibition against cholinesterase and tyrosinase. Thus, H. flavum L-EO and S-EO possess antibacterial, antioxidant, cytotoxic, and enzyme inhibitory activities with potential for exploitation in the food, cosmetic, and pharmaceutical industries.