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The present work was performed in order to study the mechanism of micellar thin layer chromatography (MTLC) and to develop a new simple and sensitive simultaneous MTLC method for separation of empagliflozin, Linagliptin and metformin hydrochloride ternary mixture. The study was done using three different surfactants; sodium dodecyl sulphate (SDS), benzalkonium chloride (BAC) and polysorbate 80 (tween 80). Chromatographic procedure was performed using micellar mobile phase that composed of aqueous solution of each surfactant and methanol (6: 4 v/v) and micellar TLC determination at λmax 237 nm. Separation using SDS (anionic surfactant) and BAC (cationic surfactant) depends on ionization potential (AMI-IP), partition coefficient (logP (o/w)) and hydrogen bond donor atoms (a-don), whereas separation using tween 80 depends mainly on the lipophilicity (RM0), solvation energy (E-sol) and Van der Waals energy (E-vdw). Quantitative structure–retention relationships study was carried out, modeled, evaluated and validated using molecular operating environment software.
Background: The search for natural anticancer agents is a worthy scientific research goal, driven by
the hope to lessen cancer's tremendous global burden.
Objective: This study aimed at evaluating the cytotoxic activity of Gardenia latifolia Ait. (Rubiaceae)
against lung (A549) and colon (HCT116) cancer cell lines. Cytotoxicity-guided isolation of the
bioactive phytochemicals was conducted, followed by various mechanistic validations of the appealing
cytotoxic metabolites.
Methods: The cytotoxic effects were determined using MTT assay. The two most cytotoxic compounds
were further evaluated for their effects on cell cycle progression and apoptotic capabilities using flow
cytometry approach. Additionally, we conducted a molecular docking analysis to reveal their potential
interactions with the human topoisomerase IIα.
Results: The phytochemical investigation led to isolation of nine compounds including a new one, (-)
1-acetyl 4,5-di-O-caffeoyl quinic acid. The latter compound was the most cytotoxic against the colon
cancer cell line (IC50 1.9 µg/ml) with a remarkable tumor-selectivity (SI ≈ 15). Moreover, the isolated
glycoside, 1-O-[6-O-(5-O-vanilloyl-β-ᴅ-apiofuranosyl)-β-ᴅ-glucopyranosyl]-3,4,5-trimethoxybenzene,
showed selective cytotoxicity towards A549 and HCT116 cells (IC50 values of 3.8 and 3.3 µg/ml,
respectively). Both compounds considerably affected the cell cycle distribution. They caused G2/M cell
cycle arrest, showed apoptotic capabilities, and displayed significant in silico topoisomerase IIα
inhibition.
Conclusion: Two cytotoxic and apoptotic compounds were reported from Gardenia latifolia.
Subsequent in vivo studies and clinical trials should be conducted to substantiate their anticipated
therapeutic values.
Promising cytotoxic effects of several Gardenia species (Rubiaceae) have been established
by many studies. The current study evaluated MTT-based cytotoxic activities of the crude
extract from Gardenia thunbergia L. f. aerial parts and four fractions thereof, including n-hexane, dichloromethane (DCM), ethyl acetate, and aqueous, against human leukemia (HL-60)
and hepatoma (HepG2) cell lines, as well as the normal (WI38) cell line. Both non-polar
fractions, n-hexane and dichloromethane, showed tumor-selective toxicities against both tested
cancerous cell lines. These results sparked our interest in chemically characterising these
bioactive fractions to reveal their cytotoxic components. The composition of n-hexane-soluble
fraction was investigated via GC-MS analysis, while column chromatographic separation was
used to isolate the components of DCM-soluble fraction. These isolated phytochemicals were
identified via spectroscopic analyses. Besides, the chemotaxonomic value of the detected
phytochemicals and their reported cytotoxic profiles were discussed
This meeting will be held in the office of Prof. Dr. / Dean of the College - Fifth Floor (Administrative Building).
Thymoquinone (TQ), a pleiotropic compound isolated from the seeds of Nigella sativa has a great potential as a chemotherapeutic agent against several cancers. However, its limited aqueous solubility and poor stability impede its clinical utility. To overcome these hurdles, TQ was encapsulated into spanlastics made using Span 60 and various edge activators. The spanlastics were evaluated for particle size, polydispersity index, zeta potential, drug entrapment efficiency and in vitro drug release. TQ anticancer efficacy was tested in vitro against breast cancer cell line MCF-7. TQ-loaded spanlastics had spherical shape, particle size in the range of 92–285 nm and negative zeta potential (around −12 to −25 mV). The particle size and zeta potential were greatly influenced by the type and concentration of used edge activator. Tween 80 spanlastics had the smallest particle size (around 90–110 nm). High drug entrapment efficiency was observed for all the tested edge activators (around 76–99 %) and it was possible to modulate it by varying the edge activator and drug concentrations. Drug release rate was also dependent on the type and concentration of the edge activator. Tween 80 spanlastics, used as an optimum formulation resulted in 11.5- and 5-fold increase in TQ cytotoxic efficacy against MCF-7 cells compared with the free drug and the drug loaded into conventional niosomes, respectively. These results confirm that Tween 80 spanlastics could be a promising nano-delivery system to enhance the anticancer efficacy of TQ or similar anticancer drugs.