CARDIOPROTECTIVE POTENTIAL OF QUERCETIN AGAINST DIESEL OR PETROL EXHAUST NANOPARTICLE INDUCED TOXICITY: A PROSPECTIVE IN VITRO PHARMACOLOGICAL STUDY IN H9C2 CELLS

Objective: Phytochemicals are known to elicit potential antioxidant activity. This study examined the cardioprotective effects of quercetin against oxidative damage to rat cardiomyocyte cells (H9c2) after treatment with Diesel Exhaust Nanoparticles (DEPs) or Petrol Exhaust Nanoparticles (PEPs). Methods: Cardiomyocyte cells were exposed to DEPs or PEPs alone and in a combination with quercetin for 24 h. Results: Results showed that quercetin had no lethal effect on H9c2 cells up to a concentration of 1.0 μg/ml. Exposure to DEPs (4.0 μg/ml) or PEPs (10.0 μg/ml) induced cytotoxicity, oxidative stress, and inflammation (p<0.05). It also provoked lipid peroxidation by an increase in MDA and a decrease in SOD activity and glutathione activity (p<0.05). Simultaneous addition of quercetin restored these parameters to near normal. Conclusion: These results thus specify that quercetin plays a protective role in cardiac cells exposed to DEPs and PEPs

In silico analysis of cubebinol for evaluating its efficiency against menacing respiratory ailments

Over the recent decade a survey states that the advent of respiratory diseases had took a rapid transmittance and transformation rate. The mortality and the morbidity rates were also exorbitant. Piper cubeba is one of the traditional plant species belongs to Piperacea family, which possess good antibacterial activity. The plant comprise of several phytocomponent one among which is cubebinol, whose specific activities have not been much explored. Hence it is subjected in this research and its antibacterial efficiency is investigated through virtual screening technique. Techniques like Auto dock, Discovery studio, Pymol are evolved in the investigation to know the unknown nature of the phytocomponent by analyzing its binding affinity along with the major respiratory disease causing organism’s macromolecules. Thus it manifests the efficiency and the potency of the plant phytocomponent, which is found to be better than that of the readily available and commercially consumed drug molecules. By both the pharmacokinetic test as well as the docking validation we found that the docked ligand compound cubebinol is a potent drug against several fatal bacterial respiratory diseases

EXTRACTION AND ISOLATION OF FLAVONOID QUERCETIN FROM THE LEAVES OF TRIGONELLA FOENUM-GRAECUM AND THEIR ANTI-OXIDANT ACTIVITY

Objective: The present study was designed for isolation of bioactive flavonoid molecule quercetin from the leaves of Trigonella foenum-graecum and their subsequent characterization. Methods: Crude extracts of fenugreek were prepared using various solvents such as hexane, ethyl acetate, and ethanol. The plant extracts were subjected for photochemical analysis and total flavonoid content. The extracts were then subjected to column chromatography followed by TLC. The isolated compound was subjected to FT-IR, 1H NMR, 13C NMR, mass spectroscopy and their free radical scavenging activity was studied.Results: The ethanol extract showed the presence of higher flavonoid content when compared with other solvent extracts. The ethanol extract was subjected to fractionalization by column chromatography. The eluted fractions were run in TLC mobile phase with the different solvent ratio. The fractions showed Rf value equal to standard quercetin in TLC were combined and crystallized. The characterization techniques confirmed that the isolated compound was found to be quercetin. The free radical scavenging activity suggests that the isolated compound quercetin could act as a potent source of antioxidants.Conclusion: The flavonoid quercetin was isolated effectively from the leaves of Trigonella foenum-graecum and their antioxidant activity was studied.Keywords: Antioxidant activity, DPPH, Flavonoids, NMR, Querceti

ACUTE DERMAL TOXICITY OF COAL FLY ASH NANOPARTICLES IN VIVO

Objectives: To study the toxicity effects of coal fly ash nanoparticles-induced acute dermal toxicity in Wistar albino rats.Methods: Acute dermal toxicity studies for coal fly ash nanoparticles (CFA-NPs) were conducted in Wistar albino rats. A single dose of various concentrations of CFA-NPs or vehicle was applied on the dorsal layer after shaving. Animals were observed for 14 days. Parameters like body weight, feed intake and histopathology were studied.Results: The CFA-NPs treated rats did not show any abnormal clinical signs. The body weight was not significantly altered when compared with the control group. Treatment with CFA-NPs showed mild to severe histological changes in all organs with increase dose-related manner in concentrations of CFA-NPs treated groups. The acute dermal LD50 of CFA-NPs was found to be greater than 2000 mg/kg body weight (bw) for rats.Conclusion: Dermal acute treatment with CFA-NPs can induce mild to significant dose-dependent histological changes in biological organs.Â

QUERCETIN, ENCAPSULATED QUERCETIN AND ITS APPLICATION- A REVIEW

Flavonoids are plant secondary metabolite shows a wide range of pharmacological and biological functions. Among the flavonoids, quercetin gained special attention for its potential therapeutic activities. The aim of this work was to summarize the medicinal property of quercetin, role of quercetin in synthesizing the silver and gold nanoparticles, pros and cons of quercetin, nanoencapsulation of quercetin and its advantages. This review article summarizes the published experimental research and scientific literature from the databases including PubMed, Google and local library searches. The results of these studies provide a complete understanding of the biological action of quercetin. Pharmaceutical effects of quercetin such as anti-oxidant, anti-inflammatory, anti-cancer, anti-toxic and immunomodulatory effects prove that quercetin has potential therapeutic value, though it has several beneficial effects on human health, it possesses some disadvantages like poor solubility, low bioavailability, the hydrophobic nature and poor permeability. To overcome the disadvantages of quercetin, it is encapsulated in the polymers to enhance its bioavailability and to increase its solubility. In this paper, a brief description about the encapsulation of quercetin and its application were focused

EVALUATION OF CYTOTOXICITY, OXIDATIVE STRESS, NUCLEAR CHANGES AND PRO-INFLAMMATORY CYTOKINES INDUCED BY MONOCROTOPHOS IN HUMAN KERATINOCYTE CELLS IN VITRO

Objective: This study was explored to identify the toxicological behaviour of monocrotophos against human keratinocyte cells (HaCaT cells) Methods: In this study HaCaT cell line was used to identify the inflammatory effect of monocrotophos on cell viability, nitric oxide secretion (NO), lactate dehydrogenase release (LDH), malondialdehyde release (MDA), nuclear changes, reactive oxygen species generation and cytokine expressionResults: From the in vitro cell viability study, it appears that the monocrotophos was toxic to HaCaT cells; IC50 value was 408.2 µg/mL during 24 h of incubation period. Significant increase in NO, LDH, MDA, nuclear changes, pro-inflammatory cytokine and ROS generation was observed compared with the control. 1/5th IC50 value treatment of HaCaT cells with monocrotophos resulted in 9.97, 8.78 and 9.45 times increase in TNF-α, IL-6 and IL-8 expression higher than the control.Conclusion: This study gives perceptiveness about the toxicity of monocrotophos and provides wide acquaintance to restrict the use of monocrotophos.Â

TRANSDERMAL PATCHES OF CHITOSAN NANOPARTICLES FOR INSULIN DELIVERY

Objectives: To develop a nanoparticle system with Chitosan for transdermal delivery of insulin.Methods: Chitosan and Tripolyphosphate (TPP) were used to prepare the insulin loaded chitosan nanoparticles based on ionotropic gelation method and characterized using Zeta-sizer Nano ZS, Scanning electron microscopy and Optical Microscope. Transdermal drug delivery system of the formulated Insulin-chitosan Nanoparticles was prepared using solvent casting method.Results: The results indicated that the nanoparticles were in the size range of 465 and 661 nm and exhibited quasi circular structure with better encapsulation efficiency. Controlled release Transdermal patches of insulin–chitosan nanoparticles were prepared using the polymer combinations HPMC, PVP K30 and PEG 400 with Tween 80 as plasticizer. The release rate of drug through patched increased simultaneously as the concentration of hydrophilic polymer was increased.Conclusion: The encapsulated insulin drug was very effectively released by patch F3.Â

<span style="font-size:15.0pt;mso-bidi-font-size:12.0pt;mso-bidi-font-weight:bold" lang="EN-GB">Characterization of coal fly ash nanoparticles and their induced <i style="mso-bidi-font-style: normal">in vitro</i> cellular toxicity and oxidative DNA damage in different cell lines </span>

585-593Coal combustion generates considerable amount of ultrafine particles and exposure to such particulate matter is a major health concern in the developing countries. In this study, we collected nano sized coal fly ash (CFA) and characterized them by scanning electron microscope-energy dispersive X-ray analysis (SEM-EDX), particle size analyzer (PSA) and transmission electron microscope (TEM), and investigated its toxicity in vitro using different cell lines. The imaging techniques showed that the coal fly ash nanoparticles (CFA-NPs) are predominately spherical shaped. The analyses have revealed that the CFA-NPs are 7-50 nm in diameter and contain several heavy metals associated with CFA particles. The studies showed significant amount of toxicity in all cell lines on treatment with CFA-NPs. The cytotoxicity and oxidative DNA damage caused by CFA-NPs were determined by inhibition of cellular metabolism (MTT), total intracellular glutathione (GSH), reactive oxygen species (ROS) and DNA fragmentation in cultured cell lines (Chang liver, HS294T and LL29). The cellular metabolism was inhibited in a dose-dependent manner in CFA-NPs treated cell lines. The CFA-NPs induced ROS and decreased the total intracellular glutathione with increased dose. Further, the CFA-NPs treated cells showed severe DNA laddering as a result of DNA fragmentation. </span

SYNTHESIS AND CHARACTERIZATION OF POLY D-L LACTIDE (PLA) NANOPARTICLES FOR THE DELIVERY OF QUERCETIN

Objectives: Synthesis and optimization of Poly D-L Lactide (PLA) nanoparticles for the delivery of an antioxidant molecule quercetin.Methods: The quercetin was encapsulated by PLA nanoparticles by nanoprecipitation method. The average particle size and the electric charge for different formulations were measured by particle size and zeta potential analyzer. The quercetin loaded PLA nanoparticles (Q-PLAN) was characterized by differential scanning calorimetry &amp; Fourier transform-Infra red spectroscopy, Scanning electron microscopy and Atomic force microscopy. The average drug content, encapsulation efficiency and drug release studies were carried out for different formulations of Q-PLAN. The antioxidant activity of the formulated Q-PLAN nanoparticles was tested using DPPH assay.Results: The formulation F3 (Quercetin 75 mg: PLA 200 mg) was found to be optimized formulation based on particle size analysis, Zeta potential, drug content, encapsulation efficiency and drug release studies. The mean diameter and zeta potential of optimized Q-PLAN and PLA nanoparticles were found to be 242±20 nm, 185±10 nm and-22.5±1.5 mV,-20.5±1.0 mV. The F3 formulation showed encapsulation efficiency of 73.3% and 5.5±0.06 mg/ml of actual drug loading. The F3 formulations showed 99.7% of drug release. The optimized Q-PLAN showed better scavenging effects when compared to the free quercetin.Conclusions: The poor aqueous solubility and stability of the antioxidant molecule quercetin have been improved by entrapping the quercetin molecules into the PLA nanoparticles.Â