Fenofibrate, an anti-hyperlipidemic drug and its phase-I biotransformed metabolite fenofibric acid, was studied for COX-1 (PDB ID: 3N8Y) and COX-2 (PDB ID: 1PXX) inhibition potentials in silico and in vitro for their effects on human recombinant COX-2 enzyme isolated from a Baculovirus expression system in sf21 cells (EC 1.14.99.1) using a conventional spectrophotometric assay. Furthermore, the compounds were also screened for their anti-inflammatory potentials in vivo using carrageenan-induced paw oedema method in Wistar rats. The test compounds fenofibric acid, fenofibrate, and the standard drug diclofenac exhibited binding energies of - 9.0, - 7.2, and - 8.0 kcal mol, respectively, against COX-2 and - 7.2, - 7.0, and - 6.5 kcal mol, respectively, against COX-1. In in vitro studies, both the test compounds inhibited COX-2 enzyme activity. Fenofibric acid showed an IC value of 48 nM followed by fenofibrate (82 nM), while diclofenac showed an IC value of 58 nM. Furthermore, under in vivo conditions in carrageenan-induced paw oedema rodent model, fenofibric acid exhibited relatively potent anti-inflammatory activity compared with fenofibrate. Hence, we conclude that fenofibric acid and fenofibrate are not only anti-hyperlipidemic but also shows potent anti-inflammatory activity, which may have an additional impact in the treatment of diabetic complications, viz., hyperlipidemia and inflammation leading to atherosclerosis.

The green synthesis of the platinum (Pt) nanocomposite was achieved using a natural biopolymer gum kondagogu (GK), a widely preferred reducing agent because of its biocompatible and biodegradable nature. The synthesised GK Pt nanoparticle (GKPtNP) were characterised by using different analytical techniques such as ultraviolet-visible spectrophotometer, transmission electron microscope, X-ray diffraction, and inductively coupled plasma mass spectroscopy (ICP-MS). The objective of the present work was to evaluate the anti-fungal activity of GKPtNP against two strains Aspergillus parasiticus and Aspergillus flavus for the first time. The results revealed that GKPtNP-treated fungal cell suspensions showed the minimum inhibitory concentration of 10 μg ml −1 for both the strains and exhibited IC 50 values as 37.2 and 29.4 μg ml −1 , against A. parasiticus and A. flavus. The mechanism of action of Pt nanocomposite on fungi outer membrane and generation of reactive oxygen species (ROS) was elucidated. It was observed that the interaction of GKPtNP caused destabilisation of fungal outer membrane signifying elevated levels of ROS leading to oxidative stress. In conclusion, the Pt nanocomposite materials acted as a fungicidal agent against A. parasiticus and A. flavus and give a significant scope in various biomedical applications.

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The molecular docking studies demonstrated the interactions of andrographolide to the crystal structure of HSA. The chromatographic and spectroscopic analysis confirmed the binding of andrographolide with HSA and their complex formation. Overall the present studies conclude the binding of andrographolide to HSA protein, favoring its pharmacokinetics.

A facile and green synthesis of platinum nanoparticles [gum kondagogu platinum nanoparticles (GKPtNP)] using biopolymer-gum kondagogu was developed. The formation of GKPtNP was confirmed by ultraviolet (UV)-visible spectroscopy, scanning electron microscopy-energy dispersive X-ray spectroscopy, transmission electron microscopy, X-ray diffraction, Zeta potential, Fourier transform infrared, inductively coupled plasma mass spectroscopy. The formed GKPtNP are well dispersed, homogeneous with a size of 2-4 ± 0.50 nm, having a negative zeta potential (−46.1 mV) indicating good stability. 5-Fluorouracil (5FU) was loaded onto the synthesised GKPtNP, which leads to the development of a new combination of nanomedicine (5FU-GKPtNP). The in vitro drug release studies of 5FU-GKPtNP in pH 7.4 showed a sustained release profile over a period of 120 min. Agrobacterium tumefaciens induced in vitro potato tumour bioassay was employed for screening the anti-tumour potentials of GKPtNP, 5FU, and 5FU-GKPtNP. The experimental results suggested a complete tumour inhibition by 5FU-GKPtNP at a lower concentration than the GKPtNP and 5FU. Furthermore, the mechanism of anti-tumour activity was assessed by their interactions with DNA using agarose gel electrophoresis and UV-spectroscopic analysis. The electrophoresis results revealed that the 5FU-GKPtNP totally diminishes DNA and the UV-spectroscopic analysis showed a hyperchromic effect with red shift indicating intercalation type of binding with DNA. Over all, the present study revealed that the combined exposure of the nanoformulation resulted in the enhanced anti-tumour effect.