Preparation and characterization of withaferin A loaded pegylated nanoliposomal formulation with high loading efficacy: In vitro and in vivo anti-tumour study.

Withaferin A (WA) is a natural steroidal lactone with promising therapeutic applications. However, its clinical application is limited due to the low bioavailability and hydrophobic nature. In this study, we had prepared PEGylated nanoliposomal withaferin A (LWA) using thin-film hydration method. Dynamic light scattering, Transmission electron microscopy, and HPLC were used to investigate the impact of prepared formulations on the size, charge, morphology, and encapsulation efficiency of the LWA. The prepared nanoliposomal system had spherical vesicles, with the mean particle size of 125 nm and had an encapsulation efficiency of 83.65% with good stability. The characterization results indicated that nanoliposomal formulation is able to improve biocompatibility and bioavailability of WA. In vitro drug release study showed that LWA had an enhanced sustained drug release effect than the free drug. In vitro studies using ascites cell lines (DLA and EAC) showed that LWA treatment could induce apoptosis in ascites cells evidenced by acridine orange/ethidium bromide, Hoechst, and Giemsa staining. In vivo tumour study revealed that LWA treatment significantly reduced tumour growth and improved survival in DLA tumour bearing mice. In vivo results further demonstrated that LWA mitigated solid tumour development by regulating Ki-67 and cyclin D1 protein expression. The overall study results reveal that nanoliposome encapsulated WA exhibits therapeutic efficacy over WA in regulating tumour development as evidenced from ascites cell apoptosis as well as experimental tumour reduction studies.

Three new species of Impatiens (Balsaminaceae) from southern Western Ghats, Kerala.

Three new species of Impatiens, Impatiensachudanandanii, I.danii, and I.shailajae, are described from Thiruvananthapuram and Idukki districts of Kerala state (SW-India). Impatiensachudanandanii is similar to I.courtallensis and I.herbicola; I.danii to I.goughii and I.shailajae is to I.minae and I.scapiflora. The newly described taxa are readily distinguished from their allied species by unique character combinations, viz. shape of lateral sepal, lower sepal, dorsal petal, seed and pollen morphology. Detailed descriptions along with illustrations and photographs are provided.

Pyrazole (1, 2-diazole) induce apoptosis in lymphoma cells by targeting BCL-2 and BCL-XL genes and mitigate murine solid tumour development by regulating cyclin-D1 and Ki-67 expression.

Pyrazole or 1,2-Diazole is a five-membered heteroaromatic ring with two nitrogen atoms which is widely used in pharmacological research and organic synthesis. Several natural and synthetic pyrazole derivatives possess anti-cancer potential and some of them have underwent clinical trials. In this aspect, an investigation into the efficiency of the pyrazole nucleus to inhibit the growth and progression of various cancer cell lines/ experimental tumours would help in giving a better clarity to the anti-cancer behaviour of pyrazole containing drugs. This paper investigates the efficiency of pyrazole against Dalton's Lymphoma Ascites (DLA) cell line. Pyrazole inhibited the growth of DLA cells in vitro by committing them towards apoptosis. In vitro results were consistent in DLA induced murine solid tumour in vivo systems. Drug-treatment improved survival, reduced tumour loads, stabilized body weights and improved the haematological and serum biochemical parameters of DLA solid tumour bearing mice, thereby improving their overall survivability. Drug administration contained the aggravation of solid tumour by targeted downregulation of Cyclin-D1 and Ki-67. In addition, the mRNA expression levels of anti-apoptotic genes, BCL-2 and BCL-XL were downregulated in solid tumours, corroborating the in vitro results that pyrazole encourage apoptotic cell death in DLA cells. The new findings establish pyrazole as a potential anti-cancer drug candidate. The results must encourage future investigations into the efficacy of the drug against various cancer types.