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Anti-inflammatory and ulcerogenic activity of newer phytoisolates of Swertia alata C.B. Clarke

Bajaj S, Wakode S, Kaur A, Fuloria S, Fuloria N

Nat Prod Res, 2021 Dec;35(23):5055-5065.
PMID: 32498574 DOI: 10.1080/14786419.2020.1775224

The present study was intended to evaluate the in vitro (COX-1/COX-2) and in vivo anti-inflammatory and ulcerogenic activity of newer phytoconstituents isolated from the aerial parts of Swertia alata C.B. Clarke (Gentianaceae). For isolation of newer phytoconstituents, the ethanolic extract of aerial parts of S. alata was subjected to column chromatography using mixture of petroleum ether and chloroform in various concentrations, which yielded two phytoisolates characterised as nonacosyl triacontanoate (SA-3) and 8-O-glucpyranosyl-(2-acetyl)-1,3-dihydroxy-5-methoxy-xanthone (SA-9). Identification of compounds was based on melting point, UV, FTIR, 1H-NMR, 13C-NMR and mass spectrometric data. The isolates were screened for in vitro COX-1/COX-2 inhibitory activity, in vivo anti-inflammatory and ulcerogenic activity. Among the two compounds, SA-3 was found to be more effective than SA-9. The ulcerogenic study revealed significant gastric tolerance of SA-3 and SA-9 in comparison to indomethacin.
Evidences of hepatoprotective and antioxidant effect of Citrullus colocynthis fruits in paracetamol induced hepatotoxicity

Vakiloddin S, Fuloria N, Fuloria S, Dhanaraj SA, Balaji K, Karupiah S

Pak J Pharm Sci, 2015 May;28(3):951-7.
PMID: 26004728

The objective of present study was to explore the hepatoprotective and antioxidant profile of Citrullus colocynthis fruits. Hepatoprotective profile of methanolic extract of Citrullus colocynthis fruits (MECCF) was investigated on rats, which were made hepatotoxic using paracetamol. The antioxidant profile of MECCF was evaluated by conducting Catalase, Super oxide Dismutase, Lipid Peroxidation and Diphenyl Picryl Hydrazyl tests. During hepatoprotective investigation, the Paracetamol treated group II showed significant increase in total bilirubin (TB), serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT) and alkaline phosphatase (ALP) level. The results so obtained showed that pretreatment of rats with MECCF 300mg/kg p.o. decreases the elevated TB, SGOT, SGPT and ALP serum levels. Also, MECCF inhibitory profile was found comparable with toxicant group (Paracetamol 2g/kg, p.o.). The present study concludes that MECCF fruit possess significant hepatoprotective and antioxidant activity.
Novel 9-(2-(1-arylethylidene)hydrazinyl)acridine derivatives: Target Topoisomerase 1 and growth inhibition of HeLa cancer cells

Haider MR, Ahmad K, Siddiqui N, Ali Z, Akhtar MJ, Fuloria N, et al.

Bioorg Chem, 2019 07;88:102962.
PMID: 31085373 DOI: 10.1016/j.bioorg.2019.102962

A series of 9-(2-(1-arylethylidene)hydrazinyl)acridine and its analogs were designed, synthesized and evaluated for biological activities. Various biochemical assays were performed to determine the free radical scavenging capacity of synthesized compounds (4a-4j). Anticancer activity of these compounds was assessed against two different human cancer cell lines viz cervical cancer cells (HeLa) and liver cancer cells (HepG2) as well as normal human embryonic kidney cell line (HEK 293). Compounds 4b, 4d and 4e showed potential anti-proliferative effects on HeLa cells. Based on results obtained from antioxidant and cytotoxicity studies, 4b, 4d and 4e were further studied in detail for different biological activities. 4b, 4d and 4e reduced the cell growth, inhibited metastatic activity and declined the potential of cell migration in HeLa cell lines. Topoisomerase1 (Top1) treated with compounds 4b, 4d and 4e exhibited inhibition of Top1 and prevented DNA replication. Molecular docking results validate that interaction of compounds 4b, 4d and 4e with Top1-DNA complex, which might be accountable for their inhibitory effects. Further it was concluded that compounds 4b, 4d and 4e arrests the cells at S phase and consequently induces cell death through DNA damage in HeLa cells.
Fulltext Evaluation of Antitumor Efficacy of Chitosan-Tamarind Gum Polysaccharide Polyelectrolyte Complex Stabilized Nanoparticles of Simvastatin

Malviya R, Raj S, Fuloria S, Subramaniyan V, Sathasivam K, Kumari U, et al.

Int J Nanomedicine, 2021;16:2533-2553.
PMID: 33824590 DOI: 10.2147/IJN.S300991

PURPOSE: The present study was intended to fabricate chitosan (Ch)-tamarind gum polysaccharide (TGP) polyelectrolyte complex stabilized cubic nanoparticles of simvastatin and evaluate their potential against human breast cancer cell lines.
MATERIALS AND METHODS: The antisolvent precipitation method was used for formulation of nanoparticles. Factorial design (32) was utilized as a tool to analyze the effect of Ch and TGP concentration on particle size and entrapment efficiency of nanoparticles.
RESULTS: Formulated nanoparticles showed high entrapment efficiency (67.19±0.42-83.36±0.23%) and small size (53.3-383.1 nm). The present investigation involved utilization of two biological membranes (egg and tomato) as biological barriers for drug release. The study revealed that drug release from tomato membranes was retarded (as compared to egg membranes) but the release pattern matched that of egg membranes. All formulations followed the Baker-Lansdale model of drug release irrespective of the two different biological barriers. Stability studies were carried out for 45 days and exhibited less variation in particle size as well as a reduction in entrapment efficiency. Simvastatin loaded PEC stabilized nanoparticles exhibited better control on growth of human breast cancer cell lines than simple simvastatin. An unusual anticancer effect of simvastatin nanoparticles is also supported by several other research studies.
CONCLUSION: The present study involves first-time synthesis of Ch-TGP polyelectrolyte complex stabilized nanoparticles of simvastatin against MCF-7 cells. It recommends that, in future, theoretical modeling and IVIVC should be carried out for perfect designing of delivery systems.