In vivo and in vitro pharmacological activities\xa0of Tacca integrifolia rhizome and\xa0investigation of possible lead compounds against breast cancer through in silico approaches

Shahriar Ahmed,Arkajyoti Paul,Bibi Humayra Khanam,Mir Muhammad Nasir Uddin,Ahmed Rakib,S M Amanat Ullah,N M Mahmudul Alam Bhuiya,Md Ashiqul Islam,Md Nazim Uddin Chy,Md Atiar Rahman,Farhana Binta Faiz,Talha Bin Emran

doi:10.1186/s40816-019-0127-x

Abstract

BackgroundThe study was conducted to evaluate the analgesic, anti-inflammatory, antipyretic properties of ethanolic extract of Tacca integrifolia rhizome (EETI) in mice and cytotoxic effects in brine shrimp nauplii followed by a PASS prediction study for some isolated compounds of T. integrifolia. Additionally, this experiment included the in silico molecular docking and ADME/T property analyses of some phytochemicals.MethodsFormalin- induced paw licking test and acetic acid-induced writhing test for analgesic activity, carrageenan-induced paw edema test for anti-inflammatory potential and Brewer’s yeast-induced pyrexia test for antipyretic activity were applied. Antinociceptive and antineoplastic activity for breast cancer were revealed with PASS program. Schrodinger suite 2015 was used to evaluate the binding interaction and ADME/T properties of selected phytoconstituents with estrogen receptor alpha.ResultsIn formalin-induced paw licking test, EETI at the doses of 200 and 400 mg/kg BW showed highly significant inhibition of writhing in both neurogenic and inflammatory phases. While EETI also exhibited highly significant, compared to control, writhing inhibition for both the doses in acetic acid-induced writhing test. Moderate anti-inflammatory effect at a dose of 400 mg/kg BW was noticed in paw-edema test. It also showed 77.51% of maximum antipyretic effect which was significantly effective compared to standard drug paracetamol (150 mg/kg) in Brewer’s yeast-induced pyrexia test. The EETI showed potential cytotoxic activity with LC50 value of 114.46 μg/mL. The PASS prediction revealed the potential antinociceptive and antineoplastic activity of target compounds. The compounds betulinic acid, quercetin-3-α-arabinoside, catsanogenin were found to be effective in molecular docking study.ConclusionIt is evident that the EETI possesses highly significant analgesic activity with remarkable anti-inflammatory and antipyretic activity. The phytoconstituents have potential antinociceptive and antineoplastic (breast cancer) activity.Graphical abstract

Highlights

IntroductionInflammation, and fever are the most common features people suffer from. The search for medication against nociception, inflammation, and pyrexia is increasing day by day due to the unwanted effects of existing anti-inflammatory, analgesics and antipyretic drugs [1]
Pain, inflammation, and fever are the most common features people suffer from
We evaluated the pharmacological attributes of Tacca integrifolia Ker Gawl. (Family: Taccaceae)

Summary

Introduction

Inflammation, and fever are the most common features people suffer from. The search for medication against nociception, inflammation, and pyrexia is increasing day by day due to the unwanted effects of existing anti-inflammatory, analgesics and antipyretic drugs [1]. The brine shrimp lethality bioassay is an effective, quick and accessible that requires only a tiny amount of sample This bio-analysis has a good contextual connection with cytotoxic activity in solid tumors and possessed pesticidal activity. The study was conducted to evaluate the analgesic, anti-inflammatory, antipyretic properties of ethanolic extract of Tacca integrifolia rhizome (EETI) in mice and cytotoxic effects in brine shrimp nauplii followed by a PASS prediction study for some isolated compounds of T. integrifolia. This experiment included the in silico molecular docking and ADME/T property analyses of some phytochemicals

Methods

Results

Discussion

Conclusion