Atranorin, an antimicrobial metabolite from lichen <i>Parmotrema rampoddense</i> exhibited in vitro anti-breast cancer activity through interaction with Akt activity

Harikrishnan, Adhikesavan; Veena, V.; Lakshmi, Baddireddi Subhadra; Shanmugavalli, R.; Theres, Sonia; Prashantha, C. N.; Shah, Tanya; Oshin, K.; Togam, Ringu; Nandi, Sisir

doi:10.1080/07391102.2020.1734482

Cited by 19 publications

(24 citation statements)

References 40 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A lichen, Parmelia sulcata Taylor, exhibited promising anticancer activity against breast cancer cells and a genotoxic effect on human lymphocytes [ 22 ]. In addition to lichen extracts, atranorin, a metabolite isolated from lichens including Stereocaulon cacspitorim , Everniastrum vexans , and Parmatrema species, exhibited anti-breast cancer activity on MDA-MB-231 and MCF-7 cells through an effect on Akt activity [ 23 ].…”

Section: Discussionmentioning

confidence: 99%

Induction of Apoptosis in MDA-MB-231 Cells Treated with the Methanol Extract of Lichen Physconia hokkaidensis

Noh

Mun

Lim

et al. 2021

JoF

View full text Add to dashboard Cite

Physconia hokkaidensis methanol extract (PHE) was studied to identify anticancer effects and reveal its mechanism of action by an analysis of cytotoxicity, cell cycles, and apoptosis biomarkers. PHE showed strong cytotoxicity in various cancer cells, including HL-60, HeLa, A549, Hep G2, AGS, MDA-MB-231, and MCF-7. Of these cell lines, the growth of MDA-MB-231 was concentration-dependently suppressed by PHE, but MCF-7 was not affected. MDA-MB-231 cells, triple-negative breast cancer (TNBC) cells, do not express estrogen receptor (ER), progesterone receptor (PR), and human epidermal growth factor receptor 2 (HER-2), whereas MCF-7 cells are ER-positive, PR-positive, and HER-2-negative breast cancer cells. The number of cells in sub-G1 phase was increased after 24 h of treatment, and annexin V/PI staining showed that the population size of apoptotic cells was increased by prolonged exposure to PHE. Moreover, PHE treatment downregulated the transcriptional levels of Bcl-2, AMPK, and p-Akt, whereas it significantly upregulated the levels of cleaved caspase-3, cleaved caspase-9, and cleaved-PARP. In conclusion, it was confirmed that the PHE exhibited selective cytotoxicity toward MDA-MB-231, not toward MCF-7, and its cytotoxic activity is based on induction of apoptosis.

show abstract

Section: Discussionmentioning

confidence: 99%

Induction of Apoptosis in MDA-MB-231 Cells Treated with the Methanol Extract of Lichen Physconia hokkaidensis

Noh

Mun

Lim

et al. 2021

JoF

View full text Add to dashboard Cite

show abstract

“…The table reports the drug, its target with Protein Data Bank (PDB) ID, the in silico/in vitro/in vivo methods used to test the drug, clinical trials, the original use, and the reference. In an another study, the interactions of atranorin (ATR), a metabolite of many lichens, with the target proteins that are overexpressed in BC, such as AKT, BCL-2, BAX, BCL-W, and BCL-XL, were studied with docking and in vitro analyses [35]. Commonly, ATR is metabolite present in numerous lichens such as Stereocaulon cacspitorim, Everniastrum vexans, Parmatrema species, and others [35].…”

Section: Natural Moleculesmentioning

confidence: 99%

“…In an another study, the interactions of atranorin (ATR), a metabolite of many lichens, with the target proteins that are overexpressed in BC, such as AKT, BCL-2, BAX, BCL-W, and BCL-XL, were studied with docking and in vitro analyses [35]. Commonly, ATR is metabolite present in numerous lichens such as Stereocaulon cacspitorim, Everniastrum vexans, Parmatrema species, and others [35]. The complex formed by ATR and AKT shows a better binding energy, but interacting residues show minor affinities to inhibiting the overexpression of BC biomarkers.…”

Section: Natural Moleculesmentioning

confidence: 99%

See 1 more Smart Citation

Integration of Molecular Docking and In Vitro Studies: A Powerful Approach for Drug Discovery in Breast Cancer

Cava

Castiglioni

2020

Applied Sciences

View full text Add to dashboard Cite

Molecular docking in the pharmaceutical industry is a powerful in silico approach for discovering novel therapies for unmet medical needs predicting drug–target interactions. It not only provides binding affinity between drugs and targets at the atomic level, but also elucidates the fundamental pharmacological properties of specific drugs. The purpose of this review was to illustrate newer and emergent uses of docking when combined with in vitro techniques for drug discovery in metastatic breast cancer. We grouped the selected articles into five main categories; namely, systematic repositioning of drugs, natural drugs, new synthesized molecules, combinations of drugs, and drug latentiation. We focused on new promising drugs that have a good affinity with their targets, thus inducing a favorable biological response. This review suggests that the integration of molecular docking and in vitro studies can accelerate cancer drug discovery showing a good consistency of the results between the two approaches.

show abstract

“…About 20% of all known fungi are thought to have been lichenized and nearly 98% of them belong to the phylum Ascomycota [ 5 , 6 , 7 ]. As much as their species diversity, lichens produce a variety of secondary metabolites [ 8 ] that exhibit antitumor [ 9 , 10 , 11 ], antimicrobial [ 12 , 13 , 14 , 15 , 16 , 17 ], anti-inflammatory [ 18 , 19 , 20 ], and antioxidant activities [ 13 , 14 , 17 , 19 ], most of these bioactive compounds are considered to be originated from mycobionts. However, there have been a very few studies focusing on the ecological roles of these lichen secondary metabolites; some studies provide evidence that lichen secondary metabolites have contributed to adapting to harsher habitats [ 21 ] and deterring herbivores [ 22 , 23 ].…”

Section: Introductionmentioning

confidence: 99%

Establishment of Agrobacterium tumefaciens-Mediated Transformation of Cladonia macilenta, a Model Lichen-Forming Fungus

Kim

Paguirigan

Jeong

et al. 2021

JoF

View full text Add to dashboard Cite

Despite the fascinating biology of lichens, such as the symbiotic association of lichen-forming fungi (mycobiont) with their photosynthetic partners and their ability to grow in harsh habitats, lack of genetic tools manipulating mycobiont has hindered studies on genetic mechanisms underpinning lichen biology. Thus, we established an Agrobacterium tumefaciens-mediated transformation (ATMT) system for genetic transformation of a mycobiont isolated from Cladonia macilenta. A set of combinations of ATMT conditions, such as input biomass of mycobiont, co-cultivation period with Agrobacterium cells, and incubation temperature, were tested to identify an optimized ATMT condition for the C. macilenta mycobiont. As a result, more than 10 days of co-cultivation period and at least 2 mg of input biomass of the mycobiont were recommended for an efficient ATMT, owing to extremely slow growth rate of mycobionts in general. Moreover, we examined T-DNA copy number variation in a total of 180 transformants and found that 88% of the transformants had a single copy T-DNA insertion. To identify precise T-DNA insertion sites that interrupt gene function in C. macilenta, we performed TAIL-PCR analyses for selected transformants. A hypothetical gene encoding ankyrin repeats at its C-terminus was interrupted by T-DNA insertion in a transformant producing dark-brown colored pigment. Although the identification of the pigment awaits further investigation, this proof-of-concept study demonstrated the feasibility of use of ATMT in construction of a random T-DNA insertion mutant library in mycobionts for studying genetic mechanisms behind the lichen symbiosis, stress tolerance, and secondary metabolite biosynthesis.

show abstract

Atranorin, an antimicrobial metabolite from lichen Parmotrema rampoddense exhibited in vitro anti-breast cancer activity through interaction with Akt activity

Cited by 19 publications

References 40 publications

Induction of Apoptosis in MDA-MB-231 Cells Treated with the Methanol Extract of Lichen Physconia hokkaidensis

Induction of Apoptosis in MDA-MB-231 Cells Treated with the Methanol Extract of Lichen Physconia hokkaidensis

Integration of Molecular Docking and In Vitro Studies: A Powerful Approach for Drug Discovery in Breast Cancer

Establishment of Agrobacterium tumefaciens-Mediated Transformation of Cladonia macilenta, a Model Lichen-Forming Fungus

Contact Info

Product

Resources

About