Antitumor Activity of Betulinic Acid and Betulin in Canine Cancer Cell Lines

Zhao, Jing; Li, Rongfang; Pawlak, Aleksandra; Henklewska, Marta; Sysak, Angelika; Wen, Lixin; Yi, Jine; Obmińska-Mrukowicz, Bożena

doi:10.21873/invivo.11349

Cited by 44 publications

(31 citation statements)

References 38 publications

(26 reference statements)

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“…The cell population increased in S-phase with increasing treatment time, with cells passing from G1-phase to S-phase while DNA synthesis stopped, showing a block at S-phase. This observation is also supported by the earlier literature reports on cytotoxic effect of BA on CL-1 and D17 cells 17 . Furthermore, a slight increase in G2/M ratio occurred due to an increase in treatment time.…”

Section: Resultssupporting

confidence: 91%

Nanoencapsulated betulinic acid analogue distinctively improves colorectal carcinoma in vitro and in vivo

Dutta

Paul

Mukherjee

et al. 2019

Sci Rep

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Betulinic acid, a plant secondary metabolite, has gained significant attention due to its antiproliferative activity over a range of cancer cells. A promising betulinic acid analogue ( 2c ) with better therapeutic efficacy than parent molecule to colon carcinoma cells has been reported. Despite impressive biological applications, low aqueous solubility and bioavailability create difficulties for its therapeutic applications. To overcome these lacunae and make it as a promising drug candidate we have encapsulated the lead betulinic acid derivative ( 2c ) in a polymeric nanocarrier system ( 2c-NP ) and evaluated its in vitro and in vivo therapeutic efficacy. Apoptosis that induces in vitro antiproliferative activity was significantly increased by 2c-NP compared to free-drug ( 2c ), as assured by MTT assay, Annexin V positivity, JC1 analysis and cell cycle study. The therapeutic potential measured in vitro and in vivo reflects ability of 2c-NP as an effective therapeutic agent for treatment of colon carcinoma and future translation to clinical trials.

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Section: Resultssupporting

confidence: 91%

Nanoencapsulated betulinic acid analogue distinctively improves colorectal carcinoma in vitro and in vivo

Dutta

Paul

Mukherjee

et al. 2019

Sci Rep

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“…In this study (+)-betulin exhibited significant cell growth inhibition in human breast cancer cells and in previous studies it did so against canine cancer cells (8). The present study demonstrated that (+)-betulin inhibits the NF-ĸB complex both in vitro (in MDA-MB-231 breast cancer cells), in vivo (in zebrafish) and in silico.…”

Section: Discussionsupporting

confidence: 76%

Apoptosis Induced by (+)-Betulin Through NF-κB Inhibition in MDA-MB-231 Breast Cancer Cells

et al. 2020

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“…Natural products are recognized as source of lead compounds for the pharmaceutical industry; an example of its active molecule is betulinic acid (BA), a pentacyclic lupane-type triterpenoid found in some plants (Figure 1). This compound is reported to be an antiviral agent and have antidiabetic, antitumoral, antihyperlipidemic, and anti-inflammatory activities [29,30,31,32,33,34]; however, the reports about its antimicrobial activity are controversial [35,36,37,38]. Taking into account the medicinal properties of BA, we evaluated its effects on the SOS response induced by ciprofloxacin, and evaluated whether this action was associated to a reduction of the progress of drug-tolerance in S. aureus .…”

Section: Introductionmentioning

confidence: 99%

Betulinic Acid Prevents the Acquisition of Ciprofloxacin-Mediated Mutagenesis in Staphylococcus aureus

et al. 2019

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The occurrence of damage on bacterial DNA (mediated by antibiotics, for example) is intimately associated with the activation of the SOS system. This pathway is related to the development of mutations that might result in the acquisition and spread of resistance and virulence factors. The inhibition of the SOS response has been highlighted as an emerging resource, in order to reduce the emergence of drug resistance and tolerance. Herein, we evaluated the ability of betulinic acid (BA), a plant-derived triterpenoid, to reduce the activation of the SOS response and its associated phenotypic alterations, induced by ciprofloxacin in Staphylococcus aureus. BA did not show antimicrobial activity against S. aureus (MIC > 5000 µg/mL), however, it (at 100 and 200 µg/mL) was able to reduce the expression of recA induced by ciprofloxacin. This effect was accompanied by an enhancement of the ciprofloxacin antimicrobial action and reduction of S. aureus cell volume (as seen by flow cytometry and fluorescence microscopy). BA could also increase the hyperpolarization of the S. aureus membrane, related to the ciprofloxacin action. Furthermore, BA inhibited the progress of tolerance and the mutagenesis induced by this drug. Taken together, these findings indicate that the betulinic acid is a promising lead molecule in the development helper drugs. These compounds may be able to reduce the S. aureus mutagenicity associated with antibiotic therapies.

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Antitumor Activity of Betulinic Acid and Betulin in Canine Cancer Cell Lines

Abstract: Both compounds showed an antitumor activity, and the effects of BA were stronger than that of BT.

Cited by 44 publications

References 38 publications

Nanoencapsulated betulinic acid analogue distinctively improves colorectal carcinoma in vitro and in vivo

Nanoencapsulated betulinic acid analogue distinctively improves colorectal carcinoma in vitro and in vivo

Apoptosis Induced by (+)-Betulin Through NF-κB Inhibition in MDA-MB-231 Breast Cancer Cells

Betulinic Acid Prevents the Acquisition of Ciprofloxacin-Mediated Mutagenesis in Staphylococcus aureus

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