Cytotoxic effects of natural and semisynthetic cucurbitacins on lung cancer cell line A549

Silva, Izabella Thaís; Geller, Fabiana Cristina; Persich, Lara; Dudek, Sabine Eva; Lang, Karen L.; Balparda, Miguel Soriano; Durán, Fernando Javier; Schenkel, Eloir Paulo; Ludwig, Stephan; Simões, Cláudia Maria Oliveira

doi:10.1007/s10637-015-0317-4

Cited by 26 publications

(13 citation statements)

References 44 publications

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“…Induction of apoptosis was determined by Annexin V-FITC assay as described previously [14]. MCF-7 human breast cancer cells were seeded in 6-well plates at a cell density of 2 × 10 6 cells per ml, incubated for 12 h and then treated with varying doses (0, 10, 50 and 100 μM) of glycyrrhizinic acid for 48 h. The cells were then harvested via trypsinization and then washed with PBS twice, resuspended and 250 μl of binding buffer comprising 20 μl each of Annexin V-FITC and propidium iodide was added to the cells.…”

Section: Apoptosis Quantification Using Annexin V-fitc Assaymentioning

confidence: 99%

Antiproliferative and apoptotic activity of glycyrrhizinic acid in MCF-7 human breast cancer cells and evaluation of its effect on cell cycle, cell migration and m-TOR/PI3K/Akt signalling pathway

Zhang¹,

Feng²,

Li³

et al. 2019

aoms

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IntroductionGlycyrrhizinic acid is a natural product of pharmacological relevance and its anticancer activity against breast cancer cell lines has not been evaluated. Therefore the main purpose of the present study was to investigate the anticancer effects of glycyrrhizinic acid in MCF-7 human breast cancer cells.Material and methodsThe MTT assay was used to evaluate the anticancer effects while a clonogenic assay was used to study its effects on colony formation tendency. Flow cytometry was used to study the effects on cell cycle phase distribution and apoptosis. Western blot assay was used to study changes in protein expression of the m-TOR/PI3K/Akt pathway.ResultsThe results indicated that glycyrrhizinic acid caused significant (p < 0.01). The growth inhibitory effects MCF-7 human breast cancer cells. The growth inhibitory effects of glycyrrhizinic acid exhibited concentration-dependent as well as time-dependent growth inhibitory trend. Different doses of glycyrrhizinic acid had a tendency to significantly (p < 0.01) inhibit the colony formation tendency of MCF-7 cells. As compared to the control group, glycyrrhizinic acid-treated cells showed a high percentage of apoptotic cells. Cells treated with a 10, 50 and 100 µM dose of glycyrrhizinic acid led to a 24.3%, 41.5% and 82.1% increase in the sub-G1 phase (apoptotic) cells. Glycyrrhizinic acid also led to significant (p < 0.01) inhibition of cell invasion along with downregulation of m-TOR/PI3K/Akt protein expression.ConclusionsGlycyrrhizinic acid inhibited MCF-7 human breast cancer cell growth and therefore may prove essential lead molecule in the treatment of breast cancer.

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Section: Apoptosis Quantification Using Annexin V-fitc Assaymentioning

confidence: 99%

Antiproliferative and apoptotic activity of glycyrrhizinic acid in MCF-7 human breast cancer cells and evaluation of its effect on cell cycle, cell migration and m-TOR/PI3K/Akt signalling pathway

Zhang¹,

Feng²,

Li³

et al. 2019

aoms

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“…Naturally derived compounds play a very paramount role in pharmaceutical industry and act as a template for synthetic and semi-synthetic modification. Most of the drugs used in the cancer therapy have been extracted from the natural resources but at the same time separation and purification of these bioactive compounds is the most crucial process 15 . Various extraction techniques such as continuous shaking extraction (CSE), microwave assisted extraction (MAE), Soxhlet extraction (SE), ultrasound assisted extraction (UAE) and steam bath assisted extraction (SBAE) have been used for the isolation of bioactive compound.…”

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confidence: 99%

Efficient extraction of cucurbitacins from Diplocyclos palmatus (L.) C. Jeffrey: Optimization using response surface methodology, extraction methods and study of some important bioactivities

Patel

Attar

Sakate

et al. 2020

Sci Rep

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Diplocyclos palmatus (L.) C. Jeffrey is an important medicinal plant used in several reproductive medicines. It serves as a wide source of tetracyclic triterpens called cucurbitacins. Response surface methodology (RSM) with Box-Behnken design (BBD) was studied to optimize the production of cucurbitacins. RSM put forth the ideal conditions such as 1:30 SS ratio (g/mL), 80 rpm (mixing extraction speed), 150 µm mean particle size, 30 min extraction time and 50 °C using chloroform in continuous shaking extraction (CSE) and showed the highest cucurbitacin I (CUI) content (2.345 ± 0.1686 mg/g DW). Similarly, the highest yield of cucurbitacin B (CUB) (1.584 ± 0.15 mg/g DW) was recorded at ideal conditions (1:40 g/mL SS ratio and 60 min time and others similar to CUI). Among the tested extraction methods, the highest CUI, CUB, and CUI + B yield (1.437 ± 0.03, 0.782 ± 0.10, 2.17 ± 0.35 mg/g DW, respectively) as well as promising DPPH radical scavenging activity (25.06 ± 0.1 µgAAE/g DW) were recorded from the SBAE (steam bath assisted extraction). In addition, MAE and UAE revealed the highest inhibition of α-amylase (68.68%) and α-glucosidase (56.27%) enzymes, respectively. Fruit extracts showed potent anticancer activity against breast (MCF-7) and colon (HT-29) cancer cell lines (LC 50 -44.27 and 46.88 µg/mL, respectively). Our study proved that SS ratio, particle size and temperature were the most positively influencing variables and served to be the most efficient for the highest recovery of CUI and CUB. Based on the present study, the fruits of D. palmatus were revealed as a potent antioxidant, anti-diabetic and anticancer bio-resource that could be explored further to develop novel drug to manage diabetes, cancer and oxidative stress related disorders.The plants from the family Cucurbitaceae are commonly called as melons, squashes, and gourds which are traditionally used in the human diet. It comprises 122 genera and 940 species of which 31 genera and 94 species are found in India 1 . Diplocyclos palmatus (L.) C. Jeffrey is a slender-stemmed tendril climber commonly called as Shivlingi. Traditionally, this plant has been used in the folk medicine and possesses several activities such as gynaecological, anti-asthmatic, anti-convulsant, anti-venom, anti-inflammatory, androgenic and antioxidant 2-4 . The family Cucurbitaceae has been recognized as a rich source of bitter compounds, called cucurbitacins 5 . The cucurbitacins are highly unsaturated triterpenes containing many keto-, hydroxy-and acetoxy-groups. They are the major active components in traditional medicine, herbal remedies and Pharmacopoeia to treat various health issues such as hepatoprotective, anti-fertility, diabroticites cardiovascular and anti-inflammatory activities 6 . In a recent study, cucurbitacin I (CUI) has been identified as a strong inhibitor of the JAK2/STAT3 signaling pathway (a common oncogenic signaling pathway), which is constitutively activated in many types of cancer; hence, it is considered as a milestone in cancer therapy 7 . Similarly...

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“…No visible sign of toxicity was observed in CuB-treated mice [10]. CuB could suppress human NSCLC cell growth in vitro through its effects on the PI3Kinase and MAPK pathways, which lead to programmed cell death induction, as well as inhibition of cell migration and cell invasion [11]. Additionally, CuB induces cell cycle arrest in A-549 cells and causes DNA double strand breaks.…”

Section: Cucurbitacin B (1′)mentioning

confidence: 97%

Cytotoxic and Antitumoral Activities of Compounds Isolated from Cucurbitaceae Plants

Méndez-Cuesta¹,

Campos²,

Sánchez³

et al. 2019

Pharmacognosy - Medicinal Plants

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The WHO says that annual cases of cancer will increase from 14 million in 2012 to 22 million in the next two decades. Cancer is the second cause of death in the world; in 2015, it caused 8.8 million deaths. On the other hand, it is necessary to consider that 70% of the total deaths due to this disease occur in developing countries, who have the least resources to acquire the drugs of choice for the treatment of this disease. Although there are treatments and these are effective, there are currently cases of resistance to drugs used to treat this disease, which has led to the search for new sources of drugs or compounds effective against the cancer being active; plants are the possible sources to achieve this. Cucurbitaceae is a family of plants widely distributed on the planet which has been used traditionally for the treatment of this disease and from they have been isolated different cucurbitanes. These compounds possess a wide biological activity, antidiabetic, anti-inflammatory, hepatoprotective, or cytotoxic and antitumoral effects. The aim of this review is to present 51 cucurbitacin compounds and 2 with different structures isolated from Cucurbitaceae plants with cytotoxic or antitumoral activity.

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Cytotoxic effects of natural and semisynthetic cucurbitacins on lung cancer cell line A549

Cited by 26 publications

References 44 publications

Antiproliferative and apoptotic activity of glycyrrhizinic acid in MCF-7 human breast cancer cells and evaluation of its effect on cell cycle, cell migration and m-TOR/PI3K/Akt signalling pathway

Antiproliferative and apoptotic activity of glycyrrhizinic acid in MCF-7 human breast cancer cells and evaluation of its effect on cell cycle, cell migration and m-TOR/PI3K/Akt signalling pathway

Efficient extraction of cucurbitacins from Diplocyclos palmatus (L.) C. Jeffrey: Optimization using response surface methodology, extraction methods and study of some important bioactivities

Cytotoxic and Antitumoral Activities of Compounds Isolated from Cucurbitaceae Plants

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