TY  - CONF
AU  - Bangay, Gabrielle
AU  - Isca, Vera
AU  - Domínguez-Martín, Eva María
AU  - Santos, Daniel J.V.A.
AU  - Díaz-Lanza, Ana María
AU  - Saraiva, Lucília
AU  - Afonso, Carlos A.M.
AU  - Jovanović, Mirna
AU  - Pešić, Milica
AU  - Rijo, Patricia
PY  - 2023
UR  - https://www.thieme-connect.com/products/ejournals/html/10.1055/s-0043-1774270
UR  - http://radar.ibiss.bg.ac.rs/handle/123456789/6435
AB  - Multidrug resistant (MDR) cancer cases continue to increase, such that the search for novel and more effective anti-cancer therapeutics is of high priority. In some MDR cancers, the overexpression of membrane transport proteins, like P-glycoprotein (P-gp), continues to be a major impediment to successful therapy. Plectranthus genus (Lamiaceae), known for their medicinal and therapeutic properties, is a well-known source of bioactive diterpenoids, such as 7α-acetoxy-6β-hydroxyroyleanone (Roy) and 6,7- dehydroroyleanone (DeRoy). Based on in silico molecular docking studies, a small library of semi-synthetic derivates was prepared. The antitumoural activity of the compounds was assessed in resistant human cancer cell lines NCI-H460/R and DLD1-TxR. Cell viability was assessed using MTT assay and cell death induction by Annexin V/PI. Overall, it was demonstrated that three of the abietane diterpenoid analogues induced P-gp inhibition in MDR cancer cell lines, presenting novel selective compounds for the possible treatment of lung and colon cancer. Moreover, Roy and DeRoy nano-formulations were successfully prepared. DeRoy hybrid nanoparticles significantly increased the efficacy of DeRoy in NCI-H460 and NCI- H460/R. Roy, conjugated with oleic acid afforded self-assembly nanoparticles, to improve aqueous solubility and bioavailability of Roy. This new nano formulation did not decrease cell viability of Vero-E6 cells when compared to Roy with potential as a pro-drug delivery system. Currently, top hit derivatives are being prepared into nano-formulations for prospective pharmaceutical use as P-gp modulators.
PB  - Georg Thieme Verlag KG
C3  - 71st International Congress and Annual Meeting of the Society for Medicinal Plant and Natural Product Research (GA); 2023 Jul 2-5; Dublin, Ireland
T1  - New formulations with royleanone derivatives from Plectranthus spp. to inhibit P-glycoprotein activity
DO  - 10.1055/s-0043-1774270
SP  - 1424
ER  - 

@conference{
author = "Bangay, Gabrielle and Isca, Vera and Domínguez-Martín, Eva María and Santos, Daniel J.V.A. and Díaz-Lanza, Ana María and Saraiva, Lucília and Afonso, Carlos A.M. and Jovanović, Mirna and Pešić, Milica and Rijo, Patricia",
year = "2023",
abstract = "Multidrug resistant (MDR) cancer cases continue to increase, such that the search for novel and more effective anti-cancer therapeutics is of high priority. In some MDR cancers, the overexpression of membrane transport proteins, like P-glycoprotein (P-gp), continues to be a major impediment to successful therapy. Plectranthus genus (Lamiaceae), known for their medicinal and therapeutic properties, is a well-known source of bioactive diterpenoids, such as 7α-acetoxy-6β-hydroxyroyleanone (Roy) and 6,7- dehydroroyleanone (DeRoy). Based on in silico molecular docking studies, a small library of semi-synthetic derivates was prepared. The antitumoural activity of the compounds was assessed in resistant human cancer cell lines NCI-H460/R and DLD1-TxR. Cell viability was assessed using MTT assay and cell death induction by Annexin V/PI. Overall, it was demonstrated that three of the abietane diterpenoid analogues induced P-gp inhibition in MDR cancer cell lines, presenting novel selective compounds for the possible treatment of lung and colon cancer. Moreover, Roy and DeRoy nano-formulations were successfully prepared. DeRoy hybrid nanoparticles significantly increased the efficacy of DeRoy in NCI-H460 and NCI- H460/R. Roy, conjugated with oleic acid afforded self-assembly nanoparticles, to improve aqueous solubility and bioavailability of Roy. This new nano formulation did not decrease cell viability of Vero-E6 cells when compared to Roy with potential as a pro-drug delivery system. Currently, top hit derivatives are being prepared into nano-formulations for prospective pharmaceutical use as P-gp modulators.",
publisher = "Georg Thieme Verlag KG",
journal = "71st International Congress and Annual Meeting of the Society for Medicinal Plant and Natural Product Research (GA); 2023 Jul 2-5; Dublin, Ireland",
title = "New formulations with royleanone derivatives from Plectranthus spp. to inhibit P-glycoprotein activity",
doi = "10.1055/s-0043-1774270",
pages = "1424"
}

Bangay, G., Isca, V., Domínguez-Martín, E. M., Santos, D. J.V.A., Díaz-Lanza, A. M., Saraiva, L., Afonso, C. A.M., Jovanović, M., Pešić, M.,& Rijo, P.. (2023). New formulations with royleanone derivatives from Plectranthus spp. to inhibit P-glycoprotein activity. in 71st International Congress and Annual Meeting of the Society for Medicinal Plant and Natural Product Research (GA); 2023 Jul 2-5; Dublin, Ireland
Georg Thieme Verlag KG., 1424.
https://doi.org/10.1055/s-0043-1774270

Bangay G, Isca V, Domínguez-Martín EM, Santos DJ, Díaz-Lanza AM, Saraiva L, Afonso CA, Jovanović M, Pešić M, Rijo P. New formulations with royleanone derivatives from Plectranthus spp. to inhibit P-glycoprotein activity. in 71st International Congress and Annual Meeting of the Society for Medicinal Plant and Natural Product Research (GA); 2023 Jul 2-5; Dublin, Ireland. 2023;:1424.
doi:10.1055/s-0043-1774270 .

Bangay, Gabrielle, Isca, Vera, Domínguez-Martín, Eva María, Santos, Daniel J.V.A., Díaz-Lanza, Ana María, Saraiva, Lucília, Afonso, Carlos A.M., Jovanović, Mirna, Pešić, Milica, Rijo, Patricia, "New formulations with royleanone derivatives from Plectranthus spp. to inhibit P-glycoprotein activity" in 71st International Congress and Annual Meeting of the Society for Medicinal Plant and Natural Product Research (GA); 2023 Jul 2-5; Dublin, Ireland (2023):1424,
https://doi.org/10.1055/s-0043-1774270 . .

TY  - JOUR
AU  - Garcia, Catarina
AU  - Ntungwe, Epole
AU  - Rebelo, Ana
AU  - Bessa, Cláudia
AU  - Stanković, Tijana
AU  - Dinić, Jelena
AU  - Díaz-Lanza, Ana
AU  - P Reis, Catarina
AU  - Roberto, Amílcar
AU  - Pereira, Paula
AU  - Cebola, Maria-João
AU  - Saraiva, Lucília
AU  - Pešić, Milica
AU  - Duarte, Noélia
AU  - Rijo, Patrícia
PY  - 2019
UR  - https://www.mdpi.com/2218-273X/9/10/616
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3492
AB  - The Plectranthus genus is commonly used in traditional medicine due to its potential to treat several illnesses, including bacterial infections and cancer. As such, aiming to screen the antibacterial and cytotoxic activities of extracts, sixteen selected Plectranthus species with medicinal potential were studied. In total, 31 extracts obtained from 16 Plectranthus spp. were tested for their antibacterial and anticancer properties. Well diffusion method was used for preliminary antibacterial screening. The minimum inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) values of the five most active acetonic extracts (P. aliciae, P. japonicus, P. madagascariensis var. "Lynne", P. stylesii, and P. strigosus) were determined. After preliminary toxicity evaluation on Artemia salina L., their cytotoxic properties were assessed on three human cancer cell lines (HCT116, MCF-7, and H460). These were also selected for mechanism of resistance studies (on NCI-H460/R and DLD1-TxR cells). An identified compound-parvifloron D-was tested in a pair of sensitive and MDR-Multidrug resistance cancer cells (NCI-H460 and NCI-H460/R) and in normal bronchial fibroblasts MRC-5. The chemical composition of the most active extract was studied through high performance liquid chromatography with a diode array detector (HPLC-DAD/UV) and liquid chromatography-mass spectrometry (LC-MS). Overall, P. strigosus acetonic extract showed the strongest antimicrobial and cytotoxic potential that could be explained by the presence of parvifloron D, a highly cytotoxic diterpene. This study provides valuable information on the use of the Plectranthus genus as a source of bioactive compounds, namely P. strigosus with the potential active ingredient the parvifloron D.
T2  - Biomolecules
T1  - Parvifloron D from Plectranthusstrigosus: Cytotoxicity Screening of Plectranthus spp. Extracts.
IS  - 10
VL  - 9
DO  - 10.3390/biom9100616
SP  - 616
ER  - 

@article{
author = "Garcia, Catarina and Ntungwe, Epole and Rebelo, Ana and Bessa, Cláudia and Stanković, Tijana and Dinić, Jelena and Díaz-Lanza, Ana and P Reis, Catarina and Roberto, Amílcar and Pereira, Paula and Cebola, Maria-João and Saraiva, Lucília and Pešić, Milica and Duarte, Noélia and Rijo, Patrícia",
year = "2019",
abstract = "The Plectranthus genus is commonly used in traditional medicine due to its potential to treat several illnesses, including bacterial infections and cancer. As such, aiming to screen the antibacterial and cytotoxic activities of extracts, sixteen selected Plectranthus species with medicinal potential were studied. In total, 31 extracts obtained from 16 Plectranthus spp. were tested for their antibacterial and anticancer properties. Well diffusion method was used for preliminary antibacterial screening. The minimum inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) values of the five most active acetonic extracts (P. aliciae, P. japonicus, P. madagascariensis var. "Lynne", P. stylesii, and P. strigosus) were determined. After preliminary toxicity evaluation on Artemia salina L., their cytotoxic properties were assessed on three human cancer cell lines (HCT116, MCF-7, and H460). These were also selected for mechanism of resistance studies (on NCI-H460/R and DLD1-TxR cells). An identified compound-parvifloron D-was tested in a pair of sensitive and MDR-Multidrug resistance cancer cells (NCI-H460 and NCI-H460/R) and in normal bronchial fibroblasts MRC-5. The chemical composition of the most active extract was studied through high performance liquid chromatography with a diode array detector (HPLC-DAD/UV) and liquid chromatography-mass spectrometry (LC-MS). Overall, P. strigosus acetonic extract showed the strongest antimicrobial and cytotoxic potential that could be explained by the presence of parvifloron D, a highly cytotoxic diterpene. This study provides valuable information on the use of the Plectranthus genus as a source of bioactive compounds, namely P. strigosus with the potential active ingredient the parvifloron D.",
journal = "Biomolecules",
title = "Parvifloron D from Plectranthusstrigosus: Cytotoxicity Screening of Plectranthus spp. Extracts.",
number = "10",
volume = "9",
doi = "10.3390/biom9100616",
pages = "616"
}

Garcia, C., Ntungwe, E., Rebelo, A., Bessa, C., Stanković, T., Dinić, J., Díaz-Lanza, A., P Reis, C., Roberto, A., Pereira, P., Cebola, M., Saraiva, L., Pešić, M., Duarte, N.,& Rijo, P.. (2019). Parvifloron D from Plectranthusstrigosus: Cytotoxicity Screening of Plectranthus spp. Extracts.. in Biomolecules, 9(10), 616.
https://doi.org/10.3390/biom9100616

Garcia C, Ntungwe E, Rebelo A, Bessa C, Stanković T, Dinić J, Díaz-Lanza A, P Reis C, Roberto A, Pereira P, Cebola M, Saraiva L, Pešić M, Duarte N, Rijo P. Parvifloron D from Plectranthusstrigosus: Cytotoxicity Screening of Plectranthus spp. Extracts.. in Biomolecules. 2019;9(10):616.
doi:10.3390/biom9100616 .

Garcia, Catarina, Ntungwe, Epole, Rebelo, Ana, Bessa, Cláudia, Stanković, Tijana, Dinić, Jelena, Díaz-Lanza, Ana, P Reis, Catarina, Roberto, Amílcar, Pereira, Paula, Cebola, Maria-João, Saraiva, Lucília, Pešić, Milica, Duarte, Noélia, Rijo, Patrícia, "Parvifloron D from Plectranthusstrigosus: Cytotoxicity Screening of Plectranthus spp. Extracts." in Biomolecules, 9, no. 10 (2019):616,
https://doi.org/10.3390/biom9100616 . .

TY  - JOUR
AU  - Matias, Diogo
AU  - Nicolai, Marisa
AU  - Saraiva, Lucília
AU  - Pinheiro, Rute
AU  - Faustino, Célia
AU  - Diaz Lanza, Ana
AU  - Pinto Reis, Catarina
AU  - Stanković, Tijana
AU  - Dinić, Jelena
AU  - Pešić, Milica
AU  - Rijo, Patrícia
PY  - 2019
UR  - http://pubs.acs.org/doi/10.1021/acsomega.9b00512
UR  - https://radar.ibiss.bg.ac.rs/handle/123456789/3349
AB  - Cytotoxicity screenings have identified Plectranthus plants as potential sources of antitumor lead compounds. In this work, several extracts from Plectranthus madagascariensis were prepared using different solvents (acetone, methanol, and supercritical CO2) and extraction techniques (maceration, ultrasound-assisted, and supercritical fluid extraction), and their chemical composition was detailed using high-performance liquid chromatography with a diode array detector. The cytotoxic activity of the major compounds identified, namely, rosmarinic acid (1) and abietane diterpenes 7α,6β-dihydroxyroyleanone (2), 7α-formyloxy-6β-hydroxyroyleanone (3), 7α-acetoxy-6β-hydroxyroyleanone (4), and coleon U (5), was evaluated in a battery of human cancer cell lines, including breast (MDA-MB-231, MCF-7), colon (HCT116), and lung (NCI-H460, NCI-H460/R) cancer, and also in healthy lung (MCR-5) cells. Royleanone (3) was isolated for the first time from P. madagascariensis, and its full spectroscopic characterization (proto...
T2  - ACS Omega
T1  - Cytotoxic Activity of Royleanone Diterpenes from <i>Plectranthus madagascariensis</i> Benth
IS  - 5
VL  - 4
DO  - 10.1021/acsomega.9b00512
SP  - 8094
EP  - 8103
ER  - 

@article{
author = "Matias, Diogo and Nicolai, Marisa and Saraiva, Lucília and Pinheiro, Rute and Faustino, Célia and Diaz Lanza, Ana and Pinto Reis, Catarina and Stanković, Tijana and Dinić, Jelena and Pešić, Milica and Rijo, Patrícia",
year = "2019",
abstract = "Cytotoxicity screenings have identified Plectranthus plants as potential sources of antitumor lead compounds. In this work, several extracts from Plectranthus madagascariensis were prepared using different solvents (acetone, methanol, and supercritical CO2) and extraction techniques (maceration, ultrasound-assisted, and supercritical fluid extraction), and their chemical composition was detailed using high-performance liquid chromatography with a diode array detector. The cytotoxic activity of the major compounds identified, namely, rosmarinic acid (1) and abietane diterpenes 7α,6β-dihydroxyroyleanone (2), 7α-formyloxy-6β-hydroxyroyleanone (3), 7α-acetoxy-6β-hydroxyroyleanone (4), and coleon U (5), was evaluated in a battery of human cancer cell lines, including breast (MDA-MB-231, MCF-7), colon (HCT116), and lung (NCI-H460, NCI-H460/R) cancer, and also in healthy lung (MCR-5) cells. Royleanone (3) was isolated for the first time from P. madagascariensis, and its full spectroscopic characterization (proto...",
journal = "ACS Omega",
title = "Cytotoxic Activity of Royleanone Diterpenes from <i>Plectranthus madagascariensis</i> Benth",
number = "5",
volume = "4",
doi = "10.1021/acsomega.9b00512",
pages = "8094-8103"
}

Matias, D., Nicolai, M., Saraiva, L., Pinheiro, R., Faustino, C., Diaz Lanza, A., Pinto Reis, C., Stanković, T., Dinić, J., Pešić, M.,& Rijo, P.. (2019). Cytotoxic Activity of Royleanone Diterpenes from <i>Plectranthus madagascariensis</i> Benth. in ACS Omega, 4(5), 8094-8103.
https://doi.org/10.1021/acsomega.9b00512

Matias D, Nicolai M, Saraiva L, Pinheiro R, Faustino C, Diaz Lanza A, Pinto Reis C, Stanković T, Dinić J, Pešić M, Rijo P. Cytotoxic Activity of Royleanone Diterpenes from <i>Plectranthus madagascariensis</i> Benth. in ACS Omega. 2019;4(5):8094-8103.
doi:10.1021/acsomega.9b00512 .

Matias, Diogo, Nicolai, Marisa, Saraiva, Lucília, Pinheiro, Rute, Faustino, Célia, Diaz Lanza, Ana, Pinto Reis, Catarina, Stanković, Tijana, Dinić, Jelena, Pešić, Milica, Rijo, Patrícia, "Cytotoxic Activity of Royleanone Diterpenes from <i>Plectranthus madagascariensis</i> Benth" in ACS Omega, 4, no. 5 (2019):8094-8103,
https://doi.org/10.1021/acsomega.9b00512 . .