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Cytotoxic Activity of Plant Extracts-2nd Edition

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (30 July 2023) | Viewed by 32782

Special Issue Editors

Special Issue Information

Dear Colleagues,

The plant world is an inexhaustible source of pharmacological agents, and many plant secondary metabolites have a role at the forefront of the discovery of new drugs. However, although the Earth has between 250,000 and 500,000 plant species, just 1–10% have been examined biologically and chemically for their potential pharmaceutical value. The exponential growth in the use of traditional and complementary alternative medicine in Western countries in the last two decades has given new impetus to the search for natural compounds or plants extracts with pharmacological activity. In cancer therapy, it has been estimated that approximately 60% of antitumor-active compounds are derived from medicinal plants and other natural sources. Moreover, the combination of phytochemicals or herbal extracts with commercial drugs may be very helpful in the treatment of cancer, and appears to be a very promising therapeutic strategy. Indeed, acting in synergy with traditional chemotherapies, relatively nontoxic natural products can bring about a positive or enhanced effect, and reduce the systemic toxicity caused by chemotherapies because of the lower doses required.  

Due to the success of the first edition, we have launched a second edition. The aim of this Special Issue is to bring together experimental scientific evidence to support the use of medicinal plants exhibiting anticancer pharmacological potential and to characterize the responsible constituents of the cytotoxic activity.

The information disseminated through this volume is hoped to serve as an interdisciplinary link between phytomedicine, cellular biochemistry, chemistry, and the extraction and analysis technologies of bioactive natural compounds.

Potential topics include but are not limited to the following:

  • In vitro and in vivo studies of the cytotoxic and chemopreventive activity of plant extracts;
  • Studies of the intracellular pathways involved in the cytotoxic mechanisms of plant extracts;
  • Synergistic activity of natural chemopreventive compounds in combination with clinical chemotherapy;
  • Isolation and characterization of new biologically active phytochemicals from medicinal plant extracts;
  • Technological innovations of the extraction and purification of phytochemicals with potential pharmacological activity.

Dr. Alessandro Attanzio
Prof. Dr. Luisa Tesoriere
Guest Editors

Manuscript Submission Information

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Keywords

  • phytomedicine
  • medicinal plants
  • plant extracts
  • natural drugs
  • isolation and characterization
  • nutraceutical
  • phytochemicals
  • chemoprevention
  • combotherapy
  • extraction methods
  • biological activity
  • technological innovations
  • agricultural and biological sciences
  • biochemistry

Published Papers (12 papers)

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Research

16 pages, 3790 KiB  
Article
Stimulation of Hemolysis and Eryptosis by α-Mangostin through Rac1 GTPase and Oxidative Injury in Human Red Blood Cells
by Sumiah A. Alghareeb, Jawaher Alsughayyir and Mohammad A. Alfhili
Molecules 2023, 28(18), 6495; https://doi.org/10.3390/molecules28186495 - 07 Sep 2023
Cited by 4 | Viewed by 833
Abstract
Background: Chemotherapy-related anemia is prevalent in up to 75% of patients, which may arise due to hemolysis and eryptosis. Alpha-mangostin (α-MG) is a polyphenolic xanthonoid found in the mangosteen tree (Garcinia mangostana) whose antitumor medicinal properties are well-established. Nevertheless, the potential [...] Read more.
Background: Chemotherapy-related anemia is prevalent in up to 75% of patients, which may arise due to hemolysis and eryptosis. Alpha-mangostin (α-MG) is a polyphenolic xanthonoid found in the mangosteen tree (Garcinia mangostana) whose antitumor medicinal properties are well-established. Nevertheless, the potential toxic effects of α-MG on red blood cells (RBCs) have, as of yet, not been as well studied. Methods: RBCs were exposed to 1–40 μM of α-MG for 24 h at 37 °C. Hemolysis and related markers were measured using colorimetric assays, eryptotic cells were identified through Annexin-V-FITC, Ca2+ was detected with Fluo4/AM, and oxidative stress was assessed through H2DCFDA using flow cytometry. The toxicity of α-MG was also examined in the presence of specific signal transduction inhibitors and in whole blood. Results: α-MG at 10–40 μM caused dose-dependent hemolysis with concurrent significant elevation in K+, Mg2+, and LDH leakage, but at 2.5 μM it significantly increased the osmotic resistance of cells. A significant increase was also noted in Annexin-V-binding cells, along with intracellular Ca2+, oxidative stress, and cell shrinkage. Moreover, acetylcholinesterase activity was significantly inhibited by α-MG, whose hemolytic potential was significantly ameliorated by the presence of BAPTA-AM, vitamin C, NSC23766, and isosmotic sucrose but not urea. In whole blood, α-MG significantly depleted intracellular hemoglobin stores and was selectively toxic to platelets and monocytes. Conclusions: α-MG possesses hemolytic and eryptotic activities mediated through Ca2+ signaling, Rac1 GTPase activity, and oxidative injury. Also, α-MG leads to accelerated cellular aging and specifically targets platelet and monocyte populations in a whole blood milieu. Full article
(This article belongs to the Special Issue Cytotoxic Activity of Plant Extracts-2nd Edition)
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22 pages, 7043 KiB  
Article
Caffeic Acid Phenethyl Ester (CAPE) Synergistically Enhances Paclitaxel Activity in Ovarian Cancer Cells
by Anna Kleczka, Radosław Dzik and Agata Kabała-Dzik
Molecules 2023, 28(15), 5813; https://doi.org/10.3390/molecules28155813 - 01 Aug 2023
Viewed by 1194
Abstract
Caffeic acid phenethyl ester (CAPE) belongs to the phenols found in propolis. It has already shown strong antiproliferative, cytotoxic and pro-apoptotic activities against head and neck cancers and against breast, colorectal, lung and leukemia cancer cells. Ovarian cancer is one of the most [...] Read more.
Caffeic acid phenethyl ester (CAPE) belongs to the phenols found in propolis. It has already shown strong antiproliferative, cytotoxic and pro-apoptotic activities against head and neck cancers and against breast, colorectal, lung and leukemia cancer cells. Ovarian cancer is one of the most dangerous gynecological cancers. Its treatment involves intensive chemotherapy with platinum salts and paclitaxel (PTX). The purpose of this study was to evaluate whether the combined use of CAPE and paclitaxel increases the effectiveness of chemotherapeutic agents. The experiment was performed on three ovarian cancer lines: OV7, HTB78, and CRL1572. The effect of the tested compounds was assessed using H-E staining, a wound-healing test, MTT and the cell death detection ELISAPLUS test. The experiment proved that very low doses of PTX (10 nM) showed a cytotoxic effect against all the cell lines tested. Also, the selected doses of CAPE had a cytotoxic effect on the tested ovarian cancer cells. An increase in the cytotoxic effect was observed in the OV7 line after the simultaneous administration of 10 nM PTX and 100 µM CAPE. The increase in the cytotoxicity was dependent on the CAPE dosage (50 vs. 100 µM) and on the duration of the experiment. In the other cell lines tested, the cytotoxic effect of PTX did not increase after the CAPE administration. The administration of PTX together with CAPE increased the percentage of apoptotic cells in the tested ovarian cancer cell lines. Moreover, the simultaneous administration of PTX and CAPE enhanced the anti-migration activity of the chemotherapeutic used in this study. Full article
(This article belongs to the Special Issue Cytotoxic Activity of Plant Extracts-2nd Edition)
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20 pages, 1759 KiB  
Article
Phytochemical Composition of Commiphora Oleogum Resins and Their Cytotoxicity against Skin Cancer Cells
by Judith Ulrich, Svenja Stiltz, Alexis St-Gelais, Menna El Gaafary, Thomas Simmet, Tatiana Syrovets and Michael Schmiech
Molecules 2022, 27(12), 3903; https://doi.org/10.3390/molecules27123903 - 17 Jun 2022
Cited by 1 | Viewed by 3055
Abstract
Oleogum resins of the genus Commiphora have been used in traditional medicines for centuries. More than 200 Commiphora species exhibit highly variable phytochemical compositions. A novel highly selective, sensitive, accurate HPLC-MS/MS method was developed and validated to quantify five characteristic phytosteroids and furanosesquiterpenoids, [...] Read more.
Oleogum resins of the genus Commiphora have been used in traditional medicines for centuries. More than 200 Commiphora species exhibit highly variable phytochemical compositions. A novel highly selective, sensitive, accurate HPLC-MS/MS method was developed and validated to quantify five characteristic phytosteroids and furanosesquiterpenoids, namely (E)-guggulsterone, (Z)-guggulsterone, curzerenone, furanoeudesma-1,3-diene, and myrrhone. The resulting contents and additionally GC analysis were used to classify and differentiate Commiphora oleogum resins of the species C. myrrha, C. erythraea, C. mukul, C. holtziana, C. confusa, and C. kua, as well as unspecified resins. Interestingly, a Commiphora sample from Ogaden, Ethiopia, comprised 446 ng/mg guggulsterones presumed to be unique to C. mukul from the Indian subcontinent. However, Commiphora from Ogaden differed considerably from C. mukul in respect to guggulsterones isomer’s ratio. Moreover, the cytotoxicity of Commiphora extracts, essential oils, botanical drugs containing Commiphora, and pure compounds against the epidermoid carcinoma A431, malignant melanoma RPMI-7951 and SK-MEL-28 cells was investigated in vitro. Thereby, especially C. mukul extract and C. myrrha essential oil exhibited high cytotoxicity against skin cancer cells with IC50 of 2.9–10.9 µg/mL, but were less toxic to normal keratinocytes. In summary, Commiphora oleogum resins and its phytochemicals warrant further investigation aiming at chemotaxonomical classification as well as application in skin cancer treatment. Full article
(This article belongs to the Special Issue Cytotoxic Activity of Plant Extracts-2nd Edition)
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14 pages, 2770 KiB  
Article
Antitumor Potential of Annona muricata Linn. An Edible and Medicinal Plant in Mexico: In Vitro, In Vivo, and Toxicological Studies
by Verenice Merlín-Lucas, Rosa María Ordoñez-Razo, Fernando Calzada, Aida Solís, Normand García-Hernández, Elizabeth Barbosa and Miguel Valdés
Molecules 2021, 26(24), 7675; https://doi.org/10.3390/molecules26247675 - 18 Dec 2021
Cited by 6 | Viewed by 3064
Abstract
Annona muricata (Am) is a plant used in traditional Mexican medicine to treat cancer. In this study, ethanol extracts of Am collected in Acapulco and Tecpan from Guerrero state were evaluated orally on Balb/c mice inoculated with 4T1 cells, for cytotoxic [...] Read more.
Annona muricata (Am) is a plant used in traditional Mexican medicine to treat cancer. In this study, ethanol extracts of Am collected in Acapulco and Tecpan from Guerrero state were evaluated orally on Balb/c mice inoculated with 4T1 cells, for cytotoxic activity (CA) on 4T1 cells, in brine shrimp lethality assay (BSLA), and for acute oral toxicity in mice. In addition, ethanol extracts were subjected to high-performance liquid chromatography (HPLC) with diode array detection. Results showed that the extracts collected in December in Acapulco (AcDe) and Tecpan (TeDe) exhibited the most significant antitumor and cytotoxic activity. In the BSLA, the most important effect was observed in the extracts from Acapulco and Tecpan collected in June (AcJu) and August (TeAg), respectively. The samples from Acapulco (AcJu, and AcAg) and Tecpan (TeJu and TeAg) showed the highest toxicity. The analysis of the extracts, AcDe and TeDe, by HPLC revealed that flavonoids, rutin, narcissin, and nicotinflorin were the major components. These findings suggest that extracts from Am collected in Acapulco and Tecpan in the month of December may be an important source to obtain flavonoid glycosides with anticancer potential specifically against breast cancer. This also supports the use of Am to treat cancer in Mexican traditional medicine. Full article
(This article belongs to the Special Issue Cytotoxic Activity of Plant Extracts-2nd Edition)
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11 pages, 652 KiB  
Article
Antioxidant Potential and Cytotoxic Effect of Isoflavones Extract from Thai Fermented Soybean (Thua-Nao)
by Kanokwan Kulprachakarn, Supakit Chaipoot, Rewat Phongphisutthinant, Narisara Paradee, Adchara Prommaban, Sakaewan Ounjaijean, Kittipan Rerkasem, Wason Parklak, Kanittha Prakit, Banthita Saengsitthisak, Nittaya Chansiw, Kanjana Pangjit and Kongsak Boonyapranai
Molecules 2021, 26(24), 7432; https://doi.org/10.3390/molecules26247432 - 08 Dec 2021
Cited by 14 | Viewed by 2824
Abstract
Thua-nao, or Thai fermented soybeans, is a traditional Lanna fermented food in Northern Thailand. It is produced by using a specific bacterial species called Bacillus subtilis var. Thua-nao. We investigated the antioxidant activity and cytotoxic effect of isoflavones from Thua-nao. The phenolic [...] Read more.
Thua-nao, or Thai fermented soybeans, is a traditional Lanna fermented food in Northern Thailand. It is produced by using a specific bacterial species called Bacillus subtilis var. Thua-nao. We investigated the antioxidant activity and cytotoxic effect of isoflavones from Thua-nao. The phenolic compound contents and total flavonoid contents were determined by spectrophotometry. The antioxidant activity was examined using the ABTS, FRAP, and DPPH assays. The isoflavone contents and phenolic compositions were examined by the high-performance liquid chromatography (HPLC) and liquid chromatography-mass spectrometry (LC-MS) techniques. The ability of isoflavones to inhibit human cancer cell growth was assessed by the MTT assay. The total phenolic content, total flavonoid content, and antioxidant activities of the isoflavones were 49.00 ± 0.51 mg GAE/g of dry extract (DE), 10.76 ± 0.82 mg QE/g of DE, 61.03 ± 0.97 µmol Trolox/g of DE, 66.54 ± 3.97 µM FeSO4/g of DE, and 22.47 ± 1.92% of DPPH inhibition, respectively. Additionally, the isoflavone extracts from Thua-nao had high isoflavone contents and polyphenolic compound compositions, especially daidzein and genistein. The isoflavone demonstrated a weak inhibition of MCF-7 and HEK293 cancer cell growth. It has a high antioxidant component, which is beneficial and can be developed for new therapeutic uses. However, further studies on the benefits of Thua-nao should be performed for realizing better and more effective uses soon. Full article
(This article belongs to the Special Issue Cytotoxic Activity of Plant Extracts-2nd Edition)
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11 pages, 890 KiB  
Article
Inflammatory and Cytotoxic Activities of Abietane Terpenoids from Nepeta bracteata Benth.
by Manli Zhang, Meiying Chen, Yong Hou, Congzhao Fan, Hongyan Wei, Leiling Shi, Guoxu Ma and Jing Zhang
Molecules 2021, 26(18), 5603; https://doi.org/10.3390/molecules26185603 - 15 Sep 2021
Cited by 6 | Viewed by 1903
Abstract
Nepeta bracteata Benth. is used clinically to treat tracheal inflammation, coughs, asthma, colds, fevers, adverse urination, and other symptoms, along with functions in clearing heat and removing dampness. However, there have been few studies characterizing the material basis of its efficacy. Therefore, the [...] Read more.
Nepeta bracteata Benth. is used clinically to treat tracheal inflammation, coughs, asthma, colds, fevers, adverse urination, and other symptoms, along with functions in clearing heat and removing dampness. However, there have been few studies characterizing the material basis of its efficacy. Therefore, the aim of this study was to screen for compounds with anti-inflammatory activities in N. bracteata Benth. Using silica gel, ODS C18, and Sephadex LH-20 column chromatography, as well as semipreparative HPLC, 10 compounds were separated from N. bracteata Benth. extract, including four new diterpenoids (14), one amide alkaloid (5), and five known diterpenoids (610). The structures of all the isolates were elucidated by HR-ESI-MS, NMR, and CD analyses. Using lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, we investigated the anti-inflammatory activities of compounds 110. It is worth noting that all were able to inhibit nitric oxide (NO) production with IC50 values < 50 μM and little effect on RAW 264.7 macrophage viability. Compounds 2 and 4 displayed remarkable inhibition with IC50 values of 19.2 and 18.8 μM, respectively. Meanwhile, screening on HCT-8 cells demonstrated that compounds 2 and 4 also had moderate cytotoxic activities with IC50 values of 36.3 and 41.4 μM, respectively, which is related to their anti-inflammatory effects. Full article
(This article belongs to the Special Issue Cytotoxic Activity of Plant Extracts-2nd Edition)
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22 pages, 3315 KiB  
Article
Anti-Cancer Activity and Phenolic Content of Extracts Derived from Cypriot Carob (Ceratonia siliqua L.) Pods Using Different Solvents
by Gregoria Gregoriou, Christiana M. Neophytou, Alexandru Vasincu, Yiota Gregoriou, Haria Hadjipakkou, Eftychia Pinakoulaki, Marios C. Christodoulou, Georgia D. Ioannou, Ioannis J. Stavrou, Atalanti Christou, Constantina P. Kapnissi-Christodoulou, Siegfried Aigner, Hermann Stuppner, Antonis Kakas and Andreas I. Constantinou
Molecules 2021, 26(16), 5017; https://doi.org/10.3390/molecules26165017 - 19 Aug 2021
Cited by 19 | Viewed by 3554
Abstract
Extracts derived from the Ceratonia siliqua L. (carob) tree have been widely studied for their ability to prevent many diseases mainly due to the presence of polyphenolic compounds. In this study, we explored, for the first time, the anti-cancer properties of Cypriot carobs. [...] Read more.
Extracts derived from the Ceratonia siliqua L. (carob) tree have been widely studied for their ability to prevent many diseases mainly due to the presence of polyphenolic compounds. In this study, we explored, for the first time, the anti-cancer properties of Cypriot carobs. We produced extracts from ripe and unripe whole carobs, pulp and seeds using solvents with different polarities. We measured the ability of the extracts to inhibit proliferation and induce apoptosis in cancer and normal immortalized breast cells, using the MTT assay, cell cycle analysis and Western Blotting. The extracts’ total polyphenol content and anti-oxidant action was evaluated using the Folin–Ciocalteu method and the DPPH assay. Finally, we used LC-MS analysis to identify and quantify polyphenols in the most effective extracts. Our results demonstrate that the anti-proliferative capacity of carob extracts varied with the stage of carob maturity and the extraction solvent. The Diethyl-ether and Ethyl acetate extracts derived from the ripe whole fruit had high Myricetin content and also displayed specific activity against cancer cells. Their mechanism of action involved caspase-dependent and independent apoptosis. Our results indicate that extracts from Cypriot carobs may have potential uses in the development of nutritional supplements and pharmaceuticals. Full article
(This article belongs to the Special Issue Cytotoxic Activity of Plant Extracts-2nd Edition)
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23 pages, 4621 KiB  
Article
Ziziphus nummularia Attenuates the Malignant Phenotype of Human Pancreatic Cancer Cells: Role of ROS
by Joelle Mesmar, Manal M. Fardoun, Rola Abdallah, Yusra Al Dhaheri, Hadi M. Yassine, Rabah Iratni, Adnan Badran, Ali H. Eid and Elias Baydoun
Molecules 2021, 26(14), 4295; https://doi.org/10.3390/molecules26144295 - 15 Jul 2021
Cited by 14 | Viewed by 3094
Abstract
Pancreatic cancer (PC) is the fourth leading cause of all cancer-related deaths. Despite major improvements in treating PC, low survival rate remains a major challenge, indicating the need for alternative approaches, including herbal medicine. Among medicinal plants is Ziziphus nummularia (family Rhamnaceae), [...] Read more.
Pancreatic cancer (PC) is the fourth leading cause of all cancer-related deaths. Despite major improvements in treating PC, low survival rate remains a major challenge, indicating the need for alternative approaches, including herbal medicine. Among medicinal plants is Ziziphus nummularia (family Rhamnaceae), which is a thorny shrub rich in bioactive molecules. Leaves of Ziziphus nummularia have been used to treat many pathological conditions, including cancer. However, their effects on human PC are still unknown. Here, we show that the treatment of human pancreatic ductal adenocarcinoma cells (Capan-2) with Ziziphus nummularia ethanolic extract (ZNE) (100–300 μg/mL) attenuated cell proliferation in a time- and concentration-dependent manner. Pretreatment with N-acetylcysteine, an ROS scavenger, attenuated the anti-proliferative effect of ZNE. In addition, ZNE significantly decreased the migratory and invasive capacity of Capan-2 with a concomitant downregulation of integrin α2 and increased cell–cell aggregation. In addition, ZNE inhibited in ovo angiogenesis as well as reduced VEGF and nitric oxide levels. Furthermore, ZNE downregulated the ERK1/2 and NF-κB signaling pathways, which are known to drive tumorigenic and metastatic events. Taken together, our results suggest that ZNE can attenuate the malignant phenotype of Capan-2 by inhibiting hallmarks of PC. Our data also provide evidence for the potential anticancer effect of Ziziphus nummularia, which may represent a new resource of novel anticancer compounds, especially ones that can be utilized for the management of PC. Full article
(This article belongs to the Special Issue Cytotoxic Activity of Plant Extracts-2nd Edition)
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11 pages, 1429 KiB  
Article
Ethiopian Medicinal Plants Traditionally Used for the Treatment of Cancer; Part 3: Selective Cytotoxic Activity of 22 Plants against Human Cancer Cell Lines
by Solomon Tesfaye, Hannah Braun, Kaleab Asres, Ephrem Engidawork, Anteneh Belete, Ilias Muhammad, Christian Schulze, Nadin Schultze, Sebastian Guenther and Patrick J. Bednarski
Molecules 2021, 26(12), 3658; https://doi.org/10.3390/molecules26123658 - 15 Jun 2021
Cited by 8 | Viewed by 3015
Abstract
Medicinal plants have been traditionally used to treat cancer in Ethiopia. However, very few studies have reported the in vitro anticancer activities of medicinal plants that are collected from different agro-ecological zones of Ethiopia. Hence, the main aim of this study was to [...] Read more.
Medicinal plants have been traditionally used to treat cancer in Ethiopia. However, very few studies have reported the in vitro anticancer activities of medicinal plants that are collected from different agro-ecological zones of Ethiopia. Hence, the main aim of this study was to screen the cytotoxic activities of 80% methanol extracts of 22 plants against human peripheral blood mononuclear cells (PBMCs), as well as human breast (MCF-7), lung (A427), bladder (RT-4), and cervical (SiSo) cancer cell lines. Active extracts were further screened against human large cell lung carcinoma (LCLC-103H), pancreatic cancer (DAN-G), ovarian cancer (A2780), and squamous cell carcinoma of the esophagus (KYSE-70) by using the crystal violet cell proliferation assay, while the vitality of the acute myeloid leukemia (HL-60) and histiocytic lymphoma (U-937) cell lines was monitored in the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) microtiter assay. Euphorbia schimperiana, Acokanthera schimperi, Kniphofia foliosa, and Kalanchoe petitiana exhibited potent antiproliferative activity against A427, RT-4, MCF-7, and SiSo cell lines, with IC50 values ranging from 1.85 ± 0.44 to 17.8 ± 2.31 µg/mL. Furthermore, these four extracts also showed potent antiproliferative activities against LCLC-103H, DAN-G, A2780, KYSE-70, HL-60, and U-937 cell lines, with IC50 values ranging from 0.086 to 27.06 ± 10.8 µg/mL. Hence, further studies focusing on bio-assay-guided isolation and structural elucidation of active cytotoxic compounds from these plants are warranted. Full article
(This article belongs to the Special Issue Cytotoxic Activity of Plant Extracts-2nd Edition)
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23 pages, 6285 KiB  
Article
Mechanistic Actions between Garcinia atroviridis Essential Oil and 2 Deoxy-d-glucose in Cultured PANC-1 Human Pancreatic Cancer Cells
by Nik Nur Syazni Nik Mohamed Kamal, Fatin Athirah Abdul Aziz, Wen-Nee Tan, Agustine Nengsih Fauzi and Vuanghao Lim
Molecules 2021, 26(12), 3518; https://doi.org/10.3390/molecules26123518 - 09 Jun 2021
Cited by 1 | Viewed by 2274
Abstract
Pancreatic cancer is an aggressive disease that progresses in a relatively symptom-free manner; thus, is difficult to detect and treat. Essential oil is reported to exhibit pharmacological properties, besides its common and well-known function as aromatherapy. Therefore, this study herein aimed to investigate [...] Read more.
Pancreatic cancer is an aggressive disease that progresses in a relatively symptom-free manner; thus, is difficult to detect and treat. Essential oil is reported to exhibit pharmacological properties, besides its common and well-known function as aromatherapy. Therefore, this study herein aimed to investigate the anti-proliferative effect of essential oil extracted from leaves of Garcinia atroviridis (EO-L) against PANC-1 human pancreatic cancer cell line. The cell growth inhibitory concentration at 50% (IC50) and selective index (SI) values of EO-L analyses were determined as 78 µg/mL and 1.23, respectively. Combination index (CI) analysis revealed moderate synergism (CI values of 0.36 to 0.75) between EO-L and 2 deoxy-d-glucose (2-DG) treatments. The treatments of PANC-1 cells with EO-L, 2-DG and EOL+2DG showed evidence of depolarization of mitochondrial membrane potential, cell growth arrest and apoptosis. The molecular mechanism causing the anti-proliferative effect between EO-L and 2-DG is potentially through pronounced up-regulation of P53 (4.40-fold), HIF1α (1.92-fold), HK2 (2.88-fold) and down-regulation of CYP3A5 (0.11-fold), as supported by quantitative mRNA expression analysis. Collectively, the current data suggest that the combination of two anti-proliferative agents, EO-L and 2-DG, can potentially be explored as therapeutic treatments and as potentiating agents to conventional therapy against human pancreatic cancer. Full article
(This article belongs to the Special Issue Cytotoxic Activity of Plant Extracts-2nd Edition)
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13 pages, 3246 KiB  
Article
Acute and Subacute Toxicity and Cytotoxicity of Opuntia Dillenii (Ker-Gawl) Haw. Seed Oil and Its Impact on the Isolated Rat Diaphragm Glucose Absorption
by Mohamed Bouhrim, Salima Boutahiri, Loubna Kharchoufa, Hamza Mechchate, Omkulthom Mohamed Al Kamaly, Ali Berraaouan, Bruno Eto, Abderrahim Ziyyat, Hassane Mekhfi, Abdelkhaleq Legssyer, Mohammed Aziz and Mohamed Bnouham
Molecules 2021, 26(8), 2172; https://doi.org/10.3390/molecules26082172 - 09 Apr 2021
Cited by 4 | Viewed by 3111
Abstract
This study aims to assess the safety of the Opuntia dillenii (Ker-Gawl) haw. seed oil (ODSO) and its effect on the glucose absorption activity of the isolated rat hemidiaphragm. This oil’s safety was studied by exploring its acute (doses 1, 3, 5, and [...] Read more.
This study aims to assess the safety of the Opuntia dillenii (Ker-Gawl) haw. seed oil (ODSO) and its effect on the glucose absorption activity of the isolated rat hemidiaphragm. This oil’s safety was studied by exploring its acute (doses 1, 3, 5, and 7 mL/kg) and subacute (doses 1 and 2 mL/kg) toxicities in albino mice and Wistar rats, respectively. The safety of the ODSO was also assessed by studying its effect on the HepG2 cell viability in vitro. The effect of ODSO, or combined with the insulin, on the glucose absorption activity of isolated rat hemidiaphragm was evaluated at the dose 1 g/L in vitro. The results demonstrated the safety of ODSO. Indeed, this study showed that this oil does not produce any mortality or signs of toxicity after the single-dose administration in mice. Additionally, the daily intake of the ODSO during four weeks does not induce a significant variation in the biochemical parameters and body weight of rats compared with the control group. Besides, the cell viability of HepG2 did not change in the presence of ODSO. On the other hand, the ODSO increased the glucose absorption activity of the isolated rat hemidiaphragm, and this activity was significantly enhanced when combined with insulin. This study confirms, on one side, the safety of this oil and its efficacy and, on the other side, encourages its potential use as a complement to treat diabetes. Full article
(This article belongs to the Special Issue Cytotoxic Activity of Plant Extracts-2nd Edition)
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11 pages, 2304 KiB  
Article
Antioxidant and Antiproliferative Activity of the Ethanolic Extract of Equisetum myriochaetum and Molecular Docking of Its Main Metabolites (Apigenin, Kaempferol, and Quercetin) on β-Tubulin
by Fabián Olazarán-Santibañez, Gildardo Rivera, Venancio Vanoye-Eligio, Arturo Mora-Olivo, Gabriel Aguirre-Guzmán, Mónica Ramírez-Cabrera and Eder Arredondo-Espinoza
Molecules 2021, 26(2), 443; https://doi.org/10.3390/molecules26020443 - 16 Jan 2021
Cited by 15 | Viewed by 3016
Abstract
Equisetum myriochaetum is a semi-aquatic plant found on riverbanks that is commonly used in traditional medicine as a diuretic agent. Additionally, the genus Equisetum stands out for its content of the flavonoid kaempferol, a well-known antiproliferative agent. Therefore, in this study, E. myriochaetum [...] Read more.
Equisetum myriochaetum is a semi-aquatic plant found on riverbanks that is commonly used in traditional medicine as a diuretic agent. Additionally, the genus Equisetum stands out for its content of the flavonoid kaempferol, a well-known antiproliferative agent. Therefore, in this study, E. myriochaetum ethanolic extract was tested in vitro against a cervical cancer cell line (SiHa). Additionally, the antioxidative activity was evaluated through a 2,2-diphenyl-1-picrilhidrazil (DPPH) assay. Finally, a molecular docking analysis of apigenin, kaempferol, and quercetin on the active site of β-tubulin was performed to investigate their potential mechanism of action. All fractions of E. myriochaetum ethanolic extract showed antioxidative activity. Fraction 14 displayed an antiproliferative capacity with a half maximal inhibitory concentration (IC50) value of 6.78 μg/mL against SiHa cells. Full article
(This article belongs to the Special Issue Cytotoxic Activity of Plant Extracts-2nd Edition)
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