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12 pages, 4414 KiB

Open AccessArticle

Involucrasin B Inhibits the Proliferation of Caco-2 Cells by Regulating the TGFβ/SMAD2-3-4 Pathway

by Zi Wang, Wanjun Lin, Meina Shi, Yu Hou, Jiachen Liu, Zifeng Huang, Xuening Zhang, Yanchao Yang, Beijia Liu, Zhuya Yang and Wenzhe Ma

Molecules 2024, 29(3), 686; https://doi.org/10.3390/molecules29030686 - 01 Feb 2024

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Abstract

(1) Background: Colorectal cancer (CRC) is the third most common malignant tumor worldwide and the second most common cause of cancer death. However, effective anti-CRC drugs are still lacking in clinical settings. This article investigated the anti-proliferative effect of involucrasin B on CRC [...] Read more.

(1) Background: Colorectal cancer (CRC) is the third most common malignant tumor worldwide and the second most common cause of cancer death. However, effective anti-CRC drugs are still lacking in clinical settings. This article investigated the anti-proliferative effect of involucrasin B on CRC Caco-2 cells. (2) Methods: This study employed a sulforhodamine B (SRB) method, colony formation experiments, flow cytometry, FastFUCCI assay, dual luciferase assay, and Western blot analysis for the investigation. (3) Results: The SRB method and colony formation experiments showed that involucrasin B exhibited an inhibitory effect on the Caco-2 cells cultured in vitro. Subsequently, the flow cytometry, FastFUCCI assay, and Western blotting results showed that involucrasin B induced cell cycle arrest in the G1 phase dose-dependently. Involucrasin B significantly enhanced the TGFβ RII protein level and SMAD3 phosphorylation, thus inhibiting the expression of CDK4 and cyclin D1 and causing G1 cell cycle arrest. (4) Conclusion: This study shows that involucrasin B exerts its anti-proliferative effect by regulating the TGFβ/SMAD2-3-4 pathway to cause G1 cycle arrest in Caco-2 cells. Full article

(This article belongs to the Special Issue Natural Products in Anticancer Activity)

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21 pages, 1796 KiB

Open AccessArticle

Bio-Guided Assay of Ephedra foeminea Forssk Extracts and Anticancer Activities: In Vivo, In Vitro, and In Silico Evaluations

by Jilan A. Nazeam, Sylvia A. Boshra, Esraa Z. Mohammed and Heba A. El Gizawy

Molecules 2024, 29(1), 199; https://doi.org/10.3390/molecules29010199 - 29 Dec 2023

Cited by 1 | Viewed by 697

Abstract

Ephedra is one of the oldest known medicinal plants and the largest genera of the Ephedraceae family. In vivo antitumor evaluation of Ephedra foeminea revealed that ethyl acetate (EtOAc) was the most bioactive fraction. Bio-guided fractionation of EtOAc fraction afforded nine compounds isolated [...] Read more.

Ephedra is one of the oldest known medicinal plants and the largest genera of the Ephedraceae family. In vivo antitumor evaluation of Ephedra foeminea revealed that ethyl acetate (EtOAc) was the most bioactive fraction. Bio-guided fractionation of EtOAc fraction afforded nine compounds isolated for the first time from the plant species. Macrocyclic spermine alkaloids (1,9), proanthocyanidins (2,4,5), quinoline alkaloids (7,8), phenolic (3), and nucleoside (6) were identified and elucidated by spectroscopic analyses including 1D and 2D NMR, ESI-MS-MS spectrometry. The tested compounds exhibited moderate anticancer activity, except for the kynurenic acid derivative (6-mKYNA) which showed significant cytotoxicity and remarkable inhibition of CA-19.9 and CA-125 tumor biomarkers. In-silico study was conducted to determine the anti-proliferative mechanism of 6-mKYNA by using the CK2 enzyme active site. Moreover, the ADME computational study suggested that 6-mKYNA is an effective candidate with a promising pharmacokinetic profile and therapeutic potential against various types of cancer. Full article

(This article belongs to the Special Issue Natural Products in Anticancer Activity)

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21 pages, 5591 KiB

Open AccessArticle

Virtual Screening of Different Subclasses of Lignans with Anticancer Potential and Based on Genetic Profile

by Mayara dos Santos Maia, Francisco Jaime Bezerra Mendonça-Junior, Gabriela Cristina Soares Rodrigues, Adriano Soares da Silva, Niara Isis Pereira de Oliveira, Pablo Rayff da Silva, Cícero Francisco Bezerra Felipe, Ana Pavla Almeida Diniz Gurgel, Anuraj Nayarisseri, Marcus Tullius Scotti and Luciana Scotti

Molecules 2023, 28(16), 6011; https://doi.org/10.3390/molecules28166011 - 11 Aug 2023

Cited by 1 | Viewed by 969

Abstract

Cancer is a multifactorial disease that continues to increase. Lignans are known to be important anticancer agents. However, due to the structural diversity of lignans, it is difficult to associate anticancer activity with a particular subclass. Therefore, the present study sought to evaluate [...] Read more.

Cancer is a multifactorial disease that continues to increase. Lignans are known to be important anticancer agents. However, due to the structural diversity of lignans, it is difficult to associate anticancer activity with a particular subclass. Therefore, the present study sought to evaluate the association of lignan subclasses with antitumor activity, considering the genetic profile of the variants of the selected targets. To do so, predictive models were built against the targets tyrosine-protein kinase ABL (ABL), epidermal growth factor receptor erbB1 (EGFR), histone deacetylase (HDAC), serine/threonine-protein kinase mTOR (mTOR) and poly [ADP-ribose] polymerase-1 (PARP1). Then, single nucleotide polymorphisms were mapped, target mutations were designed, and molecular docking was performed with the lignans with the best predicted biological activity. The results showed more anticancer activity in the dibenzocyclooctadiene, furofuran and aryltetralin subclasses. The lignans with the best predictive values of biological activity showed varying binding energy results in the presence of certain genetic variants. Full article

(This article belongs to the Special Issue Natural Products in Anticancer Activity)

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18 pages, 4405 KiB

Open AccessArticle

Extraction, Characterization, and Evaluation of the Cytotoxic Activity of Piperine in Its Isolated form and in Combination with Chemotherapeutics against Gastric Cancer

by Ingryd Nayara de Farias Ramos, Monique Feitosa da Silva, Jefferson Marcio Sanches Lopes, Jordy Neves Cruz, Fabrine Silva Alves, José de Arimatéia Rodrigues do Rego, Marcondes Lima da Costa, Paulo Pimentel de Assumpção, Davi do Socorro Barros Brasil and André Salim Khayat

Molecules 2023, 28(14), 5587; https://doi.org/10.3390/molecules28145587 - 22 Jul 2023

Cited by 3 | Viewed by 1713

Abstract

Gastric cancer is one of the most frequent types of neoplasms worldwide, usually presenting as aggressive and difficult-to-manage tumors. The search for new structures with anticancer potential encompasses a vast research field in which natural products arise as promising alternatives. In this scenario, [...] Read more.

Gastric cancer is one of the most frequent types of neoplasms worldwide, usually presenting as aggressive and difficult-to-manage tumors. The search for new structures with anticancer potential encompasses a vast research field in which natural products arise as promising alternatives. In this scenario, piperine, an alkaloid of the Piper species, has received attention due to its biological activity, including anticancer attributes. The present work proposes three heating-independent, reliable, low-cost, and selective methods for obtaining piperine from Piper nigrum L. (Black pepper). Electronic (SEM) and optical microscopies, X-ray diffraction, nuclear magnetic resonance spectroscopies (¹³C and ¹H NMR), and optical spectroscopies (UV–Vis, photoluminescence, and FTIR) confirm the obtention of piperine crystals. The MTT assay reveals that the piperine samples exhibit good cytotoxic activity against primary and metastasis models of gastric cancer cell lines from the Brazilian Amazon. The samples showed selective cytotoxicity on the evaluated models, revealing higher effectiveness in cells bearing a higher degree of aggressiveness. Moreover, the investigated piperine crystals demonstrated the ability to act as a good cytotoxicity enhancer when combined with traditional chemotherapeutics (5-FU and GEM), allowing the drugs to achieve the same cytotoxic effect in cells employing lower concentrations. These results establish piperine as a promising molecule for therapy investigations in aggressive gastric cancer, both in its isolated form or as a bioenhancer. Full article

(This article belongs to the Special Issue Natural Products in Anticancer Activity)

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17 pages, 1886 KiB

Open AccessArticle

HPLC-PDA Method for Quantification of Bioactive Compounds in Crude Extract and Fractions of Aucklandia costus Falc. and Cytotoxicity Studies against Cancer Cells

by Anil Bhushan, Dixhya Rani, Misbah Tabassum, Saajan Kumar, Prem N. Gupta, Sumeet Gairola, Ajai P. Gupta and Prasoon Gupta

Molecules 2023, 28(12), 4815; https://doi.org/10.3390/molecules28124815 - 16 Jun 2023

Cited by 1 | Viewed by 1905

Abstract

Aucklandia costus Falc. (Synonym: Saussurea costus (Falc.) Lipsch.) is a perennial herb of the family Asteraceae. The dried rhizome is an essential herb in the traditional systems of medicine in India, China and Tibet. The important pharmacological activities reported for Aucklandia costus are [...] Read more.

Aucklandia costus Falc. (Synonym: Saussurea costus (Falc.) Lipsch.) is a perennial herb of the family Asteraceae. The dried rhizome is an essential herb in the traditional systems of medicine in India, China and Tibet. The important pharmacological activities reported for Aucklandia costus are anticancer, hepatoprotective, antiulcer, antimicrobial, antiparasitic, antioxidant, anti-inflammatory and anti-fatigue activities. The objective of this study was the isolation and quantification of four marker compounds in the crude extract and different fractions of A. costus and the evaluation of the anticancer activity of the crude extract and its different fractions. The four marker compounds isolated from A. costus include dehydrocostus lactone, costunolide, syringin and 5-hydroxymethyl-2-furaldehyde. These four compounds were used as standard compounds for quantification. The chromatographic data showed good resolution and excellent linearity (r² ˃ 0.993). The validation parameters, such as inter- and intraday precision (RSD < 1.96%) and analyte recovery (97.52–110.20%; RSD < 2.00%),revealed the high sensitivity and reliability of the developed HPLC method. The compounds dehydrocostus lactone and costunolide were concentrated in the hexane fraction (222.08 and 65.07 µg/mg, respectively) and chloroform fraction (99.02 and 30.21 µg/mg, respectively), while the n-butanol fraction is a rich source of syringin (37.91 µg/mg) and 5-hydroxymethyl-2-furaldehyde (7.94 µg/mg). Further, the SRB assay was performed for the evaluation of anticancer activity using lung, colon, breast and prostate cancer cell lines. The hexane and chloroform fractions show excellent IC₅₀ values of 3.37 ± 0.14 and 7.527 ± 0.18 µg/mL, respectively, against the prostate cancer cell line (PC-3). Full article

(This article belongs to the Special Issue Natural Products in Anticancer Activity)

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19 pages, 5942 KiB

Open AccessArticle

Chitosan-Coated Solid Lipid Nanoparticles as an Efficient Avenue for Boosted Biological Activities of Aloe perryi: Antioxidant, Antibacterial, and Anticancer Potential

by Tahany Saleh Aldayel, Mohamed M. Badran, Abdullah H. Alomrani, Nora A. AlFaris, Jozaa Z. Altamimi, Ali S. Alqahtani, Fahd A. Nasr, Safina Ghaffar and Raha Orfali

Molecules 2023, 28(8), 3569; https://doi.org/10.3390/molecules28083569 - 19 Apr 2023

Cited by 2 | Viewed by 1465

Abstract

Aloe perryi (ALP) is an herb that has several biological activities such as antioxidant, antibacterial, and antitumor effects and is frequently used to treat a wide range of illnesses. The activity of many compounds is augmented by loading them in nanocarriers. In this [...] Read more.

Aloe perryi (ALP) is an herb that has several biological activities such as antioxidant, antibacterial, and antitumor effects and is frequently used to treat a wide range of illnesses. The activity of many compounds is augmented by loading them in nanocarriers. In this study, ALP-loaded nanosystems were developed to improve their biological activity. Among different nanocarriers, solid lipid nanoparticles (ALP-SLNs), chitosan nanoparticles (ALP-CSNPs), and CS-coated SLNs (C-ALP-SLNs) were explored. The particle size, polydispersity index (PDI), zeta potential, encapsulation efficiency, and release profile were evaluated. Scanning electron microscopy was used to see the nanoparticles’ morphology. Moreover, the possible biological properties of ALP were assessed and evaluated. ALP extract contained 187 mg GAE/g extract and 33 mg QE/g extract in terms of total phenolic and flavonoid content, respectively. The ALP-SLNs-F1 and ALP-SLNs-F2 showed particle sizes of 168.7 ± 3.1 and 138.4 ± 9.5 nm and the zeta potential values of −12.4 ± 0.6, and −15.8 ± 2.4 mV, respectively. However, C-ALP-SLNs-F1 and C-ALP-SLNs-F2 had particle sizes of 185.3 ± 5.5 and 173.6 ± 11.3 nm with zeta potential values of 11.3 ± 1.4 and 13.6 ± 1.1 mV, respectively. The particle size and zeta potential of ALP-CSNPs were 214.8 ± 6.6 nm and 27.8 ± 3.4 mV, respectively. All nanoparticles exhibited PDI < 0.3, indicating homogenous dispersions. The obtained formulations had EE% and DL% in the ranges of 65–82% and 2.8–5.2%, respectively. After 48 h, the in vitro ALP release rates from ALP-SLNs-F1, ALP-SLNs-F2, C-ALP-SLNs-F1, C-ALP-SLNs-F2, and ALP-CSNPs were 86%, 91%, 78%, 84%, and 74%, respectively. They were relatively stable with a minor particle size increase after one month of storage. C-ALP-SLNs-F2 exhibited the greatest antioxidant activity against DPPH radicals at 73.27%. C-ALP-SLNs-F2 demonstrated higher antibacterial activity based on MIC values of 25, 50, and 50 µg/mL for P. aeruginosa, S. aureus, and E. coli, respectively. In addition, C-ALP-SLNs-F2 showed potential anticancer activity against A549, LoVo, and MCF-7 cell lines with IC50 values of 11.42 ± 1.16, 16.97 ± 1.93, and 8.25 ± 0.44, respectively. The results indicate that C-ALP-SLNs-F2 may be promising nanocarriers for enhancing ALP-based medicines. Full article

(This article belongs to the Special Issue Natural Products in Anticancer Activity)

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14 pages, 2639 KiB

Open AccessArticle

Phytochemicals from Vanda bensonii and Their Bioactivities to Inhibit Growth and Metastasis of Non-Small Cell Lung Cancer Cells

by Tajudeen O. Jimoh, Narawat Nuamnaichati, Rungroch Sungthong, Chaisak Chansriniyom, Pithi Chanvorachote, Kittisak Likhitwitayawuid, Chatchai Chaotham and Boonchoo Sritularak

Molecules 2022, 27(22), 7902; https://doi.org/10.3390/molecules27227902 - 15 Nov 2022

Cited by 2 | Viewed by 1897

Abstract

The most prevalent lung cancer is non-small cell lung cancer (NSCLC). This lung cancer type often develops other organ-specific metastases that are critical burdens in the treatment process. Orchid species in the genus Vanda have shown their potential in folkloric medication of diverse [...] Read more.

The most prevalent lung cancer is non-small cell lung cancer (NSCLC). This lung cancer type often develops other organ-specific metastases that are critical burdens in the treatment process. Orchid species in the genus Vanda have shown their potential in folkloric medication of diverse diseases but not all its species have been investigated, and little is known about their anticancer activities against NSCLC. Here, we firstly profiled the specialized metabolites of Vanda bensonii and examined their capability to inhibit growth and metastasis of NSCLC using NCI-H460 cells as a study model. Four phytochemicals, including phloretic acid methyl ester (1), cymbinodin-A (2), ephemeranthoquinone B (3), and protocatechuic acid (4), were isolated from the whole plant methanolic extract of V. bensonii. The most distinguished cytotoxic effect on NCI-H460 cells was observed in the treatments with crude methanolic extract and compound 2 with the half maximal inhibitory concentrations of 40.39 μg mL⁻¹ and 50.82 μM, respectively. At non-cytotoxic doses (10 μg mL⁻¹ or 10 μM), only compound 1 could significantly limit NCI-H460 cell proliferation when treated for 48 h, while others excluding compound 4 showed significant reduction in cell proliferation after treating for 72 h. Compound 1 also significantly decreased the migration rate of NCI-H460 cells examined through a wound-healing assay. Additionally, the crude extract and compound 1 strongly affected survival and growth of NCI-H460 cells under anchorage-independent conditions. Our findings proved that natural products from V. bensonii could be promising candidates for the future pharmacotherapy of NSCLC. Full article

(This article belongs to the Special Issue Natural Products in Anticancer Activity)

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22 pages, 376 KiB

Open AccessReview

Natural Bacterial and Fungal Peptides as a Promising Treatment to Defeat Lung Cancer Cells

by Kamila Rybczyńska-Tkaczyk, Anna Grenda, Anna Jakubczyk and Paweł Krawczyk

Molecules 2023, 28(11), 4381; https://doi.org/10.3390/molecules28114381 - 27 May 2023

Cited by 2 | Viewed by 1718

Abstract

Despite the increasing availability of modern treatments, including personalized therapies, there is a strong need to search for new drugs that will be effective in the fight against cancer. The chemotherapeutics currently available to oncologists do not always yield satisfactory outcomes when used [...] Read more.

Despite the increasing availability of modern treatments, including personalized therapies, there is a strong need to search for new drugs that will be effective in the fight against cancer. The chemotherapeutics currently available to oncologists do not always yield satisfactory outcomes when used in systemic treatments, and patients experience burdensome side effects during their application. In the era of personalized therapies, doctors caring for non-small cell lung cancer (NSCLC) patients have been given a powerful weapon, namely molecularly targeted therapies and immunotherapies. They can be used when genetic variants of the disease qualifying for therapy are diagnosed. These therapies have contributed to the extension of the overall survival time in patients. Nevertheless, effective treatment may be hindered in the case of clonal selection of tumor cells with acquired resistance mutations. The state-of-the-art therapy currently used in NSCLC patients is immunotherapy targeting the immune checkpoints. Although it is effective, some patients have been observed to develop resistance to immunotherapy, but its cause is still unknown. Personalized therapies extend the lifespan and time to cancer progression in patients, but only those with a confirmed marker qualifying for the treatment (gene mutations/rearrangements or PD-L1 expression on tumor cells) can benefit from these therapies. They also cause less burdensome side effects than chemotherapy. The article is focused on compounds that can be used in oncology and produce as few side effects as possible. The search for compounds of natural origin, e.g., plants, bacteria, or fungi, exhibiting anticancer properties seems to be a good solution. This article is a literature review of research on compounds of natural origin that can potentially be used as part of NSCLC therapies. Full article

(This article belongs to the Special Issue Natural Products in Anticancer Activity)

28 pages, 4887 KiB

Open AccessReview

Anticancer Activity of Chalcones and Its Derivatives: Review and In Silico Studies

by Fernando Ferreira Leite, Natália Ferreira de Sousa, Bruno Hanrry Melo de Oliveira, Gabrielly Diniz Duarte, Maria Denise Leite Ferreira, Marcus Tullius Scotti, José Maria Barbosa Filho, Luís Cezar Rodrigues, Ricardo Olímpio de Moura, Francisco Jaime Bezerra Mendonça-Junior and Luciana Scotti

Molecules 2023, 28(10), 4009; https://doi.org/10.3390/molecules28104009 - 10 May 2023

Cited by 7 | Viewed by 2420

Abstract

Chalcones are direct precursors in the biosynthesis of flavonoids. They have an α,β-unsaturated carbonyl system which gives them broad biological properties. Among the biological properties exerted by chalcones, their ability to suppress tumors stands out, in addition to their low toxicity. In this [...] Read more.

Chalcones are direct precursors in the biosynthesis of flavonoids. They have an α,β-unsaturated carbonyl system which gives them broad biological properties. Among the biological properties exerted by chalcones, their ability to suppress tumors stands out, in addition to their low toxicity. In this perspective, the present work explores the role of natural and synthetic chalcones and their anticancer activity in vitro reported in the last four years from 2019 to 2023. Moreover, we carried out a partial least square (PLS) analysis of the biologic data reported for colon adenocarcinoma lineage HCT-116. Information was obtained from the Web of Science database. Our in silico analysis identified that the presence of polar radicals such as hydroxyl and methoxyl contributed to the anticancer activity of chalcones derivatives. We hope that the data presented in this work will help researchers to develop effective drugs to inhibit colon adenocarcinoma in future works. Full article

(This article belongs to the Special Issue Natural Products in Anticancer Activity)

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20 pages, 1746 KiB

Open AccessReview

Critical Review on the Different Roles of Exosomes in TNBC and Exosomal-Mediated Delivery of microRNA/siRNA/lncRNA and Drug Targeting Signalling Pathways in Triple-Negative Breast Cancer

by Manosi Banerjee and Vijayarangan Devi Rajeswari

Molecules 2023, 28(4), 1802; https://doi.org/10.3390/molecules28041802 - 14 Feb 2023

Cited by 2 | Viewed by 2646

Abstract

Triple-negative breast cancer is the most potent metastatic type of breast cancer that can spread to other body parts. Chemotherapy and surgical intervention are the sole treatments for TNBC, owing to the scarcity of therapeutic targets. Manipulation of the membranes as per the [...] Read more.

Triple-negative breast cancer is the most potent metastatic type of breast cancer that can spread to other body parts. Chemotherapy and surgical intervention are the sole treatments for TNBC, owing to the scarcity of therapeutic targets. Manipulation of the membranes as per the desired targets of exosomes has recently gained much attention as a drug delivery method. Despite their known roles in different diseases, very few studies have focused on signalling that triggers the metastasis of triple-negative breast cancer to other body parts by exosomes. This article highlights the significant roles of exosomes associated with TNBC, the involvement of exosomes in breast cancer diagnosis, progression, and the treatment of triple-negative breast cancer by the exosomes as a drug delivery system. This review paper also illustrates the role of exosomes in initiating EMT in breast cancer, including novel signalling. Full article

(This article belongs to the Special Issue Natural Products in Anticancer Activity)

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