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Pharmacological Activities of Secondary Metabolites and Derivates of Medicinal Plants around the World

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A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: 15 May 2024 | Viewed by 11838

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Dr. Fernando Calzada

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Guest Editor

Medical Research Unit in Pharmacology, Speciality Hospital, National Medical Center Siglo XXI, Av. Cuauhtémoc 330 Col Doctores, México City, CP 06725, México
Interests: pharmacognosy of Mexican medicinal plants; diabetes mellitus; cancer; diarrhea; molecular docking; secondary metabolites
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Dear Colleagues,

Since ancient times, our ancestors have sought ways to remedy the ills and diseases that afflicted them by experimenting with the use of all kinds of substances, whether of plant, animal, or mineral origin. It is estimated that approximately between 64% and 80% of the world's population use medicinal plants to treat their health problems. In this sense, medicinal plants have been the source of many secondary metabolites to which numerous pharmacological activities have been attributed, in many cases giving rise to pharmacological treatments with important activity, which are currently used in therapeutics. Considering the above, the objective of this Special Issue is to encourage researchers to share their findings on medicinal plants from different regions of the world and the secondary metabolites isolated from them with a focus on the search for new pharmacological treatments that can be applied to treat diseases that are of importance worldwide. Importantly, the exact active ingredient of the plant extract must be reported in the submitted research manuscript, since papers describing the effects of mixed extraction from plants will not be accepted.

This Special Issue is led by Dr. Fernando Calzada and assisted by our GE's assistant editor Dr. Miguel Valdes <[email protected]> (Instituto Politécnico Nacional, Sección de Estudios de Posgrado e Investigación, Escuela Superior de Medicina, México).

Dr. Fernando Calzada
Guest Editor

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Keywords

natural products
secondary metabolites
medicinal chemistry
worldwide traditional medicine
isolation and identification of secondary metabolites
experimental studies
phytochemistry
pharmacognosy
medicinal plants

Published Papers (7 papers)

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Research

12 pages, 3049 KiB

Open AccessArticle

Potential Candidate Molecule of Photosystem II Inhibitor Herbicide—Brassicanate A Sulfoxide

by Yu Wang, Dong Wang, Baozhu Dong, Jianxiu Hao, Xinyu Jia and Hongyou Zhou

Int. J. Mol. Sci. 2024, 25(4), 2400; https://doi.org/10.3390/ijms25042400 - 18 Feb 2024

Viewed by 646

Abstract

Brassicanate A sulfoxide, a secondary metabolite of broccoli, exhibited the inhibition of weed growth, but its mechanism of action on weeds remains unclear. To elucidate the mechanism by which brassicanate A sulfoxide suppresses weeds, this study explores the interaction between brassicanate A sulfoxide and the photosystem II D1 protein through molecular docking and molecular dynamics simulations. This research demonstrates that brassicanate A sulfoxide interacts with the photosystem II D1 protein by forming hydrogen bonds with Phe-261 and His-214. The successful expression of the photosystem II D1 protein in an insect cell/baculovirus system validated the molecular docking and dynamics simulations. Biolayer interferometry experiments elucidated that the affinity constant of brassicanate A sulfoxide with photosystem II was 2.69 × 10⁻³ M, suggesting that brassicanate A sulfoxide can stably bind to the photosystem II D1 protein. The findings of this study contribute to the understanding of the mode of action of brassicanate A sulfoxide and also aid in the development of natural-product-based photosynthesis-inhibiting herbicides. Full article

(This article belongs to the Special Issue Pharmacological Activities of Secondary Metabolites and Derivates of Medicinal Plants around the World)

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16 pages, 3950 KiB

Open AccessArticle

Effect of the Flavonoid Rutin on the Modulation of the Myenteric Plexuses in an Experimental Model of Parkinson’s Disease

by Livia Bacelar de Jesus, Annyta Fernandes Frota, Fillipe Mendes de Araújo, Rafael Leonne Cruz de Jesus, Maria de Fátima Dias Costa, Darizy Flavia Silva Amorim de Vasconcelos, Marcelo Biondaro Gois, Gyselle Chrystina Baccan, Victor Diogenes Amaral da Silva and Silvia Lima Costa

Int. J. Mol. Sci. 2024, 25(2), 1037; https://doi.org/10.3390/ijms25021037 - 15 Jan 2024

Cited by 1 | Viewed by 872

Abstract

Recent discoveries have shown that enteric glial cells play an important role in different neurodegenerative disorders, such as Parkinson’s disease (PD), which is characterized by motor dysfunctions caused by the progressive loss of dopaminergic neurons in the substance nigra pars compacta and non-motor symptoms including gastrointestinal dysfunction. In this study, we investigated the modulatory effects of the flavonoid rutin on the behavior and myenteric plexuses in a PD animal model and the response of enteric glia. Adult male Wistar rats were submitted to stereotaxic injection with 6-hydroxydopamine or saline, and they were untreated or treated with rutin (10 mg/kg) for 14 days. The ileum was collected to analyze tissue reactivity and immunohistochemistry for neurons (HuC/HuD) and enteric glial cells (S100β) in the myenteric plexuses. Behavioral tests demonstrated that treatment with rutin improved the motor capacity of parkinsonian animals and improved intestinal transit without interfering with the cell population; rutin treatment modulated the reactivity of the ileal musculature through muscarinic activation, reducing relaxation through the signaling pathway of nitric oxide donors, and increased the longitudinal contractility of the colon musculature in parkinsonian animals. Rutin revealed modulatory activities on the myenteric plexus, bringing relevant answers regarding the effect of the flavonoid in this system and the potential application of PD adjuvant treatment. Full article

(This article belongs to the Special Issue Pharmacological Activities of Secondary Metabolites and Derivates of Medicinal Plants around the World)

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17 pages, 3928 KiB

Open AccessArticle

Exploring the Therapeutic Potential of Ampelopsis grossedentata Leaf Extract as an Anti-Inflammatory and Antioxidant Agent in Human Immune Cells

by Arthur Chervet, Rawan Nehme, Caroline Decombat, Lucie Longechamp, Ola Habanjar, Amandine Rousset, Didier Fraisse, Christelle Blavignac, Edith Filaire, Jean-Yves Berthon, Laetitia Delort and Florence Caldefie-Chezet

Int. J. Mol. Sci. 2024, 25(1), 416; https://doi.org/10.3390/ijms25010416 - 28 Dec 2023

Cited by 1 | Viewed by 898

Abstract

Inflammation is a vital protective response to threats, but it can turn harmful if chronic and uncontrolled. Key elements involve pro-inflammatory cells and signaling pathways, including the secretion of pro-inflammatory cytokines, NF-κB, reactive oxygen species (ROS) production, and the activation of the NLRP3 inflammasome. Ampelopsis grossedentata, or vine tea, contains dihydromyricetin (DHM) and myricetin, which are known for their various health benefits, including anti-inflammatory properties. Therefore, the aim of this study is to assess the impact of an extract of A. grossedentata leaves (50 µg/mL) on inflammation factors such as inflammasome, pro-inflammatory pathways, and macrophage polarization, as well as its antioxidant properties, with a view to combating the development of low-grade inflammation. Ampelopsis grossedentata extract (APG) significantly decreased ROS production and the secretion of pro-inflammatory cytokines (IFNγ, IL-12, IL-2, and IL-17a) in human leukocytes. In addition, APG reduced LPS/IFNγ -induced M1-like macrophage polarization, resulting in a significant decrease in the expression of the pro-inflammatory cytokines TNF-α and IL-6, along with a decrease in the percentage of M1 macrophages and an increase in M0 macrophages. Simultaneously, a significant decrease in NF-κB p65 phosphorylation and in the expression of inflammasome genes (NLRP3, IL-1β and Caspase 1) was observed. The results suggest that Ampelopsis grossedentata could be a promising option for managing inflammation-related chronic diseases. Further research is needed to optimize dosage and administration methods. Full article

(This article belongs to the Special Issue Pharmacological Activities of Secondary Metabolites and Derivates of Medicinal Plants around the World)

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14 pages, 2742 KiB

Open AccessArticle

Maackiain Mimics Caloric Restriction through aak-2-Mediated Lipid Reduction in Caenorhabditis elegans

by Saveta G. Mladenova, Monika N. Todorova, Martina S. Savova, Milen I. Georgiev and Liliya V. Mihaylova

Int. J. Mol. Sci. 2023, 24(24), 17442; https://doi.org/10.3390/ijms242417442 - 13 Dec 2023

Viewed by 1118

Abstract

Obesity prevalence is becoming a serious global health and economic issue and is a major risk factor for concomitant diseases that worsen the quality and duration of life. Therefore, the urgency of the development of novel therapies is of a particular importance. A previous study of ours revealed that the natural pterocarpan, maackiain (MACK), significantly inhibits adipogenic differentiation in human adipocytes through a peroxisome proliferator-activated receptor gamma (PPARγ)-dependent mechanism. Considering the observed anti-adipogenic potential of MACK, we aimed to further elucidate the molecular mechanisms that drive its biological activity in a Caenorhabditis elegans obesity model. Therefore, in the current study, the anti-obesogenic effect of MACK (25, 50, and 100 μM) was compared to orlistat (ORST, 12 μM) as a reference drug. Additionally, the hybrid combination between the ORST (12 μM) and MACK (100 μM) was assessed for suspected synergistic interaction. Mechanistically, the observed anti-obesogenic effect of MACK was mediated through the upregulation of the key metabolic regulators, namely, the nuclear hormone receptor 49 (nhr-49) that is a functional homologue of the mammalian PPARs and the AMP-activated protein kinase (aak-2/AMPK) in C. elegans. Collectively, our investigation indicates that MACK has the potential to limit lipid accumulation and control obesity that deserves future developments. Full article

(This article belongs to the Special Issue Pharmacological Activities of Secondary Metabolites and Derivates of Medicinal Plants around the World)

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23 pages, 12774 KiB

Open AccessArticle

Kaempferol and Biomodified Kaempferol from Sophora japonica Extract as Potential Sources of Anti-Cancer Polyphenolics against High Grade Glioma Cell Lines

by Jéssica Silva dos Santos, Amanda Janaína Suzan, Gabriel Alves Bonafé, Anna Maria Alves de Piloto Fernandes, Giovanna Barbarini Longato, Márcia Aparecida Antônio, Patrícia de Oliveira Carvalho and Manoela Marques Ortega

Int. J. Mol. Sci. 2023, 24(13), 10716; https://doi.org/10.3390/ijms241310716 - 27 Jun 2023

Cited by 3 | Viewed by 1593

Abstract

The enzymatic hydrolysis of the extract of Sophora japonica by two glycosyl hydrolases (hesperidinase and galactosidase) was performed in order to obtain kaempferol (KPF)-enriched extract with an enhanced anticancer activity. The current study examined the effectiveness of both Sophora japonica extracts (before (KPF-BBR) and after (KPF-ABR) bioconversion reactions) in reducing cell viability and inducing apoptosis in human high-degree gliomas in vitro. Cytotoxicity was determined using an MTT assay. The effects of both compounds on the proliferation of glioma cell lines were measured using trypan blue exclusion, flow cytometry for cell cycle, wound healing (WH), and neurosphere formation assays. Cellular apoptosis was detected by DNA fragmentation and phosphatidylserine exposure. qPCR and luciferase assays evaluated NF-kB pathway inhibition. The survival rate of NG-97 and U-251 cells significantly decreased in a time- and dose-dependent manner after the addition of KPF-BBR or KPF-ABR. Thus, a 50% reduction was observed in NG-97 cells at 800 µM (KPF-BBR) and 600 µM (KPF-ABR) after 72 h. Both compounds presented an IC50 of 1800 µM for U251 after 72 h. The above IC50 values were used in all of the following analyses. Neither of the KPF presented significant inhibitory effects on the non-tumoral cells (HDFa). However, after 24 h, both extracts (KPF-BBR and KPF-ABR) significantly inhibited the migration and proliferation of NG-97 and U-251 cells. In addition, MMP-9 was downregulated in glioma cells stimulated by 12-O-tetradecanoylphorbol-13-acetate (TPA) plus KPF-BBR and TPA+KPF-ABR compared with the TPA-treated cells. Both KPF-BBR and KPF-ABR significantly inhibited the proliferation of glioma stem cells (neurospheres) after 24 h. DNA fragmentation assays demonstrated that the apoptotic ratio of KPF-ABR-treated cell lines was significantly higher than in the control groups, especially NG-97, which is not TMZ resistant. In fact, the flow cytometric analysis indicated that KPF-BBR and KPF-ABR induced significant apoptosis in both glioma cells. In addition, both KPF induced S and G2/M cell cycle arrest in the U251 cells. The qPCR and luciferase assays showed that both KPFs downregulated TRAF6, IRAK2, IL-1β, and TNF-α, indicating an inhibitory effect on the NF-kB pathway. Our findings suggest that both KPF-BBR and KPF-ABR can confer anti-tumoral effects on human cell glioma cells by inhibiting proliferation and inducing apoptosis, which is related to the NF-κB-mediated pathway. The KPF-enriched extract (KPF-ABR) showed an increased inhibitory effect on the cell migration and invasion, characterizing it as the best antitumor candidate. Full article

(This article belongs to the Special Issue Pharmacological Activities of Secondary Metabolites and Derivates of Medicinal Plants around the World)

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22 pages, 4265 KiB

Open AccessArticle

Dipotassium Glycyrrhizininate Improves Skin Wound Healing by Modulating Inflammatory Process

by Camila dos Santos Leite, Gabriel Alves Bonafé, Oscar César Pires, Tanila Wood dos Santos, Geovanna Pacciulli Pereira, José Aires Pereira, Thalita Rocha, Carlos Augusto Real Martinez, Manoela Marques Ortega and Marcelo Lima Ribeiro

Int. J. Mol. Sci. 2023, 24(4), 3839; https://doi.org/10.3390/ijms24043839 - 14 Feb 2023

Cited by 3 | Viewed by 4263

Abstract

Wound healing is characterized by a systemic and complex process of cellular and molecular activities. Dipotassium Glycyrrhizinate (DPG), a side product derived from glycyrrhizic acid, has several biological effects, such as being antiallergic, antioxidant, antibacterial, antiviral, gastroprotective, antitumoral, and anti-inflammatory. This study aimed to evaluate the anti-inflammatory effect of topical DPG on the healing of cutaneous wounds by secondary intention in an in vivo experimental model. Twenty-four male Wistar rats were used in the experiment, and were randomly divided into six groups of four. Circular excisions were performed and topically treated for 14 days after wound induction. Macroscopic and histopathological analyses were performed. Gene expression was evaluated by real-time qPCR. Our results showed that treatment with DPG caused a decrease in the inflammatory exudate as well as an absence of active hyperemia. Increases in granulation tissue, tissue reepithelization, and total collagen were also observed. Furthermore, DPG treatment reduced the expression of pro-inflammatory cytokines (Tnf-α, Cox-2, Il-8, Irak-2, Nf-kB, and Il-1) while increasing the expression of Il-10, demonstrating anti-inflammatory effects across all three treatment periods. Based on our results, we conclude that DPG attenuates the inflammatory process by promoting skin wound healing through the modulation of distinct mechanisms and signaling pathways, including anti-inflammatory ones. This involves modulation of the expression of pro- and anti-inflammatory cytokine expression; promotion of new granulation tissue; angiogenesis; and tissue re-epithelialization, all of which contribute to tissue remodeling. Full article

(This article belongs to the Special Issue Pharmacological Activities of Secondary Metabolites and Derivates of Medicinal Plants around the World)

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18 pages, 4601 KiB

Open AccessArticle

Identification of Potential Antiviral Hops Compounds against Chikungunya Virus

by Tsvetelina Mandova, Marielena Vogel Saivish, Leonardo La Serra, Mauricio Lacerda Nogueira and Fernando Batista Da Costa

Int. J. Mol. Sci. 2023, 24(4), 3333; https://doi.org/10.3390/ijms24043333 - 07 Feb 2023

Cited by 2 | Viewed by 1676

Abstract

Chikungunya virus (CHIKV) is an arthropod-borne virus that belongs to the genus Alphavirus (family Togaviridae). CHIKV causes chikungunya fever, which is mostly characterized by fever, arthralgia and, sometimes, a maculopapular rash. The bioactive constituents of hops (Humulus lupulus, Cannabaceae), mainly acylphloroglucinols, known as well as α- and β-acids, exerted distinct activity against CHIKV, without showing cytotoxicity. For fast and efficient isolation and identification of such bioactive constituents, a silica-free countercurrent separation method was applied. The antiviral activity was determined by plaque reduction test and was visually confirmed by a cell-based immunofluorescence assay. All hops compounds demonstrated a promising post-treatment viral inhibition, except the fraction of acylphloroglucinols, in mixture. β-acids fraction of 125 µg/mL expressed the strongest virucidal activity (EC₅₀ = 15.21 µg/mL), in a drug-addition experiment on Vero cells. Hypothesis for mechanism of action were proposed for acylphloroglucinols based on their lipophilicity and chemical structure. Therefore, inhibition of some steps of the protein kinase C (PKC) transduction cascades was also discussed. Full article

(This article belongs to the Special Issue Pharmacological Activities of Secondary Metabolites and Derivates of Medicinal Plants around the World)

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