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Pharmacology and Toxicology of Plants and Their Constituents

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A special issue of Plants (ISSN 2223-7747). This special issue belongs to the section "Phytochemistry".

Deadline for manuscript submissions: closed (15 November 2023) | Viewed by 21620

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Dr. Eduardo Madrigal-Bujaidar

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Laboratorio de Genética, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Avenida Wilfrido Massieu s/n, Col. Zacatenco, Del. Gustavo A. Madero, Ciudad de México CP 07738, México
Interests: genetic damage and its prevention; colon cancer chemoprevention; antioxidant properties of natural products
Special Issues, Collections and Topics in MDPI journals

Dr. Isela Álvarez-González

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Laboratorio de Genética, Escuela Nacional de Ciencias Biológicas, Instituto Politécnico Nacional, Avenida Wilfredo Massieu s/n, Col Zacatenco, Del. Gustavo A. Madero, Ciudad de México CP 07738, México
Interests: antigenotoxic effects of natural products; mechanisms of action; prevention of reproductive damage
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The evolution of man has been strongly correlated with the plant kingdom in numerous forms, including in relation to the practical knowledge of various plants’ utility in health and nutrition, as well as their harmful effects. Presently, research on plant pharmacology and toxicology can be segmented into various areas, including the plant itself, its extract, juice, and specific phytochemicals. Moreover, studies may investigate diverse molecular and cellular effects, the involved mechanisms of action, the participation of metabolic pathways, or the interaction between compounds.

The present Special Issue of Plants aims to give a forum to researchers and academicians to show their interest in the mentioned fields. Therefore, please accept a cordial invitation to submit original research articles or comprehensive review articles to be included in this Special Issue.

Dr. Eduardo Madrigal-Bujaidar
Dr. Isela Álvarez-González
Guest Editors

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Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Plants is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

plants
pharmacology
toxicology
toxicological genetics
pharmacognosy
chemoprevention
natural products
phytochemicals
regulations
epidemiology

Related Special Issue

Pharmacology and Toxicology of Plants and Their Constituents—Second Edition in Plants

Published Papers (14 papers)

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23 pages, 997 KiB

Open AccessArticle

Chemical Composition, Larvicidal and Molluscicidal Activity of Essential Oils of Six Guava Cultivars Grown in Vietnam

by Huynh Van Long Luu, Huy Hung Nguyen, Prabodh Satyal, Van Hoa Vo, Gia Huy Ngo, Van The Pham and William N. Setzer

Plants 2023, 12(15), 2888; https://doi.org/10.3390/plants12152888 - 07 Aug 2023

Cited by 2 | Viewed by 2091

Abstract

Diseases transmitted by mosquitoes and snails cause a large burden of disease in less developed countries, especially those with low-income levels. An approach to control vectors and intermediate hosts based on readily available essential oils, which are friendly to the environment and human health, may be an effective solution for disease control. Guava is a fruit tree grown on a large scale in many countries in the tropics, an area heavily affected by tropical diseases transmitted by mosquitoes and snails. Previous studies have reported that the extracted essential oils of guava cultivars have high yields, possess different chemotypes, and exhibit toxicity to different insect species. Therefore, this study was carried out with the aim of studying the chemical composition and pesticide activities of six cultivars of guava grown on a large scale in Vietnam. The essential oils were extracted by hydrodistillation using a Clevenger-type apparatus for 6 h. The components of the essential oils were determined using gas-chromatography–mass-spectrometry (GC-MS) analysis. Test methods for pesticide activities were performed in accordance with WHO guidelines and modifications. Essential oil samples from Vietnam fell into two composition-based clusters, one of (E)-β-caryophyllene and the other of limonene/(E)-β-caryophyllene. The essential oils PG03 and PG05 show promise as environmentally friendly pesticides when used to control Aedes mosquito larvae with values of 24 h LC_50-aegypti of 0.96 and 0.40 µg/mL while 24 h LC_{50-albopictus} of 0.50 and 0.42 µg/mL. These two essential oils showed selective toxicity against Aedes mosquito larvae and were safe against the non-target organism Anisops bouvieri. Other essential oils may be considered as molluscicides against Physa acuta (48 h LC₅₀ of 4.10 to 5.00 µg/mL) and Indoplanorbis exustus (48 h LC₅₀ of 3.85 to 7.71 µg/mL) and with less toxicity to A. bouvieri. Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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11 pages, 1365 KiB

Open AccessArticle

Dietary Supplementation with Yerba Mate (Ilex paraguariensis) Infusion Increases IRS-1 and PI3K mRNA Levels and Enhances Insulin Sensitivity and Secretion in Rat Pancreatic Islets

by Bárbara Maiztegui, Hernán Gonzalo Villagarcía, Carolina Lisi Román, Luis Emilio Flores, José María Prieto, María Cecilia Castro, María Laura Massa, Guillermo R. Schinella and Flavio Francini

Plants 2023, 12(14), 2620; https://doi.org/10.3390/plants12142620 - 12 Jul 2023

Viewed by 1047

Abstract

“Yerba mate” (YM), an aqueous extract of Ilex paraguariensis, has antioxidant, diuretic, cardio-protective and hypoglycaemic properties. Since its effect on the pancreatic islets remains unclear, we evaluated insulin sensitivity and glucose-stimulated insulin secretion (GSIS) in rats consuming YM or tap water (C) for 21 days. Glucose tolerance, glycemia, triglyceridemia, insulinemia, TBARS and FRAP serum levels were evaluated. GSIS and mRNA levels of insulin signaling pathway and inflammatory markers were measured in isolated pancreatic islets from both groups. In C rats, islets were incubated with YM extract or its phenolic components to measure GSIS. YM improved glucose tolerance, enhanced GSIS, increased FRAP plasma levels and islet mRNA levels of IRS-1 and PI3K (p110), and decreased TBARS plasma levels and islet gene expression of TNF-α and PAI-1. Islets from C rats incubated with 100 µg/mL dry YM extract, 1 µM chlorogenic acid, 0.1 and 1 µM rutin, 1 µM caffeic acid or 1 µM quercetin showed an increase in GSIS. Our results suggest that YM enhances glucose tolerance because of its positive effects on GSIS, oxidative stress rate and insulin sensitivity in rat islets, suggesting that long-term dietary supplementation with YM may improve glucose homeostasis in pre-diabetes or type 2 diabetes. Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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15 pages, 1459 KiB

Open AccessArticle

Functional Characterization and Toxicity of Pectin from Red Chilto Fruit Waste (Peels)

by María Eugenia Orqueda, Iris Catiana Zampini, Sebastian Torres and María Inés Isla

Plants 2023, 12(14), 2603; https://doi.org/10.3390/plants12142603 - 10 Jul 2023

Viewed by 1025

Abstract

Background: Food and agricultural wastes constitute a rich source of functional ingredients for the food, pharmaceutical, and cosmetic industries. In this context, by-products from the red variety of Solanum betaceum fruits (chilto) from Northwestern Argentina are suitable sources for pectin extraction. Methods: In this study, pectin from the peels of red chilto fruits was extracted and characterized. Results: The recovery yield of red chilto peel pectin was about 24%, and it was co-extracted with 40.0 mg phenolic compounds, 6.5 mg anthocyanins, and 4.7 g proteins per 100 g of pectin. The pectin obtained from red chilto showed proper technological functionality displaying water and oil holding capacities of 4.2 and 2.0%, respectively, an emulsifying capacity of 83%, emulsion stability of 87.5%, foaming capacity of 21.1%, and foaming stability of 79.1%. The pectin displayed antioxidant activity with the ability to scavenge ABTS radical, superoxide anion, and H₂O₂. The polysaccharide exhibited in vitro hypoglycemic potential and inhibited the α-amylase enzyme, retarded glucose diffusion, and improved the cellular uptake of glucose in a Saccharomyces cerevisiae model. The extract was non-toxic on acute toxicity tests. Conclusions: Red chilto pectin showed potential as a new and safe functional ingredient for the design of foods, health products, and cosmetics. Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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15 pages, 3695 KiB

Open AccessArticle

Saponin Fractions from Eryngium planum L. Induce Apoptosis in Ovarian SKOV-3 Cancer Cells

by Małgorzata Kikowska, Hanna Piotrowska-Kempisty, Małgorzata Kucińska, Marek Murias, Jaromir Budzianowski, Anna Budzianowska, Mariusz Kaczmarek, Mariusz Kowalczyk, Anna Stochmal and Barbara Thiem

Plants 2023, 12(13), 2485; https://doi.org/10.3390/plants12132485 - 29 Jun 2023

Cited by 1 | Viewed by 1148

Abstract

(1) The cytotoxicity and antioxidant activity of different fractions as well as the pro-apoptotic activity of saponin fractions from Eryngium planum L. in SKOV-3 was investigated. (2) In screening studies, the cytotoxicity of six fractions on SKOV-3 was examined by LDH and SRB assays. The most active fractions—triterpenoid saponins—were selected for further investigation. To determine the mechanism of saponin fractions’ cytotoxicity, their ability to induce apoptosis was examined via Annexin V assay. The effect of the saponin fractions on caspase 3 activity was measured using a Caspase 3 Assay Kit. The expression of 84 apoptosis-related genes was investigated in cancer cells exposed to saponin fractions from the roots. The radical scavenging capacity of different fractions was determined via DPPH assay. (3) The pronounced cytotoxic effects in SKOV-3 were demonstrated by saponin fractions from the leaves and roots. Those saponin fractions were chosen for further investigation. The treatment of cancer cell lines with saponins obtained from the roots provoked a significant increase in apoptotic cells. In the SKOV-3 cells, saponins caused upregulation of pro-apoptotic genes and a decrease in anti-apoptotic genes. The activation of caspase 3 was correlated with an increased DFFA expression level in the treated SKOV-3 cells. The most active fractions were phenolic acids from the shoots and roots. (4) To the best of our knowledge, the current study is the first to demonstrate that the barrigenol-type triterpenoid saponin fraction from the roots of E. planum inhibits SKOV-3 cell proliferation and induces apoptosis, which may be regulated by the expression of genes mostly specific to a mitochondria-related pathway. Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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13 pages, 3682 KiB

Open AccessArticle

Inhibition of the CYP Enzymatic System Responsible of Heterocyclic Amines Bioactivation by an Asclepias subulata Extract

by Samaria Lisdeth Gutiérrez-Pacheco, Etna Aida Peña-Ramos, Rebeca Santes-Palacios, Martin Valenzuela-Melendres, Adrián Hernández-Mendoza, Armando Burgos-Hernández, Ramón Enrique Robles-Zepeda and Jesús Javier Espinosa-Aguirre

Plants 2023, 12(12), 2354; https://doi.org/10.3390/plants12122354 - 17 Jun 2023

Viewed by 839

Abstract

Asclepias subulata plant extract has previously demonstrated antiproliferative activity and antimutagenicity against heterocyclic aromatic amines (HAAs) commonly found in cooked meat. The objective of this work was to evaluate the in vitro ability of an ethanolic extract from the medicinal plant Asclepias subulata extract (ASE), non-heated and heated (180 °C), to inhibit the activity of CYP1A1 and CYP1A2, which are largely responsible for HAAs bioactivation. Ethoxyresorufin and methoxyresorufin O-dealkylation assays were performed in rat liver microsomes exposed to ASE (0.002–960 µg/mL). ASE exerted an inhibitory effect in a dose-dependent manner. The half inhibitory concentration (IC₅₀) for unheated ASE was 353.6 µg/mL and 75.9 µg/mL for heated ASE in EROD assay. An IC₄₀ value of 288.4 ± 5.8 µg/mL was calculated for non-heated ASE in MROD assay. However, after heat treatment, the IC₅₀ value was 232.1 ± 7.4 µg/mL. Molecular docking of corotoxigenin-3-O-glucopyranoside, one of the main components of ASE, with CYP1A1/2 structure, was performed. Results show that the interaction of corotoxigenin-3-O-glucopyranoside with CYP1A1/2s’ α-helices, which are related with the active site and the heme cofactor, may explain the plant extract’s inhibitory properties. Results showed that ASE inhibits CYP1A enzymatic subfamily and may potentially act as a chemopreventive agent by inhibiting bioactivation of promutagenic dietary HAAs. Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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17 pages, 1984 KiB

Open AccessArticle

Chemopreventive Effect of Cooked Chickpea on Colon Carcinogenesis Evolution in AOM/DSS-Induced Balb/c Mice

by María Stephanie Cid-Gallegos, Cristian Jiménez-Martínez, Xariss M. Sánchez-Chino, Eduardo Madrigal-Bujaidar, Verónica R. Vásquez-Garzón, Rafael Baltiérrez-Hoyos and Isela Álvarez-González

Plants 2023, 12(12), 2317; https://doi.org/10.3390/plants12122317 - 14 Jun 2023

Cited by 1 | Viewed by 1248

Abstract

Chickpeas are one of the most widely consumed legumes worldwide and they might prevent diseases such as cancer. Therefore, this study evaluates the chemopreventive effect of chickpea (Cicer arietinum L.) on the evolution of colon carcinogenesis induced with azoxymethane (AOM) and dextran sodium sulfate (DSS) in a mice model at 1, 7, and 14 weeks after induction. Accordingly, the expression of biomarkers—such as argyrophilic nucleolar organizing regions (AgNOR), cell proliferation nuclear antigen (PCNA), β-catenin, inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2)—was assessed in the colon of BALB/c mice fed diets supplemented with 10 and 20% cooked chickpea (CC). The results showed that a 20% CC diet significantly reduced tumors and biomarkers of proliferation and inflammation in AOM/DSS-induced colon cancer mice. Moreover, body weight loss decreased and the disease activity index (DAI) was lower than the positive control. Lastly, tumor reduction was more evident at week 7 in the groups fed a 20% CC diet. In conclusion, both diets (10% and 20% CC) exert a chemopreventive effect. Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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14 pages, 2573 KiB

Open AccessArticle

Cinnamon Oil Alleviates Acetaminophen-Induced Uterine Toxicity in Rats by Abrogation of Oxidative Stress, Apoptosis, and Inflammation

by Sohail Hussain, Saeed Alshahrani, Rahimullah Siddiqui, Andleeb Khan, Manal Mohammed Elhassan Taha, Rayan A. Ahmed, Abdulmajeed M. Jali, Marwa Qadri, Khairat H. M. Khairat and Mohammad Ashafaq

Plants 2023, 12(12), 2290; https://doi.org/10.3390/plants12122290 - 12 Jun 2023

Cited by 1 | Viewed by 1227

Abstract

Paracetamol, or acetaminophen (APAP), is one of the first-line medications that is used for fever and pain. However, APAP can induce uterine toxicity when overused. The mode of action of APAP toxicity is due to the production of free radicals. The main goal of our study is to determine uterine toxicity from APAP overdose and the antioxidative activity of cinnamon oil (CO) in female rats. The effect of different doses of CO (50–200 mg/kg b.w.) was assessed in the uterus toxicity induced by APAP. Additionally, the imbalance in oxidative parameters, interleukins, and caspases was evaluated for the protective effects of CO. A single dose of APAP (2 g/kg b.w.) resulted in uterus toxicity, indicated by a significant increase in the level of lipid peroxidation (LPO), inflammatory interleukins cytokines (IL-1 and 6), expression of caspases 3 and 9, and a marked change in uterus tissue architecture evaluated by histopathology. Co-treatment of CO resulted in a significant amelioration of all the parameters such as LPO, interleukins IL-1β, IL-6, caspases 3 and 9 expression, and distortion of tissue architecture in a dose-dependent manner. Therefore, we can conclude that APAP-induced uterine injury due to oxidative stress can be restored by co-treatment with cinnamon oil (CO). Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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20 pages, 6537 KiB

Open AccessArticle

The Inhibitory Effects and Cytotoxic Activities of the Stem Extract of Nepenthes miranda against Single-Stranded DNA-Binding Protein and Oral Carcinoma Cells

by En-Shyh Lin, Yen-Hua Huang, Jo-Chi Chung, Hsin-Hui Su and Cheng-Yang Huang

Plants 2023, 12(11), 2188; https://doi.org/10.3390/plants12112188 - 31 May 2023

Cited by 3 | Viewed by 1197

Abstract

The carnivorous pitcher plants of the genus Nepenthes exhibit many ethnobotanical uses, including treatments of stomachache and fever. In this study, we prepared different extracts from the pitcher, stem, and leaf extracts of Nepenthes miranda obtained using 100% methanol and analyzed their inhibitory effects on recombinant single-stranded DNA-binding protein (SSB) from Klebsiella pneumoniae (KpSSB). SSB is essential for DNA replication and cell survival and thus an attractive target for potential antipathogen chemotherapy. Different extracts prepared from Sinningia bullata, a tuberous member of the flowering plant family Gesneriaceae, were also used to investigate anti-KpSSB properties. Among these extracts, the stem extract of N. miranda exhibited the highest anti-KpSSB activity with an IC₅₀ value of 15.0 ± 1.8 μg/mL. The cytotoxic effects of the stem extract of N. miranda on the survival and apoptosis of the cancer cell lines Ca9-22 gingival carcinoma, CAL27 oral adenosquamous carcinoma, PC-9 pulmonary adenocarcinoma, B16F10 melanoma, and 4T1 mammary carcinoma cells were also demonstrated and compared. Based on collective data, the cytotoxic activities of the stem extract at a concentration of 20 μg/mL followed the order Ca9-22 > CAL27 > PC9 > 4T1 > B16F10 cells. The stem extract of N. miranda at a concentration of 40 μg/mL completely inhibited Ca9-22 cell migration and proliferation. In addition, incubation with this extract at a concentration of 20 μg/mL boosted the distribution of the G2 phase from 7.9% to 29.2% in the Ca9-22 cells; in other words, the stem extract might suppress Ca9-22 cell proliferation by inducing G2 cell cycle arrest. Through gas chromatography–mass spectrometry, the 16 most abundant compounds in the stem extract of N. miranda were tentatively identified. The 10 most abundant compounds in the stem extract of N. miranda were used for docking analysis, and their docking scores were compared. The binding capacity of these compounds was in the order sitosterol > hexadecanoic acid > oleic acid > plumbagin > 2-ethyl-3-methylnaphtho[2,3-b]thiophene-4,9-dione > methyl α-d-galactopyranoside > 3-methoxycatechol > catechol > pyrogallol > hydroxyhydroquinone; thus, sitosterol might exhibit the greatest inhibitory capacity against KpSSB among the selected compounds. Overall, these results may indicate the pharmacological potential of N. miranda for further therapeutic applications. Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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15 pages, 3438 KiB

Open AccessArticle

Protective Effect of the Phycobiliproteins from Arthrospira maxima on Indomethacin-Induced Gastric Ulcer in a Rat Model

by Oscar Guzmán-Gómez, Rosa Virginia García-Rodríguez, Salud Pérez-Gutierrez, Nora Lilia Rivero-Ramírez, Yuliana García-Martínez, Saudy Saret Pablo-Pérez, Ricardo Pérez-Pastén-Borja, José Melesio Cristóbal-Luna and Germán Chamorro-Cevallos

Plants 2023, 12(8), 1586; https://doi.org/10.3390/plants12081586 - 08 Apr 2023

Cited by 3 | Viewed by 1595

Abstract

Gastric ulcers (GU) constitute a disease with a global prevalence ≈ 8.09 million. Of their causes, non-steroidal anti-inflammatory drugs (NSAIDs) such as indomethacin (IND) rank as the second most frequent etiologic agent. The pathogenic process of gastric lesions is given by the overproduction of oxidative stress, promotion of inflammatory processes, and inhibition of prostaglandin synthesis. Spirulina Arthrospira maxima (SP) is a cyanobacterium with a wide variety of substances with high nutritional and health values such as phycobiliproteins (PBPs) that have outstanding antioxidant activity, anti-inflammatories effects, and accelerate the wound healing process. This study aimed to determine the protective effect of PBPs in GU induced by IND 40 mg/kg. Our results show that the PBPs protected against IND-induced damage with a dose-dependent effect. At a dose of 400 mg/kg, a marked decrease in the number of lesions is observed, as well as the recovery of the main markers of oxidative stress damage (MDA) and antioxidant species (SOD, CAT, GPx) at close to baseline levels. The evidence derived from the present investigation suggests that the antioxidant effect of PBPs, together with their reported anti-inflammatory effects to accelerate the wound healing process, is the most reliable cause of their antiulcerogenic activity in this GU model. Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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17 pages, 3803 KiB

Open AccessArticle

A Mixture of Artemisia argyi and Saururus chinensis Improves PM_2.5-Induced Cognitive Dysfunction by Regulating Oxidative Stress and Inflammatory Response in the Lung and Brain

by Jin-Yong Kang, Jong-Min Kim, Seon-Kyeong Park, Hyo-Lim Lee and Ho-Jin Heo

Plants 2023, 12(6), 1230; https://doi.org/10.3390/plants12061230 - 08 Mar 2023

Cited by 1 | Viewed by 1334

Abstract

This study was performed to investigate the improving effect of a mixture of Artemisia argyi and Saururus chinensis (AASC) on cognitive dysfunction in mice with long-term exposure to fine particles (particulate matter smaller than 2.5 µm: PM_2.5). The main compounds of AASC were identified as dicaffeoylquinic acid isomers of A. argyi and a quercetin-3-glucoside of S. chinesis. As a result of behavioral tests for the evaluation of cognitive function, it was confirmed that cognitive dysfunction was induced in the PM_2.5 exposure group, and a tendency to improve in the AASC group was confirmed. Increased oxidative stress and inflammatory response and mitochondrial dysfunction were observed in the brain and lung tissues of the PM group. Damage to the brain and lung affected the accumulation of amyloid beta (Aβ) in the brain. It increased Aβ and induced the cholinergic dysfunction, hyperphosphorylation of the tau protein, and activation of apoptosis, leading to cognitive impairment. However, AASC suppressed brain and lung oxidative stress and inflammation, thereby suppressing brain Aβ expression. Consequently, this study shows the potential that a steady intake of plant resources with antioxidant and anti-inflammatory activity could prevent cognitive impairment caused by PM_2.5. Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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20 pages, 1222 KiB

Open AccessArticle

Effects of Extraction Methods on Phenolic Content, Antioxidant and Antiplatelet Activities of Tomato Pomace Extracts

by Andrea Plaza, Lyanne Rodríguez, Anibal A. Concha-Meyer, René Cabezas, Elsie Zurob, Gastón Merlet, Iván Palomo and Eduardo Fuentes

Plants 2023, 12(5), 1188; https://doi.org/10.3390/plants12051188 - 06 Mar 2023

Cited by 4 | Viewed by 2077

Abstract

Aqueous and ethanolic extracts of tomato pomace were examined with the aim of optimizing the extraction process of compounds with cardioprotective activity. Once the results of the ORAC response variables, total polyphenols, °Brix, and antiplatelet activity of the extracts were obtained, a multivariate statistical analysis was performed using the Statgraphics Centurion XIX software. This analysis showed that the most relevant positive effects in the inhibition of platelet aggregation were 83 ± 2% when using the agonist TRAP-6, when the working conditions were the type of tomato pomace conditioning (drum-drying process at 115 °C), phase ratio (1/8), type of solvent (ethanol 20%), and type of extraction (ultrasound-assisted solid–liquid extraction). The extracts with the best results were microencapsulated and characterized by HPLC. The presence of chlorogenic acid (0.729 mg/mg of dry sample) was found, a compound that has a potential cardioprotective effect documented in various studies, in addition to rutin (2.747 mg/mg of dry sample) and quercetin (0.255 mg/mg of dry sample). These results show that the extraction efficiency of compounds with cardioprotective activity depends largely on the polarity of the solvent, thus playing an important role in the antioxidant capacity of the extracts of tomato pomace. Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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21 pages, 3737 KiB

Open AccessArticle

Neuroprotective Effect of Methanolic Ajwa Seed Extract on Lipopolysaccharide-Induced Memory Dysfunction and Neuroinflammation: In Vivo, Molecular Docking and Dynamics Studies

by Vasudevan Mani, Minhajul Arfeen, Devendra Kumar Dhaked, Hamdoon A. Mohammed, Palanisamy Amirthalingam and Hossam A. Elsisi

Plants 2023, 12(4), 934; https://doi.org/10.3390/plants12040934 - 18 Feb 2023

Cited by 4 | Viewed by 1591

Abstract

Islamic literature has indicated that daily consumption of Ajwa dates heals a variety of chronic diseases and disorders. The current research investigates the neuroprotective effect of methanolic Ajwa seed extract (MASE) on lipopolysaccharide (LPS)-induced cognitive deficits using multiple approaches. For animal studies, MASE (200 and 400 mg/kg, p.o.) was administrated for thirty consecutive days, and four doses of LPS (250 µg/kg, i.p.) were injected to induce neurotoxicity. Memory functions were evaluated using elevated plus-maze and novel object recognition tests. Acetylcholine (ACh) and neuroinflammatory markers (cyclooxygenase (COX)-2, tumor necrosis factor (TNF)-α, interleukin (IL)-6, IL-10, and transforming growth factor (TGF)-β1) were estimated in brain tissues. Studies of molecular docking and dynamics were conducted to provide insight into the molecular-level mechanisms. MASE administration resulted in a significant reversal of LPS-induced memory impairment in both maze models. Both doses of MASE elevated the ACh levels in an LPS-treated rat brain. In addition, the extract lowered COX-2 and proinflammatory cytokines (TNF-α and IL-6) while increasing anti-inflammatory cytokines (IL-10 and TGF-β1) in LPS-treated brain tissues. Molecular modeling results revealed that the compound’s ellagic acid, epicatechin, catechin, kaempferol, quercetin, and apigenin have the potential to act as a dual inhibitor of acetylcholinesterase (AChE) and COX-2 and can be responsible for the improvement of both cholinergic and inflammatory conditions, while the cinnamic acid, hesperidin, hesperetin, narengin, and rutin compounds are responsible only for the improvement of cholinergic transmission. The above compounds acted by interacting with the key residues Trp84, Asp72, Gly118, Ser200, Tyr334, and His440, which are responsible for the hydrolysis of ACh in AChE, while the COX-2 is inhibited by interacting with the residues (Val349, Leu352, Tyr355, Tyr385, Ala527, Ser530, and Leu531) of the hydrophobic channel. By promoting cholinergic activity and protecting neuroinflammation in the rat brain, MASE provides neuroprotection against LPS-induced cognitive deficits. Our preliminary findings will help with further drug discovery processes related to neuroinflammation-related neurodegeneration. Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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Review

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29 pages, 3469 KiB

Open AccessReview

Potential Pharmacological Applications of Nigella Seeds with a Focus on Nigella sativa and Its Constituents against Chronic Inflammatory Diseases: Progress and Future Opportunities

by Shadma Wahab and Abdulrhman Alsayari

Plants 2023, 12(22), 3829; https://doi.org/10.3390/plants12223829 - 11 Nov 2023

Cited by 2 | Viewed by 2543

Abstract

The leading cause of death worldwide has been identified as chronic illnesses, according to the World Health Organization (WHO). Chronic inflammatory conditions such as asthma, cancer, diabetes, heart disease, and obesity account for three out of every five deaths. Although many people benefit from using nonsteroidal anti-inflammatory medicines (NSAIDs) for pain and inflammation relief, there are significant adverse effects to using these medications. Medicinal plants possess anti-inflammatory properties with minimal or no side effects. Nigella sativa (NS), also known as black cumin, is one of the plants used in traditional medicine the most. Many studies on the NS have shown that their therapeutic properties are attributed to the seed, oil, and secondary metabolites. This plant has been studied extensively and has many medical uses, such as anti-inflammatory. NS or its phytochemical compounds, such as thymoquinone, can cause cell apoptosis via oxidative stress, block efflux pumps, enhance membrane permeability, and exert potent biocidal effects. Notwithstanding the extensively documented anti-inflammatory effectiveness observed in the experimental model, the precise mechanisms underlying its anti-inflammatory effects in diverse chronic inflammatory diseases and its multi-targeting characteristics remain largely unexplored. This review examines NS or its secondary metabolites, a valuable source for the therapeutic development of chronic inflammatory diseases. Most clinical studies were done for diabetes and cardiovascular disease; therefore, more studies are required to examine the NS extracts and phytoconstituents to treat cancer, obesity, diabetes, asthma, neurological disorders, and COVID-19. This study will be a significant resource for clinicians and biologists seeking a pharmaceutical solution for inflammatory diseases. Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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29 pages, 10467 KiB

Open AccessReview

Occurrence of Alkenylbenzenes in Plants: Flavours and Possibly Toxic Plant Metabolites

by Mario E. Götz, Andreas Eisenreich, Janine Frenzel, Benjamin Sachse and Bernd Schäfer

Plants 2023, 12(11), 2075; https://doi.org/10.3390/plants12112075 - 23 May 2023

Cited by 1 | Viewed by 1501

Abstract

Alkenylbenzenes are naturally occurring secondary plant metabolites. While some of them are proven genotoxic carcinogens, other derivatives need further evaluation to clarify their toxicological properties. Furthermore, data on the occurrence of various alkenylbenzenes in plants, and especially in food products, are still limited. In this review, we tempt to give an overview of the occurrence of potentially toxic alkenylbenzenes in essential oils and extracts from plants used for flavoring purposes of foods. A focus is layed on widely known genotoxic alkenylbenzenes, such as safrole, methyleugenol, and estragole. However, essential oils and extracts that contain other alkenylbenzenes and are also often used for flavoring purposes are considered. This review may re-raise awareness of the need for quantitative occurrence data for alkenylbenzenes in certain plants but especially in final plant food supplements, processed foods, and flavored beverages as the basis for a more reliable exposure assessment of alkenylbenzenes in the future. Full article

(This article belongs to the Special Issue Pharmacology and Toxicology of Plants and Their Constituents)

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