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Editorial

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3 pages, 174 KiB

Open AccessEditorial

Editorial to the Special Issue “Biological and Pharmacological Activity of Plant Natural Compounds”

by Raffaele Pezzani and Sara Vitalini

Molecules 2021, 26(1), 63; https://doi.org/10.3390/molecules26010063 - 25 Dec 2020

Cited by 1 | Viewed by 1757

Abstract

Plant natural products are a valuable source of compounds with a healthy potential effect on living organisms, including animals and humans [...] Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

Research

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14 pages, 1718 KiB

Open AccessArticle

Mahonia aquifolium Extracts Promote Doxorubicin Effects against Lung Adenocarcinoma Cells In Vitro

by Ana Damjanović, Branka Kolundžija, Ivana Z. Matić, Ana Krivokuća, Gordana Zdunić, Katarina Šavikin, Radmila Janković, Jelena Antić Stanković and Tatjana P. Stanojković

Molecules 2020, 25(22), 5233; https://doi.org/10.3390/molecules25225233 - 10 Nov 2020

Cited by 5 | Viewed by 2493

Abstract

Mahonia aquifolium and its secondary metabolites have been shown to have anticancer potential. We performed MTT, scratch, and colony formation assays; analyzed cell cycle phase distribution and doxorubicin uptake and retention with flow cytometry; and detected alterations in the expression of genes involved [...] Read more.

Mahonia aquifolium and its secondary metabolites have been shown to have anticancer potential. We performed MTT, scratch, and colony formation assays; analyzed cell cycle phase distribution and doxorubicin uptake and retention with flow cytometry; and detected alterations in the expression of genes involved in the formation of cell–cell interactions and migration using quantitative real-time PCR following treatment of lung adenocarcinoma cells with doxorubicin, M. aquifolium extracts, or their combination. MTT assay results suggested strong synergistic effects of the combined treatments, and their application led to an increase in cell numbers in the subG1 phase of the cell cycle. Both extracts were shown to prolong doxorubicin retention time in cancer cells, while the application of doxorubicin/extract combination led to a decrease in MMP9 expression. Furthermore, cells treated with doxorubicin/extract combinations were shown to have lower migratory and colony formation potentials than untreated cells or cells treated with doxorubicin alone. The obtained results suggest that nontoxic M. aquifolium extracts can enhance the activity of doxorubicin, thus potentially allowing the application of lower doxorubicin doses in vivo, which may decrease its toxic effects in normal tissues. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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15 pages, 3322 KiB

Open AccessArticle

Zingerone [4-(3-Methoxy-4-hydroxyphenyl)-butan-2] Attenuates Lipopolysaccharide-Induced Inflammation and Protects Rats from Sepsis Associated Multi Organ Damage

by Adil Farooq Wali, Muneeb U Rehman, Mohammad Raish, Mohsin Kazi, Padma G. M. Rao, Osamah Alnemer, Parvaiz Ahmad and Ajaz Ahmad

Molecules 2020, 25(21), 5127; https://doi.org/10.3390/molecules25215127 - 4 Nov 2020

Cited by 18 | Viewed by 3029

Abstract

The present investigation aimed to evaluate the protective effect of Zingerone (ZIN) against lipopolysaccharide-induced oxidative stress, DNA damage, and cytokine storm in rats. For survival study the rats were divided into four groups (n = 10). The control group was treated with normal [...] Read more.

The present investigation aimed to evaluate the protective effect of Zingerone (ZIN) against lipopolysaccharide-induced oxidative stress, DNA damage, and cytokine storm in rats. For survival study the rats were divided into four groups (n = 10). The control group was treated with normal saline; Group II received an intraperitoneal (i.p) injection (10 mg/kg) of LPS as disease control. Rats in Group III were treated with ZIN 150 mg/kg (p.o) 2 h before LPS challenge and rats in Group IV were given ZIN only. Survival of the rats was monitored up to 96 h post LPS treatment. In another set, the animals were divided into four groups of six rats. Animals in Group I served as normal control and were treated with normal saline. Animals in Group II were treated with lipopolysaccharide (LPS) and served as disease control. Group III animals were treated with ZIN 2 h before LPS challenge. Group IV served as positive control and were treated with ZIN (150 mg/kg orally). The blood samples were collected and used for the analysis of biochemical parameters like alanine transaminase (ALT), alkaline phosphatase (ALP), aspartate transaminase (AST), blood urea nitrogen (BUN), Cr, Urea, lactate dehydrogenase (LDH), albumin, bilirubin (BIL), and total protein. Oxidative stress markers malondialdehyde (MDA), glutathione peroxidase (GSH), myeloperoxidase (MPO), and (DNA damage marker) 8-OHdG levels were measured in different organs. Level of nitric oxide (NO) and inflammatory markers like TNF-α, IL-1ß, IL-1α, IL-2, IL-6, and IL-10 were also quantified in plasma. Procalcitonin (PCT), a sepsis biomarker, was also measured. ZIN treatment had shown significant (p < 0.5) restoration of plasma enzymes, antioxidant markers and attenuated plasma proinflammatory cytokines and sepsis biomarker (PCT), thereby preventing the multi-organ and tissue damage in LPS-induced rats also confirmed by histopathological studies of different organs. The protective effect of ZIN may be due to its potent antioxidant potential. Thus ZIN can prevent LPS-induced oxidative stress as well as inflammatory and multi-organ damage in rats when administered to the LPS treated animals. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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18 pages, 2043 KiB

Open AccessArticle

New Sustainable Process for Hesperidin Isolation and Anti-Ageing Effects of Hesperidin Nanocrystals

by Danijela Stanisic, Leticia H. B. Liu, Roney V. dos Santos, Amanda F. Costa, Nelson Durán and Ljubica Tasic

Molecules 2020, 25(19), 4534; https://doi.org/10.3390/molecules25194534 - 3 Oct 2020

Cited by 49 | Viewed by 4828

Abstract

Hesperidin, a secondary orange (Citrus sinensis) metabolite, was extracted from orange bagasse. No organic solvents or additional energy consumption were used in the clean and sustainable process. Hesperidin purity was approximately 98% and had a yield of 1%. Hesperidin is a [...] Read more.

Hesperidin, a secondary orange (Citrus sinensis) metabolite, was extracted from orange bagasse. No organic solvents or additional energy consumption were used in the clean and sustainable process. Hesperidin purity was approximately 98% and had a yield of 1%. Hesperidin is a known supplement due to antioxidant, chelating, and anti-ageing properties. Herein, hesperidin application to eliminate dark eye circles, which are sensitive and thin skin regions, was studied. In addition, the proposed method for its aqueous extraction was especially important for human consumption. Further, the most effective methods for hesperidin nanonization were explored, after which the nanoemulsions were incorporated into a cream formulation that was formulated for a tropical climate. Silky cream formulations (oil in water) were tested in vitro on artificial 3D skin from cultured cells extracted from skin residues after plastic surgery. The proposed in vitro assay avoided tests of the different formulations in human volunteers and animals. It was shown that one of the nanonized hesperidin formulations was the most skin-friendly and might be used in cosmetics. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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12 pages, 1118 KiB

Open AccessArticle

Phenolic Compounds in Extracts of Hibiscus acetosella (Cranberry Hibiscus) and Their Antioxidant and Antibacterial Properties

by Jae Il Lyu, Jaihyunk Ryu, Chang Hyun Jin, Dong-Gun Kim, Jung Min Kim, Kyoung-Sun Seo, Jin-Baek Kim, Sang Hoon Kim, Joon-Woo Ahn, Si-Yong Kang and Soon-Jae Kwon

Molecules 2020, 25(18), 4190; https://doi.org/10.3390/molecules25184190 - 12 Sep 2020

Cited by 26 | Viewed by 4686

Abstract

Hibiscus species are rich in phenolic compounds and have been traditionally used for improving human health through their bioactive activities. The present study investigated the phenolic compounds of leaf extracts from 18 different H. acetosella accessions and evaluated their biofunctional properties, focusing on [...] Read more.

Hibiscus species are rich in phenolic compounds and have been traditionally used for improving human health through their bioactive activities. The present study investigated the phenolic compounds of leaf extracts from 18 different H. acetosella accessions and evaluated their biofunctional properties, focusing on antioxidant and antibacterial activity. The most abundant phenolic compound in H. acetosella was caffeic acid, with levels ranging from 14.95 to 42.93 mg/100 g. The antioxidant activity measured by the ABTS assay allowed the accessions to be classified into two groups: a high activity group with red leaf varieties (74.71–84.02%) and a relatively low activity group with green leaf varieties (57.47–65.94%). The antioxidant activity was significantly correlated with TAC (0.933), Dp3-Sam (0.932), Dp3-Glu (0.924), and Cy3-Sam (0.913) contents (p < 0.001). The H. acetosella phenolic extracts exhibited antibacterial activity against two bacteria, with zones of inhibition between 12.00 and 13.67 mm (Staphylococcus aureus), and 10.67 and 13.33 mm (Pseudomonas aeruginosa). All accessions exhibited a basal antibacterial activity level (12 mm) against the Gram-positive S. aureus, with PI500758 and PI500764 exhibiting increased antibacterial activity (13.67 mm), but they exhibited a more dynamic antibacterial activity level against the Gram-negative P. aeruginosa. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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10 pages, 1266 KiB

Open AccessArticle

A Lanosteryl Triterpene (RA-3) Exhibits Antihyperuricemic and Nephroprotective Effects in Rats

by Nomadlozi Blessings Hlophe, Andrew Rowland Opoku, Foluso Oluwagbemiga Osunsanmi, Trayana Georgieva Djarova-Daniels, Oladipupo Adejumobi Lawal and Rebamang Anthony Mosa

Molecules 2020, 25(17), 4010; https://doi.org/10.3390/molecules25174010 - 2 Sep 2020

Cited by 6 | Viewed by 2553

Abstract

Considering the global health threat posed by kidney disease burden, a search for new nephroprotective drugs from our local flora could prove a powerful strategy to respond to this health threat. In this study we investigated the antihyperuricemic and nephroprotective potential of RA-3, [...] Read more.

Considering the global health threat posed by kidney disease burden, a search for new nephroprotective drugs from our local flora could prove a powerful strategy to respond to this health threat. In this study we investigated the antihyperuricemic and nephroprotective potential of RA-3, a plant-derived lanosteryl triterpene. The antihyperuricemic and nephroprotective effect of RA-3 was investigated using the adenine and gentamicin induced hyperuricemic and nephrotoxicity rat model. Following the induction of hyperuricemia and nephrotoxicity, the experimental model rats (Sprague Dawley) were orally administered with RA-3 at 50 and 100 mg/kg body weight, respectively, daily for 14 days. Treatment of the experimental rats with RA-3, especially at 100 mg/kg, effectively lowered the serum renal dysfunction (blood urea nitrogen and creatinine) and hyperuricemic (uric acid and xanthine oxidase) biomarkers. These were accompanied by increased antioxidant status with decrease in malondialdehyde content. A much improved histomorphological structure of the kidney tissues was also observed in the triterpene treated groups when compared to the model control group. It is evident that RA-3 possesses the antihyperuricemic and nephroprotective properties, which could be vital for prevention and amelioration of kidney disease. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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13 pages, 2734 KiB

Open AccessArticle

Juglone Suppresses LPS-induced Inflammatory Responses and NLRP3 Activation in Macrophages

by Nam-Hun Kim, Hong-Ki Kim, Ji-Hak Lee, Seung-Il Jo, Hye-Min Won, Gyeong-Seok Lee, Hyoun-Su Lee, Kung-Woo Nam, Wan-Jong Kim and Man-Deuk Han

Molecules 2020, 25(13), 3104; https://doi.org/10.3390/molecules25133104 - 7 Jul 2020

Cited by 12 | Viewed by 4726

Abstract

The NLRP3 (NACHT, LRR and PYD domains-containing protein 3) inflammasome has been implicated in a variety of diseases, including atherosclerosis, neurodegenerative diseases, and infectious diseases. Thus, inhibitors of NLRP3 inflammasome have emerged as promising approaches to treat inflammation-related diseases. The aim of this [...] Read more.

The NLRP3 (NACHT, LRR and PYD domains-containing protein 3) inflammasome has been implicated in a variety of diseases, including atherosclerosis, neurodegenerative diseases, and infectious diseases. Thus, inhibitors of NLRP3 inflammasome have emerged as promising approaches to treat inflammation-related diseases. The aim of this study was to explore the effects of juglone (5-hydroxyl-1,4-naphthoquinone) on NLRP3 inflammasome activation. The inhibitory effects of juglone on nitric oxide (NO) production were assessed in lipopolysaccharide (LPS)-stimulated J774.1 cells by Griess assay, while its effects on reactive oxygen species (ROS) and NLRP3 ATPase activity were assessed. The expression levels of NLRP3, caspase-1, and pro-inflammatory cytokines (IL-1β, IL-18) and cytotoxicity of juglone in J774.1 cells were also determined. Juglone was non-toxic in J774.1 cells when used at 10 μM (p < 0.01). Juglone treatment inhibited the production of ROS and NO. The levels of NLRP3 and cleaved caspase-1, as well as the secretion of IL-1β and IL-18, were decreased by treatment with juglone in a concentration-dependent manner. Juglone also inhibited the ATPase activities of NLRP3 in LPS/ATP-stimulated J774.1 macrophages. Our results suggested that juglone could inhibit inflammatory cytokine production and NLRP3 inflammasome activation in macrophages, and should be considered as a therapeutic strategy for inflammation-related diseases. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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13 pages, 2658 KiB

Open AccessArticle

Active Compound of Pharbitis Semen (Pharbitis nil Seeds) Suppressed KRAS-Driven Colorectal Cancer and Restored Muscle Cell Function during Cancer Progression

by Jisu Song, Heejung Seo, Mi-Ryung Kim, Sang-Jae Lee, Sooncheol Ahn and Minjung Song

Molecules 2020, 25(12), 2864; https://doi.org/10.3390/molecules25122864 - 22 Jun 2020

Cited by 6 | Viewed by 2733

Abstract

Kirsten rat sarcoma viral oncogene homolog (KRAS)-driven colorectal cancer (CRC) is notorious to target with drugs and has shown ineffective treatment response. The seeds of Pharbitis nil, also known as morning glory, have been used as traditional medicine in East Asia. We focused [...] Read more.

Kirsten rat sarcoma viral oncogene homolog (KRAS)-driven colorectal cancer (CRC) is notorious to target with drugs and has shown ineffective treatment response. The seeds of Pharbitis nil, also known as morning glory, have been used as traditional medicine in East Asia. We focused on whether Pharbitis nil seeds have a suppressive effect on mutated KRAS-driven CRC as well as reserving muscle cell functions during CRC progression. Seeds of Pharbitis nil (Pharbitis semen) were separated by chromatography and the active compound of Pharbitis semen (PN) was purified by HPLC. The compound PN efficiently suppressed the proliferation of mutated KRAS-driven CRC cells and their clonogenic potentials in a concentration-dependent manner. It also induced apoptosis of SW480 human colon cancer cells and cell cycle arrest at the G2/M phase. The CRC related pathways, including RAS/ERK and AKT/mTOR, were assessed and PN reduced the phosphorylation of AKT and mTOR. Furthermore, PN preserved muscle cell proliferation and myotube formation in cancer conditioned media. In summary, PN significantly suppressed mutated KRAS-driven cell growth and reserved muscle cell function. Based on the current study, PN could be considered as a promising starting point for the development of a nature-derived drug against KRAS-mutated CRC progression. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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13 pages, 5288 KiB

Open AccessArticle

Nootkatone Inhibits Acute and Chronic Inflammatory Responses in Mice

by Lindaiane Bezerra Rodrigues Dantas, Ana Letícia Moreira Silva, Cícero Pedro da Silva Júnior, Isabel Sousa Alcântara, Maria Rayane Correia de Oliveira, Anita Oliveira Brito Pereira Bezerra Martins, Jaime Ribeiro-Filho, Henrique Douglas Melo Coutinho, Fabíolla Rocha Santos Passos, Lucindo José Quintans-Junior, Irwin Rose Alencar de Menezes, Raffaele Pezzani and Sara Vitalini

Molecules 2020, 25(9), 2181; https://doi.org/10.3390/molecules25092181 - 7 May 2020

Cited by 32 | Viewed by 4457

Abstract

Nootkatone (NTK) is a sesquiterpenoid found in essential oils of many species of Citrus (Rutaceae). Considering previous reports demonstrating that NTK inhibited inflammatory signaling pathways, this study aimed to investigate the effects of this compound in mice models of acute and chronic inflammation. [...] Read more.

Nootkatone (NTK) is a sesquiterpenoid found in essential oils of many species of Citrus (Rutaceae). Considering previous reports demonstrating that NTK inhibited inflammatory signaling pathways, this study aimed to investigate the effects of this compound in mice models of acute and chronic inflammation. Murine models of paw edema induced by carrageenan, dextran, histamine, and arachidonic acid, as well as carrageenan-induced peritonitis and pleurisy, were used to evaluate the effects of NTK on acute inflammation. A murine model of granuloma induced by cotton pellets was used to access the impact of NTK treatment on chronic inflammation. In the acute inflammation models, NTK demonstrated antiedematogenic effects and inhibited leukocyte recruitment, which was associated with decreased vascular permeability, inhibition of myeloperoxidase (MPO), interleukin (IL)1-β, and tumor necrosis factor (TNF)-α production. In silico analysis suggest that NTZ anti-inflammatory effects may also occur due to inhibition of cyclooxygenase (COX)-2 activity and antagonism of the histamine receptor type 1 (H₁). These mechanisms might have contributed to the reduction of granuloma weight and protein concentration in the homogenates, observed in the chronic inflammation model. In conclusion, NTK exerted anti-inflammatory effects that are associated with inhibition of IL1-β and TNF-α production, possibly due to inhibition of COX-2 activity and antagonism of the H1 receptor. However, further studies are required to characterize the effects of this compound on chronic inflammation. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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13 pages, 633 KiB

Open AccessArticle

Influence of the Phenological State of in the Antioxidant Potential and Chemical Composition of Ageratina havanensis. Effects on the P-Glycoprotein Function

by Trina H. García, Claudia Quintino da Rocha, Livan Delgado-Roche, Idania Rodeiro, Yaiser Ávila, Ivones Hernández, Cindel Cuellar, Miriam Teresa Paz Lopes, Wagner Vilegas, Giulia Auriemma, Iraida Spengler and Luca Rastrelli

Molecules 2020, 25(9), 2134; https://doi.org/10.3390/molecules25092134 - 2 May 2020

Cited by 2 | Viewed by 2424

Abstract

Ageratina havanensis (Kunth) R. M. King & H. Robinson is a species of flowering shrub in the family Asteraceae, native to the Caribbean and Texas. The aim of this work was to compare the quantitative chemical composition of extracts obtained from Ageratina havanensis [...] Read more.

Ageratina havanensis (Kunth) R. M. King & H. Robinson is a species of flowering shrub in the family Asteraceae, native to the Caribbean and Texas. The aim of this work was to compare the quantitative chemical composition of extracts obtained from Ageratina havanensis in its flowering and vegetative stages with the antioxidant potential and to determine the effects on P-glycoprotein (P-gp) function. The quantitative chemical composition of the extracts was determined quantifying their major flavonoids by UPLC-ESI-MS/MS and by PCA analysis. The effects of the extracts on P-gp activity was evaluated by Rhodamine 123 assay; antioxidant properties were determined by DPPH, FRAP and inhibition of lipid peroxidation methods. The obtained results show that major flavonoids were present in higher concentrations in vegetative stage than flowering stage. In particular, the extracts obtained in the flowering season showed a significantly higher ability to sequester free radicals compared to those of the vegetative season, meanwhile, the extracts obtained during the vegetative stage showed a significant inhibitory effect against brain lipid peroxidation and a strong reductive capacity. This study also showed the inhibitory effects of all ethanolic extracts on P-gp function in 4T1 cell line; these effects were unrelated to the phenological stage. This work shows, therefore, the first evidence on: the inhibition of P-gp function, the antioxidant effects and the content of major flavonoids of Ageratina havanensis. According to the obtained results, the species Ageratina havanensis (Kunth) R. M. King & H. Robinson could be a source of new potential inhibitors of drug efflux mediated by P-gp. A special focus on all these aspects must be taking into account for future studies. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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20 pages, 2135 KiB

Open AccessArticle

The Impact of Maltodextrin and Inulin on the Protection of Natural Antioxidants in Powders Made of Saskatoon Berry Fruit, Juice, and Pomace as Functional Food Ingredients

by Sabina Lachowicz, Anna Michalska-Ciechanowska and Jan Oszmiański

Molecules 2020, 25(8), 1805; https://doi.org/10.3390/molecules25081805 - 15 Apr 2020

Cited by 14 | Viewed by 3090

Abstract

The objective of this study was to examine the effect of inulin and maltodextrin applied during vacuum drying of Saskatoon berry fruit, juice, and pomace on the retention of bioactive compounds and antioxidant capacity (radical scavenging capacity (ABTS), ferric reducing antioxidant potential (FRAP)) [...] Read more.

The objective of this study was to examine the effect of inulin and maltodextrin applied during vacuum drying of Saskatoon berry fruit, juice, and pomace on the retention of bioactive compounds and antioxidant capacity (radical scavenging capacity (ABTS), ferric reducing antioxidant potential (FRAP)) of powders obtained. Ultra-high performance liquid chromatography (UPLC-PDA-ESI-MS/MS) was used to identify major groups of polyphenolic compounds, such as: flavan-3-ols (35% of all polyphenols for fruit powder, 33% for juice powder, and 39% for pomace powders of all polyphenols), anthocyanins (26% for fruit powder, 5% for juice powder, and 34% for pomace), phenolic acids (33% for fruit powder, 55% for juice powder, and 20% for pomace powder), and flavanols (6% for fruit powder, 6% for juice powder, and 7% for pomace powder). In general, the content of polyphenols was more dependent on the content than on the type of carrier used for drying, regardless of the matrix tested. The average sum of polyphenols and the antioxidant activity (for ABTS and FRAP assay) of the powders with 30% of carrier addition were 5054.2 mg/100 g dry matter (d.m.) as well as 5.3 and 3.6 mmol Trolox/100 g d.m. in the ABTS and FRAP tests, respectively. The increase in carrier concentration by 20% caused a decrease of 1.5-fold in the content of polyphenols and a 1.6-fold and 1.5-fold in the antioxidant potential, regardless of the matrix tested. The principal component analysis (PCA) analysis indicated that the freeze-drying process led to the lowest degradation of the identified compounds, regardless of the matrix tested, with the exception of juice and pomace powders dried by vacuum drying at 60 °C. In this case, the release of (−)-epicatechin was observed, causing an increase in the flavanol contents. Thus, this work demonstrated the effect of processing and matrix composition on the preservation of antioxidant bioactives in Saskatoon berry powders. Properly designed high-quality Saskatoon berry powders with the mentioned carriers may be used as nutraceutical additives to fortify food products and to improve their functional properties. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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14 pages, 3399 KiB

Open AccessArticle

Multifloroside Suppressing Proliferation and Colony Formation, Inducing S Cell Cycle Arrest, ROS Production, and Increasing MMP in Human Epidermoid Carcinoma Cell Lines A431

by Xin Zhang, Yamei Li, Zhengping Feng, Yaling Zhang, Ye Gong, Huanhuan Song, Xiaoli Ding and Yaping Yan

Molecules 2020, 25(1), 7; https://doi.org/10.3390/molecules25010007 - 18 Dec 2019

Cited by 6 | Viewed by 3188

Abstract

Multifloroside (4), together with 10-hydroxyoleoside 11-methyl ester (1), 10-hydroxyoleoside dimethyl ester (2), and 10-hydroxyligustroside (3), are all secoiridoids, which are naturally occurring compounds that possess a wide range of biological and pharmacological activities. However, the [...] Read more.

Multifloroside (4), together with 10-hydroxyoleoside 11-methyl ester (1), 10-hydroxyoleoside dimethyl ester (2), and 10-hydroxyligustroside (3), are all secoiridoids, which are naturally occurring compounds that possess a wide range of biological and pharmacological activities. However, the anti-cancer activity of 1–4 has not been evaluated yet. The objective of this work was to study the anti-cancer activities of 1–4 in the human epidermoid carcinoma cell lines A431 and the human non-small cell lung cancer (NSCLC) cell lines A549. The results indicate that 1–4 differ in potency in their ability to inhibit the proliferation of human A431 and A549 cells, and multifloroside (4) display the highest inhibitory activity against A431 cells. The structure-activity relationships suggest that the o-hydroxy-p-hydroxy-phenylethyl group may contribute to the anti-cancer activity against A431 cells. Multifloroside treatment can also inhibit cell colony formation, arrest the cell cycle in the S-phase, increase the levels of reactive-oxygen-species (ROS), and mitochondrial membrane potential (MMP), but it did not significantly induce cell apoptosis at low concentrations. The findings indicated that multifloroside (4) has the tendency to show selective anti-cancer effects in A431 cells, along with suppressing the colony formation, inducing S cell cycle arrest, ROS production, and increasing MMP. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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Review

Jump to: Editorial, Research

16 pages, 1657 KiB

Open AccessReview

Tabebuia impetiginosa: A Comprehensive Review on Traditional Uses, Phytochemistry, and Immunopharmacological Properties

by Jianmei Zhang, Stephanie Triseptya Hunto, Yoonyong Yang, Jongsung Lee and Jae Youl Cho

Molecules 2020, 25(18), 4294; https://doi.org/10.3390/molecules25184294 - 18 Sep 2020

Cited by 11 | Viewed by 6716

Abstract

Tabebuia impetiginosa, a plant native to the Amazon rainforest and other parts of Latin America, is traditionally used for treating fever, malaria, bacterial and fungal infections, and skin diseases. Additionally, several categories of phytochemicals and extracts isolated from T. impetiginosa have been [...] Read more.

Tabebuia impetiginosa, a plant native to the Amazon rainforest and other parts of Latin America, is traditionally used for treating fever, malaria, bacterial and fungal infections, and skin diseases. Additionally, several categories of phytochemicals and extracts isolated from T. impetiginosa have been studied via various models and displayed pharmacological activities. This review aims to uncover and summarize the research concerning T. impetiginosa, particularly its traditional uses, phytochemistry, and immunopharmacological activity, as well as to provide guidance for future research. A comprehensive search of the published literature was conducted to locate original publications pertaining to T. impetiginosa up to June 2020. The main inquiry used the following keywords in various combinations in titles and abstracts: T. impetiginosa, Taheebo, traditional uses, phytochemistry, immunopharmacological, anti-inflammatory activity. Immunopharmacological activity described in this paper includes its anti-inflammatory, anti-allergic, anti-autoimmune, and anti-cancer properties. Particularly, T. impetiginosa has a strong effect on anti-inflammatory activity. This paper also describes the target pathway underlying how T. impetiginosa inhibits the inflammatory response. The need for further investigation to identify other pharmacological activities as well as the exact target proteins of T. impetiginosa was also highlighted. T. impetiginosa may provide a new strategy for prevention and treatment of many immunological disorders that foster extensive research to identify potential anti-inflammatory and immunomodulatory compounds and fractions as well as to explore the underlying mechanisms of this herb. Further scientific evidence is required for clinical trials on its immunopharmacological effects and safety. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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65 pages, 14346 KiB

Open AccessReview

Ethnopharmacology of Fruit Plants: A Literature Review on the Toxicological, Phytochemical, Cultural Aspects, and a Mechanistic Approach to the Pharmacological Effects of Four Widely Used Species

by Aline T. de Carvalho, Marina M. Paes, Mila S. Cunha, Gustavo C. Brandão, Ana M. Mapeli, Vanessa C. Rescia, Silvia A. Oesterreich and Gustavo R. Villas-Boas

Molecules 2020, 25(17), 3879; https://doi.org/10.3390/molecules25173879 - 26 Aug 2020

Cited by 10 | Viewed by 7134

Abstract

Fruit plants have been widely used by the population as a source of food, income and in the treatment of various diseases due to their nutritional and pharmacological properties. The aim of this study was to review information from the most current research [...] Read more.

Fruit plants have been widely used by the population as a source of food, income and in the treatment of various diseases due to their nutritional and pharmacological properties. The aim of this study was to review information from the most current research about the phytochemical composition, biological and toxicological properties of four fruit species widely used by the world population in order to support the safe medicinal use of these species and encourage further studies on their therapeutic properties. The reviewed species are: Talisia esculenta, Brosimum gaudichaudii, Genipa americana, and Bromelia antiacantha. The review presents the botanical description of these species, their geographical distribution, forms of use in popular medicine, phytochemical studies and molecules isolated from different plant organs. The description of the pharmacological mechanism of action of secondary metabolites isolated from these species was detailed and toxicity studies related to them were reviewed. The present study demonstrates the significant concentration of phenolic compounds in these species and their anti-inflammatory, anti-tumor, photosensitizing properties, among others. Such species provide important molecules with pharmacological activity that serve as raw materials for the development of new drugs, making further studies necessary to elucidate mechanisms of action not yet understood and prove the safety for use in humans. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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29 pages, 865 KiB

Open AccessFeature PaperReview

Preclinical Activities of Epigallocatechin Gallate in Signaling Pathways in Cancer

by Mehdi Sharifi-Rad, Raffaele Pezzani, Marco Redaelli, Maira Zorzan, Muhammad Imran, Anees Ahmed Khalil, Bahare Salehi, Farukh Sharopov, William C. Cho and Javad Sharifi-Rad

Molecules 2020, 25(3), 467; https://doi.org/10.3390/molecules25030467 - 22 Jan 2020

Cited by 76 | Viewed by 7652

Abstract

Epigallocatechin gallate (EGCG) is the main bioactive component of catechins predominantly present in various types of tea. EGCG is well known for a wide spectrum of biological activities as an anti-oxidative, anti-inflammatory, and anti-tumor agent. The effect of EGCG on cell death mechanisms [...] Read more.

Epigallocatechin gallate (EGCG) is the main bioactive component of catechins predominantly present in various types of tea. EGCG is well known for a wide spectrum of biological activities as an anti-oxidative, anti-inflammatory, and anti-tumor agent. The effect of EGCG on cell death mechanisms via the induction of apoptosis, necrosis, and autophagy has been documented. Moreover, its anti-proliferative action has been demonstrated in many cancer cell lines. It was also involved in the modulation of cyclooxygenase-2, oxidative stress and inflammation of different cellular processes. EGCG has been reported as a promising agent target for plasma membrane proteins, such as epidermal growth factor receptor. In addition, it has been demonstrated a mechanism of action relying on the inhibition of ERK1/2, p38 MAPK, NF-κB, and vascular endothelial growth factor. Furthermore, EGCG and its derivatives were used in proteasome inhibition and they were involved in epigenetic mechanisms. In summary, EGCG is the most predominant and bioactive constituent of tea and may play a role in cancer prevention. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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Open AccessReview

Antidepressant Potential of Cinnamic Acids: Mechanisms of Action and Perspectives in Drug Development

by Lúcio Ricardo Leite Diniz, Marilia Trindade de Santana Souza, Joice Nascimento Barboza, Reinaldo Nóbrega de Almeida and Damião Pergentino de Sousa

Molecules 2019, 24(24), 4469; https://doi.org/10.3390/molecules24244469 - 6 Dec 2019

Cited by 22 | Viewed by 8610

Abstract

Depression is a health problem that compromises the quality of life of the world′s population. It has different levels of severity and a symptomatic profile that affects social life and performance in work activities, as well as a high number of deaths in [...] Read more.

Depression is a health problem that compromises the quality of life of the world′s population. It has different levels of severity and a symptomatic profile that affects social life and performance in work activities, as well as a high number of deaths in certain age groups. In the search for new therapeutic options for the treatment of this behavioral disorder, the present review describes studies on antidepressant activity of cinnamic acids, which are natural products found in medicinal plants and foods. The description of the animal models used and the mechanisms of action of these compounds are discussed. Full article

(This article belongs to the Special Issue Biological and Pharmacological Activity of Plant Natural Compounds)

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