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21 pages, 3626 KiB

Open AccessArticle

In Vitro Antiglycation and Methylglyoxal Trapping Effect of Peppermint Leaf (Mentha × piperita L.) and Its Polyphenols

by Izabela Fecka, Katarzyna Bednarska and Adam Kowalczyk

Molecules 2023, 28(6), 2865; https://doi.org/10.3390/molecules28062865 - 22 Mar 2023

Cited by 2 | Viewed by 1946

Abstract

The most significant reactive α-dicarbonyl RCS involved in the pathomechanism of glycation and related diseases is methylglyoxal (MGO). Hyperglycemia promotes the generation of MGO and leads to the formation of advanced glycation end products (AGEs). Therefore, MGO trapping and glycation inhibition appear to [...] Read more.

The most significant reactive α-dicarbonyl RCS involved in the pathomechanism of glycation and related diseases is methylglyoxal (MGO). Hyperglycemia promotes the generation of MGO and leads to the formation of advanced glycation end products (AGEs). Therefore, MGO trapping and glycation inhibition appear to be important therapeutic targets in prediabetes, diabetes, and in the early prevention of hyperglycemic complications. Peppermint leaf is commonly used as herbal tea, rich in polyphenols. Eriocitrin, its predominant component, in a double-blind, randomized controlled study reversed the prediabetic condition in patients. However, the antiglycation activity of this plant material and its polyphenols has not been characterized to date. Therefore, the aim of this study was to evaluate the ability of a peppermint leaf dry extract and its polyphenols to inhibit non-enzymatic protein glycation in a model with bovine serum albumin (BSA) and MGO as a glycation agent. Peppermint polyphenols were also evaluated for their potential to trap MGO in vitro, and the resulting adducts were analyzed by UHPLC-ESI-MS. To relate chemical composition to glycation inhibitory activity, the obtained peppermint extract was subjected to qualitative and quantitative analysis. The capability of peppermint leaf polyphenols to inhibit glycation (27.3–77.2%) and form adducts with MGO was confirmed. In the case of flavone aglycones, mono- and di-adducts with MGO were observed, while eriodictyol and eriocitrin effectively produced only mono-adducts. Rosmarinic acid and luteolin-7-O-glycosides did not reveal this action. IC₅₀ of the peppermint leaf dry extract was calculated at 2 mg/mL, equivalent to a concentration of 1.8 μM/mL of polyphenols, including ~1.4 μM/mL of flavonoids and ~0.4 μM/mL of phenolic acids. The contribution of the four major components to the anti-AGE activity of the extract was estimated at 86%, including eriocitrin 35.4%, rosmarinic acid 25.6%, luteolin-7-O-rutinoside 16.9%, luteolin-7-O-β-glucuronoside 8.1%, and others 14%. The effect of peppermint dry extract and polyphenols in inhibiting MGO-induced glycation in vitro was comparable to that of metformin used as a positive control. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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12 pages, 1197 KiB

Open AccessArticle

Antioxidant Activity and Photosynthesis Efficiency in Melissa officinalis Subjected to Heavy Metals Stress

by Dorota Adamczyk-Szabela, Ewa Chrześcijańska, Piotr Zielenkiewicz and Wojciech M. Wolf

Molecules 2023, 28(6), 2642; https://doi.org/10.3390/molecules28062642 - 14 Mar 2023

Cited by 5 | Viewed by 1174

Abstract

The aim of this study was to assess influence of cadmium and zinc treatments on antioxidant activity combined with the photosynthesis efficiency in a popular herb lemon balm (Melissa officinalis L.). Plants were grown under greenhouse conditions by the pot method. The [...] Read more.

The aim of this study was to assess influence of cadmium and zinc treatments on antioxidant activity combined with the photosynthesis efficiency in a popular herb lemon balm (Melissa officinalis L.). Plants were grown under greenhouse conditions by the pot method. The Mn, Cu, Cd, and Zn contents in soil and plants were measured by HR-CS FAAS. The activity of net photosynthesis, stomatal conductance, transpiration rate, intercellular CO₂, and index of chlorophyll in leaves were determined for all investigated species. Reduction of the net photosynthesis was observed for cultivations subjected to either Zn or Cd treatments. Phenolic contents were determined by the chemical Folin-Ciocalteu method, while enhanced voltammetric analysis was applied to assess the antioxidant properties of plant extracts. Both of these approaches yielded similar results. Herbal extracts had exceptional antioxidant capacities and were good scavengers of free radicals and reactive oxygen species. Structural similarity of cadmium and zinc facilitated their mutual structural exchange and prompted substantial expansion of phenolics under the mixed Zn and Cd treatments. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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16 pages, 3692 KiB

Open AccessArticle

Comparison of In Vitro Estrogenic Activity of Polygoni multiflori Radix and Cynanchi wilfordii Radix via the Enhancement of ERα/β Expression in MCF7 Cells

by Reshmi Akter, Dong Uk Yang, Jong Chan Ahn, Muhammad Awais, Jinnatun Nahar, Zelika Mega Ramadhania, Jong Yun Kim, Gyong Jai Lee, Gi-Young Kwak, Dong Wook Lee, Byoung Man Kong, Deok Chun Yang and Seok-Kyu Jung

Molecules 2023, 28(5), 2199; https://doi.org/10.3390/molecules28052199 - 27 Feb 2023

Cited by 3 | Viewed by 1552

Abstract

Postmenopausal women experience several symptoms, including inflammation and a sharp rise in oxidative stress caused by estrogen deprivation. Although estrogen replacement therapy (ERT) is generally regarded as an effective treatment for menopause, it has been used less frequently due to some adverse effects [...] Read more.

Postmenopausal women experience several symptoms, including inflammation and a sharp rise in oxidative stress caused by estrogen deprivation. Although estrogen replacement therapy (ERT) is generally regarded as an effective treatment for menopause, it has been used less frequently due to some adverse effects and high costs. Therefore, there is an immediate need to develop an effective herbal-based treatment that is affordable for low-income populations. Acordingly, this study explored the estrogen-like properties of methanol extracts from Cynanchum wilfordii (CW) and Poligonum multiflorum (PM), two important medicinal plants in Republic of Korea, Japan, and China. Due to the similar names and morphologies of these two radixes, they are frequently confused in the marketplace. Our previous colleagues discriminated between these two plants. In this study, we investigated the estrogenic activity of PM and CW using several in vitro assays with their possible mechanism of action. First, their phytochemical contents, such as gallic acid, 2,3,5,4′-tetrahydroxystilbene-2-O-glucoside (TSG) and emodin, were quantified using high-performance liquid chromatography (HPLC). Secondly, estrogen-like activity was assessed utilizing the well-known E-screen test and gene expression analysis in estrogen receptor (ER)-positive MCF7 cells. ROS inhibition and anti-inflammatory effects were analyzed using HaCaT and Raw 264.7 cells, respectively. Our findings demonstrate that PM extracts significantly increased the expression of the estrogen-dependent genes (ERα, ERβ, pS2) and boosted MCF7 cell proliferation in comparison to CW extracts. Additionally, PM extract demonstrated a significant reduction in reactive oxygen species (ROS) production as well as an enhanced antioxidant profile compared to the CW extract. Further, the PM extract treatment significantly reduced the generation of nitric oxide (NO) in RAW 264.7 cells, a murine macrophage cell line, demonstrating the anti-inflammatory properties of the extract. Finally, this research offers an experimental foundation for the use of PM as a phytoestrogen to minimize menopausal symptoms. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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14 pages, 642 KiB

Open AccessArticle

Behavioral Despair Is Blocked by the Flavonoid Chrysin (5,7-Dihydroxyflavone) in a Rat Model of Surgical Menopause

by Luis Ángel Flores-Aguilar, Jonathan Cueto-Escobedo, Abraham Puga-Olguín, Oscar Jerónimo Olmos-Vázquez, Gilberto Uriel Rosas-Sánchez, Blandina Bernal-Morales and Juan Francisco Rodríguez-Landa

Molecules 2023, 28(2), 587; https://doi.org/10.3390/molecules28020587 - 06 Jan 2023

Cited by 1 | Viewed by 1371

Abstract

Women have a high susceptibility to the negative effects of stress. Hormonal changes experienced throughout their reproductive life partially contribute to a higher incidence of anxiety and depression symptoms, particularly, during natural or surgical menopause. In preclinical research, the flavonoid chrysin (5,7-dihydroxyflavone) exerts [...] Read more.

Women have a high susceptibility to the negative effects of stress. Hormonal changes experienced throughout their reproductive life partially contribute to a higher incidence of anxiety and depression symptoms, particularly, during natural or surgical menopause. In preclinical research, the flavonoid chrysin (5,7-dihydroxyflavone) exerts anxiolytic- and anti-despair-like effects; however, it is unknown whether chrysin exerts a protective effect against the behavioral changes produced by acute stress on locomotor activity and behavioral despair in rats at 12-weeks post-ovariectomy. Ovariectomized female Wistar rats were assigned to eight groups: vehicle group (10% DMSO), three groups with chrysin and three groups with the same dose of allopregnanolone (0.5, 1, and 2 mg/kg), and one group with diazepam (2 mg/kg). The treatments were administered for seven consecutive days and the effects were evaluated in the locomotor activity and swimming tests. Chrysin (2 mg/kg) increased the latency to first immobility and decreased the total immobility time in the swimming test as the reference drugs allopregnanolone and diazepam (2 mg/kg); while locomotor activity prevented the behavioral changes produced by swimming. In conclusion, chrysin exerts a protective effect against the behavioral changes induced by acute stress, similarly to the neurosteroid allopregnanolone and the benzodiazepine diazepam in rats subjected to a surgical menopause model. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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13 pages, 2311 KiB

Open AccessArticle

Plumbagin Suppresses Breast Cancer Progression by Downregulating HIF-1α Expression via a PI3K/Akt/mTOR Independent Pathway under Hypoxic Condition

by Supawan Jampasri, Somrudee Reabroi, Duangjai Tungmunnithum, Warisara Parichatikanond and Darawan Pinthong

Molecules 2022, 27(17), 5716; https://doi.org/10.3390/molecules27175716 - 05 Sep 2022

Cited by 7 | Viewed by 1927

Abstract

Hypoxia-inducible factor-1α (HIF-1α) is a major transcriptional regulator that plays a crucial role in the hypoxic response of rapidly growing tumors. Overexpression of HIF-1α has been associated with breast cancer metastasis and poor clinical prognosis. Plumbagin, the main phytochemical from Plumbago indica, [...] Read more.

Hypoxia-inducible factor-1α (HIF-1α) is a major transcriptional regulator that plays a crucial role in the hypoxic response of rapidly growing tumors. Overexpression of HIF-1α has been associated with breast cancer metastasis and poor clinical prognosis. Plumbagin, the main phytochemical from Plumbago indica, exerts anticancer effects via multiple mechanisms. However, its precise mechanisms on breast cancer cells under hypoxic conditions has never been investigated. This study aims to examine the anticancer effect of plumbagin on MCF-7 cell viability, transcriptional activity, and protein expression of HIF-1α under normoxia and hypoxia-mimicking conditions, as well as reveal the underlying signaling pathways. The results demonstrate that plumbagin decreased MCF-7 cell viability under normoxic conditions, and a greater extent of reduction was observed upon exposure to hypoxic conditions induced by cobalt chloride (CoCl₂). Mechanistically, MCF-7 cells upregulated the expression of HIF-1α protein, mRNA, and the VEGF target gene under CoCl₂-induced hypoxia, which were abolished by plumbagin treatment. In addition, inhibition of HIF-1α and its downstream targets did not affect the signaling transduction of the PI3K/Akt/mTOR pathway under hypoxic state. This study provides mechanistic insight into the anticancer activity of plumbagin in breast cancer cells under hypoxic conditions by abolishing HIF-1α at transcription and post-translational modifications. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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21 pages, 2998 KiB

Open AccessArticle

Therapeutic Versus Preventative Use of Ginkgo biloba Extract (EGb 761) against Indomethacin-Induced Gastric Ulcer in Mice

by Ahmed M. Abd-Eldayem, Sulaiman Mohammed Alnasser, Hanan H. Abd-Elhafeez, Soha A. Soliman and Rania A. Abdel-Emam

Molecules 2022, 27(17), 5598; https://doi.org/10.3390/molecules27175598 - 31 Aug 2022

Cited by 6 | Viewed by 2632

Abstract

The main bioactive constituents in the standardized Ginkgo biloba leaf extract (EGb 761) are the terpene lactones and flavonoid glycosides. EGb 761’s antioxidant and anti-inflammatory properties have previously been demonstrated. Indomethacin-induced gastric ulcers have a multifactorial etiology and represent a major restriction to [...] Read more.

The main bioactive constituents in the standardized Ginkgo biloba leaf extract (EGb 761) are the terpene lactones and flavonoid glycosides. EGb 761’s antioxidant and anti-inflammatory properties have previously been demonstrated. Indomethacin-induced gastric ulcers have a multifactorial etiology and represent a major restriction to its therapeutic utility. The underlying ulcerogenic process involves oxidative and inflammatory biomolecular insults. This study was performed to explore the curative and preventative benefits of EGb 761 in experimentally-induced ulcers. To develop gastric ulcers in mice, indomethacin (40 mg/kg) was administered orally. EGb 761 (200 mg/kg) was given by gavage for 7 days before (preventative) and after (therapeutic) indomethacin administration. The histological alterations and macroscopic mucosal lesions were assessed. In gastric tissue homogenates, malondialdehyde (MDA), reduced glutathione (GSH), nitric oxide (NO), and inflammatory cytokines were measured. The expressions of cyclooxygenase-2 (COX-2), cytokines, and proliferating cell nuclear antigen (PCNA) in the stomach mucosa were also investigated. The ulcer index, histological alterations, gastric oxidants, and inflammatory biomarkers were all significantly increased by indomethacin. In stomach specimens, it increased COX-2 and PCNA expression. EGb 761 treatments, both prophylactic and therapeutic, resulted in significant reductions in ulcer lesions, nitrosative and oxidative damage, and inflammatory markers, along with the lowering of COX-2 and PCNA expressions. Furthermore, in the fight against stomach ulcers, EGb 761 treatment was found to be more efficient than prevention. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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18 pages, 2954 KiB

Open AccessArticle

Tamarind Seed Coat: A Catechin-Rich Source with Anti-Oxidation, Anti-Melanogenesis, Anti-Adipogenesis and Anti-Microbial Activities

by Roongrawee Wandee, Khaetthareeya Sutthanut, Jenjira Songsri, Siriyakorn Sonsena, Ornnicha Krongyut, Patcharaporn Tippayawat, Wipawee Tukummee and Theera Rittirod

Molecules 2022, 27(16), 5319; https://doi.org/10.3390/molecules27165319 - 20 Aug 2022

Cited by 4 | Viewed by 2637

Abstract

Tamarindus indica L. or tamarind seed is an industrial by-product of interest to be investigated for its potential and value-added application. An ethanolic tamarind seed coat (TS) extract was prepared using the maceration technique and used to determine the phytochemical composition and bioactivities. [...] Read more.

Tamarindus indica L. or tamarind seed is an industrial by-product of interest to be investigated for its potential and value-added application. An ethanolic tamarind seed coat (TS) extract was prepared using the maceration technique and used to determine the phytochemical composition and bioactivities. The total phenolic and flavonoid contents were determined using colorimetric methods; moreover, chemical constituents were identified and quantified compared to the standard compounds using the HPLC-UV DAD technique. Bioactivities were investigated using various models: antioxidative activity in a DPPH assay model, anti-melanogenesis in B16 melanoma cells, anti-adipogenesis in 3T3-L1 adipocytes, and anti-microbial activity against S. aureus, P. aeruginosa, E. coli, and C. albican using agar disc diffusion and microdilution methods. The results manifested a high content of catechin as a chemical constituent and multiple beneficiary bioactivities of TS extract, including superior antioxidation to ascorbic acid and catechin, comparable anti-melanogenesis to deoxyarbutin, and significant anti-adipogenesis through inhibition of pre-adipocyte differentiation and reduction of lipid and triglyceride accumulation, and a broad spectral anti-microbial activity with a selectively high susceptibility to S. aureus when compared to 1% Parabens. Conclusively, TS extract has been revealed as a potential bioactive agent as well as an alternative preservative for application in food, cosmetic, and pharmaceutical product development. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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17 pages, 2092 KiB

Open AccessArticle

Evaluation of Phytochemistry and Pharmacological Properties of Alnus nitida

by Moniba Sajid, Muhammad Rashid Khan, Muhammad Umar Ijaz, Hammad Ismail, Muhammad Zeeshan Bhatti, Sayed Afzal Shah, Saima Ali, Muhammad Usman Tareen, Saqer S. Alotaibi, Sarah M. Albogami and Gaber El-Saber Batiha

Molecules 2022, 27(14), 4582; https://doi.org/10.3390/molecules27144582 - 18 Jul 2022

Cited by 4 | Viewed by 1827

Abstract

In the current study, the anti-inflammatory and analgesic potential of Alnus nitida (leaves and fruits) was evaluated in the Sprague-Dawley rat. Traditionally, A. nitida was used for the treatment of inflammatory ailments. However, A. nitida leaves and fruits have not been yet reported [...] Read more.

In the current study, the anti-inflammatory and analgesic potential of Alnus nitida (leaves and fruits) was evaluated in the Sprague-Dawley rat. Traditionally, A. nitida was used for the treatment of inflammatory ailments. However, A. nitida leaves and fruits have not been yet reported regarding any potential medicinal effects. Leaves/fruits of A. nitida were extracted with methanol and fractionated to attain n-hexane, chloroform, ethyl acetate and aqueous fractions. These extracts were then evaluated for in vivo analgesic and anti-inflammatory potential. For in vivo anti-inflammatory activity, carrageenan-induced paw edema assay, Freunds’ complete adjuvant-induced edema, xylene-induced ear edema and histamine-induced paw edema models were used in rats, which showed significant (p < 0.01) reduction (70–80%) in edema in comparison of inflammatory controls. On other hand, for the analgesic assessment, hot plate assay and acetic acid-induced writhing tests were used, which showed a significant (p < 0.01) rise in latency time (40–60%) as compared with pain-induced controls. These results were comparable with standard drugs in a concentration-dependent manner and no mortality or toxicity was observed during all experiments. Then, for the identification of chemical constituents gas chromatography–mass spectrometry (GC-MS) analysis was performed, which indicated the presence of neophytadiene, 3,7,11,15-Tetramethyl-2-hexadecen-1-ol, phytol and vitamin E, justifying the use of A. nitida to treat inflammatory disorders. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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15 pages, 534 KiB

Open AccessArticle

Effects of Seed Roasting Temperature on Sesame Oil Fatty Acid Composition, Lignan, Sterol and Tocopherol Contents, Oxidative Stability and Antioxidant Potential for Food Applications

by Radia Arab, Susana Casal, Teresa Pinho, Rebeca Cruz, Mohamed Lamine Freidja, José Manuel Lorenzo, Christophe Hano, Khodir Madani and Lila Boulekbache-Makhlouf

Molecules 2022, 27(14), 4508; https://doi.org/10.3390/molecules27144508 - 14 Jul 2022

Cited by 17 | Viewed by 2533

Abstract

Roasting is a key step for preparing sesame oil that leads to important changes in its organoleptic properties and quality. In this study, white sesame seeds were roasted for 20 min in an electric oven at different temperatures (120, 150, 180, 210, 250 [...] Read more.

Roasting is a key step for preparing sesame oil that leads to important changes in its organoleptic properties and quality. In this study, white sesame seeds were roasted for 20 min in an electric oven at different temperatures (120, 150, 180, 210, 250 and 300 °C). The oils extracted from unroasted and roasted seeds were compared for their chemical composition: fatty acids (including trans isomers), phytosterols, lignans (sesamin and sesamolin), tocopherols and total phenolic compounds, as well as their oxidative stability and antiradical capacity. There were no obvious differences in the oil densities, refractive indexes or iodine values, but the saponification values were affected by temperature. Relevant primary and secondary lipid oxidation were observed at T > 250 °C, resulting in a higher p-anisidine value and K232 as well as K268 values. Roasting improved oil yield (from 33.5 to 62.6%), increased its induction period (from 5.5 to 10.5 h) and enhanced the total phenolic content (from 152 to 194 mg/100 g) and antiradical activity of the extracted oil. Depending on roasting temperature, a gradual decline was recorded in total amounts of phytosterols (up to 17.4%), γ-tocopherol (up to 10.6%), sesamolin (maximum of 27.5%) and sesamin (maximum of 12.5%). All the investigated oils presented a low quantity in triglyceride polymers, clearly below the maximum tolerated quantity according to the European regulation. The optimal roasting temperature for obtaining high nutritional grade oil within the permissible values was 210 °C. The unsaponifiable components (including lignans and sterols) extracted from roasted seeds have been shown to be natural additives to fresh meatball products to extend shelf life. The results of this study may help to boost the nutritional content of plant-based diets by allowing for the use of roasted sesame seed oil and its components. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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15 pages, 668 KiB

Open AccessArticle

In Vitro and In Vivo Genotoxicity Assessments and Phytochemical Analysis of the Traditional Herbal Prescription Siryung-Tang

by Chang-Seob Seo, Mi-Sook Jung, Hyeun-Kyoo Shin and Mee-Young Lee

Molecules 2022, 27(13), 4066; https://doi.org/10.3390/molecules27134066 - 24 Jun 2022

Cited by 3 | Viewed by 1348

Abstract

Siryung-tang (SRT) is a traditional herbal prescription containing Oryeong-san and Soshiho-tang that is used to treat digestive system diseases. We performed safety evaluations of SRT based on genotoxicity and developed an assay for quality control using high-performance liquid chromatography with a photodiode array [...] Read more.

Siryung-tang (SRT) is a traditional herbal prescription containing Oryeong-san and Soshiho-tang that is used to treat digestive system diseases. We performed safety evaluations of SRT based on genotoxicity and developed an assay for quality control using high-performance liquid chromatography with a photodiode array detector. Genotoxicity was evaluated based on bacterial reverse mutation (Salmonella typhimurium TA1535, TA98, TA100, and TA1537, and Escherichia coli WP2 uvrA), chromosomal aberration (Chinese hamster lung cells), and micronucleus (mouse) tests. Quality control analysis was conducted using a SunFire C₁₈ column and gradient elution with a distilled water–acetonitrile mobile phase system containing 0.1% (v/v) formic acid for 12 markers (5-(hydroxy-methyl)furfural, 3,4-dihydroxybenzaldehyde, liquiritin apioside, liquiritin, coumarin, baicalin, wogonoside, cinnamaldehyde, baicalein, glycyrrhizin, wogonin, and atractylenolide III). SRT showed no genotoxicity in three tests. Ames tests showed that SRT at 313–5000 μg/plate did not significantly increase the number of revertant colonies with or without metabolic activation among five bacterial strains. Moreover, in vivo micronucleus testing showed that SRT did not increase the frequency of bone marrow micronuclei. The number of chromosomal aberrations associated with SRT was similar to that observed in the negative controls. The 12 markers were detected at 0.04–16.86 mg/g in a freeze-dried SRT sample and completely eluted within 45 min. The extraction recovery was 95.39–104.319% and the relative standard deviation value of the precision was ≤2.09%. Our study will be used as basic data for the safety and standardization of SRT. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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13 pages, 1518 KiB

Open AccessArticle

Identifying Major Drivers of Antioxidant Activities in Complex Polyphenol Mixtures from Grape Canes

by Manon Ferrier, Kévin Billet, Samantha Drouet, Duangjai Tungmunnithum, Magdalena Anna Malinowska, Cécile Marchal, Sandrine Dedet, Nathalie Giglioli-Guivarc’h, Christophe Hano and Arnaud Lanoue

Molecules 2022, 27(13), 4029; https://doi.org/10.3390/molecules27134029 - 23 Jun 2022

Cited by 6 | Viewed by 1918

Abstract

Grape canes represent a valuable source of numerous polyphenols with antioxidant properties, whose compositions vary depending on the genotype and environmental factors. Antioxidant activities of pure molecules are often reported without considering possible interactions that may occur in complex polyphenol mixture. Using UPLC-MS-based [...] Read more.

Grape canes represent a valuable source of numerous polyphenols with antioxidant properties, whose compositions vary depending on the genotype and environmental factors. Antioxidant activities of pure molecules are often reported without considering possible interactions that may occur in complex polyphenol mixture. Using UPLC-MS-based metabolomics and unsupervised classification, we explored the polyphenol variations in grape cane extracts from a collection of European varieties. Antioxidant activities were assessed using ORAC, ABTS, DPPH, FRAP, CUPRAC and chelation assays. Pairwise correlations between polyphenols and antioxidant capacities were performed to identify molecules that contributed more to the antioxidant capacities within a complex mixture of polyphenols. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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14 pages, 2255 KiB

Open AccessArticle

Anticonvulsant Effect of Turmeric and Resveratrol in Lithium/Pilocarpine-Induced Status Epilepticus in Wistar Rats

by Isaac Zamora-Bello, Eduardo Rivadeneyra-Domínguez and Juan Francisco Rodríguez-Landa

Molecules 2022, 27(12), 3835; https://doi.org/10.3390/molecules27123835 - 14 Jun 2022

Cited by 3 | Viewed by 2035

Abstract

Epilepsy is a chronic neurological disorder that lacks a cure. The use of plant-derived antioxidant molecules such as those contained in turmeric powder and resveratrol may produce short-term anticonvulsant effects. A total of 42 three-month-old male Wistar rats were divided into six groups [...] Read more.

Epilepsy is a chronic neurological disorder that lacks a cure. The use of plant-derived antioxidant molecules such as those contained in turmeric powder and resveratrol may produce short-term anticonvulsant effects. A total of 42 three-month-old male Wistar rats were divided into six groups (n = 7 in each group): Vehicle (purified water), turmeric (150 and 300 mg/kg, respectively), and resveratrol (30 and 60 mg/kg, respectively), administered per os (p.o.) every 24 h for 35 days. Carbamazepine (300 mg/kg/5 days) was used as a pharmacological control for anticonvulsant activity. At the end of the treatment, status epilepticus was induced using the lithium–pilocarpine model [3 mEq/kg, intraperitoneally (i.p.) and 30 mg/kg subcutaneously (s.c.), respectively]. Seizures were evaluated using the Racine scale. The 300 mg/kg of turmeric and 60 mg/kg of resveratrol groups had an increased latency to the first generalized seizure. The groups treated with 150 and 300 mg/kg of turmeric and 60 mg/kg of resveratrol also had an increased latency to status epilepticus and a decreased number of generalized seizures compared to the vehicle group. The chronic administration of turmeric and resveratrol exerts anticonvulsant effects without producing kidney or liver damage. This suggests that both of these natural products of plant origin could work as adjuvants in the treatment of epilepsy. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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16 pages, 2643 KiB

Open AccessArticle

Differential Flavonoid and Other Phenolic Accumulations and Antioxidant Activities of Nymphaea lotus L. Populations throughout Thailand

by Duangjai Tungmunnithum, Samantha Drouet, Laurine Garros and Christophe Hano

Molecules 2022, 27(11), 3590; https://doi.org/10.3390/molecules27113590 - 02 Jun 2022

Cited by 3 | Viewed by 1907

Abstract

Nymphaea lotus L. is a potential plant in the Nymphaeaceae family that is well-recognized as an economic and traditional medicinal plant in Thailand and other countries. Its pharmacological and medicinal effects have been confirmed. However, there is no study going deeper into the [...] Read more.

Nymphaea lotus L. is a potential plant in the Nymphaeaceae family that is well-recognized as an economic and traditional medicinal plant in Thailand and other countries. Its pharmacological and medicinal effects have been confirmed. However, there is no study going deeper into the population level to examine the phytochemical variation and biological activity of each population that benefits phytopharmaceutical and medical applications using this plant as raw material. This study was intensely conducted to complete this important research gap to investigate the flavonoid profiles from its floral parts, the stamen and perianth, as well as the antioxidant potential of the 13 populations collected from every floristic region by (1) analyzing their flavonoid profiles, including the HPLC analysis, and (2) investigating the antioxidant capacity of these populations using three assays to observe different antioxidant mechanisms. The results indicated that the northeastern and northern regions are the most abundant floristic regions, and flavonoids are the main phytochemical class of both stamen and perianth extracts from N. lotus. The stamen offers higher flavonoids and richer antioxidant potential compared with the perianth. This finding is also the first completed report at the population level to describe the significant correlation between the phytochemical profiles in floral parts extracts and the main antioxidant activity, which is mediated by the electron transfer mechanism. The results from the Pearson correlation coefficients between several phytochemicals and different antioxidant assessments highlighted that the antioxidant capability of these extracts is the result of complex phytochemical combinations. The frontier knowledge from these current findings helps to open up doors for phytopharmaceutical industries to discover their preferred populations and floral parts that fit with their targeted products. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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20 pages, 3229 KiB

Open AccessArticle

Andrographolide Exhibits Anticancer Activity against Breast Cancer Cells (MCF-7 and MDA-MB-231 Cells) through Suppressing Cell Proliferation and Inducing Cell Apoptosis via Inactivation of ER-α Receptor and PI3K/AKT/mTOR Signaling

by Ruhainee Tohkayomatee, Somrudee Reabroi, Duangjai Tungmunnithum, Warisara Parichatikanond and Darawan Pinthong

Molecules 2022, 27(11), 3544; https://doi.org/10.3390/molecules27113544 - 31 May 2022

Cited by 15 | Viewed by 3660

Abstract

Breast cancer is the most common cancer among women worldwide. Chemotherapy followed by endocrine therapy is the standard treatment strategy after surgery or radiotherapy. However, breast cancer is highly resistant to the treatments leading to the recurrence of breast cancer. As a result, [...] Read more.

Breast cancer is the most common cancer among women worldwide. Chemotherapy followed by endocrine therapy is the standard treatment strategy after surgery or radiotherapy. However, breast cancer is highly resistant to the treatments leading to the recurrence of breast cancer. As a result, the development of alternative medicines derived from natural plants with fewer side effects is being emphasized. Andrographolide isolated from Andrographis paniculata is one of the potential substances with anti-cancer properties in a variety of cell types, including breast cancer cells. This study aims to investigate the anti-cancer effects of andrographolide in breast cancer cells by evaluating cell viability and apoptosis as well as its underlying mechanisms through estrogen receptor (ER)-dependent and PI3K/AKT/mTOR signaling pathways. Cell viability, cell apoptosis, mRNA or miRNA, and protein expression were examined by MTT assay, Annexin V-FITC, qRT-PCR, and Western blot analysis, respectively. MCF-7 and MDA-MB-231 cell viability was reduced in a concentration- and time-dependent manner after andrographolide treatment. Moreover, andrographolide induced cell apoptosis in both MCF-7 and MDA-MB-231 cells by inhibiting Bcl-2 and enhancing Bax expression at both mRNA and protein levels. In MCF-7 cells, the ER-positive breast cancer, andrographolide showed an inhibitory effect on cell proliferation through downregulation of ERα, PI3K, and mTOR expression levels. Andrographolide also inhibited MDA-MB-231 breast cancer cell proliferation via induction of cell apoptosis. However, the inhibition of MCF-7 and MDA-MB-231 cell proliferation of andrographolide treatment did not disrupt miR-21. Our findings showed that andrographolide possesses an anti-estrogenic effect by suppressing cell proliferation in MCF-7 cells. The effects were comparable to those of the anticancer drug fulvestrant in MCF-7 cells. This study provides new insights into the anti-cancer effect of andrographolide on breast cancer and suggests andrographolide as a potential alternative from the natural plant for treating breast cancer types that are resistant to tamoxifen and fulvestrant. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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Review

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19 pages, 1168 KiB

Open AccessReview

Effects of Hydroxytyrosol in Endothelial Functioning: A Comprehensive Review

by Ubashini Vijakumaran, Janushaa Shanmugam, Jun Wei Heng, Siti Sarah Azman, Muhammad Dain Yazid, Nur Atiqah Haizum Abdullah and Nadiah Sulaiman

Molecules 2023, 28(4), 1861; https://doi.org/10.3390/molecules28041861 - 16 Feb 2023

Cited by 9 | Viewed by 3513

Abstract

Pharmacologists have been emphasizing and applying plant and herbal-based treatments in vascular diseases for decades now. Olives, for example, are a traditional symbol of the Mediterranean diet. Hydroxytyrosol is an olive-derived compound known for its antioxidant and cardioprotective effects. Acknowledging the merit of [...] Read more.

Pharmacologists have been emphasizing and applying plant and herbal-based treatments in vascular diseases for decades now. Olives, for example, are a traditional symbol of the Mediterranean diet. Hydroxytyrosol is an olive-derived compound known for its antioxidant and cardioprotective effects. Acknowledging the merit of antioxidants in maintaining endothelial function warrants the application of hydroxytyrosol in endothelial dysfunction salvage and recovery. Endothelial dysfunction (ED) is an impairment of endothelial cells that adversely affects vascular homeostasis. Disturbance in endothelial functioning is a known precursor for atherosclerosis and, subsequently, coronary and peripheral artery disease. However, the effects of hydroxytyrosol on endothelial functioning were not extensively studied, limiting its value either as a nutraceutical supplement or in clinical trials. The action of hydroxytyrosol in endothelial functioning at a cellular and molecular level is gathered and summarized in this review. The favorable effects of hydroxytyrosol in the improvement of endothelial functioning from in vitro and in vivo studies were scrutinized. We conclude that hydroxytyrosol is capable to counteract oxidative stress, inflammation, vascular aging, and arterial stiffness; thus, it is beneficial to preserve endothelial function both in vitro and in vivo. Although not specifically for endothelial dysfunction, hydroxytyrosol safety and efficacy had been demonstrated via in vivo and clinical trials for cardiovascular-related studies. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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24 pages, 2547 KiB

Open AccessReview

Pharmacotherapeutics Applications and Chemistry of Chalcone Derivatives

by Jagjit Singh Dhaliwal, Said Moshawih, Khang Wen Goh, Mei Jun Loy, Md. Sanower Hossain, Andi Hermansyah, Vijay Kotra, Nurolaini Kifli, Hui Poh Goh, Sachinjeet Kaur Sodhi Dhaliwal, Hayati Yassin and Long Chiau Ming

Molecules 2022, 27(20), 7062; https://doi.org/10.3390/molecules27207062 - 19 Oct 2022

Cited by 29 | Viewed by 4326

Abstract

Chalcones have been well examined in the extant literature and demonstrated antibacterial, antifungal, anti-inflammatory, and anticancer properties. A detailed evaluation of the purported health benefits of chalcone and its derivatives, including molecular mechanisms of pharmacological activities, can be further explored. Therefore, this review [...] Read more.

Chalcones have been well examined in the extant literature and demonstrated antibacterial, antifungal, anti-inflammatory, and anticancer properties. A detailed evaluation of the purported health benefits of chalcone and its derivatives, including molecular mechanisms of pharmacological activities, can be further explored. Therefore, this review aimed to describe the main characteristics of chalcone and its derivatives, including their method synthesis and pharmacotherapeutics applications with molecular mechanisms. The presence of the reactive α,β-unsaturated system in the chalcone’s rings showed different potential pharmacological properties, including inhibitory activity on enzymes, anticancer, anti-inflammatory, antibacterial, antifungal, antimalarial, antiprotozoal, and anti-filarial activity. Changing the structure by adding substituent groups to the aromatic ring can increase potency, reduce toxicity, and broaden pharmacological action. This report also summarized the potential health benefits of chalcone derivatives, particularly antimicrobial activity. We found that several chalcone compounds can inhibit diverse targets of antibiotic-resistance development pathways; therefore, they overcome resistance, and bacteria become susceptible to antibacterial compounds. A few chalcone compounds were more active than conventional antibiotics, like vancomycin and tetracycline. On another note, a series of pyran-fused chalcones and trichalcones can block the NF-B signaling complement system implicated in inflammation, and several compounds demonstrated more potent lipoxygenase inhibition than NSAIDs, such as indomethacin. This report integrated discussion from the domains of medicinal chemistry, organic synthesis, and diverse pharmacological applications, particularly for the development of new anti-infective agents that could be a useful reference for pharmaceutical scientists. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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17 pages, 4769 KiB

Open AccessReview

Pharmacological, Neurochemical, and Behavioral Mechanisms Underlying the Anxiolytic- and Antidepressant-like Effects of Flavonoid Chrysin

by Juan Francisco Rodríguez-Landa, León Jesús German-Ponciano, Abraham Puga-Olguín and Oscar Jerónimo Olmos-Vázquez

Molecules 2022, 27(11), 3551; https://doi.org/10.3390/molecules27113551 - 31 May 2022

Cited by 13 | Viewed by 3136

Abstract

Chrysin (5,7-dihydroxyflavone) is a flavonoid isolated from plants, such as Passiflora coerulea, Passiflora incarnata, and Matricaria chamomilla. This natural molecule exerts diverse pharmacological effects, which includes antioxidant, anti-inflammatory, anti-cancer, neuroprotective, and anti-apoptotic effects. Additionally, in brain structures, such as the [...] Read more.

Chrysin (5,7-dihydroxyflavone) is a flavonoid isolated from plants, such as Passiflora coerulea, Passiflora incarnata, and Matricaria chamomilla. This natural molecule exerts diverse pharmacological effects, which includes antioxidant, anti-inflammatory, anti-cancer, neuroprotective, and anti-apoptotic effects. Additionally, in brain structures, such as the hippocampus, prefrontal cortex, raphe nucleus, and striatum, involved in the physiopathology of anxiety and depression disorders, several neuropharmacological activities, including the activation of neurotransmitter systems (GABAergic, serotonergic, dopaminergic, and noradrenergic), neurotrophic factors, such as brain-derived neurotrophic factor and the nerve growth factor, and some signaling pathways are affected. The results showed that the anxiolytic and antidepressant-like effects of chrysin occurs through its interaction with specific neurotransmitter systems, principally the GABAergic and the serotonergic, and activation of other neurotrophic factors. However, it is not possible to discard the antioxidant and anti-inflammatory activities of chrysin while producing its anxiolytic- and antidepressant-like effects. Although these results have been obtained principally from pre-clinical research, they consistently demonstrate the potential therapeutic use of flavonoid chrysin as an anxiolytic and antidepressant agent. Therefore, this flavonoid could be considered as a promising novel therapy for anxiety and depression disorders. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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15 pages, 776 KiB

Open AccessReview

Nigella sativa L. and COVID-19: A Glance at The Anti-COVID-19 Chemical Constituents, Clinical Trials, Inventions, and Patent Literature

by Mohd Imran, Shah Alam Khan, Abida, Mohammed Kanan Alshammari, Saif M. Alkhaldi, Fayez Nafea Alshammari, Mehnaz Kamal, Ozair Alam, Syed Mohammed Basheeruddin Asdaq, A. Khuzaim Alzahrani and Shahamah Jomah

Molecules 2022, 27(9), 2750; https://doi.org/10.3390/molecules27092750 - 25 Apr 2022

Cited by 16 | Viewed by 4586

Abstract

COVID-19 has had an impact on human quality of life and economics. Scientists have been identifying remedies for its prevention and treatment from all possible sources, including plants. Nigella sativa L. (NS) is an important medicinal plant of Islamic value. This review highlights [...] Read more.

COVID-19 has had an impact on human quality of life and economics. Scientists have been identifying remedies for its prevention and treatment from all possible sources, including plants. Nigella sativa L. (NS) is an important medicinal plant of Islamic value. This review highlights the anti-COVID-19 potential, clinical trials, inventions, and patent literature related to NS and its major chemical constituents, like thymoquinone. The literature was collected from different databases, including Pubmed, Espacenet, and Patentscope. The literature supports the efficacy of NS, NS oil (NSO), and its chemical constituents against COVID-19. The clinical data imply that NS and NSO can prevent and treat COVID-19 patients with a faster recovery rate. Several inventions comprising NS and NSO have been claimed in patent applications to prevent/treat COVID-19. The patent literature cites NS as an immunomodulator, antioxidant, anti-inflammatory, a source of anti-SARS-CoV-2 compounds, and a plant having protective effects on the lungs. The available facts indicate that NS, NSO, and its various compositions have all the attributes to be used as a promising remedy to prevent, manage, and treat COVID-19 among high-risk people as well as for the therapy of COVID-19 patients of all age groups as a monotherapy or a combination therapy. Many compositions of NS in combination with countless medicinal herbs and medicines are still unexplored. Accordingly, the authors foresee a bright scope in developing NS-based anti-COVID-19 composition for clinical use in the future. Full article

(This article belongs to the Special Issue Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications)

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