Research

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27 pages, 16055 KiB

Open AccessArticle

Acute and Sub-Chronic Intraperitoneal Toxicity Studies of the Elsholtzia ciliata Herbal Extract in Balb/c Mice

by Regina Mačianskienė, Vilma Zigmantaitė, Inga Andriulė, Dalia Pangonytė, Ilona Sadauskienė, Odeta Arandarčikaitė, Arūnas Stankevičius, Juozas Grigas, Arnoldas Pautienius, Rimantas Treinys, Antanas Navalinskas, Ramunė Grigalevičiūtė, Audrius Kučinskas, Lauryna Pudžiuvelytė, Jurga Bernatonienė and Jonas Jurevičius

Pharmaceutics 2023, 15(10), 2417; https://doi.org/10.3390/pharmaceutics15102417 - 03 Oct 2023

Cited by 1 | Viewed by 1106

Abstract

Elsholtzia ciliata essential oil (E. ciliata) has been reported to have an impact on the cardiovascular system. However, its toxicity remains unknown. Therefore, the objective of this investigation was to evaluate the toxicological aspects of the E. ciliata extract. Male Balb/c [...] Read more.

Elsholtzia ciliata essential oil (E. ciliata) has been reported to have an impact on the cardiovascular system. However, its toxicity remains unknown. Therefore, the objective of this investigation was to evaluate the toxicological aspects of the E. ciliata extract. Male Balb/c mice were subjected to either acute (a single dose administered for 24 h) or sub-chronic (daily dose for 60 days) intraperitoneal injections of the E. ciliata extract. The mice were assessed for blood hematological/biochemical profiles, mitochondrial functions, and histopathological changes. Additionally, in vitro cytotoxicity assessments of the E. ciliata extract were performed on immobilized primate kidney cells (MARC-145, Vero) and rat liver cells (WBF344) to evaluate cell viability. The control groups received an equivalent volume of olive oil or saline. Our results demonstrated no significant detrimental effects on hematological and biochemical parameters, mitochondrial functions, cellular cytotoxicity, or pathological alterations in vital organs following the intraperitoneal administration of the E. ciliata extract over the 60-day sub-chronic toxicity study. In general, E. ciliata displayed no indications of toxicity, suggesting that the E. ciliata extract is a safe natural product with a well-defined therapeutic and protective index (found to be 90 and 54, respectively) in Balb/c mice. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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23 pages, 4026 KiB

Open AccessArticle

Therapeutic Effects of Oral Application of Menthol and Extracts from Tormentil (Potentilla erecta), Raspberry Leaves (Rubus idaeus), and Loosestrife (Lythrum salicaria) during Acute Murine Campylobacteriosis

by Rasmus Bandick, Lia V. Busmann, Soraya Mousavi, Nizar W. Shayya, Jakub P. Piwowarski, Sebastian Granica, Matthias F. Melzig, Stefan Bereswill and Markus M. Heimesaat

Pharmaceutics 2023, 15(10), 2410; https://doi.org/10.3390/pharmaceutics15102410 - 01 Oct 2023

Cited by 1 | Viewed by 1081

Abstract

Human food-borne infections with the enteropathogen Campylobacter jejuni are becoming increasingly prevalent worldwide. Since antibiotics are usually not indicated in campylobacteriosis, alternative treatment regimens are important. We here investigated potential disease-alleviating effects of menthol and of extracts from tormentil, raspberry leaves, and loosestrife [...] Read more.

Human food-borne infections with the enteropathogen Campylobacter jejuni are becoming increasingly prevalent worldwide. Since antibiotics are usually not indicated in campylobacteriosis, alternative treatment regimens are important. We here investigated potential disease-alleviating effects of menthol and of extracts from tormentil, raspberry leaves, and loosestrife in acute murine campylobacteriosis. Therefore, C. jejuni-infected microbiota-depleted IL-10^−/− mice were orally treated with the compounds alone or all in combination from day 2 until day 6 post-infection. Whereas neither treatment regimen affected gastrointestinal pathogen loads, the combination of compounds alleviated C. jejuni-induced diarrheal symptoms in diseased mice on day 6 post-infection. Furthermore, the therapeutic application of tormentil and menthol alone and the combination of the four compounds resulted in lower colonic T cell numbers in infected mice when compared to placebo counterparts. Notably, pro-inflammatory cytokines measured in mesenteric lymph nodes taken from C. jejuni-infected mice following tormentil, menthol, and combination treatment did not differ from basal concentrations. However, neither treatment regimen could dampen extra-intestinal immune responses, including systemic pro-inflammatory cytokine secretion on day 6 post-infection. In conclusion, the combination of menthol and of extracts from tormentil, raspberry leaves, and loosestrife constitutes an antibiotic-independent approach to alleviate campylobacteriosis symptoms. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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17 pages, 2618 KiB

Open AccessArticle

Enhancing Wound Healing: A Novel Topical Emulsion Combining CW49 Peptide and Lavender Essential Oil for Accelerated Regeneration and Antibacterial Protection

by Valentina Jaramillo, Erika Díaz, Laura N. Muñoz, Andrés Fernando González-Barrios, Jader Rodríguez-Cortina, Juan C. Cruz and Carolina Muñoz-Camargo

Pharmaceutics 2023, 15(6), 1739; https://doi.org/10.3390/pharmaceutics15061739 - 15 Jun 2023

Cited by 4 | Viewed by 3025

Abstract

Wound healing is a complex process involving blood cells, extracellular matrix, and parenchymal cells. Research on biomimetics in amphibian skin has identified the CW49 peptide from Odorrana grahami, which has been demonstrated to promote wound regeneration. Additionally, lavender essential oil exhibits anti-inflammatory [...] Read more.

Wound healing is a complex process involving blood cells, extracellular matrix, and parenchymal cells. Research on biomimetics in amphibian skin has identified the CW49 peptide from Odorrana grahami, which has been demonstrated to promote wound regeneration. Additionally, lavender essential oil exhibits anti-inflammatory and antibacterial activities. Given these considerations, we propose an innovative emulsion that combines the CW49 peptide with lavender oil. This novel formulation could serve as a potent topical treatment, potentially fostering the regeneration of damaged tissues and providing robust antibacterial protection for skin wounds. This study investigates the physicochemical properties, biocompatibility, and in vitro regenerative capacity of the active components and the emulsion. The results show that the emulsion possesses appropriate rheological characteristics for topical application. Both the CW49 peptide and lavender oil exhibit high viability in human keratinocytes, indicating their biocompatibility. The emulsion induces hemolysis and platelet aggregation, an expected behavior for such topical treatments. Furthermore, the lavender-oil emulsion demonstrates antibacterial activity against both Gram-positive and Gram-negative bacterial strains. Finally, the regenerative potential of the emulsion and its active components is confirmed in a 2D wound model using human keratinocytes. In conclusion, the formulated emulsion, which combines the CW49 peptide and lavender oil, shows great promise as a topical treatment for wound healing. Further research is needed to validate these findings in more advanced in vitro models and in vivo settings, potentially leading to improved wound-care management and novel therapeutic options for patients with skin injuries. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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14 pages, 2382 KiB

Open AccessArticle

Pomegranate Peel Extract Attenuates Isoprenaline-Induced Takotsubo-like Myocardial Injury in Rats

by Sonja T. Marinković, Đorđe Đukanović, Mladen Duran, Zorislava Bajic, Tanja Sobot, Snežana Uletilović, Nebojša Mandić-Kovacević, Tanja Cvjetković, Žana M. Maksimović, Uglješa Maličević, Nikolina Vesić, Sanja Jovičić, Maja Katana, Katarina Šavikin, Dragan M. Djuric, Miloš P. Stojiljković and Ranko Škrbić

Pharmaceutics 2023, 15(6), 1697; https://doi.org/10.3390/pharmaceutics15061697 - 09 Jun 2023

Viewed by 976

Abstract

Takotsubo syndrome (TTS) is an acute heart failure syndrome characterised by catecholamine-induced oxidative tissue damage. Punica granatum, a fruit-bearing tree, is known to have high polyphenolic content and has been proven to be a potent antioxidant. This study aimed to investigate the [...] Read more.

Takotsubo syndrome (TTS) is an acute heart failure syndrome characterised by catecholamine-induced oxidative tissue damage. Punica granatum, a fruit-bearing tree, is known to have high polyphenolic content and has been proven to be a potent antioxidant. This study aimed to investigate the effects of pomegranate peel extract (PoPEx) pre-treatment on isoprenaline-induced takotsubo-like myocardial injury in rats. Male Wistar rats were randomised into four groups. Animals in the PoPEx(P) and PoPEx + isoprenaline group (P + I) were pre-treated for 7 days with 100 mg/kg/day of PoPEx. On the sixth and the seventh day, TTS-like syndrome was induced in rats from the isoprenaline(I) and P + I groups by administering 85 mg/kg/day of isoprenaline. PoPEx pre-treatment led to the elevation of superoxide dismutase and catalase (p < 0.05), reduced glutathione (p < 0.001) levels, decreased the thiobarbituric acid reactive substances (p < 0.001), H₂O₂, O₂⁻ (p < 0.05), and NO₂⁻ (p < 0.001), in the P + I group, when compared to the I group. In addition, a significant reduction in the levels of cardiac damage markers, as well as a reduction in the extent of cardiac damage, was found. In conclusion, PoPEx pre-treatment significantly attenuated the isoprenaline-induced myocardial damage, primarily via the preservation of endogenous antioxidant capacity in the rat model of takotsubo-like cardiomyopathy. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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10 pages, 376 KiB

Open AccessArticle

Comparative Assessment of Antioxidant Activity and Functional Components of Chionanthus virginicus and Chionanthus pubescens from the Andean Region of Ecuador

by Raluca A. Mihai, Iván A. Espinoza Caiza, Erly J. Melo Heras, Larisa I. Florescu and Rodica D. Catana

Pharmaceutics 2023, 15(6), 1676; https://doi.org/10.3390/pharmaceutics15061676 - 08 Jun 2023

Viewed by 1113

Abstract

The present study aims to provide information about the antioxidant capacity and secondary metabolites from different plant parts of two species that are grown in Ecuador: Chionanthus pubescens (the Ecuadorian national tree), and Chionanthus virginicus (the fringe tree—endemic to the United States of [...] Read more.

The present study aims to provide information about the antioxidant capacity and secondary metabolites from different plant parts of two species that are grown in Ecuador: Chionanthus pubescens (the Ecuadorian national tree), and Chionanthus virginicus (the fringe tree—endemic to the United States of America and adapted to Ecuador’s physiographical and ecological conditions). These two species have still not been investigated for these characteristics. A comparative estimation of the antioxidant activities between the leaf, fruit, and inflorescence extracts was performed. In the quest for new medicines, the extracts were analyzed for phenolic, anthocyanin, and flavonoid content. A slight difference was observed between C. pubescens and C. virginicus flowers, the highest antioxidant activity being found in the C. pubescens leaf (DPPH IC₅₀ = 62.8866 mg/mL, ABTS IC₅₀ = 55.852 mg/mL, and FRAP IC₅₀ = 2.8466 g/mL). Our results showed correlations between antioxidant activity, total phenolic content, and flavonoids. This study confirmed that the C. pubescens leaves and fruits from the Andean region of Ecuador represent a good source of antioxidants, especially due to the presence of a high content of phenolic compounds (homovanillic acid, 3,4 dimethoxyphenylacetic acid, vanillic acid, gallic acid, etc.) as determined by the HPLC-DAD method. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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17 pages, 4256 KiB

Open AccessArticle

Herb Robert’s Gift against Human Diseases: Anticancer and Antimicrobial Activity of Geranium robertianum L.

by Łukasz Świątek, Inga Wasilewska, Anastazja Boguszewska, Agnieszka Grzegorczyk, Jakub Rezmer, Barbara Rajtar, Małgorzata Polz-Dacewicz and Elwira Sieniawska

Pharmaceutics 2023, 15(5), 1561; https://doi.org/10.3390/pharmaceutics15051561 - 22 May 2023

Cited by 1 | Viewed by 1536

Abstract

Geranium robertianum L. is a widely distributed plant used as a traditional herbal medicine, but the knowledge of its biological properties still needs to be improved. Thus, the purpose of this presented research was to assess the phytochemical profile of extracts from aerial [...] Read more.

Geranium robertianum L. is a widely distributed plant used as a traditional herbal medicine, but the knowledge of its biological properties still needs to be improved. Thus, the purpose of this presented research was to assess the phytochemical profile of extracts from aerial parts of G. robertianum, commercially available in Poland and to study their anticancer potential and antimicrobial properties, including the antiviral, antibacterial, and antifungal effects. Additionally, the bioactivity of fractions obtained from the hexane and ethyl acetate extract was analyzed. The phytochemical analysis revealed the presence of organic and phenolic acids, hydrolysable tannins (gallo- and ellagitannins), and flavonoids. Significant anticancer activity was found for G. robertianum hexane extract (GrH) and ethyl acetate extract (GrEA) with an SI (selectivity index) between 2.02 and 4.39. GrH and GrEA inhibited the development of HHV-1-induced cytopathic effect (CPE) in virus-infected cells and decreased the viral load by 0.52 log and 1.42 log, respectively. Among the analyzed fractions, only those obtained from GrEA showed the ability to decrease the CPE and reduce the viral load. The extracts and fractions from G. robertianum showed a versatile effect on the panel of bacteria and fungi. The highest activity was observed for fraction GrEA4 against Gram-positive bacteria, including Micrococcus luteus ATCC 10240 (MIC 8 μg/mL), Staphylococcus epidermidis ATCC 12228 (MIC 16 μg/mL), Staphylococcus aureus ATCC 43300 (MIC 125 μg/mL), Enterococcus faecalis ATCC 29212 (MIC 125 μg/mL), and Bacillus subtilis ATCC 6633 (MIC 125 μg/mL). The observed antibacterial effect may justify the traditional use of G. robertianum to treat hard-to-heal wounds. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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17 pages, 1877 KiB

Open AccessArticle

Photoprotection and Antiaging Activity of Extracts from Honeybush (Cyclopia sp.)—In Vitro Wound Healing and Inhibition of the Skin Extracellular Matrix Enzymes: Tyrosinase, Collagenase, Elastase and Hyaluronidase

by Anna Hering, Justyna Stefanowicz-Hajduk, Magdalena Gucwa, Bartosz Wielgomas and Jadwiga Renata Ochocka

Pharmaceutics 2023, 15(5), 1542; https://doi.org/10.3390/pharmaceutics15051542 - 19 May 2023

Cited by 7 | Viewed by 1544

Abstract

Cyclopia sp. (honeybush) is an African shrub known as a rich source of polyphenols. The biological effects of fermented honeybush extracts were investigated. The influence of honeybush extracts on extracellular matrix (ECM) enzymes responsible for the skin malfunction and aging process—collagenase, elastase, tyrosinase [...] Read more.

Cyclopia sp. (honeybush) is an African shrub known as a rich source of polyphenols. The biological effects of fermented honeybush extracts were investigated. The influence of honeybush extracts on extracellular matrix (ECM) enzymes responsible for the skin malfunction and aging process—collagenase, elastase, tyrosinase and hyaluronidase—was analysed. The research also included assessment of the in vitro photoprotection efficiency of honeybush extracts and their contribution to the wound healing process. Antioxidant properties of the prepared extracts were evaluated, and quantification of the main compounds in the extracts was achieved. The research showed that the analysed extracts had a significant ability to inhibit collagenase, tyrosinase and hyaluronidase and a weak influence on elastase activity. Tyrosinase was inhibited effectively by honeybush acetone (IC₅₀ 26.18 ± 1.45 µg/mL), ethanol (IC₅₀ 45.99 ± 0.76 µg/mL) and water (IC₅₀ 67.42 ± 1.75 µg/mL) extracts. Significant hyaluronidase inhibition was observed for ethanol, acetone and water extracts (IC₅₀ were 10.99 ± 1.56, 13.21 ± 0.39 and 14.62 ± 0.21µg/mL, respectively). Collagenase activity was inhibited effectively by honeybush acetone extract (IC₅₀ 42.5 ± 1.05 μg/mL). The wound healing properties of the honeybush extracts, estimated in vitro in human keratinocytes (HaCaTs), were indicated for water and ethanol extracts. In vitro sun protection factor (SPF in vitro) showed medium photoprotection potential for all the honeybush extracts. The quantity of polyphenolic compounds was estimated with the use of high-performance liquid chromatography equipped with diode-array detection (HPLC-DAD), indicating the highest mangiferin contents in ethanol, acetone and n-butanol extracts, while in the water extract hesperidin was the dominant compound. The antioxidant properties of the honeybush extracts were estimated with FRAP (2,4,6-Tris(2-pyridyl)-s-triazine) and DPPH (2,2-diphenyl-1-picrylhydrazyl) tests, indicating their strong antioxidant activity, similar to ascorbic acid for the acetone extract in both tests. The wound healing abilities, estimation of SPF in vitro and the direct influence on selected enzymes (elastase, tyrosinase, collagenase and hyaluronidase) of the tested honeybush extracts were analysed for the first time, indicating a high potential of these well-known herbal tea for antiaging, anti-inflammation, regeneration and protection of the skin. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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14 pages, 4153 KiB

Open AccessArticle

Luteolin and Vernodalol as Bioactive Compounds of Leaf and Root Vernonia amygdalina Extracts: Effects on α-Glucosidase, Glycation, ROS, Cell Viability, and In Silico ADMET Parameters

by Francine Medjiofack Djeujo, Valentina Stablum, Elisa Pangrazzi, Eugenio Ragazzi and Guglielmina Froldi

Pharmaceutics 2023, 15(5), 1541; https://doi.org/10.3390/pharmaceutics15051541 - 19 May 2023

Cited by 5 | Viewed by 1639

Abstract

The aqueous decoctions of Vernonia amygdalina (VA) leaves and roots are widely used in traditional African medicine as an antidiabetic remedy. The amount of luteolin and vernodalol in leaf and root extracts was detected, and their role was studied regarding α-glucosidase activity, bovine [...] Read more.

The aqueous decoctions of Vernonia amygdalina (VA) leaves and roots are widely used in traditional African medicine as an antidiabetic remedy. The amount of luteolin and vernodalol in leaf and root extracts was detected, and their role was studied regarding α-glucosidase activity, bovine serum albumin glycation (BSA), reactive oxygen species (ROS) formation, and cell viability, together with in silico absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties. Vernodalol did not affect α-glucosidase activity, whereas luteolin did. Furthermore, luteolin inhibited the formation of advanced glycation end products (AGEs) in a concentration-dependent manner, whereas vernodalol did not reduce it. Additionally, luteolin exhibited high antiradical activity, while vernodalol demonstrated a lower scavenger effect, although similar to that of ascorbic acid. Both luteolin and vernodalol inhibited HT-29 cell viability, showing a half-maximum inhibitory concentration (IC₅₀) of 22.2 µM (−Log IC₅₀ = 4.65 ± 0.05) and 5.7 µM (−Log IC₅₀ = 5.24 ± 0.16), respectively. Finally, an in silico ADMET study showed that both compounds are suitable candidates as drugs, with appropriate pharmacokinetics. This research underlines for the first time the greater presence of vernodalol in VA roots compared to leaves, while luteolin is prevalent in the latter, suggesting that the former could be used as a natural source of vernodalol. Consequently, root extracts could be proposed for vernodalol-dependent antiproliferative activity, while leaf extracts could be suggested for luteolin-dependent effects, such as antioxidant and antidiabetic effects. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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14 pages, 1462 KiB

Open AccessArticle

Isolation of Secondary Metabolites from Achillea grandifolia Friv. (Asteraceae) and Main Compounds’ Effects on a Glioblastoma Cellular Model

by Olga S. Tsiftsoglou, Nikos Krigas, Christos Gounaris, Christina Papitsa, Maria Nanouli, Evrysthenis Vartholomatos, Georgios S. Markopoulos, Rafaela Isyhou, George Alexiou and Diamanto Lazari

Pharmaceutics 2023, 15(5), 1383; https://doi.org/10.3390/pharmaceutics15051383 - 30 Apr 2023

Cited by 3 | Viewed by 1321

Abstract

This study aims at the isolation and structural determination of the secondary metabolites of the herbaceous perennial plant Achillea grandifolia Friv. (Asteraceae). The examination of the non-volatile content of the leaves and flowers of A. grandifolia afforded the isolation of sixteen secondary metabolites. [...] Read more.

This study aims at the isolation and structural determination of the secondary metabolites of the herbaceous perennial plant Achillea grandifolia Friv. (Asteraceae). The examination of the non-volatile content of the leaves and flowers of A. grandifolia afforded the isolation of sixteen secondary metabolites. On the basis of NMR spectra, the identified compounds included ten sesquiterpene lactones; three guaianolides—rupicolin A (1), rupicolin B (2), and (4S,6aS,9R,9aS,9bS)-4,6a,9-trihydroxy-9-methyl-3,6-dimethylene-3a,4,5,6,6a,9,9a,9b-octahydro-3H-azuleno [4,5-b]furan-2-one (3); two eudesmanolides—artecalin (4) and ridentin B (5); two sesquiterpene methyl esters—(1S,2S,4αR,5R,8R,8αS)-decahydro-1,5,8-trihydroxy-4α,8-dimethyl–methylene-2-naphthaleneacetic acid methylester (6) and 1β, 3β, 6α-trihydroxycostic acid methyl ester (7); three secoguaianolides—acrifolide (8), arteludovicinolide A (9), and lingustolide A (10); and an iridoid—loliolide (11). Moreover, five known flavonoids, i.e., apigenin, luteolin, eupatolitin, apigenin 7-O-glucoside, and luteolin 7-O-glucoside (12-16) were also purified from the aerial parts of the plant material. We also investigated the effect of rupicolin A (1) and B (2) (main compounds) on U87MG and T98G glioblastoma cell lines. An MTT assay was performed to define cytotoxic effects and to calculate the IC50, while flow cytometry was employed to analyze the cell cycle. The IC50 values of reduced viability during the 48 h treatment for compound (1) and (2) were 38 μM and 64 μM for the U87MG cells and 15 μM and 26 μM for the T98G cells, respectively. Both rupicolin A and B induced a G2/M cell cycle arrest. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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14 pages, 1933 KiB

Open AccessArticle

Saponin Fraction CIL1 from Lysimachia ciliata L. Enhances the Effect of a Targeted Toxin on Cancer Cells

by Paulina Koczurkiewicz-Adamczyk, Karolina Grabowska, Elżbieta Karnas, Kamil Piska, Dawid Wnuk, Katarzyna Klaś, Agnieszka Galanty, Katarzyna Wójcik-Pszczoła, Marta Michalik, Elżbieta Pękala, Hendrik Fuchs and Irma Podolak

Pharmaceutics 2023, 15(5), 1350; https://doi.org/10.3390/pharmaceutics15051350 - 28 Apr 2023

Viewed by 1321

Abstract

Saponins are plant metabolites that possess multidirectional biological activities, among these is antitumor potential. The mechanisms of anticancer activity of saponins are very complex and depend on various factors, including the chemical structure of saponins and the type of cell they target. The [...] Read more.

Saponins are plant metabolites that possess multidirectional biological activities, among these is antitumor potential. The mechanisms of anticancer activity of saponins are very complex and depend on various factors, including the chemical structure of saponins and the type of cell they target. The ability of saponins to enhance the efficacy of various chemotherapeutics has opened new perspectives for using them in combined anticancer chemotherapy. Co-administration of saponins with targeted toxins makes it possible to reduce the dose of the toxin and thus limit the side effects of overall therapy by mediating endosomal escape. Our study indicates that the saponin fraction CIL1 of Lysimachia ciliata L. can improve the efficacy of the EGFR-targeted toxin dianthin (DE). We investigated the effect of cotreatment with CIL1 + DE on cell viability in a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, on proliferation in a crystal violet assay (CV) and on pro-apoptotic activity using Annexin V/7 Actinomycin D (7-AAD) staining and luminescence detection of caspase levels. Cotreatment with CIL1 + DE enhanced the target cell-specific cytotoxicity, as well as the antiproliferative and proapoptotic properties. We found a 2200-fold increase in both the cytotoxic and antiproliferative efficacy of CIL1 + DE against HER14-targeted cells, while the effect on control NIH3T3 off-target cells was less profound (6.9- or 5.4-fold, respectively). Furthermore, we demonstrated that the CIL1 saponin fraction has a satisfactory in vitro safety profile with a lack of cytotoxic and mutagenic potential. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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Review

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40 pages, 11335 KiB

Open AccessReview

Molecular Hybridization as a Strategy for Developing Artemisinin-Derived Anticancer Candidates

by Elena Marchesi, Daniela Perrone and Maria Luisa Navacchia

Pharmaceutics 2023, 15(9), 2185; https://doi.org/10.3390/pharmaceutics15092185 - 23 Aug 2023

Cited by 3 | Viewed by 1251

Abstract

Artemisinin is a natural compound extracted from Artemisia species belonging to the Asteraceae family. Currently, artemisinin and its derivatives are considered among the most significant small-molecule antimalarial drugs. Artemisinin and its derivatives have also been shown to possess selective anticancer properties, however, there [...] Read more.

Artemisinin is a natural compound extracted from Artemisia species belonging to the Asteraceae family. Currently, artemisinin and its derivatives are considered among the most significant small-molecule antimalarial drugs. Artemisinin and its derivatives have also been shown to possess selective anticancer properties, however, there are several limitations and gaps in knowledge that retard their repurposing as effective anticancer agents. Hybridization resulting from a covalent combination of artemisinin with one or more active pharmacophores has emerged as a promising approach to overcome several issues. The variety of hybridization partners allows improvement in artemisinin activity by tuning the ability of conjugated artemisinin to interact with various molecule targets involved in multiple biological pathways. This review highlights the current scenario of artemisinin-derived hybrids with potential anticancer activity. The synthetic approaches to achieve the corresponding hybrids and the structure–activity relationships are discussed to facilitate further rational design of more effective candidates. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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21 pages, 1701 KiB

Open AccessReview

Vitis vinifera (Vine Grape) as a Valuable Cosmetic Raw Material

by Marta Sharafan, Magdalena A. Malinowska, Halina Ekiert, Beata Kwaśniak, Elżbieta Sikora and Agnieszka Szopa

Pharmaceutics 2023, 15(5), 1372; https://doi.org/10.3390/pharmaceutics15051372 - 29 Apr 2023

Cited by 7 | Viewed by 2660

Abstract

This review refers to botanical, ecological and phytochemical characteristics of Vitis vinifera L. (vine grape)–a species, the valuable properties of which are widely exploited in the food industry and in recent times in medicine as well as in phytocosmetology. The general characteristic of [...] Read more.

This review refers to botanical, ecological and phytochemical characteristics of Vitis vinifera L. (vine grape)–a species, the valuable properties of which are widely exploited in the food industry and in recent times in medicine as well as in phytocosmetology. The general characteristic of V. vinifera, followed by the chemical composition and biological activities of different extracts obtained from the plant (fruit, skin, pomace, seed, leaf and stem extracts), are provided. A concise review of the extraction conditions of grape metabolites and the methods of their analysis are also presented. The biological activity of V. vinifera is determined by the presence of high contents of polyphenols, mainly flavonoids (e.g., quercetin, kaempferol), catechin derivatives, anthocyanins and stilbenoids (e.g., trans-resveratrol, trans-ε-viniferin). The review pays particular attention to the application of V. vinifera in cosmetology. It has been proven that V. vinifera possesses strong cosmetological-related properties, such as anti-ageing properties, anti-inflammatory properties and skin-whitening properties. Moreover, a review of studies on V. vinifera biological activities, which are of particular interest for dermatologic problems, are disclosed. Furthermore, the work also emphasises the importance of biotechnological studies on V. vinifera. The last part of the review is addressed to the safety of the use of V. vinifera. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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31 pages, 3980 KiB

Open AccessReview

Natural Products as New Approaches for Treating Bladder Cancer: From Traditional Medicine to Novel Drug Discovery

by Yoo Kang, Chelin Park, Heemin Lee, Sojin Kang, Chunhoo Cheon and Bonglee Kim

Pharmaceutics 2023, 15(4), 1117; https://doi.org/10.3390/pharmaceutics15041117 - 31 Mar 2023

Cited by 1 | Viewed by 2519

Abstract

Bladder cancer (BC) is a heterogeneous disease that a tumor develops in the bladder lining and in some cases, the bladder muscle. Chemotherapy and immunotherapy are commonly used to treat bladder cancer. However, chemotherapy can cause burning and irritation in the bladder while [...] Read more.

Bladder cancer (BC) is a heterogeneous disease that a tumor develops in the bladder lining and in some cases, the bladder muscle. Chemotherapy and immunotherapy are commonly used to treat bladder cancer. However, chemotherapy can cause burning and irritation in the bladder while BCG immunotherapy, which is the main type of intravesical immunotherapy for bladder cancer, can also cause burning in the bladder and flu-like symptoms. Thus, drugs originating from natural products have attracted much attention due to the reports that they have anti-cancer properties with low adverse effects. In this study, eighty-seven papers that dealt with natural products preventing or treating bladder cancer were reviewed. The studies were classified into the following mechanism: 71 papers on cell death, 5 papers on anti-metastasis, 3 papers on anti-angiogenesis, 1 paper on anti-resistance, and 7 papers on clinical trials. Most of the natural products that induced apoptosis up-regulated proteins such as caspase-3 and caspase-9. Regarding anti-metastasis, MMP-2 and MMP-9 are regulated frequently. Regarding anti-angiogenesis, HIF-1α and VEGF-A are down-regulated frequently. Nevertheless, the number of papers regarding anti-resistance and clinical trial are too few, so more studies are needed. In conclusion, this database will be useful for future in vivo studies of the anti-bladder cancer effect of natural products, in the process of selecting materials used for the experiment. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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33 pages, 5979 KiB

Open AccessReview

Recent Advances in Using Natural Antibacterial Additives in Bioactive Wound Dressings

by Meysam Firoozbahr, Peter Kingshott, Enzo A. Palombo and Bita Zaferanloo

Pharmaceutics 2023, 15(2), 644; https://doi.org/10.3390/pharmaceutics15020644 - 14 Feb 2023

Cited by 8 | Viewed by 2836

Abstract

Wound care is a global health issue with a financial burden of up to US $96.8 billion annually in the USA alone. Chronic non-healing wounds which show delayed and incomplete healing are especially problematic. Although there are more than 3000 dressing types in [...] Read more.

Wound care is a global health issue with a financial burden of up to US $96.8 billion annually in the USA alone. Chronic non-healing wounds which show delayed and incomplete healing are especially problematic. Although there are more than 3000 dressing types in the wound management market, new developments in more efficient wound dressings will require innovative approaches such as embedding antibacterial additives into wound-dressing materials. The lack of novel antibacterial agents and the misuse of current antibiotics have caused an increase in antimicrobial resistance (AMR) which is estimated to cause 10 million deaths by 2050 worldwide. These ongoing challenges clearly indicate an urgent need for developing new antibacterial additives in wound dressings targeting microbial pathogens. Natural products and their derivatives have long been a significant source of pharmaceuticals against AMR. Scrutinising the data of newly approved drugs has identified plants as one of the biggest and most important sources in the development of novel antibacterial drugs. Some of the plant-based antibacterial additives, such as essential oils and plant extracts, have been previously used in wound dressings; however, there is another source of plant-derived antibacterial additives, i.e., those produced by symbiotic endophytic fungi, that show great potential in wound dressing applications. Endophytes represent a novel, natural, and sustainable source of bioactive compounds for therapeutic applications, including as efficient antibacterial additives for chronic wound dressings. This review examines and appraises recent developments in bioactive wound dressings that incorporate natural products as antibacterial agents as well as advances in endophyte research that show great potential in treating chronic wounds. Full article

(This article belongs to the Special Issue Biomedical Applications of Natural Plant Extract)

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