Bioactive Phytochemicals from Plant Essential Oils

Topic Information

Dear Colleagues,

Abundant plant resources in the world contain plenty of phytochemicals/natural products with medicinal or healthy functions. Most phytochemicals from herbal and woody plants are flavonoids, lignans, phenylpropanoids, quinoids, tannins, stilbenes, terpenoids, steroids, saponins, alkaloids, glycosides, and others. Plant natural products exhibit numerous bioactive properties, including antibacterial activity, antifungal activity, insecticidal property, xanthine oxidase inhibitory effect, antityrosinase activity, antioxidant activity, cytotoxicity, anti-aging effect, etc. Extraction of phytochemicals having specific bioactivities and/or medicinal properties from plants is one of the important developments of natural product research. Additionally, through innovative development of chromatographic and spectroscopic technologies, more bioactive phytochemicals are separated and identified from various plants. This Special Issue aims to explore more bioactive plant essential oils and extracts, to isolate and identify phytochemicals possessing specific bioactivities, and to illustrate the mechanism of enzyme kinetic assays, model organism studies, molecular docking analysis, and so on. Through more research, it is expected that bioactive essential oils, extracts, and phytochemicals can be obtained from plants with great potential as pharmaceuticals or healthy products.

Prof. Dr. Hui-Ting Chang
Prof. Dr. Nour Eddine Es-Safi
Topic Editors

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Participating Journals

Journal Name	Impact Factor	CiteScore	Launched Year	First Decision (median)	APC
Antioxidants antioxidants	6.0	10.6	2012	16.9 Days	CHF 2900
Molecules molecules	4.2	7.4	1996	15.1 Days	CHF 2700
Pharmaceuticals pharmaceuticals	4.3	6.1	2004	13.9 Days	CHF 2900
Pharmaceutics pharmaceutics	4.9	7.9	2009	15.5 Days	CHF 2900
Plants plants	4.0	6.5	2012	18.9 Days	CHF 2700

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Published Papers (8 papers)

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11 pages, 1693 KiB  

Open AccessArticle

In Vitro and In Vivo Antimelanogenesis Effects of Leaf Essential Oil from Agathis dammara

by Yu-Tung Ho, I-Hsuan Liu, Shang-Tzen Chang, Sheng-Yang Wang and Hui-Ting Chang

Pharmaceutics 2023, 15(9), 2269; https://doi.org/10.3390/pharmaceutics15092269 - 2 Sep 2023

Cited by 4 | Viewed by 2391

Abstract

Agathis species are widely distributed around Southeast Asia, Australasia, South Pacific islands, and etc. Traditionally, Agathis species have been used as the folk medicines, the common ethnopharmacological uses of Agathis genus are the treatments of headache and myalgia. This study aims to investigate [...] Read more.

Agathis species are widely distributed around Southeast Asia, Australasia, South Pacific islands, and etc. Traditionally, Agathis species have been used as the folk medicines, the common ethnopharmacological uses of Agathis genus are the treatments of headache and myalgia. This study aims to investigate the chemical composition of Agathis dammara (Lamb.) Rich. leaf essential oil and to explore its antimelanogenesis effect. The chemical constituents of leaf essential oil are analyzed using gas chromatography-mass spectrometry (GC-MS), the major constituents of leaf essential oil are sesquiterpenoids. The major constituents are δ-cadinene (16.12%), followed by γ-gurjunene (15.57%), 16-kaurene (12.43%), β-caryophyllene (8.58%), germacrene D (8.53%), and γ-cadinene (5.33%). As for the in vitro antityrosinase activity, leaf essential oil inhibit the tyrosinase activity of mushroom when the substrate is 3,4-dihydroxyphenylalanine (L-DOPA). Leaf essential oil prevents tyrosinase from acting as diphenolase and catalyzing L-DOPA to dopaquinone, and converting into dark melanin pigments. A. dammara leaf essential oil also exhibits the in vivo antimelanogenesis effect, leaf essential oil reduces 43.48% of melanin formation in zebrafish embryos at the concentration of 50 μg/mL. Results reveal A. dammara leaf essential oil has the potential for developing the skin whitening drug and depigmentation ingredient for hyperpigmentary disorders. Full article

(This article belongs to the Topic Bioactive Phytochemicals from Plant Essential Oils)

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43 pages, 5589 KiB  

Open AccessReview

A New Biomaterial Derived from Aloe vera—Acemannan from Basic Studies to Clinical Application

by Yingjie Bai, Yimeng Niu, Shengao Qin and Guowu Ma

Pharmaceutics 2023, 15(7), 1913; https://doi.org/10.3390/pharmaceutics15071913 - 9 Jul 2023

Cited by 26 | Viewed by 6471

Abstract

Aloe vera is a kind of herb rich in polysaccharides. Acemannan (AC) is considered to be a natural polysaccharide with good biodegradability and biocompatibility extracted from Aloe vera and has a wide range of applications in the biomedical field due to excellent immunomodulatory, [...] Read more.

Aloe vera is a kind of herb rich in polysaccharides. Acemannan (AC) is considered to be a natural polysaccharide with good biodegradability and biocompatibility extracted from Aloe vera and has a wide range of applications in the biomedical field due to excellent immunomodulatory, antiviral, antitumor, and tissue regeneration effects. In recent years, clinical case reports on the application of AC as a novel biomedical material in tissue regenerative medicine have emerged; it is mainly used in bone tissue engineering, pulp–dentin complex regeneration engineering, and soft tissue repair, among other operations. In addition, multiple studies have proved that the new composite products formed by the combination of AC and other compounds have excellent biological and physical properties and have broader research prospects. This paper introduces the preparation process, surface structure, and application forms of AC; summarizes the influence of acetyl functional group content in AC on its functions; and provides a detailed review of the functional properties, laboratory studies, clinical cutting-edge applications, and combined applications of AC. Finally, the current application status of AC from basic research to clinical treatment is analyzed and its prospects are discussed. Full article

(This article belongs to the Topic Bioactive Phytochemicals from Plant Essential Oils)

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16 pages, 2729 KiB  

Open AccessArticle

Skin Wound Healing and Anti-Wrinkle-Promoting In Vitro Biological Activities of Caragana sinica Flower Absolute and Its Chemical Composition

by Mi Jung Kim, Kyung Jong Won, Do Yoon Kim, Yu Rim Won, Nan Young Kim, Da Kyoung Lee, Bok Sil Hong and Hwan Myung Lee

Pharmaceuticals 2023, 16(2), 235; https://doi.org/10.3390/ph16020235 - 3 Feb 2023

Cited by 8 | Viewed by 2791

Abstract

Caragana sinica (CS; family Legume) was used as a medicinal material to treat neuralgia and arthritis in folk remedies and has been shown to have antioxidant, neuroprotective, and anti-apoptotic effects. However, CS is unknown for its biological activities related to skin. The present [...] Read more.

Caragana sinica (CS; family Legume) was used as a medicinal material to treat neuralgia and arthritis in folk remedies and has been shown to have antioxidant, neuroprotective, and anti-apoptotic effects. However, CS is unknown for its biological activities related to skin. The present study explored the effects of CS flower absolute (CSFAb) on skin repair responses, viz., wound healing and anti-wrinkle-related responses using keratinocytes. CSFAb was extracted using hexane, and its composition was analyzed by GC/MS. The effects of CSFAb on human keratinocytes (HaCaT cells) were evaluated using Boyden chamber, sprouting, water-soluble tetrazolium salt, 5-bromo-2′-deoxyuridine incorporation, ELISA, zymography, and immunoblotting assays. GC/MS detected 46 components in CSFAb. In addition, in HaCaT cells, CSFAb increased the proliferation, migration, and sprout outgrowth and the phosphorylation of ERK1/2, JNK, p38 MAPK, and AKT, and also increased collagen type I and IV synthesis, reduced TNF-α-increased MMP-2 and MMP-9 activities, and upregulated hyaluronic acid (HA) and HA synthase-2 levels. These effects of CSFAb on wound healing and anti-wrinkle-related responses in keratinocytes suggest its potential use for skin repair and care preparations. Full article

(This article belongs to the Topic Bioactive Phytochemicals from Plant Essential Oils)

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10 pages, 906 KiB  

Open AccessArticle

In Vitro Metabolism and CYP-Modulating Activity of Lavender Oil and Its Major Constituents

by Goutam Mondal, Olivia R. Dale, Yan-Hong Wang, Shabana I. Khan, Ikhlas A. Khan and Charles R. Yates

Molecules 2023, 28(2), 755; https://doi.org/10.3390/molecules28020755 - 12 Jan 2023

Cited by 3 | Viewed by 2892

Abstract

The application of essential oils has historically been limited to topical (massage therapy) and inhalational (aromatherapy) routes of administration. More recently, however, evaluation of the therapeutic effects of essential oils has expanded to include the oral route of administration, which increases the herb–drug [...] Read more.

The application of essential oils has historically been limited to topical (massage therapy) and inhalational (aromatherapy) routes of administration. More recently, however, evaluation of the therapeutic effects of essential oils has expanded to include the oral route of administration, which increases the herb–drug interaction potential. The purpose of this study was to evaluate the herb–drug interaction potential of lavender essential oil and two of its primary phytoactive constituents, namely linalool and linalyl acetate. The metabolic stability of linalool and linalyl acetate was determined in human liver microsomes (HLM) and S9 fractions by quantitative analysis using UPLC-MS/MS system. Linalool was metabolically unstable in HLM and S9 fractions with an intrinsic clearance of 31.28 mL·min⁻¹·kg⁻¹, and 7.64 mL·min⁻¹·kg⁻¹, respectively. Interestingly, it was observed that linalyl acetate converted to linalool both in HLM and S9 fractions. Lavender oil showed weak inhibitory effect on the catalytic activity of CYP3A4 and CYP1A2 enzymes (IC₅₀ 12.0 and 21.5 µg/mL). Linalyl acetate inhibited CYP3A4 (IC₅₀ 4.75 µg/mL) while linalool did not show any inhibitory effect on any of the enzymes. The lavender oil and its constituents did not activate PXR to a considerable extent, and no activation of AhR was observed, suggesting a lack of potential to modify the pharmacokinetic and pharmacodynamic properties of conventional medications if used concurrently. Full article

(This article belongs to the Topic Bioactive Phytochemicals from Plant Essential Oils)

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23 pages, 7868 KiB  

Open AccessArticle

Essential Oils from the Leaves, Stem, and Roots of Blumea lanceolaria (Roxb.) Druce in Vietnam: Determination of Chemical Composition, and In Vitro, In Vivo, and In Silico Studies on Anti-Inflammatory Activity

by Thi Thanh Huyen Do, Thi Uyen Nguyen, Thi Thu Huyen Nguyen, Thi Yen Ho, Thi Luong Hang Pham, Tho Son Le, Thi Hong Van Nguyen, Phi-Hung Nguyen, Quang Huy Nguyen and Van Sang Nguyen

Molecules 2022, 27(22), 7839; https://doi.org/10.3390/molecules27227839 - 14 Nov 2022

Cited by 4 | Viewed by 2908

Abstract

Blumea lanceolaria (Roxb.) Druce, a flowering plant, is used for treating cancer and inflammatory diseases. In this study, we determined the chemical composition of the EOs extracted from the leaves (LBEO), stem (SBEO), and roots (RBEO) of B. lanceolaria and analyzed their anti-inflammation [...] Read more.

Blumea lanceolaria (Roxb.) Druce, a flowering plant, is used for treating cancer and inflammatory diseases. In this study, we determined the chemical composition of the EOs extracted from the leaves (LBEO), stem (SBEO), and roots (RBEO) of B. lanceolaria and analyzed their anti-inflammation potential. Overall, 30 compounds representing 99.12%, 98.44%, and 96.89% of total EO constituents of the leaves, stem, and roots, respectively, were identified using GC-MS. ELISA, Western blotting, and qRT-PCR studies showed that LBEO, SBEO, and RBEO inhibited multiple steps in the inflammatory responses in the RAW 264.7 cell model, including NO production; TNF-α, IL-6, iNOS, and COX-2 transcription and translation; and phosphorylation of IκBα and p65 of the NF-κB pathway. In the carrageenan-induced paw edema model, all three EOs inhibited paw edema at both early and delayed phases. Molecular docking studies indicated that the main components of B. lanceolaria EOs (BEOs) targeted and inhibited major components of inflammation-related pathways, including the arachidonic acid metabolic pathway, NF-κB pathway, and MAPK pathway. We present the first study to characterize the chemical composition of BEOs and confirm their potent anti-inflammatory effects in in vitro, in vivo, and in silico analysis. These results can facilitate the development of effective anti-inflammatory drugs with limited side effects in the future. Full article

(This article belongs to the Topic Bioactive Phytochemicals from Plant Essential Oils)

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17 pages, 328 KiB  

Open AccessArticle

Chemistry and Bioactivities of Six Tunisian Eucalyptus Species

by Habiba Kouki, Flavio Polito, Laura De Martino, Yassine Mabrouk, Lamia Hamrouni, Ismail Amri, Florinda Fratianni, Vincenzo De Feo and Filomena Nazzaro

Pharmaceuticals 2022, 15(10), 1265; https://doi.org/10.3390/ph15101265 - 14 Oct 2022

Cited by 9 | Viewed by 2840

Abstract

The complex taxonomy of Eucalyptus genus, the renewed interest in natural compounds able to combat microbial strains, the overuse of synthetic pesticides, the consequent request for alternative control methods were the reasons for this research. The essential oils (Eos) of Eucalyptus bosistoana, [...] Read more.

The complex taxonomy of Eucalyptus genus, the renewed interest in natural compounds able to combat microbial strains, the overuse of synthetic pesticides, the consequent request for alternative control methods were the reasons for this research. The essential oils (Eos) of Eucalyptus bosistoana, Eucalyptus melliodora, Eucalyptus odorata, Eucalyptus paniculata, Eucalyptus salmonopholia, and Eucalyptus transcontinentalis were analyzed by GC/MS and their potential phytotoxic activity was evaluated against the germination and radicle elongation of Sinapis arvensis, Raphanus sativus and Lolium multiflorum. The antibiofilm activity was assayed against both Gram-positive (Staphylococcus aureus and Listeria monocytogenes) and Gram-negative (Pseudomonas aeruginosa, Escherichia coli, and Acinetobacter baumannii) bacteria. Monoterpenoids were the most representative constituents in all EOs and eucalyptol was the dominant component except in E. melliodora EO, in which p-cymene was the most abundant. In phytotoxic assays, the EOs from E. odorata and E. paniculata were the most active against germination and radical elongation of the tested seeds. Finally, the Eucalyptus EOs proved their capacity to effectively inhibit the adhesion process of all five pathogen strains, with percentages often reaching and exceeding 90%. These Eucalytpus EOs could have possible employments in the food, health and agricultural fields. Full article

(This article belongs to the Topic Bioactive Phytochemicals from Plant Essential Oils)

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27 pages, 13869 KiB  

Open AccessArticle

Microfluidic-Based Formulation of Essential Oils-Loaded Chitosan Coated PLGA Particles Enhances Their Bioavailability and Nematocidal Activity

by Mohamed A. Helal, Ahmed M. Abdel-Gawad, Omnia M. Kandil, Marwa M. E. Khalifa, Alison A. Morrison, David J. Bartley, Gareth W. V. Cave and Hany M. Elsheikha

Pharmaceutics 2022, 14(10), 2030; https://doi.org/10.3390/pharmaceutics14102030 - 23 Sep 2022

Cited by 9 | Viewed by 3302

Abstract

In this study, poly (lactic-co-glycolic) acid (PLGA) particles were synthesized and coated with chitosan. Three essential oil (EO) components (eugenol, linalool, and geraniol) were entrapped inside these PLGA particles by using the continuous flow-focusing microfluidic method and a partially water-miscible solvent mixture (dichloromethane: [...] Read more.

In this study, poly (lactic-co-glycolic) acid (PLGA) particles were synthesized and coated with chitosan. Three essential oil (EO) components (eugenol, linalool, and geraniol) were entrapped inside these PLGA particles by using the continuous flow-focusing microfluidic method and a partially water-miscible solvent mixture (dichloromethane: acetone mixture (1:10)). Encapsulation of EO components in PLGA particles was confirmed by Fourier transform infrared spectroscopy, thermogravimetric analysis, and X-ray diffraction, with encapsulation efficiencies 95.14%, 79.68%, and 71.34% and loading capacities 8.88%, 8.38%, and 5.65% in particles entrapped with eugenol, linalool, and geraniol, respectively. The EO components’ dissociation from the loaded particles exhibited an initial burst release in the first 8 h followed by a sustained release phase at significantly slower rates from the coated particles, extending beyond 5 days. The EO components encapsulated in chitosan coated particles up to 5 μg/mL were not cytotoxic to bovine gut cell line (FFKD-1-R) and had no adverse effect on cell growth and membrane integrity compared with free EO components or uncoated particles. Chitosan coated PLGA particles loaded with combined EO components (10 µg/mL) significantly inhibited the motility of the larval stage of Haemonchus contortus and Trichostrongylus axei by 76.9%, and completely inhibited the motility of adult worms (p < 0.05). This nematocidal effect was accompanied by considerable cuticular damage in the treated worms, reflecting a synergistic effect of the combined EO components and an additive effect of chitosan. These results show that encapsulation of EO components, with a potent anthelmintic activity, in chitosan coated PLGA particles improve the bioavailability and efficacy of EO components against ovine gastrointestinal nematodes. Full article

(This article belongs to the Topic Bioactive Phytochemicals from Plant Essential Oils)

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16 pages, 371 KiB  

Open AccessArticle

Chemical Profiling and Biological Activities of Pelargonium graveolens Essential Oils at Three Different Phenological Stages

by Samiah Hamad Al-Mijalli, Hanae Naceiri Mrabti, Hamza Assaggaf, Ammar A. Attar, Munerah Hamed, Aicha EL Baaboua, Nasreddine El Omari, Naoual El Menyiy, Zakaria Hazzoumi, Ryan A Sheikh, Gokhan Zengin, Stefania Sut, Stefano Dall’Acqua and Abdelhakim Bouyahya

Plants 2022, 11(17), 2226; https://doi.org/10.3390/plants11172226 - 27 Aug 2022

Cited by 31 | Viewed by 4658

Abstract

The aim of this work was the determination of Pelargonium graveolens (aerial parts) volatile compounds at three developmental stages and the evaluation of their antioxidant, antidiabetic, dermaprotective, anti-inflammatory, and antibacterial effects. The aerial parts of Pelargonium graveolens were collected at three stages, namely [...] Read more.

The aim of this work was the determination of Pelargonium graveolens (aerial parts) volatile compounds at three developmental stages and the evaluation of their antioxidant, antidiabetic, dermaprotective, anti-inflammatory, and antibacterial effects. The aerial parts of Pelargonium graveolens were collected at three stages, namely the vegetative, beginning, and full flowering. Pelargonium graveolens essential oils were extracted from the dried materials of these aerial parts by hydrodistillation. The volatiles were analyzed by Gas Chromatography-Mass Spectrometry GC-MS, and the antioxidant activity was assessed by DPPH, ABTS, H₂O₂, and FRAP assays. The in vitro antidiabetic effect was evaluated by the inhibition of α-amylase, α-glucosidase, and lipase enzymes, while the antibacterial activity was assessed against six bacterial strains using an agar well diffusion assay and a microdilution method. The main constituents were menthol, menthene, eremophilene, isoborneol, isogeraniol, α-pinene, linalyl acetate, and 3-carene, with quantitative differences at the three phenological stages. The essential oil at the full flowering stage showed the best antioxidant activity, with IC₅₀ values of 83.26 ± 0.01, 116.42 ± 0.07, 132.25 ± 0.11, and 48.67 ± 0.04 μg/mL for DPPH, FRAP, ABTS, and H₂O₂ assays, respectively. This oil also exhibited significant effects against α-amylase (IC₅₀ = 43.33 ± 0.01 μg/mL), α-glucosidase (IC₅₀ = 19.04 ± 0.01 μg/mL), lipase (IC₅₀ = 24.33 ± 0.05 μg/mL), 5-lipoxygenase (IC₅₀ = 39.31 ± 0.01 μg/mL), and tyrosinase (IC₅₀ = 124.49 ± 0.07 μg/mL). The essential oil extracted at the full flowering stage showed the best antibacterial effect against a panel of microorganisms with diameter inhibition zones ranging between 11.00 ± 0.17 mm and 17.30 ± 0.17 mm and MIC values from 0.25% to 2% v/v. Overall, the results presented here suggest that the full flowering stage is the best optimal harvest time of Pelargonium graveolens for food and pharmaceutical applications. Full article

(This article belongs to the Topic Bioactive Phytochemicals from Plant Essential Oils)

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