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Bioactive Compounds from Nature: New Research and Prospects

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A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: closed (31 July 2022) | Viewed by 40321

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Special Issue Editor

Prof. Dr. Charng-Cherng Chyau

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Guest Editor

Department of Biotechnology, Hung Kuang University, Taichung, Taiwan
Interests: phytochemicals; bioactive compounds; extraction and purification; nonalcoholic fatty liver

Special Issue Information

Dear Colleagues,

There are abundant phytochemical compounds in nature, which have a protective effect on human health. These natural products can often be found to have primary biologically active ingredients, including small molecule compounds or macromolecular polysaccharides, etc. These natural compounds can be separated from the secondary metabolites of plants or fermentation products from microorganisms. The process for isolating bioactive compounds involves extraction, separation, and purification techniques. These isolated components are identified through various analytical techniques, including GC/MS, LC/MS, IR or NMR, etc. To further prove the potential bioactivities of isolated compounds, in vitro, in vivo, or even clinical trials are conducted to confirm that these isolated targets have specific physiological effects to provide references for future development in health care agents’ pharmaceuticals. Our goal is to invite relevant research teams to provide new research findings or new screening techniques to quickly identify possible screen targets from complex natural products and conduct research on the mechanism of action to prevent or improve related diseases. This Special Issue invites researchers to contribute reviews and original research reports of their recent work on preparing and identifying phytochemicals and their physiological mechanisms in health benefits.

Prof. Dr. Charng-Cherng Chyau
Guest Editor

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Keywords

Phytochemicals
Plants
Fermentation products
Preparation and identification
Bioactivity
Health benefits

Published Papers (11 papers)

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Research

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13 pages, 2732 KiB

Open AccessArticle

Phytochemical Analysis and Molecular Identification of Green Macroalgae Caulerpa spp. from Bali, Indonesia

by I Gede Putu Wirawan, Ni Kadek Emi Sintha Dewi, Maria Malida Vernandes Sasadara, I Gde Nengah Adhilaksman Sunyamurthi, I Made Jawi, I Nyoman Wijaya, Ida Ayu Putri Darmawati, I Ketut Suada and Anak Agung Keswari Krisnandika

Molecules 2022, 27(15), 4879; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27154879 - 30 Jul 2022

Cited by 3 | Viewed by 2514

Abstract

The studies of the Bulung Boni and Bulung Anggur (Caulerpa spp.) species and secondary metabolites are still very limited. Proper identification will support various aspects, such as cultivation, utilization, and economic interests. Moreover, understanding the secondary metabolites will assist in developing algae-based products. This study aimed to identify these indigenous Caulerpa algae and analyze their bioactive components. The tufA sequence was employed as a molecular marker in DNA barcoding, and its bioactive components were identified using the GC-MS method. The phylogenetic tree was generated in MEGA 11 using the maximum likelihood method, and the robustness of the tree was evaluated using bootstrapping with 1000 replicates. This study revealed that Bulung Boni is strongly connected to Caulerpa cylindracea. However, Bulung Anggur shows no close relationship to other Caulerpa species. GC-MS analysis of ethanolic extracts of Bulung Boni and Bulung Anggur showed the presence of 11 and 13 compounds, respectively. The majority of the compounds found in these algae have been shown to possess biological properties, such as antioxidant, antibacterial, anticancer, anti-inflammation, and antidiabetic. Further study is necessary to compare the data obtained using different molecular markers in DNA barcoding, and to elucidate other undisclosed compounds in these Caulerpa algae. Full article

(This article belongs to the Special Issue Bioactive Compounds from Nature: New Research and Prospects)

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19 pages, 814 KiB

Open AccessArticle

Physicochemical Properties of a New Green Honey from Banggi Island, Sabah

by Nanthini Rajindran, Roswanira Abdul Wahab, Nurul Huda, Norliza Julmohammad, Amir Husni Mohd Shariff, Norjihada Izzah Ismail and Fahrul Huyop

Molecules 2022, 27(13), 4164; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27134164 - 29 Jun 2022

Cited by 4 | Viewed by 4600

Abstract

Green honey is exclusively available on the island of Banggi in Sabah, and its uniqueness sees the commodity being sold at a high market price. Therefore, green honey is prone to adulteration by unscrupulous individuals, possibly compromising the health of those consuming this food commodity for its curative properties. Moreover, an established standard for reducing sugar in green honey is unavailable. Ipso facto, the study aimed to profile green honey’s physical and chemical properties, such as its pH, moisture content, free acidity, ash content, electroconductivity, hydroxymethylfurfural (HMF), total phenolic content, total flavonoid content, DPPH, colour, total sugar content, total protein content, and heavy metals as well as volatile organic compounds, the data of which are profoundly valuable in safeguarding consumers’ safety while providing information for its quality certification for local consumption and export. The results revealed that the honey’s physicochemical profile is comparable to other reported kinds of honey. The honey’s naturally green colour is because of the chlorophyll from the nectar from various flowers on the island. The raw honey showed free acidity between 28 and 33 Meq/100 g, lower than the standard’s 50 Meq/100 g. The hydroxymethylfurfural content is the lowest compared to other reported honey samples, with the total phenolic content between 16 and 19 mg GAE/100 g. The honey’s reducing sugar content is lower (~37.9%) than processed ones (56.3%) because of water removal. The protein content ranged from 1 to 2 gm/kg, 4- to 6-fold and 2-fold higher than local and manuka honey, respectively. The exceptionally high content of trans-4-hydroxyproline in raw honey is its source of collagen and other healing agents. Interestingly, low levels of arsenic, lead, nickel, cadmium, copper, and cobalt were detected in the honey samples, presumably due to their subterranean hives. Nevertheless, the honey is fit for general consumption as the concentrations were below the maxima in the Codex Alimentarius Commission of 2001. Full article

(This article belongs to the Special Issue Bioactive Compounds from Nature: New Research and Prospects)

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13 pages, 6906 KiB

Open AccessArticle

Garcinia Biflavonoid 1 Improves Lipid Metabolism in HepG2 Cells via Regulating PPARα

by Hai-Xin Chen, Fan Yang, Xin-Qian He, Ting Li, Yong-Zhi Sun, Jian-Ping Song, Xin-An Huang and Wen-Feng Guo

Molecules 2022, 27(6), 1978; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27061978 - 18 Mar 2022

Cited by 5 | Viewed by 2181

Abstract

Garcinia biflavonoid 1 (GB1) is one of the active chemical components of Garcinia kola and is reported to be capable of reducing the intracellular lipid deposition, which is the most significant characteristic of non-alcoholic fatty liver disease. However, its bioactive mechanism remains elusive. In the current study, the lipid deposition was induced in HepG2 cells by exposure to oleic acid and palmitic acid (OA&PA), then the effect of GB1 on lipid metabolism and oxidative stress and the role of regulating PPARα in these cells was investigated. We found that GB1 could ameliorate the lipid deposition by reducing triglycerides (TGs) and upregulate the expression of PPARα and SIRT6, suppressing the cell apoptosis by reducing the oxidative stress and the inflammatory factors of ROS, IL10, and TNFα. The mechanism study showed that GB1 had bioactivity in a PPARα-dependent manner based on its failing to improve the lipid deposition and oxidative stress in PPARα-deficient cells. The result revealed that GB1 had significant bioactivity on improving the lipid metabolism, and its potential primary action mechanism suggested that GB1 could be a potential candidate for management of non-alcoholic fatty liver disease. Full article

(This article belongs to the Special Issue Bioactive Compounds from Nature: New Research and Prospects)

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18 pages, 1063 KiB

Open AccessArticle

Hazelnut Shells as Source of Active Ingredients: Extracts Preparation and Characterization

by Alessandro Di Michele, Cinzia Pagano, Agnese Allegrini, Francesca Blasi, Lina Cossignani, Enrico Di Raimo, Marco Faieta, Eleonora Oliva, Paola Pittia, Sara Primavilla, Manuel Sergi, Camilla Vicino, Maurizio Ricci, Bartolomeo Schirone and Luana Perioli

Molecules 2021, 26(21), 6607; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26216607 - 31 Oct 2021

Cited by 17 | Viewed by 2893

Abstract

Hazelnut shells represent a waste material (about 42% of the total biomass) deriving from hazelnut harvest. These are mainly used as a heating source; however, they represent an interesting source of polyphenols useful in health field. The impact on phenolic profile and concentrations of hazelnut shell extracts obtained by three extraction methods (maceration, ultrasonic bath, and high-power ultrasonic), as well as temperature, extraction time, and preventive maceration, was studied. The prepared extracts were characterized in terms of chemical composition, antioxidant and antimicrobial activities. Eighteen different phenolic compounds were identified and quantified by chemical analysis and gallic acid was the most abundant in all the extracts analyzed. Other relevant compounds were chlorogenic acid, protocatechuic acid and catechin. Preventive maceration had a positive effect on the extraction of different types of compounds regardless of the method performed. Application of the high-power ultrasonic method had different effects, either positive or negative, depending on the type of compound and extraction time. All the prepared extracts showed antioxidant activity especially those prepared by maceration, and many of them were able to inhibit the growth of both B. subtilis and B. cereus. Full article

(This article belongs to the Special Issue Bioactive Compounds from Nature: New Research and Prospects)

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13 pages, 2159 KiB

Open AccessArticle

Extraction and Purification of R-Phycoerythrin Alpha Subunit from the Marine Red Algae Pyropia Yezoensis and Its Biological Activities

by Selvakumari Ulagesan, Taek-Jeong Nam and Youn-Hee Choi

Molecules 2021, 26(21), 6479; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26216479 - 27 Oct 2021

Cited by 20 | Viewed by 3114

Abstract

Phycoerythrin is a major light-harvesting pigment of red algae and cyanobacteria that is widely used as a fluorescent probe or as a colorant in the food and cosmetic industries. In this study, phycoerythrin was extracted from the red algae Pyropia yezoensis and purified by ammonium sulfate precipitation and various chromatography methods. The purified phycoerythrin was analyzed by UV-visible and fluorescence spectroscopy. The isolated pigment had the typical spectrum of R-phycoerythrin, with a trimmer state with absorbance maxima at 497, 536, and 565 nm. It was further purified and identified by LC-MS/MS and Mascot search. It showed a 100% sequence similarity with the R-phycoerythrin alpha subunit of Pyropia yezoensis. The molecular mass was 17.97 kDa. The antioxidant activity of the purified R-phycoerythrin alpha subunit was analyzed. It showed significant antioxidant activity in ABTS and FRAP assays and had significant cytotoxicity against HepG2 cells. Full article

(This article belongs to the Special Issue Bioactive Compounds from Nature: New Research and Prospects)

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16 pages, 6745 KiB

Open AccessArticle

Characterization, Antioxidant and Anti-Inflammation Capacities of Fermented Flammulina velutipes Polyphenols

by Sheng Ma, Hongcai Zhang and Jianxiong Xu

Molecules 2021, 26(20), 6205; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26206205 - 14 Oct 2021

Cited by 16 | Viewed by 2012

Abstract

This work investigated the preparation, characterization, antioxidant, and anti-inflammation capacities of Flammulina velutipes polyphenols (FVP) and fermented FVP (FFVP). The results revealed that the new syringic acid, accounting for 22.22%, was obtained after fermentation (FFVP). FFVP exhibits higher antioxidant and anti-inflammation activities than FVP, enhancing cell viability and phagocytosis, inhibiting the secretion of NO and ROS, and reducing the inflammatory response of RAW264.7 cells. This study revealed that FFVP provides a theoretical reference for in-depth study of its regulatory mechanisms and further development of functional antioxidants that are applicable in the food and health industry. Full article

(This article belongs to the Special Issue Bioactive Compounds from Nature: New Research and Prospects)

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13 pages, 1697 KiB

Open AccessArticle

Patient-Derived Tumor Chemosensitization of GKB202, an Antrodia Cinnamomea Mycelium-Derived Bioactive Compound

by Tsung-Ju Li, Ting-Wei Lin, Shih-Pei Wu, Hsin-Tung Chu, Yu-Hsuan Kuo, Jeng-Fong Chiou, Long-Sheng Lu and Chin-Chu Chen

Molecules 2021, 26(19), 6018; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26196018 - 04 Oct 2021

Cited by 9 | Viewed by 3786

Abstract

Oral cancers, hepatocellular carcinoma, and colorectal cancers are the three most common cancers, leading to 18,000 cases of cancer-related mortality in Taiwan per year. To bridge the gap towards clinical translation, we developed a circulating tumor cell (CTC) organoid culture workflow that efficiently expands CTC from patients to test Antrodia Cinnamomea mycelium-derived bioactive compounds. Three ACM-derived bioactive compounds were evaluated for tumor chemosensitization characteristics. Significant and consistent cytotoxic/5-FU sensitizing effects of GKB202 were found on 8 different patient-derived tumors. Acute toxicity profile and hepatic metabolism of GKB202 in rats suggest GKB202 is rapidly cleared by liver and is well tolerated up to the dose of 20 mg/kg. This comprehensive study provides new evidence that liquid fermentation of Antrodia cinnamomea mycelium (ACM) contains bioactive compounds that lead to effective control of CTC, especially when combined with 5-FU. Together, these data suggest ACM-derived GKB202 may be considered for further clinical investigation in the context of 5-FU-based combination therapy. Full article

(This article belongs to the Special Issue Bioactive Compounds from Nature: New Research and Prospects)

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10 pages, 917 KiB

Open AccessArticle

High Throughput Screening of the NatureBank ‘Marine Collection’ in a Haemonchus Bioassay Identifies Anthelmintic Activity in Extracts from a Range of Sponges from Australian Waters

by Aya C. Taki, Joseph J. Byrne, Abdul Jabbar, Kah Yean Lum, Sasha Hayes, Russell S. Addison, Kelsey S. Ramage, Andreas Hofmann, Merrick G. Ekins, Tao Wang, Bill C. H. Chang, Rohan A. Davis and Robin B. Gasser

Molecules 2021, 26(19), 5846; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26195846 - 27 Sep 2021

Cited by 6 | Viewed by 2232

Abstract

Widespread resistance in parasitic nematodes to most classes of anthelmintic drugs demands the discovery and development of novel compounds with distinct mechanisms of action to complement strategic or integrated parasite control programs. Products from nature—which assume a diverse ‘chemical space’—have significant potential as a source of anthelmintic compounds. In the present study, we screened a collection of extracts (n = 7616) derived from marine invertebrates sampled from Australian waters in a high throughput bioassay for in vitro anti-parasitic activity against the barber’s pole worm (Haemonchus contortus)—an economically important parasitic nematode of livestock animals. In this high throughput screen (HTS), we identified 58 active extracts that reduced larval motility by ≥70% (at 90 h), equating to an overall ‘hit rate’ of ~0.8%. Of these 58 extracts, 16 also inhibited larval development by ≥80% (at 168 h) and/or induced ‘non-wild-type’ (abnormal) larval phenotypes with reference to ‘wild-type’ (normal) larvae not exposed to extract (negative controls). Most active extracts (54 of 58) originated from sponges, three from chordates (tunicates) and one from a coral; these extracts represented 37 distinct species/taxa of 23 families. An analysis of samples by ¹H NMR fingerprinting was utilised to dereplicate hits and to prioritise a set of 29 sponge samples for future chemical investigation. Overall, these results indicate that a range of sponge species from Australian waters represents a rich source of natural compounds with nematocidal or nematostatic properties. Our plan now is to focus on in-depth chemical investigations of the sample set prioritised herein. Full article

(This article belongs to the Special Issue Bioactive Compounds from Nature: New Research and Prospects)

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14 pages, 2132 KiB

Open AccessArticle

Preclinical Bioavailability, Tissue Distribution, and Protein Binding Studies of Erinacine A, a Bioactive Compound from Hericium erinaceus Mycelia Using Validated LC-MS/MS Method

by Pei-Ching Tsai, Yi-Kai Wu, Jun-Hao Hu, I-Chen Li, Ting-Wei Lin, Chin-Chu Chen and Chia-Feng Kuo

Molecules 2021, 26(15), 4510; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26154510 - 27 Jul 2021

Cited by 10 | Viewed by 3494

Abstract

Erinacine A, derived from the mycelia of Hericium erinaceus, has attracted much attention due to its neuroprotective properties. However, very few studies have been conducted on the bioavailability, tissue distribution, and protein binding of erinacine A. This study aimed to investigate the bioavailability, tissue distribution, and protein binding of erinacine A in Sprague-Dawley rats. After oral administration (po) and intravenous administration (iv) of 2.381 g/kg BW of the H. erinaceus mycelia extract (equivalent to 50 mg/kg BW of erinacine A) and 5 mg/kg BW of erinacine A, respectively, the absolute bioavailability of erinacine A was estimated as 24.39%. Erinacine A was detected in brain at 1 h after oral dosing and reached the peak at 8 h. Protein binding assay showed unbound erinacine A fractions in brain to blood ratio is close to unity, supporting passive diffusion as the dominating transport. Feces was the major route for the elimination of erinacine A. This study is the first to show that erinacine A can penetrate the blood-brain barrier of rats by the means of passive diffusion and thus support the development of H. erinaceus mycelia for the improvement of neurohealth. Full article

(This article belongs to the Special Issue Bioactive Compounds from Nature: New Research and Prospects)

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Review

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11 pages, 281 KiB

Open AccessReview

Haematococcus pluvialis as a Potential Source of Astaxanthin with Diverse Applications in Industrial Sectors: Current Research and Future Directions

by Siti Nur Hazwani Oslan, Joo Shun Tan, Siti Nurbaya Oslan, Patricia Matanjun, Ruzaidi Azli Mohd Mokhtar, Rossita Shapawi and Nurul Huda

Molecules 2021, 26(21), 6470; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26216470 - 27 Oct 2021

Cited by 26 | Viewed by 4621

Abstract

Haematococcus pluvialis, a green microalga, appears to be a rich source of valuable bioactive compounds, such as astaxanthin, carotenoids, proteins, lutein, and fatty acids (FAs). Astaxanthin has a variety of health benefits and is used in the nutraceutical and pharmaceutical industries. Astaxanthin, for example, preserves the redox state and functional integrity of mitochondria and shows advantages despite a low dietary intake. Because of its antioxidant capacity, astaxanthin has recently piqued the interest of researchers due to its potential pharmacological effects, which include anti-diabetic, anti-inflammatory, and antioxidant activities, as well as neuro-, cardiovascular-, ocular, and skin-protective properties. Astaxanthin is a popular nutritional ingredient and a significant component in animal and aquaculture feed. Extensive studies over the last two decades have established the mechanism by which persistent oxidative stress leads to chronic inflammation, which then mediates the majority of serious diseases. This mini-review provides an overview of contemporary research that makes use of the astaxanthin pigment. This mini-review provides insight into the potential of H. pluvialis as a potent antioxidant in the industry, as well as the broad range of applications for astaxanthin molecules as a potent antioxidant in the industrial sector. Full article

(This article belongs to the Special Issue Bioactive Compounds from Nature: New Research and Prospects)

19 pages, 1564 KiB

Open AccessReview

Mexican Oregano (Lippia graveolens Kunth) as Source of Bioactive Compounds: A Review

by Israel Bautista-Hernández, Cristóbal N. Aguilar, Guillermo C. G. Martínez-Ávila, Cristian Torres-León, Anna Ilina, Adriana C. Flores-Gallegos, Deepak Kumar Verma and Mónica L. Chávez-González

Molecules 2021, 26(17), 5156; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules26175156 - 25 Aug 2021

Cited by 24 | Viewed by 6891

Abstract

Lippia graveolens is a traditional crop and a rich source of bioactive compounds with various properties (e.g., antioxidant, anti-inflammatory, antifungal, UV defense, anti-glycemic, and cytotoxicity) that is primarily cultivated for essential oil recovery. The isolated bioactive compounds could be useful as additives in the functional food, nutraceuticals, cosmetics, and pharmaceutical industries. Carvacrol, thymol, β-caryophyllene, and p-cymene are terpene compounds contained in oregano essential oil (OEO); flavonoids such as quercetin O-hexoside, pinocembrin, and galangin are flavonoids found in oregano extracts. Furthermore, thermoresistant compounds that remain in the plant matrix following a thermal process can be priced in terms of the circular economy. By using better and more selective extraction conditions, the bioactive compounds present in Mexican oregano can be studied as potential inhibitors of COVID-19. Also, research on extraction technologies should continue to ensure a higher quality of bioactive compounds while preventing an undesired chemical shift (e.g., hydrolysis). The oregano fractions can be used in the food, health, and agricultural industries. Full article

(This article belongs to the Special Issue Bioactive Compounds from Nature: New Research and Prospects)

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