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Plant Secondary Metabolites with Health Effects: Discovery and Engineering
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Plant Secondary Metabolites with Health Effects: Discovery and Engineering

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

Deadline for manuscript submissions: 31 May 2024 | Viewed by 9469

Special Issue Editors

Dr. Giuseppe Dionisio

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Guest Editor
Department of Agroecology - Crop Genetics and Biotechnology, Aarhus University, Forsøgsvej 1, 4200 Slagelse, Denmark
Interests: crop biotechnology; plant storage proteins; plant proteases; plant protease inhibitors; plant hydrolases
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Vittorio Calabrese

E-Mail Website
Guest Editor
Department of Biological and Biotechnological Sciences, Section of Medical Biochemistry, University of Catania, 95125 Catania, Italy
Interests: oxidative stress; nutritional antioxidants; vitagenes; brain resilience; hormesis
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Plant secondary metabolites include a plethora of organic compounds that plants synthetize for different reasons. The plant itself uses such compounds as antioxidants, defense mechanisms, hyperparasite attraction pheromones, weed controls, and antifungals. Furthermore, we have used plants’ active compounds as medicines for a long time. Indeed, Aristotle, in his treatise “Plants”, described the existence of a connection among the environment, nature, and plants. This connection, he said, is functional, i.e., each plant contains “something” that is functional for human health. Besides, each plant synthetizes a particular class of secondary metabolites that are important and serve as relief of a particular disease. Many clinical studies have demonstrated the importance of a specific plant metabolite to ameliorate a human medical condition. Traditional Chinese medicine has incorporated these known compounds into its pharmacopoeia. Occidental and American pharmacopoeia is dominated by Big Pharma, which looks back to the power of nature to re-adapt synthetic/semisynthetic drugs to mimic natural plant secondary metabolites. However, nowadays, in planta genetic engineering by introducing cognate wild type genes (lost by breeding) via cis-genesis and CRISPR/Cas9 genome editing is able to modify the plant secondary metabolite pathways in order to use the plants as a biofactory for the sustainable production of natural and metabolically forced/deviated metabolites, such as antioxidants, food colorants, fragrances, and anticancer natural compounds. In vitro and in vivo studies have demonstrated that many secondary metabolites are able to accumulate in the liver or in the skin and exert beneficial functions. However, toxicological studies demonstrate the importance of the dosage effects by introducing a titration of the active compounds from plants in pills/capsules containing the correct dosage for the plant metabolites after extraction, purification, and concentration. The modern medicinal/food chemistry industry is therefore looking forward to improvements in the production yield of particular plant secondary metabolites of known function, which can be achieved with chemical stability by in-plant biochemical modification, including genetic engineering of the biosynthetic pathway.

Dr. Giuseppe Dionisio
Prof. Dr. Vittorio Calabrese
Guest Editors

Manuscript Submission Information

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • plant secondary metabolites with health benefits
  • biochemical pathways engineering
  • phenolics and flavonoids
  • terpenoids
  • alkaloids
  • sterols
  • saponins
  • tannins
  • genome editing
  • CRISPR/Cas9
  • cis-genesis

Published Papers (4 papers)

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Research

19 pages, 11204 KiB  
Article
Phytochemicals, Health-Promoting Effects, and Enzyme Inhibition Traits of Phlomis stewartii Extracts
by Mamoon Ur Rasheed, Syed Ali Raza Naqvi, Fahad Al-Asmari, Muhammad Abdul Rahim and Mohamed Fawzy Ramadan
Molecules 2024, 29(5), 1049; https://doi.org/10.3390/molecules29051049 - 28 Feb 2024
Viewed by 519
Abstract
Phlomis stewartii is a wild, perennial woody plant used for diverse therapeutic targets. The present work evaluated the influence of independent variables such as extraction time, solvent concentration, and speed in the range of (100 mL, 150 mL, and 200 mL), (2 h, [...] Read more.
Phlomis stewartii is a wild, perennial woody plant used for diverse therapeutic targets. The present work evaluated the influence of independent variables such as extraction time, solvent concentration, and speed in the range of (100 mL, 150 mL, and 200 mL), (2 h, 5 h, and 8 h), and (100 rpm, 150 rpm, and 200 rpm), respectively, on extraction yields, phytochemical components, total phenolic contents (TPC), and total flavonoid contents (TFC) of P. stewartii extract. In the present work, response surface methodology (RSM) was applied to optimize the extraction yield. High-performance liquid chromatography (HPLC) was performed to detect the bioactive constituents of the extracts. The potent extracts were analyzed to study α-amylase and α-glucosidase inhibitory activities. Under the optimized conditions of solvent concentration (200 mL), extraction time (8 h), and speed (150 rpm), the whole plant methanol extract (WPME) showed a maximum extraction yield of 13.5%, while the leaves methanol extract (LME) showed a maximum TPC of 19.5 ± 44 mg of gallic acid equivalent (GAE) per gram of extract and a maximum TFC of 4.78 ± 0.34 mg of quercetin equivalent (QE) per gram of extract. HPLC analysis showed the presence of p-coumaric, gallic acid, quercetin, salicylic acid, sinapic acid, and vanillic acid. LME showed the highest α-amylase inhibitory activity (IC50 = 46.86 ± 0.21 µg/mL) and α-glucosidase inhibitory activity (IC50 value of 45.81 ± 0.17 µg/mL). Therefore, in conclusion, LME could be considered to fix the α-amylase and α-glucosidase-mediated disorders in the human body to develop herbal phytomedicine. Full article
(This article belongs to the Special Issue Plant Secondary Metabolites with Health Effects: Discovery and Engineering)
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12 pages, 2125 KiB  
Article
Cool Temperature Enhances Growth, Ferulic Acid and Flavonoid Biosynthesis While Inhibiting Polysaccharide Biosynthesis in Angelica sinensis
by Han Dong, Meiling Li, Ling Jin, Xiaorong Xie, Mengfei Li and Jianhe Wei
Molecules 2022, 27(1), 320; https://doi.org/10.3390/molecules27010320 - 05 Jan 2022
Cited by 15 | Viewed by 2621
Abstract
Angelica sinensis, a perennial herb that produces ferulic acid and phthalides for the treatment of cardio-cerebrovascular diseases, prefers growing at an altitude of 1800–3000 m. Geographical models have predicted that high altitude, cool temperature and sunshade play determining roles in geo-authentic formation. [...] Read more.
Angelica sinensis, a perennial herb that produces ferulic acid and phthalides for the treatment of cardio-cerebrovascular diseases, prefers growing at an altitude of 1800–3000 m. Geographical models have predicted that high altitude, cool temperature and sunshade play determining roles in geo-authentic formation. Although the roles of altitude and light in yield and quality have been investigated, the role of temperature in regulating growth, metabolites biosynthesis and gene expression is still unclear. In this study, growth characteristics, metabolites contents and related genes expression were investigated by exposing A. sinensis to cooler (15 °C) and normal temperatures (22 °C). The results showed that plant biomass, the contents of ferulic acid and flavonoids and the expression levels of genes related to the biosynthesis of ferulic acid (PAL1, 4CLL4, 4CLL9, C3H, HCT, CCOAMT and CCR) and flavonoids (CHS and CHI) were enhanced at 15 °C compared to 22 °C. The contents of ligustilide and volatile oils exhibited slight increases, while polysaccharide contents decreased in response to cooler temperature. Based on gene expression levels, ferulic acid biosynthesis probably depends on the CCOAMT pathway and not the COMT pathway. It can be concluded that cool temperature enhances plant growth, ferulic acid and flavonoid accumulation but inhibits polysaccharide biosynthesis in A. sinensis. These findings authenticate that cool temperature plays a determining role in the formation of geo-authentic and also provide a strong foundation for regulating metabolites production of A. sinensis. Full article
(This article belongs to the Special Issue Plant Secondary Metabolites with Health Effects: Discovery and Engineering)
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18 pages, 19616 KiB  
Article
Integrated Metabolomic and Transcriptomic Analysis Reveals Differential Mechanism of Flavonoid Biosynthesis in Two Cultivars of Angelica sinensis
by Tiantian Zhu, Minghui Zhang, Hongyan Su, Meiling Li, Yuanyuan Wang, Ling Jin and Mengfei Li
Molecules 2022, 27(1), 306; https://doi.org/10.3390/molecules27010306 - 04 Jan 2022
Cited by 14 | Viewed by 2677
Abstract
Angelica sinensis is a traditional Chinese medicinal plant that has been primarily used as a blood tonic. It largely relies on its bioactive metabolites, which include ferulic acid, volatile oils, polysaccharides and flavonoids. In order to improve the yield and quality of A. [...] Read more.
Angelica sinensis is a traditional Chinese medicinal plant that has been primarily used as a blood tonic. It largely relies on its bioactive metabolites, which include ferulic acid, volatile oils, polysaccharides and flavonoids. In order to improve the yield and quality of A. sinensis, the two cultivars Mingui 1 (M1), with a purple stem, and Mingui 2 (M2), with a green stem, have been selected in the field. Although a higher root yield and ferulic acid content in M1 than M2 has been observed, the differences of flavonoid biosynthesis and stem-color formation are still limited. In this study, the contents of flavonoids and anthocyanins were determined by spectrophotometer, the differences of flavonoids and transcripts in M1 and M2 were conducted by metabolomic and transcriptomic analysis, and the expression level of candidate genes was validated by qRT-PCR. The results showed that the contents of flavonoids and anthocyanins were 1.5- and 2.6-fold greater in M1 than M2, respectively. A total of 26 differentially accumulated flavonoids (DAFs) with 19 up-regulated (UR) and seven down-regulated (DR) were obtained from the 131 identified flavonoids (e.g., flavonols, flavonoid, isoflavones, and anthocyanins) in M1 vs. M2. A total 2210 differentially expressed genes (DEGs) were obtained from the 34,528 full-length isoforms in M1 vs. M2, and 29 DEGs with 24 UR and 5 DR were identified to be involved in flavonoid biosynthesis, with 25 genes (e.g., CHS1, CHI3, F3H, DFR, ANS, CYPs and UGTs) mapped on the flavonoid biosynthetic pathway and four genes (e.g., RL1, RL6, MYB90 and MYB114) belonging to transcription factors. The differential accumulation level of flavonoids is coherent with the expression level of candidate genes. Finally, the network of DAFs regulated by DEGs was proposed. These findings will provide references for flavonoid production and cultivars selection of A. sinensis. Full article
(This article belongs to the Special Issue Plant Secondary Metabolites with Health Effects: Discovery and Engineering)
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15 pages, 5833 KiB  
Article
Physiological and Transcriptomic Analysis Provide Insight into Low Temperature Enhancing Hypericin Biosynthesis in Hypericum perforatum
by Hongyan Su, Jie Li, Sijin Chen, Ping Sun, Hua Xing, Delong Yang, Xiaona Zhang, Mengfei Li and Jianhe Wei
Molecules 2021, 26(8), 2294; https://doi.org/10.3390/molecules26082294 - 15 Apr 2021
Cited by 5 | Viewed by 2357
Abstract
Hypericin (Hyp), well-known as an antidepressant, is mainly extracted from Hypericum perforatum. Although Hyp accumulation and biomass are greater at lower compared to higher temperature, the regulation mechanism has not been reported. Here, the physiological characteristics and transcriptome of H. perforatum grown [...] Read more.
Hypericin (Hyp), well-known as an antidepressant, is mainly extracted from Hypericum perforatum. Although Hyp accumulation and biomass are greater at lower compared to higher temperature, the regulation mechanism has not been reported. Here, the physiological characteristics and transcriptome of H. perforatum grown at 15 and 22 °C were determined and analyzed by HPLC and de novo sequencing. The results showed that the stomatal density and opening percentages were 1.1- and 1.4-fold more, and the Hyp content was 4.5-fold greater at 15 °C compared to 22 °C. A total of 1584 differentially expressed genes (DEGs) were observed at 15 versus 22 °C, with 749 characterized genes, 421 upregulated (UR) and 328 downregulated (DR). Based on biological functions, 150 genes were associated with Hyp biosynthesis, plant growth and the stress response, including photosynthesis, carbohydrate metabolism, fatty acids metabolism, cytochrome P450 (CYPs), morpho-physiological traits, heat shock proteins (HSPs), cold-responsive proteins (CRPs) and transcription factors (TFs). The differential expression levels of the master genes were confirmed by qRT-PCR and almost consistent with their Reads Per kb per Million (RPKM) values. This physiological and transcriptomic analyses provided insight into the regulation mechanisms of low temperature enhancing Hyp biosynthesis in H. perforatum. Full article
(This article belongs to the Special Issue Plant Secondary Metabolites with Health Effects: Discovery and Engineering)
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