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Different Approaches in Discovery and Resupply of Plant-Derived Natural Products

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A special issue of Plants (ISSN 2223-7747). This special issue belongs to the section "Phytochemistry".

Deadline for manuscript submissions: closed (15 November 2021) | Viewed by 25450

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Dr. Cinzia Sanna

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Department of Life and Environmental Sciences, University of Cagliari, Via Sant’Ignazio da Laconi 13, 09123 Cagliari, Italy
Interests: medicinal plants; plant extracts; ethnobotany; endemic species; phytochemistry; bioactivity
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The last several decades have seen an increase in plant-based drug discovery processes. Indeed, natural products possess a superior chemical diversity as compared to synthetic ones, leading to a renewal in the search for new plant-based drugs. In the selection of starting plant material to submit to phytochemical and biological/pharmacological studies, different strategies can be pursued: the classical ethnopharmacological approach based on the traditional medicinal use of plants provides hints for compounds which are therapeutically effective in humans; the chemosystematic or phylogenetic approach, making use of chemotaxonomic knowledge and molecular phylogenetic data in order to select plant species from genera or families known to produce compound classes associated with a certain bioactivity; the ecological approach, based on the observation of interactions between organisms and their environment that might lead to the production of bioactive natural compounds; the random approach, based on the selection of plant species mainly on the basis of their availability (this strategy might be highly advantageous when applied in regions of high biodiversity and endemism, since the chemical diversity of natural products can reflect the biodiversity of their source organisms) ; and computational methods based on the selection of test samples relying on in silico bioactivity predictions for the constituents of certain plant species. This Special Issue aims to collect relevant scientific papers on new possible approaches for the identification, characterization, and resupply of natural products that may address some of the challenges related with the development of plant-based therapeutics.

Dr. Cinzia Sanna
Guest Editor

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Keywords

Ethnobotany
chemotaxonomy
biodiversity
phytochemical screening
plant-based drug discovery
plant selection
herbal and plant extracts

Published Papers (9 papers)

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16 pages, 1369 KiB

Open AccessArticle

Comparative Study of the Antioxidant Constituents, Activities and the GC-MS Quantification and Identification of Fatty Acids of Four Selected Helichrysum Species

by Kolajo Adedamola Akinyede, Gail Denise Hughes, Okobi Eko Ekpo and Oluwafemi Omoniyi Oguntibeju

Plants 2022, 11(8), 998; https://doi.org/10.3390/plants11080998 - 7 Apr 2022

Cited by 3 | Viewed by 1886

Abstract

Helichrysum Mill. (Asteraceae) is a plant genus comprising distinctively of aromatic plants of about 500–600 species. Since most of these plants have not been previously studied, extensive profiling helps to validate their folkloric uses and determine their potential value as sources of plant-derived drug candidates. This study, therefore, aims to investigate the antioxidant activity (DPPH, NO, FRAP); total antioxidant capacity, total phenolic, total flavonoid, and fatty acid compositions of the aqueous acetone extracts from four Helichrysum plants namely, Helichrysum pandurifolium, Helichrysum foetidum, Helichrysum petiolare, and Helichrysum cymocum. The results obtained showed that the H. cymocum extract had the best DPPH radical scavenging activity (IC₅₀ = 11.85 ± 3.20 µg/mL) and H. petiolare extract had the best nitric oxide scavenging activity (IC₅₀ = 20.81 ± 3.73 µg/mL), while H. pandurifolium Schrank extract (0.636 ± 0.005 µg/mL) demonstrated the best ferrous reducing power, all of which are comparable with results from ascorbic acid used as the standard. The IC₅₀ values of the radical scavenging activity ranged from 11.85–41.13 µg/mL (DPPH), 20.81–36.19 µg/mL (NO), and 0.505–0.636 µg/mL (FRAP), for all the plants studied. The H. petiolare has the highest total antioxidant capacity (48.50 ± 1.55 mg/g), highest total phenolic content (54.69 ± 0.23 mg/g), and highest total flavonoid content (56.19 ± 1.01 mg/g) compared with other species. The fatty acid methyl esters were analysed using gas chromatography-mass spectrometry (GC-MS). The results obtained showed variations in the fatty acid composition of the plant extracts, with H. petiolare having the highest saturated fatty acid (SFA) content (7184 µg/g) and polyunsaturated fatty acid (PUFA) content (7005.5 µg/g). In addition, H. foetidum had the highest monounsaturated fatty acid (MUFA) content (1150.3 µg/g), while H. cymocum had the highest PUFA:SFA ratio of 1.202. In conclusion, the findings from this study revealed that H. pandurifolium Schrank, H. foetidum, H. petiolare, and H. cymocum are repositories of natural bioactive compounds with potential health-promoting benefits that need to be investigated, for both their antioxidant activity in a number of disease conditions and for further exploration in drug discovery and development projects. Full article

(This article belongs to the Special Issue Different Approaches in Discovery and Resupply of Plant-Derived Natural Products)

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17 pages, 5182 KiB

Open AccessArticle

Phytochemical Analysis and In Vitro Cytotoxic Activity against Colorectal Adenocarcinoma Cells of Hippophae rhamnodies L., Cymbopogon citratus (D.C.) Stapf, and Ocimum basilicum L. Essential Oils

by Alina Dolghi, Roxana Buzatu, Amadeus Dobrescu, Flavius Olaru, Grigore Alexandru Popescu, Iasmina Marcovici, Iulia Pinzaru, Dan Navolan, Octavian Marius Cretu, Iuliana Popescu and Cristina Adriana Dehelean

Plants 2021, 10(12), 2752; https://doi.org/10.3390/plants10122752 - 14 Dec 2021

Cited by 7 | Viewed by 2769

Abstract

Colorectal carcinoma (CRC) is one of the most frequently diagnosed cancer types with current deficient and aggressive treatment options, but various studied alternative therapies are able to efficiently contribute to its management. Essential oils (EOs) contain valuable compounds, with antibacterial, anti-inflammatory, and anticancer properties, which might serve as effective solutions in CRC prophylaxis or treatment. The aim of the present work was to evaluate the phytochemical composition and in vitro biological activity of essential oils derived from Hippophae rhamnoides (Hr_EO), Cymbopogon citratus (Cc_EO), and Ocimum basilicum (Ob_EO) species on HT-29 and Caco-2 human colorectal adenocarcinoma cell lines. The main compounds identified by GC-MS analysis were estragole (Hr_EO, Ob_EO), alpha- and beta-citral (Cc_EO). All tested EOs exerted a dose-dependent cytotoxicity on both cell lines by reducing the cell viability, especially in the case of Cc_EO, where at 75 µg/mL the viability percentages reached the values of 62.69% (Caco-2) and 64.09% (HT-29), respectively. The nuclear morphology evaluation highlighted significant dysmorphologies on both lines after their treatment with EOs at 75 µg/mL. Full article

(This article belongs to the Special Issue Different Approaches in Discovery and Resupply of Plant-Derived Natural Products)

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13 pages, 3401 KiB

Open AccessArticle

Variation of Triterpenic Acids in 12 Wild Syzygium formosum and Anti-Inflammation Activity on Human Keratinocyte HaCaT

by Hyun-ah Park, Mi Yoon Kim, Nan-Young Lee, Jaeyoon Lim, Kyu-been Park, Chang-Kyu Lee, Van Dao Nguyen, Jaehan Kim, Jong-Tae Park and Jong-Il Park

Plants 2021, 10(11), 2428; https://doi.org/10.3390/plants10112428 - 10 Nov 2021

Cited by 3 | Viewed by 2016

Abstract

Syzygium formosum (Wall.) Masam leaf is known as a Vietnamese traditional herbal medicine used to treat atopic dermatitis and stomach ulcers. Recently, its potent anti-allergic effects were reported with possible active compounds analysis. Here, we collected S. formosum leaves from 12 wild trees and compared compositions of triterpenic acids (TA) with Centella asiatica. Anti-inflammatory activities of S. formosum leaf extract (SFLE) was compared with C. asiatica extract (CAE) using human keratinocyte, HaCaT. In this study, up to seven TAs were identified in SFLE, while only madecassic and asiatic acids were detected in the CAE. Total TA content varied among SFLE, but asiatic, corosolic, and betulinic acids were the major components. Surprisingly, wild tree sample 12 (S12) contained total TA of 27.2 mg/g dry-leaves that was 5-fold greater than that in the C. asiatica sample, and S4 had the highest content of asiatic acid (12.6 mg/g dry-leaves) that accounted for 50% of the total TA. S4 and S12 showed more than 3-fold higher anti-oxidative power than the CAE. In the UVB irradiation model, S4 and S12 (5 μg/mL) strongly repressed mRNA levels of pro-inflammatory cytokines (IL-1β, IL-6, and IL-8) and COX-2, while the CAE at the same condition showed moderate or weak repression. The difference in anti-inflammation effects between the SFLE and the CAE was also confirmed by protein quantifications. Taken together, SFLE has great potentials as a new cosmeceutical ingredient with a higher amount of skin-active phytochemicals. Full article

(This article belongs to the Special Issue Different Approaches in Discovery and Resupply of Plant-Derived Natural Products)

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11 pages, 1738 KiB

Open AccessArticle

Compositional Characteristics of Glucuronide Conjugates in Regional Glechoma hederacea var. longituba Herbal Extracts Using a Set of Polyphenolic Marker Compounds

by Young Hye Hahm, Kun Cho and Yeong Hee Ahn

Plants 2021, 10(11), 2353; https://doi.org/10.3390/plants10112353 - 30 Oct 2021

Cited by 4 | Viewed by 1546

Abstract

Glechoma hederacea var. longituba (GHL) is one of many herbal plants widely used in hot herbal teas and in oriental prescriptions to treat various diseases. Although the beneficial effects of GHL may be influenced by differences in the composition of active constituents in the herbal extracts, there are few reports on the compositional characteristics of GHL herbal extracts to date. In this study, liquid chromatography–mass spectrometry technology was used for comparative analysis of constituents in hot-water extracts of GHL samples obtained from various cultivating provinces in South Korea. A set of marker panel consisting of nine polyphenolic compounds, including glucuronide conjugates in particular, was constructed and used to monitor the compositional characteristics in each GHL extract. Our findings show that some of the marker compounds, including rosmarinic acid, were persistently observed as major constituents in the analyses of the 22 GHL sample extracts, whereas, interestingly, other marker compounds such as polyphenol-glucuronic acid conjugates displayed dramatic differences in compositional ratios. This chromatographic approach using the marker compound panel can be applied to qualitatively and quantitatively evaluate compositional characteristics in the GHL extracts, and can also be useful for quality assays of the GHL herbal plant in medicinal and industrial fields. Full article

(This article belongs to the Special Issue Different Approaches in Discovery and Resupply of Plant-Derived Natural Products)

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14 pages, 681 KiB

Open AccessArticle

Extraction and Encapsulation of Phenolic Compounds of Tunisian Rosemary (Rosmarinus officinalis L.) Extracts in Silk Fibroin Nanoparticles

by Kheiria Hcini, Antonio A. Lozano-Pérez, José Luis Cenis, María Quílez and Maria José Jordán

Plants 2021, 10(11), 2312; https://doi.org/10.3390/plants10112312 - 27 Oct 2021

Cited by 18 | Viewed by 2913

Abstract

Rosemary (Rosmarinus officinalis L.) is known to be an effective potential source of natural antioxidants which confer benefits to human health. Their bioactive properties are mainly due to phenolic compounds but these molecules are highly vulnerable to oxidants, light, heat, pH, water and enzymatic activities. Therefore, the stability and shelf life of phenolic compounds should be increased by being protected from chemical and physical damage by means of encapsulation prior to application. Encapsulation is becoming increasingly important in the pharmaceutical, food, cosmetics, textile, personal care, chemical, biotechnology, and medicinal industries due to its potential for stabilization and delivery of delicate and precious bioactive compounds. The aim of the present work was to describe the polyphenolic profile of Tunisian Rosemary, collected from two different bioclimatic areas, and further loading in silk fibroin nanoparticles. The loaded nanoparticles were characterized in terms of morphology, size, polydispersity, Z-potential, secondary structure of the protein, encapsulation efficiency, loading content, and antioxidant activity. On one hand, HPLC analysis revealed the presence of 18 polyphenolic compounds of whichcarnosic acid and carnosol were found to be the most abundant compounds (46.3 to 76.4 and 22.4 to 43.5 mg of compound per gram of dry plant weight (mg/g DPW) respectively), Total phenolic content (TPC) ranged from 85.8 to 137.3 mg of gallic acid equivalent (GAE)/g DPW in post-distilled rosemary extracts andantioxidant activity reached the values of 5.9 to 8.3 µmol of ascorbic acid equivalent (AAE)/g DPW). On the other hand loaded nanoparticles were almost spherical and presented nanometric size and negative Z-potential. Although the encapsulation efficiency in silk fibroin nanoparticles and the drug loading content were low in the conditions of the assay, the encapsulated polyphenols retained near 85% of the radical scavenging activity against DPPH· after 24 h. of incubation at 37 °C. The results showed that post-distilled rosemary residues had an effective potential as natural antioxidants due to their significant antioxidant activity and seemed to be useful in both pharmaceutical and food industries with beneficial properties that might confer benefits to human health and these silk fibroin nanoparticles loaded with rosemary extracts are thus a promising combination for several applications in food technology or nanomedicine. Full article

(This article belongs to the Special Issue Different Approaches in Discovery and Resupply of Plant-Derived Natural Products)

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11 pages, 819 KiB

Open AccessArticle

In Vitro Anti-HIV-1 Reverse Transcriptase and Integrase Properties of Punica granatum L. Leaves, Bark, and Peel Extracts and Their Main Compounds

by Cinzia Sanna, Arianna Marengo, Stefano Acquadro, Alessia Caredda, Roberta Lai, Angela Corona, Enzo Tramontano, Patrizia Rubiolo and Francesca Esposito

Plants 2021, 10(10), 2124; https://doi.org/10.3390/plants10102124 - 7 Oct 2021

Cited by 15 | Viewed by 3069

Abstract

In a search for natural compounds with anti-HIV-1 activity, we studied the effect of the ethanolic extract obtained from leaves, bark, and peels of Punica granatum L. for the inhibition of the HIV-1 reverse transcriptase (RT)-associated ribonuclease H (RNase H) and integrase (IN) LEDGF-dependent activities. The chemical analyses led to the detection of compounds belonging mainly to the phenolic and flavonoid chemical classes. Ellagic acid, flavones, and triterpenoid molecules were identified in leaves. The bark and peels were characterized by the presence of hydrolyzable tannins, such as punicalins and punicalagins, together with ellagic acid. Among the isolated compounds, the hydrolyzable tannins and ellagic acid showed a very high inhibition (IC₅₀ values ranging from 0.12 to 1.4 µM and 0.065 to 0.09 µM of the RNase H and IN activities, respectively). Of the flavonoids, luteolin and apigenin were found to be able to inhibit RNase H and IN functions (IC₅₀ values in the 3.7–22 μM range), whereas luteolin 7-O-glucoside showed selective activity for HIV-1 IN. In contrast, betulinic acid, ursolic acid, and oleanolic acid were selective for the HIV-1 RNase H activity. Our results strongly support the potential of non-edible P. granatum organs as a valuable source of anti-HIV-1 compounds. Full article

(This article belongs to the Special Issue Different Approaches in Discovery and Resupply of Plant-Derived Natural Products)

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10 pages, 1117 KiB

Open AccessArticle

Immunomodulatory Effect of Helleborus purpurascens Waldst. & Kit.

by Alice Grigore, Corina Bubueanu, Lucia Pirvu, Georgeta Neagu, Ionica Bejanaru, Virginia Vulturescu, Minerva Panteli and Iuksel Rasit

Plants 2021, 10(10), 1990; https://doi.org/10.3390/plants10101990 - 23 Sep 2021

Cited by 3 | Viewed by 1649

Abstract

(1) Background: Helleborus purpurascens Waldst. & Kit. (hellebore) is a plant species found mainly in Balkans and the Carpathians, and it is traditionally used for a variety of ailments since the time of Hippocrates. The aim of this study was to investigate the immunomodulatory effect of hellebore extracts correlated with relevant chemical compounds and the extraction method. (2) Methods: A methanolic (H1) and a hydroalcoholic extract (H2) were prepared by standard methods. Qualitative (HPTLC) and quantitative (HPLC) chemical analysis were conducted to reveal the ecdysones and polyphenolic compounds. In vitro studies were performed using rat macrophages, murine fibroblasts and immortalized human T-lymphocytes, and their viability was determined by MTS assay. In vivo studies involved a rat immunodepression model. (3) Results: In vitro assays revealed the stronger effect of H2 on cellular proliferation, compared to H1. In the in vivo assay, H2 revealed an immunostimulatory effect in the context of experimentally induced immunosuppression with dexamethasone, a superior effect to levamisole treatment according to the same regimen, in two doses every 24 h. There was no correlation between pharmacological effect and the reference compounds evaluated. (4) Conclusions: The immunomodulatory effect of methanolic and hydroalcoholic hellebore extracts is not due to ecdysones and polyphenolic compounds, but other polar substances, possible steroid glycosides. Full article

(This article belongs to the Special Issue Different Approaches in Discovery and Resupply of Plant-Derived Natural Products)

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19 pages, 2032 KiB

Open AccessArticle

Quantitative Ethnobotanical Analysis of Medicinal Plants of High-Temperature Areas of Southern Punjab, Pakistan

by Muhammad Usman, Allah Ditta, Faridah Hanum Ibrahim, Ghulam Murtaza, Muhammad Nawaz Rajpar, Sajid Mehmood, Mohd Nazre Bin Saleh, Muhammad Imtiaz, Seemab Akram and Waseem Razzaq Khan

Plants 2021, 10(10), 1974; https://doi.org/10.3390/plants10101974 - 22 Sep 2021

Cited by 12 | Viewed by 5993

Abstract

Lack of proper infrastructure and the poor economic conditions of rural communities make them dependent on herbal medicines. Thus, there is a need to obtain and conserve the historic and traditional knowledge about the medicinal importance of different plants found in different areas of the world. In this regard, a field study was conducted to document the medicinal importance of local plants commonly used by the inhabitants of very old historic villages in Southern Punjab, Pakistan. In total, 58 plant species were explored, which belonged to 28 taxonomic families, as informed by 200 experienced respondents in the study area. The vernacular name, voucher number, plant parts used, and medicinal values were also documented for each species. Among the documented species, Poaceae remained the most predominant family, followed by Solanaceae and Asteraceae. The local communities were dependent on medicinal plants for daily curing of several ailments, including asthma, common cold, sore throat, fever, cardiovascular diseases, and digestive disorders. Among the reported species, leaves and the whole plant remained the most commonly utilized plant parts, while extracts (38.8%) and pastes (23.9%) were the most popular modes of utilization. Based on the ICF value, the highest value was accounted for wound healing (0.87), followed by skincare, nails, hair, and teeth disorders (0.85). The highest RFC value was represented by Acacia nilotica and Triticum aestivum (0.95 each), followed by Azadirachta indica (0.91). The highest UV was represented by Conyza canadensis and Cuscuta reflexa (0.58 each), followed by Xanthium strumarium (0.37). As far as FL was concerned, the highest value was recorded in the case of Azadirachta indica (93.4%) for blood purification and Acacia nilotica (91.1%) for sexual disorders. In conclusion, the local inhabitants primarily focus on medicinal plants for the treatment of different diseases in the very old historic villages of Southern Punjab, Pakistan. Moreover, there were various plants in the study area that have great ethnobotanical potential to treat various diseases, as revealed through different indices. Full article

(This article belongs to the Special Issue Different Approaches in Discovery and Resupply of Plant-Derived Natural Products)

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Other

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11 pages, 515 KiB

Open AccessBrief Report

Chemical Composition and Antiproliferative Activity of the Ethanolic Extract of Cyperus articulatus L. (Cyperaceae)

by Éden Bruno Sousa da Silva, Lauro Euclides Soares Barata, Michelly Rios Arévalo, Leda Quercia Vieira, Waldionê Castro, Ana Lúcia Tasca Gois Ruiz, Adriana Della Torre, Kelly Christina Ferreira Castro, Adilson Sartoratto, Leopoldo C. Baratto, Maxwell Barbosa de Santana, Antonio Humberto Hamad Minervino and Waldiney Pires Moraes

Plants 2021, 10(10), 2084; https://doi.org/10.3390/plants10102084 - 1 Oct 2021

Cited by 9 | Viewed by 2506

Abstract

Cyperus articulatus L. (Priprioca) is a plant of the Cyperaceae family traditionally used in traditional medicine in the Amazon region. Studies of the essential oil of this species have identified many terpene compounds. However, little is known about the possible uses of solid waste generated by the extraction of essential oils. This study aimed to investigate the chemical composition of volatile compounds and to evaluate the antiproliferative activity of the ethanolic extract of solid residues generated by the extraction of the essential oil of C. articulatus L. rizhomes in experimental models in vitro using peritoneal macrophages of mice and human tumor cell lines. The analysis of the chemical composition of volatile compounds indicated the presence of sesquiterpenes and particularly sequiterpenic ketones as main constituents. The results showed that the treatment with ethanolic extract of C. articulatus L. reduced the activity of the enzyme arginase and proliferation of cancer cells (p < 0.0001). The extract also showed no cytotoxicity in macrophages in concentrations between 12.5; 25 and 50 mg/mL (p < 0.0001). The results indicated that the extract of C. articulatus L. exerts antiproliferative activity (p < 0.0001) with low toxicity on healthy cells in experimental models in vitro. Full article

(This article belongs to the Special Issue Different Approaches in Discovery and Resupply of Plant-Derived Natural Products)

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