Current Bioactive Compounds - Volume 18, Issue 4, 2022

Medicinal plants have been globally exploiting as an alternative to chemical drugs in the treatment of several diseases due to low unwanted side effects, environmentally friendly nature, and low production costs. Therefore, it is important to analyze the therapeutic properties of various medicinal plants to understand their potential bioactivity. Uncaria tomentosa is one of these medicinal plants with many health-promoting effects. Although the geographical resources of cat's claw go back to the remote tropics of the Amazon, industrialized countries use the plant extensively in trade. Various parts of the plants such as flowers, leaves, Stem, hooks, and seeds are mainly used medicinally to treat inflammation, asthma, allergies, skin impurities, microbial infections, neurodegenerative diseases, cancer, cirrhosis, gastrointestinal disorders, arthritis, heart disease, rheumatism, and fever. The endpoint of this review article is to prospectively scrutinize in vitro and in vivo the therapeutic potential of this plant, especially in terms of its nutritional applications and healthbeneficial effects.

Background: Bioactive compounds obtained from natural sources like plants, algae, mushrooms and marine have become of utmost importance in the pharmaceutical, food and cosmetic industries. Many bioactive chemicals have been found to have health-promoting characteristics, including antioxidant, antidiabetic, antibacterial, and anticancer activities. Extraction of these bioactive chemicals from natural sources is difficult since they are present in extremely low concentrations inside the cell. Methods: The complete cropping of bioactive compounds from natural sources depends on several physicochemical parameters such as solvent, solvent concentration, temperature, pressure, time, etc., and they play a crucial role in determining the efficiency of extraction. Furthermore, these factors are not inherently connected to one another, but when they are combined, they change not just the extraction efficiency but also the process cost. As a result, the physicochemical parameters must be properly adjusted in order to increase the extraction efficiency as well as the biological characteristics of isolated molecules. Results: The article provides a thorough examination of several extraction strategies, as well as the mechanism and concepts that underpin them. Also, the review highlights the impact of various physicochemical parameters on the effective extraction of bioactive compounds from natural sources to meet the standards of industrial requirements. Conclusion: Many of the tests have been conducted at the laboratory level; as a result, recommendations for scaling up the extraction process have been provided in order to assess the performance of small-scale to large-scale industrial operations.

Background: The laurel is a shrub native to the Mediterranean basin. It is too often wrongly relegated to the kitchen as a simple condiment while it possesses many therapeutic properties and virtues. The valorization of this plant in terms of bioactive compounds seems to be important. Objective: The aim of the present study is to optimize total phenolic content (TPC) extraction and antioxidant activity from dried bay leaves using conventional process and response surface methodology (RSM). Methods: The study of optimization firstly tested three extraction methods (maceration, ultrasonicassisted extraction (UAE), and Microwave-assisted extraction (MAE)) then the best one was considered for RSM. Results: The results for the sequential procedure indicated that MAE was the best method for TPC extraction and antioxidant activity of Laurus nobilis leaves. The mathematical modeling of MEA using response surface methodology showed that optimal conditions for phenolic compounds extraction were 57% methanol with microwaves power of 602W during 3.48 minutes. These conditions allowed TPC extraction of 83.53 mg/g and manifested an antioxidant activity of 32.51 mg EAG/g. Conclusion: The validation of models indicated that experimental values were in accordance with predicted ones, demonstrating the suitability of developed models and the success of RSM in the optimization of antioxidants extraction from Laurus nobilis leaves. Therefore, the bay leaves could be considered as an interesting source of phenolic antioxidants.

Background: Medicinal plants, together with their isolated bioactive compounds, are known for their antioxidant properties, which constitute therapeutic agents that are routinely employed in the treatment of liver diseases. Aims of the Study: The current study sought to explore the protective role of Warburgia salutaris and its isolated compound, iso-mukaadial acetate, against carbon tetrachloride (CCl4)-induced hepatic injury. Methods: Thirty-five male Sprague Dawley rats were divided into seven groups of five animals each and injected with CCl4 to induce hepatic injury. Results: Treatment with the crude extract of W. salutaris and iso-mukaadial acetate significantly reduced the levels of alkaline phosphatase, alanine and aspartate amino transaminases, and total bilirubin and malondialdehyde in a dose-dependent manner compared to untreated groups. Liver histology revealed a reduction in hepatic necrosis and inflammation. Conclusion: The current investigation has demonstrated that W. salutaris extract and iso-mukaadial acetate could mitigate the acute liver injury inflicted by a hepatotoxic inducer in rats.

Background and Objective: Nowadays, the conventional chemical compounds used in the food, pharmaceutical, and cosmetic sectors have proven to be less efficient from an economic and health point of view. Research has therefore focused on the isolation of bioactive molecules from plants or microorganisms . Methods: The study focused on the leaf’s volatile compounds determination from Myrtus communis (McEOs) and Mentha spicata (MsEOs) as well as the evaluation of phytochemical fractions and biological activities from their methanol extracts (McME and MsME). Results: Phenolic compounds analysis revealed interesting concentrations of total phenols, flavonoids, and condensed tannins. The antibacterial activity tested on seven pathogenic bacteria has to be effectuated by the gel diffusion method. The extracts showed much better DPPH radical scavenging activity than the volatile compounds. The McEOs and MsEOs profiles analyzed by CG-MS showed a mixture of several compounds with a predominance of 1,8-Cineole (48.1%) and α-pinene (39.02%) in the case of McEOs. In the case of MsEOs, the predominant compounds were D-Carvone (78.79%), dihydrocarvone (6.16%), and 1.8 Cineole (2.33%). Conclusion: It emerges from this study that the M. communis and M. spicata leaves, rich in phenolic and terpenic compounds, constitute a promising source of diversified biological activities and can be used in agro-food, cosmetic, and pharmaceutical sectors.

Background: This study assessed the effects of solvent proportion, time and power intensity of ultrasound processing on the extraction, bioaccessibility, antioxidant and antimicrobial activity of phenolic compounds (PC) from acerola (Malpighia glabra DC) coproduct (ACP). Methods: The ultrasound process with water as a solvent in a ratio of 1:2, power intensity of 75 W/cm2 during 10 min was selected as the optimal condition to provide higher extraction of the total phenolic compounds (4126 mg gallic acid.100 g-1 with total antioxidant activity of 98.62 μMTrolox. g^-1). Power intensity and solid: solvent proportion were the parameters that increased the total PC quantification. The main phenolic compounds from the ACP tentatively identified by UPLC-ESI-QTOF-MS/MS were rutin, luteolin, and quercetin. Ultrasound extraction also improved antimicrobial activity against Listeria monocytogenes and Staphylococcus aureus (40 mg.L ^-1). Results: These results indicate that antioxidant and antimicrobial activities in the ACP phenolic extracts are quite potent and implicate the presence of compounds with potent free-radical-scavenging activity. Conclusion: It is possible to extract phenolic compounds from acerola coproducts using sustainable “green” technology, only using water as a solvent and ultrasound processing.

Background: Triazoles are heterocyclic synthetic compounds that have gained relevance after studies by Sharpless on regioselective methodologies for the synthesis of 1,2,3-triazole derivatives. In addition, they have a wide range of biological properties. Objective: The objective of this study is to develop a synthetic methodology aligned with the principles of click chemistry for the synthesis of 1,2,3-triazole derivatives and verify the profile of these compounds in biological assays. Methods: Initially, a model reaction was selected and an optimization study involving synthetic conditions was carried out. Using the most efficient condition, a series of compounds was developed by the reactions between 2-azido-1-phenylethan-1-one derivatives and terminal alkynes. In sequence, bactericidal and antitumoral assays were performed. Results: It was possible to synthesise ten examples using water as a sustainable solvent, in 1 hour, with good yields of 73-99%, including three compounds described for the first time. Two products presented bactericidal activity, one against the gram-negative Escherichia coli ATCC 25922 and other against the gram-positive Paenibacillus alvei CBMAI 2221. Moreover, other two triazole derivatives presented antitumoral activity for prostate and pancreas cancer cells in this screening study with the bioactivity quantified for compound 1-([1,1'-biphenyl]-4-yl)-2-(4-(p-tolyl)- 1H-1,2,3-triazol-1-yl)ethan-1-one (IC50 = 132 μM). Conclusion: Herein, an efficient methodology for the synthesis of 1,2,3-triazole derivatives with high yields and using water as solvent was developed. Furthermore, some compounds presented positive results to bactericidal and antitumoral assays, justifying further exploration of these novel compounds and their biological properties.

Background: The aim of the present study is to evaluate the protective effect of n- BuOH fraction of Genista vepres Pomel and Vitamin E against Isoniazid and Rifampicin (INH- RIF)-induced liver injury. Methods: Male Wistar Albino rats were divided into eight equal groups treated with plant fraction (50 mg/kg, 100 mg/kg), vitamin E (100 mg/kg) and INH-RIF (100 mg/kg body weight /day each). At the end of the experiment, animals were dissected and samples (blood, liver tissue) were removed and isolated for biochemical and histological studies. Results: Administration of INH-RIF for 21 days resulted in hepatic failure as evidenced by the elevation of biochemical parameters levels and hepatic oxidative stress, which was associated with extensive hepatic parenchyma alteration. The pretreatment of the rat with G. vepres Pomel attenuated the increase of hepatic dysfunction markers, significantly decreased the level of malondialdehyde (MDA), and increased GSH level, GPx and catalase activities compared to INH-RIF treated group. However, the Vitamin E co-treatment decreased MDA level and increased GPx activity but did not show any effect on catalase or GSH parameters. The histopathological studies on the liver of rats also supported that both plant fraction and vitamin E markedly reduced the toxicity of INH-RIF and preserved the histoarchitecture of liver tissue. Conclusion: The results suggested that the n-BuOH fraction of G. vepres Pomel acts as a potent hepatoprotective agent against INH-RIF-induced Hepatic dysfunction in rats.