ABSTRACT
SUMMARY: High-intensity physical exercises can cause oxidative stress and muscle damage. Several medicinal plants have been used as antioxidant and anti-inflammatory agents. The present study evaluated high-intensity resistance exercise (HIRE) associated with Schinus Terebentifholius ethanolic extract (EE) on oxidative parameters and muscle damage in Wistar rats. Animals were divided into 04 groups (n=10/group): 1. Control (CG) - animals that did not undergo HIRE and were treated with vehicle (distilled water, orally); 2. Acute exercise (AE) - animals submitted to acute exercise session; 3. Exercise + vehicle (EV) - animals that underwent HIRE and were treated with vehicle and 4. Exercise + extract (EX) animals administered with Schinus terebenthifolius EE (100mg/Kg, orally) and submitted to the exercise session. Schinus terebenthifolius EE showed high in vitro antioxidant activity (13.88 ± 0.36 mg/mL). Before the experimental period, lactate was measured at pre and post moments of AE (p<0.0001) and EX (p<0.0001) groups. After the acute session, the following were evaluated: oxidative stress {malondialdehyde (MDA), sulfhydryl groups (SH) and ferric reducing antioxidant power (FRAP)}, muscle damage (creatine kinase (CK) and lactate dehydrogenase (LDH)), alanine aminotransferase (ALT) and aspartate aminotransferase (AST). In the in vivo analyses of the EX group compared to AE and EV groups, respectively: hepatic (MDA: p<0.0001 and SH: p=0.0033, in both; FRAP: p=0.0011 and p=0.0047), muscle (MDA, SH and FRAP: p<0.0001, in both; CK: p=0.0001 and p<0.0001; LDH: p<0.0001, in both), serum levels (MDA: p=0.0003, p=0.0012, SH: p=0.0056, p=0.0200, FRAP: p=0.0017 and p=0.0165) were significant. There was no significant difference in ALT and AST markers. It could be concluded that Schinus terebenthifolius EE associated with HIRE attenuated oxidative stress and muscle damage in rats.
RESUMEN: Los ejercicios físicos de alta intensidad pueden causar estrés oxidativo y daño muscular. Varias plantas medicinales se han utilizado como agentes antioxidantes y antiinflamatorios. El presente estudio evaluó el ejercicio de resistencia de alta intensidad (HIRE) asociado con el extracto etanólico (EE) de Schinus terebentifholius sobre los parámetros oxidativos y el daño muscular en ratas Wistar. Los animales se dividieron en 4 grupos (n=10/grupo): 1. Control (GC) - animales que no se sometieron a HIRE y fueron tratados con vehículo (agua destilada, por vía oral); 2. Ejercicio agudo (AE) - animales sometidos a sesión de ejercicio agudo; 3. Ejercicio + vehículo (EV) - animales que se sometieron a HIRE y fueron tratados con vehículo y 4. Ejercicio + extracto (EX) animales administrados con Schinus terebenthifolius EE (100 mg/kg, por vía oral) y sometidos a la sesión de ejercicio. Schinus terebenthifolius EE mostró una alta actividad antioxidante in vitro (13,88 ± 0,36 mg/mL). Antes del período experimental, se midió el lactato en los momentos pre y post de los grupos AE (p<0,0001) y EX (p<0,0001). Tras la sesión aguda, se evaluaron: el estrés oxidativo malondialdehído (MDA), grupos sulfhidrilo (SH) y poder antioxidante reductor férrico (FRAP), daño muscular (creatina quinasa (CK) y lactato deshidrogenasa (LDH)), alanina aminotransferasa (ALT) y aspartato aminotransferasa (AST). En los análisis in vivo del grupo EX frente a los grupos AE y EV, respectivamente: hepático (MDA: p<0,0001 y SH: p=0,0033, en ambos; FRAP: p=0,0011 y p=0,0047), muscular (MDA, SH y FRAP: p<0,0001, en ambos; CK: p=0,0001 y p<0,0001; LDH: p<0,0001, en ambos), niveles séricos (MDA: p=0,0003, p=0,0012, SH: p=0,0056, p=0,0200, FRAP: p=0,0017 y p=0,0165) fueron significativas. No hubo diferencia significativa en los marcadores ALT y AST. Se podría concluir que Schinus terebenthifolius EE asociado con HIRE atenuó el estrés oxidativo y el daño muscular en ratas.
Subject(s)
Animals , Rats , Plant Extracts/administration & dosage , Exercise , Anacardiaceae , Antioxidants/administration & dosage , Physical Endurance , Plants, Medicinal , Plant Extracts/pharmacology , Biomarkers , Rats, Wistar , Oxidative Stress , Dietary Supplements , Antioxidants/pharmacologyABSTRACT
Introduction: Staphylococcus aureus and Escherichia coli are pathogens that cause chronic infections due to antibiotic resistance mechanisms and their ability to adhere to surfaces and to form biofilms. The search for new agents from natural resources to counter microbial biofilms is an urgent priority in healthcare. Objetive: chemical composition, antibacterial and anti-biofilm activity of Plectranthus amboinicus essential oil (PAEO) and carvacrol were investigated against E. coli and S. aureus. Methodology: PAEO was chemically analyzed using gas chromatography coupled to a mass spectrometer. Antimicrobial activity was assessed by the disc diffusion method and broth microdilution method to determine minimum inhibitory concentrations (MICs). Antibiofilm activity was investigated using 96-well plates with a crystal violet assay. Results: carvacrol (85.25%) was the major component of PAEO. The disc diffusion test confirmed the ability of PAEO and carvacrol in inhibiting bacteria in their planktonic form. The MICs of PAEO against S. aureus and E. coli were 0.31 and 1.25%, respectively, with bactericidal effect. Carvacrol demonstrated a significant antibacterial property (MIC = 0.31%), exhibiting bacteriostatic effects against S. aureus and bactericidal effects against E. coli. Carvacrol considerably inhibited E. coli biofilm formations (58.9%). Moreover, carvacrol inactivated the mature biofilms. Conclusion: the data obtained are promising, and facilitates the development of new therapeutic alternatives. These results indicate the potential of carvacrol in treating diseases caused by E. coli and S. aureus
Introdução: Escherichia coli e Staphylococcus aureus são patógenos que podem causar infecções persistentes devido aos mecanismos de resistência e à sua capacidade de aderir e formar biofilme. A busca por novos agentes a partir de recursos naturais para combater o biofilme é uma prioridade na área da saúde. Objetivo: a composição química, a atividade antibacteriana e anti-biofilme do óleo essencial de Plectranthus amboinicus (PAEO) e do carvacrol foram investigadas frente a S. aureus e E. coli. Metodologia: a análise química do PAEO foi realizada por cromatografia gasosa acoplada a espectrômetro de massa. A atividade antimicrobiana foi avaliada por difusão em disco e microdiluição em caldo para determinar as concentrações inibitórias mínimas (CIMs). As atividades do anti-biofilme foram investigadas usando placas de 96 poços pelo ensaio de cristal violeta. Resultados: o carvacrol (85,25%) foi o principal componente do PAEO. A capacidade do PAEO e do carvacrol para inibir bactérias planctônica foi confirmada por difusão em disco. A CIM do PAEO para S. aureus e E. coli foi de 0,31 e 1,25%, respectivamente, com efeito bactericida. O carvacrol demonstrou uma propriedade antibacteriana significativa (CIM=0,31%), exibindo efeito bacteriostático frente a S. aureus e efeito bactericida para E. coli. O carvacrol inibiu significativamente a formação de biofilme de E. coli (58,9%) e promoveu a desestabilização do biofilme maduro. Conclusão: os dados obtidos são promissores, possibilitando o desenvolvimento de novas alternativas terapêuticas e revelam a potencialidade do carvacrol como fonte para o tratamento de doenças causadas por E. coli e S. aureus.
Subject(s)
Staphylococcus aureus/drug effects , Oils, Volatile/pharmacology , Biofilms/drug effects , Plectranthus/chemistry , Escherichia coli/drug effects , Anti-Bacterial Agents/pharmacology , Microbial Sensitivity Tests/methodsABSTRACT
With the acceleration of the aging process of our country's population, the impact of aging-related diseases - Alzheimer's disease (AD) on society and families has become increasingly prominent. AD is caused by multiple mechanisms, and the pathogenesis has not been fully elucidated. Most of the clinical treatments are single therapy, which mainly focuses on improving symptoms and are difficult to reverse the disease process. Therefore, the development of drugs that can both improve symptoms and reverse the disease process is extremely urgent in clinical. Increasing number of studies has shown that traditional Chinese medicine plays an important role in the prevention and treatment of AD. The natural products have many advantages, such as novel structures, multiple targets and diverse activities, which can be used as an important source of leading compounds for the treatment of AD. The review summarizes the main clinical treatment methods and the research progress of natural ingredients in traditional Chinese medicine, and provides a reference for the follow-up clinical treatment of AD combined with the advantages of traditional Chinese medicine treatment.
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Five new megastigmanes (1-5) were isolated from a decoction of Uncaria rhynchophylla by separation techniques of column chromatography using a combination of multiple stationary phases, including macroporous adsorbent resin, MCI resin, silica gel, Sephadex LH-20, and Toyopearl HW-40F, and reversed phase HPLC. Their structures were characterized by spectroscopic data analysis of HR-ESI-MS, NMR, and CD, in combination with Mosher's mothed as well as ECD and NMR calculations. The new compounds were named uncarphyllonone A (1), uncarphyllonols A (2) and B (3), and uncarphabscisic acids A (4) and B (5). Although the structures of 3 and 4 were previously reported, the reported NMR spectroscopic data were incorrect or do not support the assigned structures in literatures. This is also the first report of discovery of new megastigmane natural products from the Uncaria genus.
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Molecular glues are a class of small molecules that induce the formation of protein-protein interactions to confer new biological function or therapeutic effects. As a unique pharmacological modality, molecular glues could target proteins without druggable binding pockets. It exhibits a variety of functions, including regulating signal transduction, stabilization or degradation of targeted proteins, through sticking different proteins together. This review will summarize the development and current status of molecular glues derived from natural products and analogs by illustrating the discovery and interaction mechanism. We hope to present a systematic view, provide valuable clues for researchers and encourage them to explore more efficient and rational molecular glue discovery strategies.
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Although current synthetic anti-gout drugs have significant therapeutic effects in reducing serum uric acid levels, they have serious side effects such as allergic reactions and liver and kidney damage. Natural products with a wide range of uric acid-lowering and high safety have played a critical role in anti-gout drug discovery and development. This paper reviews the natural products with uric acid-lowering or anti-gout pharmacological effects and the investigation on their mechanisms of action, to provide information for drug discovery and development.
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Target identification of bioactive compounds is important for understanding their mechanisms of action and provides critical insights into their therapeutic utility. While it remains a challenge, unbiased chemoproteomics strategy using clickable photoaffinity probes is a useful and validated approach for target identification. One major limitation of this approach is the efficient synthesis of appropriately substituted clickable photoaffinity probes. Herein, we describe an efficient and consistent method to prepare such probes. We further employed this method to prepare a highly stereo-congested probe based on naturally occurring triterpenoid betulinic acid. With this photoaffinity probe, we identified tropomyosin as a novel target for betulinic acid that can account for the unique biological phenotype on cellular cytoskeleton induced by betulinic acid.
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Lysine specific demethylase 1 (LSD1), a transcriptional corepressor or coactivator that serves as a demethylase of histone 3 lysine 4 and 9, has become a potential therapeutic target for cancer therapy. LSD1 mediates many cellular signaling pathways and regulates cancer cell proliferation, invasion, migration, and differentiation. Recent research has focused on the exploration of its pharmacological inhibitors. Natural products are a major source of compounds with abundant scaffold diversity and structural complexity, which have made a major contribution to drug discovery, particularly anticancer agents. In this review, we briefly highlight recent advances in natural LSD1 inhibitors over the past decade. We present a comprehensive review on their discovery and identification process, natural plant sources, chemical structures, anticancer effects, and structure-activity relationships, and finally provide our perspective on the development of novel natural LSD1 inhibitors for cancer therapy.
Subject(s)
Antineoplastic Agents/therapeutic use , Enzyme Inhibitors/therapeutic use , Histone Demethylases/metabolism , Humans , Lysine/therapeutic use , Neoplasms/drug therapyABSTRACT
Objective: To investigate the effect of piperine on human breast cancer cells. Methods: The effect of piperine on proliferation and migration of human breast cancer cells, MCF-7 and MDA-MB-231, was investigated using colony formation assays, wound healing assays, Matrigel migration assays, flow cytometry, RT-qPCR, and Western blotting assays. Results: Piperine inhibited the growth of MCF-7 and MDA-MB-231 cells and suppressed colony formation. Cell reduction at the G 0 / G 1 phase and cell arrest at the G 2 /M phase were observed in breast cancer cells. However, the significant effect was only demonstrated in MDA-MB-231 cells. Moreover, cancer cell migration was suppressed by piperine at low concentration. RT-qPCR and Western blotting assays showed that piperine downregulated Rac1 gene and protein expression. Conclusions: Piperine could inhibit growth and migration of breast cancer cells by reducing Rac1 gene and protein expression.
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Objective: To enhance the pharmaceutical potential and oral bioavailability of quercetin contents of Allium cepa peel extract by novel nanosuspension technology. Methods: Nanoprecipitation approach was successfully used for the formulation of nanosuspension. To obtain pharmaceutical-grade nanosuspension with minimum particle size and polydispersity index, sodium lauryl sulphate was selected as a stabilizer. Important formulation parameters were statistically optimized by the response surface methodology approach. The optimized nanosuspension was subjected to stability and in vitro dissolution testing and characterized by scanning electron microscopy, atomic force microscopy, Fourier transform infrared spectroscopy, and zeta sizer. To evaluate the preeminence of nanosuspension over coarse suspension, comparative bioavailability studies were carried out in male albino rats. The pharmaceutical potential of developed nanosuspension was evaluated by antioxidant, antimicrobial, and toxicity studies. Results: The optimized nanosuspension showed an average particle size of 275.5 nm with a polydispersity index and zeta potential value of 0.415 and -48.8 mV, respectively. Atomic force microscopy revealed that the average particle size of nanosuspension was below 100 nm. The formulated nanosuspension showed better stability under refrigerated conditions. Nanosuspension showed an improved dissolution rate and a 2.14-fold greater plasma concentration of quercetin than coarse suspension. Moreover, the formulated nanosuspension exhibited enhanced antioxidant and antimicrobial potential and was non-toxic. Conclusions: Optimization of nanosuspension effectively improves the pharmaceutical potential and oral bioavailability of Allium cepa extract.
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Objective: To explore the effect of ethyl acetate gum resin extract of Boswellia serrata on lipopolysaccharide (LPS) induced inflammation and oxidative damage in hepatic and renal tissues of rats. Methods: The rats were divided into four groups: control, LPS, LPS+Boswellia serrata extracts (100 mg/kg and 200 mg/kg). LPS (1 mg/kg) and the extract (100 and 200 mg/kg, 30 min before LPS) were administered intraperitoneally for 3 weeks. The levels of liver enzymes, albumin, total protein, creatinine, blood urea nitrogen (BUN), interleukin (IL)-6, malondialdehyde (MDA), and total thiol groups and superoxide dismutase (SOD) and catalase (CAT) activities were measured. Results: The levels of liver enzymes, creatinine, and BUN, IL-6, MDA in the LPS group were markedly increased (P<0.001) while albumin, total protein, and total thiol concentration, as well as SOD and CAT activities, were decreased compared with the control group (P<0.05 or 0.01). Boswellia serrata extracts diminished the levels of liver enzymes, creatinine, BUN, IL-6, and MDA (P<0.01 and P<0.001), and elevated the concentration of total protein and total thiol and SOD and CAT activities (P<0.05 or 0.01). Conclusions: The ethyl acetate gum resin extract of Boswellia serrata reduces LPS-induced inflammatory reactions and oxidative damage, thus ameliorating hepatic and renal function.
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Objective: To investigate the antioxidative and antidiabetic effects of Harpephyllum caffrum bark infusion as well as its effects on glucogenic and nucleotide hydrolyzing enzyme activities in FeSO 4 - induced oxidative stress in rat hepatic tissue. Methods: Harpephyllum caffrum infusion was prepared from dried plant materials (40 g) infused in boiling water (400 mL) for 20 min at room temperature. The antioxidative and inhibitory activities against carbohydrate digestive enzymes of the infusion were determined using established protocols. The liver tissues of rats were used for glucose uptake assay and to evaluate the infusion's effect on endogenous antioxidant, glucogenic, and nucleotide hydrolyzing enzyme activities in FeSO 4 -induced hepatic injury. Results: The Harpephyllum caffrum infusion significantly reduced ferric iron (FRAP) and free radicals (OH • and DPPH) in a dose- dependent manner. It inhibited -amylase and -glucosidase activities and increased glucose uptake in hepatic tissues. FeSO 4 significantly decreased glutathione concentration, catalase, and superoxide dismutase activities while increasing malondialdehyde level, glycogen phosphorylase, fructose-1,6-bisphosphatase, and adenosine triphosphatase activities. However, treatment with Harpephyllum caffrum infusion reversed FeSO 4 -induced changes. Characterization of the infusion revealed the presence of catechol, O-pyrocatechuic acid, mequinol, maltol, and glycoside derivatives. Conclusions: The Harpephyllum caffrum infusion demonstrates antidiabetic and antioxidative potentials in in vitro models of type 2 diabetes as depicted by its ability to inhibit carbohydrate digestive enzymes, mitigate oxidative imbalance, and regulate glucogenic and nucleotide hydrolyzing enzyme activities in oxidative hepatic injury.
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MicroRNAs (miRNAs), small non-coding RNAs, play important roles in regulating host defense against pathogenic infections. This review provides information on the role of miRNAs in the antimycobacterial immune response and summarizes their possible diagnostic utility. It was compiled using scientific literature retrieved from such databases as PubMed, Scopus, ScienceDirect, Google Scholar, and PubMed Central. Relevant articles published in the English language until December 2020 were taken into consideration. It has been revealed that specific host miRNAs induced by Mycobacterium tuberculosis can target diverse factors and pathways in immune signaling to ensure longer pathogen survival inside the phagocytes. The potential use of miRNAs in tuberculosis diagnosis or therapeutic strategies has been attracting increasing attention in recent years. However, despite considerable efforts devoted to miRNA profiling, further studies are needed to elucidate the full potential of miRNAs as novel tuberculosis biomarkers or therapeutic targets.
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Objective: To elucidate the cytotoxic effect of the secondary metabolites of Barrientosiimonas humi (B. humi) on MCF-7 and MDA-MB-231 human breast cancer cells and its underlying mechanisms of action. Methods: The extract was obtained from the fermentation of B. humi and fractionation of the crude extract was conducted via column chromatography. Cytotoxicity of the B. humi extract was determined by using MTT assay and real-time cellular analysis. Morphological changes, cell cycle profiles, mode of cell death, and caspase expressions of control and treated breast cancer cells were determined. Results: The ethyl acetate extract isolated from B. humi was cytotoxic against MCF-7 and MDA-MB-231 cell lines. One of the dichloromethane (DCM) fractions, designated as DCM-F2, exhibited the strongest activity among all the fractions and thereby was selected for further studies. DCM-F2 had selective cytotoxicity on target cells by inducing apoptosis, particularly in the early stage, and cell cycle arrest. Treated cells caused inhibition of cell cycle progression at 72 h leading to a significant increase (P < 0.05) in the G0/G1 population. DCM-F2 treated MDA-MB-231 cells showed caspase-dependent apoptosis, whereas DCM-F2 treated MCF-7 cells showed a caspase-independent apoptosis pathway. Five compounds were successfully isolated from B. humi. Cyclo (Pro-Tyr) was the most cytotoxic and selective compound against MCF-7 cells. Conclusions: B. humi ethyl acetate extract exhibits significant cytotoxicity against MCF-7 and MDA-MB-231 cells via induction of apoptosis and cell cycle arrest.
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Objective: To explore the protective role of Glinus lotoides ethanolic extract in a depression model through modulating oxidant/antioxidant enzyme system and inflammatory status. Methods: Phytochemical constituents of Glinus lotoides ethanolic extract were evaluated qualitatively and quantitatively along with HPLC. Rats were divided into six groups. The normal control and the intoxicated groups received normal saline, and the standard group received imipramine, while the remaining groups received 100, 300, and 500 mg/kg Glinus lotoides ethanolic extract. All groups received treatments for 14 d. Lipopolysaccharides (LPS) were then administered i.p. (0.83 mg/kg) to all groups except the normal control group. After 24 h, anxiety and depression-like behaviors were evaluated by performing behavioral analysis (open field, tail suspension, forced swim, sucrose preference test), and determining total oxidant status, total antioxidant capacity, catalase, and biochemical parameters [malondialdehyde, glutathione, superoxide dismutase, tumor necrosis factor (TNF)-alpha and interleukin (IL)-6]. Results: Phytochemical studies confirmed the presence of phenols and flavonoids and HPLC analysis showed the presence of gallic acid, quercetin, chlorogenic, and caffeic acid. Total oxidant status was significantly decreased, while total antioxidant capacity was significantly increased in the Glinus lotoides ethanolic extract treated groups. Moreover, Glinus lotoides ethanolic extract diminished malondialdehyde, IL-6, and TNF-alpha levels, while increasing superoxide dismutase, catalase, and glutathione activities. Conclusions: Glinus lotoides ethanolic crude extract shows significant antidepressant activity by modulating oxidative and biochemical parameters that supports its folkloric use in traditional systems of medicine.
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Objective: To assess the anti-tumor effects of Pistacia atlantica methanolic extract (PAME) compared with cyclophosphamide against Ehrlich solid tumors in mice. Methods: Swiss albino mice (n=40) were divided into five groups: normal control mice, mice with Ehrlich solid tumors treated with normal saline, mice with Ehrlich solid tumors treated with cyclophosphamide intraperitoneally once a day for 14 d, or 50 mg/kg or 100 mg/kg PAME orally once a day for 14 d. Tumor growth inhibition, body weight, tumor markers, liver and kidney enzymes, oxidative stress markers, antioxidant enzymes, tumor necrosis factor-alpha level (TNF-α), and apoptosis-regulatory gene expression were evaluated. Results: Treatment of mice bearing Ehrlich solid tumors with PAME at 50 and 100 mg/kg orally significantly decreased tumor volume, body weight, tumor markers, liver and kidney enzymes, oxidative stress markers and TNF-α level in comparison with mice with Ehrlich solid tumors receiving normal saline. whereas PAME at 50 and 100 mg/kg/day significantly elevated the level of antioxidant enzymes (P<0.05). Conclusions: Pistacia atlantica methanolic extract has potent antitumor activity in mice. Therefore, the extract might be considered as an alternative anticancer agent against tumors, however, additional studies especially in the clinical setting are required to confirm this finding.
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In recent years, the oceans have provided an important source of highly promising new anti-tumor drugs for innovation and screening, with approximately 56% of biologically active compounds being discovered to have anti-tumor effects each year. In this study, we classified and summarized the approved drugs of marine origin in terms of anti-tumor therapy, and firstly, we briefly overviewed the role of the immune system in cancer pathogenesis and discussed the current dilemma of cancer immunotherapy and highlighted the main anti-tumor targets of marine drugs. Further, with a focus on tumor immunity, we classified and outlined the history of currently approved marine original drugs by species origin, structural features, relevant pathways, and clinical application and therapy. Lastly, the limitations of current marine drug research were discussed, as well as prospects and trends in new drug development.
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Algae are a large group of photosynthetic organisms responsible for approximately half of the earth's total photosynthesis. In addition to their fundamental ecological roles as oxygen producers and as the food base for almost all aquatic life, algae are also a rich source of bioactive natural products, including several clinical drugs. Cytochrome P450 enzymes (P450s) are a superfamily of biocatalysts that are extensively involved in natural product biosynthesis by mediating various types of reactions. In the post-genome era, a growing number of P450 genes have been discovered from algae, indicating their important roles in algal life-cycle. However, the functional studies of algal P450s remain limited. Benefitting from the recent technical advances in algae cultivation and genetic manipulation, the researches on P450s in algal natural product biosynthesis have been approaching to a new stage. Moreover, some photoautotrophic algae have been developed into "photo-bioreactors" for heterologous P450s to produce high-value added pharmaceuticals and chemicals in a carbon-neutral or carbon-negative manner. Here, we comprehensively review these advances of P450 studies in algae from 2000 to 2021.
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Triterpenoid saponins are widely used in medicine, health cares, cosmetics, food additives and agriculture because of their unique chemical properties and rich pharmacological activities. UDP-dependent glycosyltransferases (UGTs) are the key enzymes involved in triterpenoid saponin biosynthesis, and play important roles in the diversity of triterpenoid saponin structures and pharmacological activities. This review summarized the UGTs involved in plant triterpenoid saponin biosynthesis based on the sources of UGTs and the types of receptors. Moreover, the application of UGTs in heterologous biosynthesis of triterpenoid saponins based on synthetic biology was also discussed.
Subject(s)
Glycosyltransferases/genetics , Plants , Saponins/chemistry , TriterpenesABSTRACT
Abatsract Pseudomonas aeruginosa is an important nosocomial pathogen and its clinical importance is mainly related to nosocomial infections. Increased rates of bacterial resistance in recent years has led WHO to publish a global priority list to guide research and discovery of new antibiotics, where P. aeruginosa is among the group of bacteria for which there is a critical level of priority for new drugs to be discovered. In this context, isoeugenol appears as an interesting alternative and the objective of this study was to investigate its action against P. aeruginosa. Isoeugenol presented significant antibacterial activity, with minimum inhibitory concentration (MIC) of 64µg/mL and minimum bactericidal concentration (MBC) of 128µg/mL, and was considered bactericidal against this species. Molecular docking revealed interactions that suggest that isoeugenol may bind to the enzyme Penicillin-Binding Protein 3 and interfere with the bacterial cell wall synthesis process. This study reinforces the antibacterial potential of this compound and emphasizes that more studies are needed in order to better investigate its mechanism of antibacterial action.