Natural Products Journal, The - Online First
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Mechanistic Overview on Therapeutic Potential of Phenols Targeting the Breast Cancer: Molecular Insights and Future Road to Drug Design
Available online: 04 February 2025More LessBreast cancer is the most common malignancy globally. It is associated with genetic and lifestyle risk factors. Many chemotherapeutic agents are currently available for breast cancer. Despite their moderate efficacy in breast cancer therapy, many of these chemotherapeutic agents are associated with adverse effects. A few patients also have the possibility of developing resistance to these drugs over time. The resistance to these chemotherapeutic agents illustrates the necessity to seek novel therapeutic strategies. Phenols are a class of plant-derived compounds that have an aromatic ring with at least one hydroxyl group. They are well known for their antioxidant, anti-inflammatory, and anti-proliferative effects. A diet rich in fruits and vegetables has a high content of polyphenols. Various in vitro and in vivo studies in the past two decades have demonstrated the therapeutic potential of phenol in breast cancer. Each of these polyphenol compounds has promising potential to modulate breast cancer in various stages, including proliferation, angiogenesis, invasion, and metastasis. This review focuses on the various in vitro and in vivo studies done in both phenolic compounds and phenolic extracts and the efficacy of phenols in modulating breast carcinogenesis by various mechanisms. The potential of phenols to inhibit various oncogenes and tumor-associated proteins is also discussed. The ability of polyphenols to sensitize hormone-resistant and chemoresistant breast cancer cell lines to various chemotherapeutic agents has also been highlighted.
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Therapeutic Applications of Oxalate-degrading Bacteria in Kidney Stone Prevention
Available online: 03 February 2025More LessUrolithiasis is a condition where kidney stones exit through the renal pelvis, causing chronic pain. Kidney stones are usually formed due to the deposition of calcium and oxalate crystals. It is known to be a prevalent health condition that affects a large portion of the global human population. Inopportunely, no medications that show effective prevention of urolithiasis are currently available. Extensive research has highlighted the significant role of commensal microbes in regulating host oxalate homeostasis and oxalate-associated pathological conditions. However, limited knowledge of the pathophysiology of urolithiasis poses difficulties in designing target-based therapeutics. Growing evidence suggests the role of gut microbiota and probiotics in helping reduce the disease burden. Understanding the intricate relationship between gut-associated microbiota and its host symbiosis reveals the therapeutic potential of specific bacteria to prevent and/or treat such metabolic diseases. Oxalobacter formigenes, a bacterium, is considered crucial for degrading dietary oxalates through the oxalyl-CoA decarboxylase enzyme. The absence of this enzyme leads to hyperoxaluria and calcium oxalate urolithiasis, underscoring the impact of microbiota on kidney stone formation. Studies on the urinary microbiome, including those focusing on Oxalobacter formigenes, Lactobacillus, Bifidobacterium, Eubacterium lentum, Enterococcus faecalis, and Escherichia coli, elucidate the metabolism of dietary oxalates, providing a novel approach to kidney stone management. This review aims to consolidate the present information on the urinary microbiome, aetiology, pathogenesis, and disease prevention.
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Natural Products: A Promising Avenue for Aquaporin-targeted Drug Discovery
Available online: 30 January 2025More LessAquaporins are one of the important but challenging targets in drug discovery. They are of great interest owing to their diverse physiological roles in health and diseases and their broad tissue distribution. However, there has been little progress so far in this quest and some have started to doubt whether AQPs are druggable at all. Essential challenges in AQP drug development seem to be difficult in modeling selective inhibitors and a lack of robust and reliable in vitro and in vivo assays. Numerous studies report natural products modulating AQPs at the expression level, directly inhibiting AQPs and disturbing their interaction with other intracellular proteins. Since direct targeting of AQPs has not yielded promising results, using natural products as AQP modulators could be a new possibility.
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Potential Plant-based Remedies for Gouty Arthritis: A Comprehensive Review on Counterweighing the Inflammatory Pathways
Authors: Rupama Thakuria, Purbajit Chetia and Abu Saif MustaqueAvailable online: 24 January 2025More LessThe complex etiology of Gouty Arthritis (GA) makes it a multidimensional illness for which there are now no effective therapeutic therapies that can stop its development entirely. This review examines how effectively different plants and their constituents reduce blood uric acid levels and lessen the predisposition to gout. Research has looked at the possible roles of oxidative stress markers, inflammatory pathways, important transport and signaling proteins, and the health benefits of different plants and their components in the development of GA. Plant remedies have been used for a long time to treat human and animal ailments. Most people in developing countries use traditional plant-based medicine for basic care due to its affordability, availability, and cultural acceptability. This review aims to gather comprehensive information on plants and their compounds that exhibit anti-gout activities, focusing on in vitro and in vivo investigations. The scientific database was searched by using different keywords, and papers published between March 2008 and December 2023 were considered. The inclusion criteria were publications on inflammatory mediators, free radicals, oxidative stress, or proteins in gout etiology or evolution, along with plant-based remedies. Finally, 27 publications based on inclusion and exclusion criteria reported the active compounds and analyzed parameters and outcomes of research carried out with these medicinal plants. This paper extensively explores the potential mechanism of employing medicinal herbs for the management of gout. However, more investigation is needed to fully comprehend the role that various biomarkers play in the development of GA, as well as to investigate the possible functions of different plants and the substances found in them.
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Medicinal Benefits of Frankincense: Future Approach to Effective Drug Design
Available online: 21 January 2025More LessFrankincense is obtained from the tree, which belongs to the Bowellia family. Frankincense is found in China, India, Middle-East Asia, the Arabian Peninsula, and different parts of Africa. Incisions are given on the tree trunk to obtain the gum, which hardens to form frankincense. It has been used as a traditional medicine to treat diarrhea, infection, tuberculosis, asthma, arthritis, cancer, wounds, gingivitis, psoriasis, and other inflammatory conditions. Frankincense gum is used for its aromatic properties and fragrance. Frankincense contains essential oils, gum resins, alcohol, and water-soluble resins. The chemical compounds present in the natural product and their yield depend on various factors such as geographical location, the surface area of the wood, climatic conditions in which it is grown, the age of the tree, and the methods of collection. Among the active compounds, unique pentacyclic triterpene acids such as boswellic acid (BA) are present. The phytochemicals include β-boswellic acid, acetyl-β-boswellic acid (ABA), 11-keto-β-boswellic acid (KBA), and 3-acetyl-11-keto-β-boswellic acid (AKBA) form the major components. BA possesses anti-inflammatory action due to its control of cytokine production. The active compounds in frankincense act on 5-lipooxygenase and cyclooxygenase, thereby producing an anti-inflammatory effect. We discuss the role of frankincense on the integumentary, nervous, cardiovascular, respiratory, digestive, endocrine, musculoskeletal, and immune systems with special emphasis on the molecular basis of action and signaling pathways. Recent approaches in therapeutics by designing new nanoformulations of frankincense may be beneficial for better drug delivery to the desired site, help in controlled release, increase solubility and bioavailability, and reduce toxicity.
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Green Tea's EGCG: Brewing Hope in the Battle against Breast Cancer
Authors: Manoj Kumar, Roop Lal, Amit Sehgal, Suman Rawat, Ankit Kumar, Santosh Kumar and Sunil Kumar DhatwaliaAvailable online: 21 January 2025More LessBreast cancer, a pervasive global malignancy, is anticipated to undergo a significant increase by 2040. Despite the conventional armamentarium of treatments including chemotherapy, radiation therapy, and surgery, the intricate landscape of breast cancer, characterized by its multifaceted surface receptors and signalling pathways, presents formidable challenges to treatment efficacy. Epigallocatechin-3-gallate (EGCG), extracted from Camellia sinensis, has emerged as a subject of interest due to its robust antioxidative properties stemming from its chemical structure. EGCG exerts its effects on pivotal stages of tumour growth and proliferation by modulating key signalling pathways such as MAPK, PI3K, NFkB, and ERK1/2 influencing apoptosis and cell cycle regulation. Clinical trials have provided insights into EGCG's potential impact on breast cancer such as mammographic density and pharmacokinetics, indicating its potential as a potent therapeutic agent. Moreover, when administered with conventional chemotherapy, EGCG demonstrates synergistic effects, enhancing therapeutic outcomes. Nevertheless, further research is warranted to validate the safety and efficacy of EGCG in breast cancer prevention and treatment.
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Inflammation and Cancer Development: Basic Mechanisms and Evidence of its Regulation by Hibiscus sabdariffa Natural Extracts
Available online: 21 January 2025More LessBackgroundHibiscus sabdariffa is a plant used in traditional medicine for intestinal treatments and nowadays for critical diseases like hypertension, diabetes, and cancer. Multidisciplinary approaches have demonstrated, through Hibiscus sabdariffa extracts, anti-inflammation and anti-cancer beneficial properties from compounds like phenols, flavonoids, and anthocyanins that are ubiquitously distributed in whole plants.
ObjectiveThe objective of this study is to identify the bioactive compounds and their underlying mechanisms of action that drive the anti-cancer and anti-inflammatory properties of Hibiscus sabdariffa extracts.
MethodsWe searched databases for publications in English from all years that reported beneficial anti-inflammation and anti-cancer properties from Hibiscus sabdariffa extracts and their proposed mechanism of action. We used Pubmed, Google Scholar, Scopus, and ScienceDirect for original articles that included different Hibiscus sabdariffa extracts evaluated for their anti-inflammation, and anti-cancer properties, using the following search terms: “H. sabdariffa”, “H. sabdariffa extracts”, “H. sabdariffa and inflammation”, and “H. sabdariffa and cancer”. Some articles from the reference list were used to collect additional information, and we used 73 articles in total.
ResultsIn general, extracts from Hibiscus sabdariffa are obtained by different methods that affect the final concentration of the compounds. Several in vivo and in vitro experiments show their anti-inflammatory and anti-cancer properties.
ConclusionHibiscus sabdariffa extracts have the potential bioactivity to modulate inflammation and cancer in several cellular and molecular mechanisms of action involving the downregulation of key signaling pathways such as NFκB, MAPK, BCL-2, p53, among others, and the upregulation of protective pathways such as Nrf2. However, research needs to be further evaluated on the exact compounds that have this effect, in order to know if the extracts work individually or synergistically.
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Qualitative and Structural Insights into Levantilides C/D via LC-MS
Authors: Wei Zhao, Jian Zhou, Nan-Nan Chen, Jingming Zhou, Hong Jiang and Bin WuAvailable online: 20 January 2025More LessIn this study, we utilized high-performance liquid chromatography coupled with quadrupole-time of flight mass spectrometry (HPLC-Q-TOF/MS/MS), combined with electrospray ionization in the positive mode (ESI+), to establish a comprehensive framework for chromatographic separation and mass spectrometric detection.
The primary focus was on performing collision-induced dissociation (CID) experiments on levantilide D, a newly identified macrolide, and its well-established analog, levantilide C, in order to elucidate their mass spectral fragmentation patterns.
The results revealed that the cleavage patterns of levantilides were successfully characterized when ionized in the positive mode. These fragmentation profiles provide valuable insights for the rapid and accurate structural identification and quantitative analysis of levantilides when they often occur in trace amounts.
Furthermore, this methodology offers crucial technical references for environmental pollutant monitoring and pharmacokinetic investigations for levantilide-related compounds.
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Recent Insights into the Potential Roles of Crocin and Safranal in Alleviating Skin Aging: A Mini-Review
Available online: 16 January 2025More LessResearch has been carried out regarding the benefits and influence of saffron and its derivatives on skin health. Crocin from Crocus sativus L., Gardenia jasminoides, and Nyctanthes arbor-tristis, and safranal from Crocus sativus L. might alleviate skin aging effects. This literature review discusses the mechanism of crocin and safranal as anti-inflammatory agents in reversing oxidative stress and improving aging effects on the skin. Based on the literature review, crocin and safranal have strong antioxidant capacity. The mechanism that allows crocin to reduce oxidative stress is by directly neutralizing reactive oxygen species in human dermal fibroblasts and modifying keratinocyte O-linked glycobiology in human keratinocytes. Crocin also increases skin thickness and protects against blue light stress; its derivative, crocetin, could act like melatonin. Meanwhile, safranal also has a potential mechanism for alleviating skin aging in the form of nanoparticles (liposome and solid nanoparticles) or pure safranal through inhibiting dermal enzymes that are involved in the process of skin aging, such as elastase, collagenase, and hyaluronidase.
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Vitiligo Treatment with Natural Bioactive: A Narrative Review
Authors: Sudhanshu Kumar Jha, Vaibhav Charde, Vijay Kumar and Ch. Venkata NarasimhajiAvailable online: 15 January 2025More LessThe lack of melanin-producing cells in the epidermis causes white patches to develop in vitiligo, a chronic skin disorder. Although vitiligo seldom causes physical injury, it can have serious psychological and social consequences, such as diminished self-confidence and feelings of inadequacy. While there is no known cure for vitiligo, there are several treatments that can help control the illness and lessen its impact on people's lives. In this review, we take a look at the literature on phytoconstituents and plant extracts as prospective therapeutic agents for vitiligo. Traditional medicine has a long history of using plant extracts for the treatment of many ailments, including skin diseases. The pharmacological effects of natural bioactive substances are diverse, including antioxidant, anti-inflammatory, and immunomodulatory capabilities. For this reason, they hold great promise as a vitiligo cure.
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A Comprehensive Review of Aloe vera: Composition, Properties, Processing, and Applications
Authors: Parul Sharma and Ramandeep KaurAvailable online: 15 January 2025More LessAloe vera, a drought-resistant succulent, is renowned for its wide-ranging medicinal properties. It has significant health benefits, including anticancer, wound and burn healing, hypoglycemic, gastroprotective, antifungal, and antiinflammatory properties. These properties have led to its use in various commercial applications, particularly in skincare, cosmetics, and medicinal products. Additionally, Aloe vera is increasingly employed as an edible coating for fruits and vegetables, providing a natural alternative to postharvest chemical treatments. This review highlights Aloe vera's diagnostic properties and diverse applications, focusing on its rich polysaccharides, enzymes, vitamins, and minerals composition. Advances in analytical chemistry are enhancing the chemical characterization of Aloe vera, promising more information and broader applications shortly. The study also explores the plant's processing into juice, concentrate, and powder forms, underscoring its extensive use in pharmaceuticals, cosmetics, and functional foods, particularly for its antioxidant and anti-inflammatory benefits.
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Improving Antioxidant Effect of Stemona tuberosa by Fermentation with Endophytic Fungus Penicillium expansum STRB13
Authors: Jian-Wei Dong, Xue-Jiao Li, Hui Zhao and Xue-Xian WangAvailable online: 13 January 2025More LessBackgroundStemona tuberosa Lour. is a plant belonging to the genus Stemona (Stemonaceae) that has been utilized in traditional Chinese medicine (TCM) for its antitussive and antiparasitic properties. Endophytic fungi have been shown to play an important role in the growth and metabolism of plants. Fermentation involving endophytic fungi tends to result in the production of new or more potent pharmacological compounds.
ObjectiveThe study aims to enhance the antioxidant activity of S. tuberosa by fermenting it with a symbiotic endophytic fungus.
MethodsSeven symbiotic endophytic fungi were used to screen and ferment S. tuberosa to improve antioxidant activity estimated by 2,2’-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity and ferric ion-reducing antioxidant power (FRAP). The chemical constituent changes were characterized by ultraviolet (UV) spectrum and high-performance liquid chromatography (HPLC) analysis.
ResultsPenicillium expansum STRB13, an endophytic fungus associated with S. tuberosa, was screened for its ability to enhance antioxidant capacity through fermentation. The fermentation of S. tuberosa using P. expansum STRB13 significantly improved its DPPH radical scavenging activity, achieving an IC50 value of 24.2 μg/mL. Additionally, the ferric reducing antioxidant power (FRAP) of the fermented sample was fourteen times greater, measuring 388.1 ± 32.6 μmol/L compared to 27.5 ± 1.0 μmol/L in the blank sample. Differences observed between the blank and P. expansum STRB13 fermented S. tuberosa (FST) in UV spectra and HPLC analysis indicated the production of new aromatic phenolic compounds through fermentation, which contributed to the enhanced antioxidant activity.
ConclusionThis is the first time reporting on the fermentation processing of S. tuberosa with symbiotic endophytic fungus. This study revealed that P. expansum STRB13 FST will be an alternative natural antioxidant. Fermentation with symbiotic endophytic fungus is a new approach to processing TCM and discovering new compounds.
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Deep Learning Approaches for Predicting Bioactivity of Natural Compounds
Authors: Parixit Prajapati, Princy Shrivastav, Jigna Prajapati and Bhupendra PrajapatiAvailable online: 10 January 2025More LessThe investigation of computational techniques to forecast the bioactivity of natural substances has been spurred by the growing interest in utilizing their medicinal potential. A branch of artificial intelligence called deep learning has been particularly useful for predicting outcomes in a variety of fields, such as bioactivity prediction and drug discovery, by evaluating large amounts of complex data. An overview of current developments in the application of deep learning techniques to the prediction of natural chemical bioactivity has been presented in this article. The advantages provided by deep learning approaches, such as convolutional neural networks (CNNs), recurrent neural networks (RNNs), and graph neural networks (GNNs), have been highlighted, and the difficulties connected with conventional methods of bioactivity prediction have been examined. Moreover, a variety of molecular representations—such as molecular fingerprints, graph representations, and molecular descriptors—that are fed into deep learning models have been studied. Additionally, included in this study is the integration of many data sources, including omics data, chemical structures, and biological tests, to enhance the precision and resilience of bioactivity prediction models. Furthermore, this review covers the uses of deep learning in target prediction, virtual screening, and poly-pharmacology study of natural substances. The paper concludes by discussing the field's present issues and potential paths forward, such as the requirement for standardized benchmark datasets, the interpretability of deep learning models, and the incorporation of experimental validation techniques. All things considered, this study sheds light on the most recent developments in deep learning techniques for estimating the bioactivity of natural substances and their possible effects on drug development and discovery.
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Lavender Oil: A Versatile Natural Therapeutic – Extraction, Composition, Applications, and Innovative Formulation Strategies
Authors: Farooque Shaikh, Manoj Harde and Rashmi MallyaAvailable online: 07 January 2025More LessThe present review comprehensively explores an overview of a versatile essential oil from genus Lavandula. Oil finds wide application in the aromatherapy and cosmetic industry. This paper emphasizes the chemical constituents of the oil that are responsible for the diverse therapeutic applications. Various extraction techniques, such as steam distillation, hydro distillation, supercritical liquid extraction and ultrasound assisted extraction are discussed. Also the article elucidates the mechanism of action that explains the therapeutic application of the oil in microbial infections, oxidative stress and neurodegenerative diseases. This review also extensively discusses the preclinical and clinical studies of the use of the oil for the management or treatment of psoriasis, depression, wound, anxiety, Alzheimer’s’ disease, myocardial infarction, acute lung injury and acute inflammation. Additionally, the article highlights granted patents and the novel formulation strategies such as hydrogels, nanofibers, emulsions and nanoparticles used to enhance the bioavailability and the targeted delivery of the oil. The review also provides future perspectives, emphasizing the need for further research for harnessing the potential of lavender oil.
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Recent Advances in the Chemistry of Herbal Drugs for the Management of Breast Cancer: An Update
Authors: Kriti Seksaria, Damini Patial, Aarzoo Aneja, Pinky Arora and Shubham KumarAvailable online: 06 January 2025More LessBreast cancer remains a significant health concern worldwide, prompting extensive research into alternative therapies, such as herbal medicine. This review paper will provide insight into the potential of four herbal remedies, namely Thymus vulgaris (thyme), Hibiscus, Artemisia annua (sweet wormwood), and Moringa oleifera, in the management of breast cancer. Thymus vulgaris exhibits anti-cancer properties through its bioactive compounds, including thymol and carvacrol, which demonstrate cytotoxic effects against breast cancer cells. Hibiscus extracts have been shown to inhibit breast cancer cell proliferation, induce apoptosis, and suppress tumor growth by targeting various molecular pathways. Artemisia annua, particularly its active component artemisinin, exhibits promising anti-cancer effects through the induction of apoptosis, inhibition of angiogenesis, and modulation of cell cycle progression in breast cancer cells. Additionally, Moringa oleifera, rich in bioactive compounds like quercetin and kaempferol, exhibits anti-cancer properties by inhibiting cell proliferation, inducing apoptosis, and suppressing metastasis in breast cancer. These herbal remedies offer potential avenues for further investigation as adjunct therapies or standalone treatments for breast cancer management. However, rigorous clinical trials are warranted to elucidate their efficacy, safety profiles, and optimal dosages for clinical use.
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Recent Advances in the Microbial Oxidation and Ring Rearrangement of Terpenoidal Compounds by Aspergillus niger
Authors: Mohammad Yasin Mohammad and M. Iqbal ChoudharyAvailable online: 24 December 2024More LessIn this review, recent advances in the microbial oxidation and ring rearrangement of various terpenoidal compounds by Aspergillus niger are reviewed. Studies on hydroxylation, acid and keto formations, Baeyer-Villiger oxidation, and ring rearrangements are also explored. Moreover, various terpenoidal compound substrates and their metabolites used for fungal biotransformations are compiled. This review attempts to cover the latest developments in the scientific literature from 2018 to 2023.
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Harzianolides H-J: Three New Butenolides Isolated from the Fungus Trichoderma harzianum
Authors: Chengzeng Zhou, Yichao Ge and Bin WuAvailable online: 16 December 2024More LessBackgroundMarine fungi have been recognized as new sources for the discovery of valuable secondary metabolites, providing lead compounds for drug discovery and development.
ObjectiveThe objective of this study was to isolate and identify the secondary metabolites from the marine-derived fungus Trichoderma harzianum ZN-4 and evaluate their antifungal activity.
MethodFungus strain Trichoderma harzianum ZN-4 was initially fermentated using a PDB liquid medium. Subsequently, extensive chromatographic methods were applied to isolate the fermentation cultures of ZN-4, and the chemical structures of isolate compounds were elucidated by 1D and 2D NMR, ECD, and HRESIMS. The antifungal activity was evaluated using the broth microdilution method.
ResultThree new butenolides, harzianolides H–J (1–3), were isolated from T. harzianum ZN-4, and cultivated on a sterilized PDB medium. Activity evaluation showed that compounds 1−3 exhibited potent antifungal activity with MIC values of 12.5−100 μg/mL against the phytopathogenic fungus Pestalotiopsis theae.
ConclusionThis study not only enriched the structural diversity of the harzianolide family but also revealed their anti-P. theae activity, which may be potential antifungal agents.
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A Comprehensive Review on the Chinese Herbal Medicine Quzhiqiao
Authors: Lixia Wang, Jiayu Pan, Jianfeng Song, Xingliang Yang, Bo Yang, Lihua Mao and Yihan MaAvailable online: 06 December 2024More LessQuzhiqiao is a Chinese herbal medicine widely used in Zhejiang Province of China, which originates from the cultivar Citrus aurantiun ‘Changshanhuyou’, named Changshanhuyou in Chinese. Citrus aurantiun ‘Changshanhuyou’ is a botanical variety of C. aurantium L., which is obtained after long-term domestication. It belongs to the Rutaceae family and mainly grows in Changshan County, Zhejiang Province, China. Quzhiqiao is an authentic Chinese medicinal material in the Zhejiang area with various pharmacological and curative effects. A comprehensive review and in-depth analysis of scientific literature on Quzhiqiao was conducted, utilizing diverse electronic databases and additional sources. This review provides a comprehensive overview of its chemical components, standardized quality control, pharmacological activity, and mechanism of action, which also outlines future perspectives, highlighting the necessity for further research for harnessing the potential of the therapeutic use of Quzhiqiao.
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Antimicrobial Macrolide Levantilide D from Rare Marine Micromonospora sp.
Authors: Wei Zhao, Jian Zhou, Honglei Jiang, Yichao Ge, Jingming Zhou, Meilu Zhao, Ru Lin, Hong Jiang and Bin WuAvailable online: 10 October 2024More LessIntroductionOne new levantilide D (2) with a 20-membered macrolide, along with one known levantilide C (1), was isolated from a rare marine actinomycetes Micromonospora sp. (FIMYZ52).
MethodThe structural elucidation of the compounds was based on integrated analyses involving 1D and 2D NMR spectroscopy and HR-ESI-MS.
ResultThe relative and absolute configurations of compounds 1 and 2 were ascertained by integrating multispectral ROESY and NOESY information from analogs in conjunction with theoretical TDDFT-ECD calculations. Levantilide D (2) exhibited antibacterial activity against Staphylococcus aureus.
ConclusionA plausible biosynthetic pathway of the macrolide compounds (1-2) was proposed.
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