Natural Product
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Belinda E. Hetzler ◽  
Dirk Trauner ◽  
Andrew L. Lawrence

Zewen Wen ◽  
Yuxi Zhao ◽  
Zhengyang Gong ◽  
Yuanyuan Tang ◽  
Yanpeng Xiong ◽  

The increasing emergence of infectious diseases associated with multidrug-resistant Gram-positive pathogens has raised the urgent need to develop novel antibiotics. GA (15:1) is a natural product derived from Ginkgo biloba and possesses a wide range of bioactivities, including antimicrobial activity.

2022 ◽  
Vol 18 ◽  
Meenu Aggarwal ◽  
Raman Singh ◽  
Priyanka Ahlawat ◽  
Kuldeep Singh

Abstract: Natural products have stimulated chemists owing to their abundant structural diversity and complexity. Indeed, natural products have performed an essential role, particularly in the cure of cancerous and infectious diseases, thereby posing medicinal researchers with a scope of unexplored chemotypes for the innovation of new drugs. Fusion of chemical derivatization and combinatorial synthesis forms the basis of the concept of chemo diversification of plants. Diverse libraries of natural product analogs are constructed through existing biological and chemical approaches using unique schemes to expand natural product frameworks. This review aims to present several approaches employed to offer innovative opportunities to synthesize NP-inspired compound libraries. Reactive molecular fragments present in most natural products are chemically converted to chemically engineered extracts (CEEs) or semisynthetic compounds constituting distinct libraries. Bio-guided isolation for natural products required vital tools like reverse phase chromatography and bioautographic assays. Different established strategies from DTS, BIOS, CtD, FOS, FBDD to Late-stage diversification facilitate the expansion of molecules with physicochemical properties. In particular, fragment-like natural products with novel skeletons may be used as preliminary points for chemical biology and medicinal chemistry programs with great capacity. In this review, we sum up how NPs have proven fruitful for the novel methodologies responsible for the diversification of complex natural products; thereby, it is worthy of going over the upcoming integration of natural products with combinatorial chemistry.

2022 ◽  
Vol 19 ◽  
Min Wu ◽  
Lijia Xu ◽  
Mingwei, Song ◽  
Ying, Li ◽  
Yingying Wang ◽  

Abstract: The first total synthesis of the natural product iopsoralenoside, isolated from the n-butyl alcohol extract of Fructus Psoraleae (FP), was achieved in 17% yield over 7 steps. The key steps of the process are the glycosylation and irradiation promoted by ultraviolet light. This synthesis provides a sufficient amount of synthesized trans- and cis-isopsoralenoside for further bioassays.

2022 ◽  
Vol 2022 ◽  
pp. 1-11
Zhe Li ◽  
Tingting Zhao ◽  
Jiaxin Li ◽  
Qingying Yu ◽  
Yu Feng ◽  

Natural products have antitumor, anti-inflammatory, antioxidant, and other pharmacological activities and are an important source of drugs for prevention and treatment of various diseases. However, the inherent defects of natural products in physiological media such as poor solubility and stability and short biological half-life limit their clinical application. In recent years, more and more attention has been paid to the science of drug delivery by nanoscale materials. A large number of in vitro and in vivo studies have further confirmed the efficacy and safety of nanomedicine based on natural products in preclinical models of various diseases. In this review, we summarized the achievements of nanomaterials in improving the efficacy of natural products, introduced the research progress in several key fields of natural product-based nanomedicine in medical application, and discussed the challenges and prospects of clinical transformation of nanomedicine.

Crystals ◽  
2022 ◽  
Vol 12 (1) ◽  
pp. 87
Magdalena Mititelu ◽  
Denisa Ioana Udeanu ◽  
Mirela Nedelescu ◽  
Sorinel Marius Neacsu ◽  
Anca Cecilia Nicoara ◽  

Honey is a natural product recognized and appreciated for its nutritional value and therapeutic potential. However, the quality of bee honey is essential because various contaminants can seriously affect consumers’ health. In the experimental part of the work, we analyzed different types of honey (linden, black locust, rapeseed and multifloral honey) and propolis, which were collected from Romanian accredited beekeepers who placed beehives in two areas characterized by different industrial activity: area 1 (A1) is an area with intense industrial activity, with other industries existing nearby, including a refinery, while area 2 (A2) is entirely devoid of industrial activity, but with moderate agricultural activity. A total of 144 samples were collected, twelve samples for each variety of honey, propolis and soil, corresponding to each area analyzed. In addition, seven heavy metals and three pesticides were tested for in the samples collected. Finally, the correlation between the degree of contamination with soil pollutants and the contamination of the bee products harvested from the analyzed areas was studied. Cadmium, lead, copper, zinc and the sum of DDT metabolites exceeded the maximum allowable levels in honey samples, with differences between different types of honey.

Molecules ◽  
2022 ◽  
Vol 27 (2) ◽  
pp. 349
Asim Najmi ◽  
Sadique A. Javed ◽  
Mohammed Al Bratty ◽  
Hassan A. Alhazmi

Natural products represents an important source of new lead compounds in drug discovery research. Several drugs currently used as therapeutic agents have been developed from natural sources; plant sources are specifically important. In the past few decades, pharmaceutical companies demonstrated insignificant attention towards natural product drug discovery, mainly due to its intrinsic complexity. Recently, technological advancements greatly helped to address the challenges and resulted in the revived scientific interest in drug discovery from natural sources. This review provides a comprehensive overview of various approaches used in the selection, authentication, extraction/isolation, biological screening, and analogue development through the application of modern drug-development principles of plant-based natural products. Main focus is given to the bioactivity-guided fractionation approach along with associated challenges and major advancements. A brief outline of historical development in natural product drug discovery and a snapshot of the prominent natural drugs developed in the last few decades are also presented. The researcher’s opinions indicated that an integrated interdisciplinary approach utilizing technological advances is necessary for the successful development of natural products. These involve the application of efficient selection method, well-designed extraction/isolation procedure, advanced structure elucidation techniques, and bioassays with a high-throughput capacity to establish druggability and patentability of phyto-compounds. A number of modern approaches including molecular modeling, virtual screening, natural product library, and database mining are being used for improving natural product drug discovery research. Renewed scientific interest and recent research trends in natural product drug discovery clearly indicated that natural products will play important role in the future development of new therapeutic drugs and it is also anticipated that efficient application of new approaches will further improve the drug discovery campaign.

2022 ◽  
Jonathan Keim ◽  
Andrew Cummins ◽  
Scott Snyder

In contrast to the tremendous power of Pd-based Mizoroki–Heck reactions, methods to achieve such processes with other metals, particularly Ni, are generally lacking. Herein, we delineate specific conditions that can enable cascade variants of these C–C bond forming events to proceed smoothly under Ni catalysis. Critically, these reactions work with equal facility as their Pd-initiated counterparts when conducted intramolecularly, and in many cases are devoid of any Ni–H-mediated alkene isomerization within the starting materials and/or products as has typically been observed with previous Ni-based protocols. When conducted intermolecularly, the developed variant affords unique regioselectivity in product formation, substantively favoring 6-endo additions over the more standard 5-exo counterparts observed under Pd-based conditions. Finally, applications of the developed procedures to two different natural product syntheses are described

Gut Pathogens ◽  
2022 ◽  
Vol 14 (1) ◽  
Madita Brauer ◽  
Jennifer Herrmann ◽  
Daniela Zühlke ◽  
Rolf Müller ◽  
Katharina Riedel ◽  

AbstractThe anaerobic, gastrointestinal pathogen Clostridioides difficile can cause severe forms of enterocolitis which is mainly mediated by the toxins it produces. The RNA polymerase inhibitor Fidaxomicin is the current gold standard for the therapy of C. difficile infections due to several beneficial features including its ability to suppress toxin synthesis in C. difficile. In contrast to the Rifamycins, Fidaxomicin binds to the RNA polymerase switch region, which is also the binding site for Myxopyronin B. Here, serial broth dilution assays were performed to test the susceptibility of C. difficile and other anaerobes to Myxopyronin B, proving that the natural product is considerably active against C. difficile and that there is no cross-resistance between Fidaxomicin and Myxopyronin B in a Fidaxomicin-resistant C. difficile strain. Moreover, mass spectrometry analysis indicated that Myxopyronin B is able to suppress early phase toxin synthesis in C. difficile to the same degree as Fidaxomicin. Conclusively, Myxopyronin B is proposed as a new lead structure for the design of novel antibiotics for the therapy of C. difficile infections.

Marine Drugs ◽  
2022 ◽  
Vol 20 (1) ◽  
pp. 52
Sam Afoullouss ◽  
Anthony R. Sanchez ◽  
Laurence K. Jennings ◽  
Younghoon Kee ◽  
A. Louise Allcock ◽  

Sponges are at the forefront of marine natural product research. In the deep sea, extreme conditions have driven secondary metabolite pathway evolution such that we might expect deep-sea sponges to yield a broad range of unique natural products. Here, we investigate the chemodiversity of a deep-sea tetractinellid sponge, Characella pachastrelloides, collected from ~800 m depth in Irish waters. First, we analyzed the MS/MS data obtained from fractions of this sponge on the GNPS public online platform to guide our exploration of its chemodiversity. Novel glycolipopeptides named characellides were previously isolated from the sponge and herein cyanocobalamin, a manufactured form of vitamin B12, not previously found in nature, was isolated in a large amount. We also identified several poecillastrins from the molecular network, a class of polyketide known to exhibit cytotoxicity. Light sensitivity prevented the isolation and characterization of these polyketides, but their presence was confirmed by characteristic NMR and MS signals. Finally, we isolated the new betaine 6-methylhercynine, which contains a unique methylation at C-2 of the imidazole ring. This compound showed potent cytotoxicity towards against HeLa (cervical cancer) cells.

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