Spirocyclic motifs are emerging privileged structures for drug discovery. They are also omnipresent in the natural products domain. However, until today, no attempt to analyze the structural diversity of various spirocyclic motifs occurring in natural products and their relative populations with unique compounds reported in the literature has been undertaken. This review aims to fill that void and analyze the diversity of structurally unique natural products containing spirocyclic moieties of various sizes.

Spirocyclic Motifs in Natural Products

Gelsemium elegans Benth (GEB), also known as heartbreak grass, is a highly poisonous plant belonging to the family Loganiaceae and genus Gelsemium that has broad application prospects in medicine. This article reviews its chemical components, pharmacological effects, toxicity mechanisms, and research progress in clinical applications in recent years. Indole alkaloids are the main active components of GEB and have a variety of pharmacological and biological functions. They have anti-tumor, anti-inflammatory, analgesic, and immunomodulation properties, with the therapeutic dose being close to the toxic dose. Application of small-dose indole alkaloids fails to work effectively, while high-dose usage is prone to poisoning, aggravating the patient’s conditions. Special caution is needed, especially to observe the changes in the disease condition of the patients in clinical practice. In-depth research on the chemical components and mechanisms of GEB is essential to the development of promising lead compounds and lays the foundation for extensive clinical application and safe usage of GEB in the future.

Gelsemium elegans Benth: Chemical Components, Pharmacological Effects, and Toxicity Mechanisms

Asymmetric [4 + 3] Annulations for Constructing Divergent Oxepane Frameworks via Cooperative Tertiary Amine/Transition Metal Catalysis.

Abstract Monoterpenoid indole alkaloids (MIAs) represent a major class of active ingredients from the plants of the genus Gelsemium. Gelsemium MIAs with diverse chemical structures can be divided into six categories: gelsedine-, gelsemine-, humantenine-, koumine-, sarpagine- and yohimbane-type. Additionally, gelsemium MIAs exert a wide range of bioactivities, including anti-tumour, immunosuppression, anti-anxiety, analgesia, and so on. Owing to their fascinating structures and potent pharmaceutical properties, these gelsemium MIAs arouse significant organic chemists’ interest to design state-of-the-art synthetic strategies for their total synthesis. In this review, we comprehensively summarised recently reported novel gelsemium MIAs, potential pharmacological activities of some active molecules, and total synthetic strategies covering the period from 2013 to 2022. It is expected that this study may open the window to timely illuminate and guide further study and development of gelsemium MIAs and their derivatives in clinical practice.

https://doi.org/10.1080/14756366.2022.2155639

Recent progress in chemistry and bioactivity of monoterpenoid indole alkaloids from the genus gelsemium: a comprehensive review

Background The herbal pairing of Dangshen (DS) [Codonopsis pilosula (Franch.) Nannf.] and Huangqi (HQ) [Astragalus membranaceus (Fisch.) Bge.] (DHP) is a traditional Chinese herbal medicine that is frequently used to treat chronic heart failure (CHF) in China. However, the pharmacological mechanism of DHP has not been fully elucidated. This is the first study aimed to reveal the active mechanism of DHP in the treatment of CHF by using network pharmacology methods. Methods The active ingredients of DHP were obtained from the TCMSP database, and the potential targets of DHP were predicted using the SwissTargetPrediction database. CHF-related targets were searched by the DisGeNET and GeneCards databases. The common targets between the disease and herbs were obtained using a Venn diagram. The STRING database was utilized to obtain the protein-protein interaction data. Next, we used Cytoscape 3.7.2 software to construct and analyze the herb-ingredient-potential targets-disease network. Topology analysis was used to identify the key ingredients and hub genes. Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analyses were performed using the Metascape database to reveal the mechanism. Furthermore, molecular docking simulation was performed using AutoDock Vina software to assess the affinity of the key ingredients and hub genes. Results Five key ingredients and six hub genes were screened. The six hub genes were closely related to PI3K /AKT or ERK1/2 pathways. The KEGG pathways mainly involved the TNF signaling pathway, calcium signaling pathway, and cancer-related pathways. The GO enrichment analysis results showed that DHP might act on biological processes including positive regulation of kinase activity and cellular response to nitrogen compound via the three above-mentioned pathways in the treatment of CHF. Finally, the molecular docking results showed that the five key ingredients exhibited strong affinities to the six hub genes. Conclusions This study revealed the molecular mechanism that the flavonoids in DHP may alleviate endothelial dysfunction and cardiac hypertrophy via regulation of the TNF pathway and its downstream PI3K/Akt or ERK1/2 signaling pathways, or improve excitation-contraction coupling by regulating calcium signaling pathway, thereby improving CHF. These results provide insights for further experimentation on its pharmacological effects.

/pdf/integration-of-network-pharmacology-and-molecular-docking-3kr260ujjx.pdf

Integration of network pharmacology and molecular docking technology reveals the mechanism of the herbal pairing of Codonopsis Pilosula (Franch.) Nannf and Astragalus Membranaceus (Fisch.) Bge on chronic heart failure.

Indole alkaloids from Gelsemium elegans.

Due to the complexity of urban environments, the synthetic aperture radar (SAR) based mapping of floodwater is impacted by different factors such as water depth, building orientation and the density of built-up areas. Several studies have proven that both SAR multitemporal intensity and interferometric SAR (InSAR) coherence data acquired in VV and VH polarizations support the urban flood mapping. We propose a deep learning (DL) based method using dual-polarization Sentinel-1 multitemporal intensity and coherence data combined with prior information to map floodwater in urbanized areas. The proposed method aims at mapping flooded areas in urbanized regions and bare soils/sparsely vegetated areas within the entire frame of a Sentinel-1 image. In this paper, our method is evaluated for the Houston (US) urban flood event in 2017 via a qualitative and quantitative comparison with two established DL models. The proposed method has the lowest number of false alarms in flooded urban areas, indicating that the prior information from the probabilistic urban mask is valuable.

Prior Information in Support of Deep Learning Methods to Map Floodwater in Urbanized Areas

https://export.arxiv.org/pdf/2512.12053v1.pdf

Adaptive Federated Learning for Ship Detection Across Diverse Satellite Imagery Sources

Extraction of built-up areas using Sentinel-1 and Sentinel-2 data with automated training data sampling and label noise robust cross-fusion neural networks

Previous references indicated that surface wind gusts associated with deep convection can be observed and estimated from Sentinel-1 images. They also presented the relationship between surface wind patterns and deep convective clouds observed on Meteosat geostationary (GEO) images. To strengthen this relationship, this paper presents the comparison between surface wind speed retrieved from Sentinel-1 data, wind magnitude measured by the weather stations, and deep convective clouds observed on GOES-16 GEO images over the Gulf of Mexico. The results show that a mesoscale surface wind pattern (a squall line) observed on Sentinel-1 images corresponds to deep convective cloud locations. In particular, the peaks of wind intensity measured by the weather stations match the Sentinel-1 wind gusts and the deep convective clouds.

Assessment of Sentinel-1-Estimated Sea Surface Convective wind Gusts with in-situ wind Measurements

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