Natural Products Research Articles

Production of Polyphenolic Natural Products by Bract-Derived Tissue Cultures of Three Medicinal Tilia spp.: A Comparative Untargeted Metabolomics Study.

Medicinal plant tissue cultures are potential sources of bioactive compounds. In this study, we report the chemical characterization of the callus cultures of three medicinal Tilia spp. (Tilia cordata, Tilia vulgaris and Tilia tomentosa), along with the comparison to bracts and flowers of the same species. Our aim was to show that calli of Tilia spp. are good alternatives to the calli of T. americana for the production of polyphenols and are better sources of a subset of polyphenolic metabolites, compared to the original organs. Calli were initiated from young bracts and grown on woody plant medium containing 1 mg L-1 2,4-D and 0.1 mg L-1 BAP. For chemical characterization, a quality-controlled untargeted metabolomics approach and the quantification of several bioactive compounds was performed with the use of LC-ESI-MS/MS. While bracts and flowers contained flavonoid glycosides (astragalin, isoquercitrin) as major polyphenols, calli of all species contained catechins, coumarins (fraxin, esculin and scopoletin) and flavane aglyca. T. tomentosa calli contained 5397 µg g DW-1 catechin, 201 µg g DW-1 esculin, 218 µg g DW-1 taxifolin and 273 µg g DW-1 eriodictyol, while calli from other species contained lower amounts. T. cordata and T. tomentosa flowers were rich in isoquercitrin, containing 8134 and 6385 µg g DW-1, respectively. The currently tested species contained many of the bioactive metabolites described from T. americana. The production of catechin was shown to be comparable to the most efficient tissue cultures reported. Flowers and bracts contained flavonoid glycosides, including tiliroside, resembling bioactive fractions of T. americana. In addition, untargeted metabolomics has shown fingerprint-like differences among species, highlighting possible chemotaxonomic and quality control applications, especially for bracts.

Xylarkarynone A and B:Two Bioactive Eremophilane Sesquiterpenes from Xylaria sp. HHY-2.

A new compound xylarkarynone A (1), a first reported natural product compound xylarkarynone B (2) and eight known compounds (3-10) were isolated from Xylaria sp. HHY-2. Their structures were elucidated by spectroscopic methods, DP4+ probability analyses and electronic circular dichroism (ECD) calculations. The bioactivities of isolated compounds were assayed. Compound 1 exhibited obvious activity against A549 cells with an IC50 value of 6.12 ± 0.28 µM. Additionally, compound 1 showed moderate antifungal activities against Plectosphaerella cucumerina and Aspergillus niger with minimum inhibitory concentrations (MICs) of both 16 µg/mL, which was at the same grade with positive control nystatin. Most compounds exhibited varying degrees of inhibitory activity against P. cucumerina, indicating that Xylaria sp. has potential as inhibitors against P. cucumerina.

Synthesis of 1,4‐Disubstituted and 1‐Substituted β‐Carbolines via 3‐Substituted 2‐Acylindoles

Abstractβ‐Carbolines represent a large class of bioactive natural products, whereby most of these alkaloids bear residues at C1, and occasionally at C3, and only limited examples of 1,4‐disubstituted β‐carbolines are known. In this project we worked out a novel approach to 1,4‐disubstituted β‐carbolines and performed a comprehensive analysis of the scope and limitations of this methodology. The 1,4‐disubstituted β‐carbolines were synthesized via 3‐substituted 2‐acylindoles, for which effective synthesis procedures were developed. Our studies revealed that a broad range of target compounds with electron‐withdrawing substituents at C4 are accessible. Limitations of this method arose from competing CH and NH acidities of precursors. Nevertheless, the work described herein provides a unique approach to highly substituted β‐carbolines. In addition, intermediates from this route opened a novel approach to 1‐substituted β‐carbolines utilizing a chemoselective Mo(CO)6‐catalyzed amide reduction with tetramethyldisiloxane.

Challenges in Optimizing Nanoplatforms Used for Local and Systemic Delivery in the Oral Cavity.

In this study, we focused on innovative approaches to improve drug administration in oral pathology, especially by transmucosal and transdermal pathways. These improvements refer to the type of microneedles used (proposing needles in the saw), to the use of certain enhancers such as essential oils (which, besides the amplifier action, also have intrinsic actions on oral health), to associations of active substances with synergistic action, as well as the use of copolymeric membranes, cemented directly on the tooth. We also propose a review of the principles of release at the level of the oral mucosa and of the main release systems used in oral pathology. Controlled failure systems applicable in oral pathology include the following: fast dissolving films, mucoadhesive tablets, hydrogels, intraoral mucoadhesive films, composite wafers, and smart drugs. The novelty elements brought by this paper refer to the possibilities of optimizing the localized drug delivery system in osteoarthritis of the temporomandibular joint, neuropathic pain, oral cancer, periodontitis, and pericoronitis, as well as in maintaining oral health. We would like to mention the possibility of incorporating natural products into the controlled failure systems used in oral pathology, paying special attention to essential oils.

Aspergillus clavatonanicus HSF015 possesses the talent in producing bioactive secondary metabolites

Mangrove-associated fungi are excellent sources of bioactive natural products. To explore the value of producing bioactive secondary, the genome and transcriptome of mangrove-associated fungus named A. clavatonanicus HSF015 are sequenced for the first time. According to the genome (8737 function gene), A. clavatonanicus HSF015 with 58.05 % genes expressing shows high performance in metabolism and secondary metabolism. Forty secondary metabolite biosynthesis gene clusters are successfully annotated from 13 contigs in the genome. Thereinto, ten biosynthesis gene clusters can synthesize 17 known compounds with various activities and application values. The remaining 30 gene clusters are unknown secondary metabolite synthesis gene clusters, which are worth exploring. In addition, three known compounds with antioxidant and antibacterial activities were isolated from the broth of A. clavatonanicus HSF015. Hence, A. clavatonanicus HSF015 with the great talent in producing bioactive secondary metabolites is worth further study.

Influence of structure-forming recipe ingredients on the quality of pumpkin marmalade

Analyzing the assortment of the market for marmalade products, it is worth noting that there is a tendency to introduce natural products in the form of vegetable or fruit puree into the recipe composition, as the demand for confectionery products for therapeutic, prophylactic, and functional purposes, as well as for products with dietary properties, is growing. This work aims to study the influence of structure-forming recipe ingredients on the quality of pumpkin jelly marmalade. Pumpkin puree was used as the primary raw material for producing jelly marmalade, food agar was used as a gelling agent, and natural honey was used as a sweetener. During the study, organoleptic, physicochemical, and microbiological quality indicators of semi-finished pumpkin products and finished marmalade samples were determined. The color assessment of the finished products was carried out using a colorimeter NR-UO (China). Pumpkin semi-finished and finished products meet regulatory documentation requirements regarding organoleptic, physico-chemical, and microbiological quality indicators. When food agar is used as a gelling agent, the degree of color increases due to the transparency of the structure, and the red (+a*) and yellow (+b*) components in samples containing food agar are successfully combined and give the finished product an attractive orange color. To increase the nutritional -value, it is proposed to use cinnamon or coconut flakes, which have beneficial properties, to sprinkle the surface of finished products. The price for 1 kg of pumpkin jelly marmalade was: control sample - 335.46 rubles, “Məkhəbbət” with cinnamon - 748.85 rubles, “Məkhəbbət” with coconut flakes - 725.36 rubles. For a new type of confectionery products, regulatory and technical documentation STO, TI, RC 00493497-005-2022 “Halal” pumpkin jelly marmalade “Məkhəbbət” has been drawn up.

Advanced high-resolution chromatographic strategies for efficient isolation of natural products from complex biological matrices: from metabolite profiling to pure chemical entities

Advanced high-resolution chromatographic strategies for efficient isolation of natural products from complex biological matrices: from metabolite profiling to pure chemical entities

In-vitro and molecular docking studies of plant secondary metabolites isolated from Hypericum oblongifolium as antibacterial agents and lipoxygenase (5-LOX) inhibitors

Natural Products are bases for modern pharmaceuticals as they are precursors for many synthetic drugs. People also use natural products directly in the form of herbal medicines due to their less harmful effects. This research project aimed to investigate the new pharmacological potential of natural products found in Hypericum oblongifolium. Five compounds were identified from chloroform and ethyl acetate soluble fractions of H. oblongifolium. These compounds were identified as 21-β-hydroxyursolic acid (1), β-sitosterol (2), 7,4′-dihydroxy-5,3′-dimethoxyisoflavone (3), α-D-glucopyranosyl-6′-O-hexadecanoate (4), Quercetin-3′-O-ß-D-glucopyranoside (5). When these compounds were tested for antibacterial potential compound 5 showed maximum inhibition against gram-positive Bacillus subtilis and was highly active against Escherichia coli gram-negative bacterium. Minimum inhibition was shown by compounds 2 and 3 against Shigella flexneri among gram-negative bacteria. Compound 5 also exhibited the least binding energy in the molecular modeling of these compounds against Escherichia coli proteins GlcN-6-P synthase (PDB ID: 1MOQ). Compound 5 also showed good inhibition of lipoxygenase (5-LOX) enzyme with an IC50 value of 30.1 ± 0.20 as it exhibited maximum hydrogen bondings and minimum energy when docked with LOX-5 (PDB ID 3V99) using a patch dock.

Bioactivity of hydroalcoholic extracts from tropaeolum majus L. (tropaeolaceae) on the germination, initial plant development and cell cycle of Lactuca sativa L

ABSTRACT Natural products are usually considered harmless; however, these substances need to be consumed with caution. Biological assays with plant models are a suitable alternative for prospective studies to assess natural product-initiated toxicity. The aim of this study was to examine the toxic potential of leaf and flower extracts derived from Tropaeolum majus L. a widely used plant in traditional medicine. Seeds of Lactuca sativa L. were exposed to T. majus extracts and based upon the seedling growth curve values, the 50% Inhibition Concentration (IC50) was calculated and applied for cell cycle analysis exposure. Both extracts contained organic acids, proteins, amino acids, and terpene steroids. Sesquiterpene lactones and depside were detected in leaf extracts. The higher concentration tested exhibited a marked phytotoxic effect. The extracts induced clastogenic, aneugenic cytotoxic, and potential mutagenic effects. The possible relationships between the classes of compounds found in the extracts and effects on cells and DNA were determined.

The effectiveness of natural indigo/kaolinite composite powder in the development of latent fingermarks

BackgroundComposites are materials that have multiple phases and have attracted much attention as they are able to improve physical and chemical properties of an isolated material. In this sense, these composites are commonly used as key components for two purposes: coloring and improving the operational properties; besides that, they have alternative synthesis routes that respect the principles of green chemistry. Thus, this reports the development of a new composite using natural products, indigo and kaolinite, for application in papilloscopy as a new nontoxic fingermark developer.ResultsThe composite was obtained via green procedures and was characterized by spectroscopic and chromatographic techniques. Thus, to investigate the potential of the material as a fingermark developer, different techniques were applied such as depletion, aging, comparison with commercial powder, and development of latent fingermarks on different surfaces. Tests revealed that the composite presented good contrast and adhesion with the latent fingermarks, even after 15 days of deposition.ConclusionsThis study presents a natural indigo/kaolinite composite powder that showed similar or higher efficiency when compared to the commercial fingerprint powder and was able to develop identifiable natural and sebaceous fingermarks.Key points• A composite was formed from eco-friendly materials.• The composite formation follows the concepts of green chemistry and low cost.•The composite was applied as a latent fingermark developer.

Genetic Diversity and Population Structure of Actinidia eriantha by ITS Sequences

Background: Actinidia eriantha Benth is a widely used natural product from Traditional Chinese Medicine in the Actinidiaceae family. However, its wild resources have been declining due to over-exploitation. It has become urgent to investigate the genetic diversity for the conservation of A. eriantha, to evaluate the current species and discover strategies for preservation. Methods: The internal transcribed spacer (ITS) was used to evaluate the genetic diversity among and within populations of this species. Dnasp, PERMUT and Arlequin 3.0 software were used to calculate the genetic diversity index, and MEGA 5.0 software was used to construct the neighbor-joining (NJ) tree. Results: A total of 27 haplotypes were obtained by ITS sequence analysis of 12 populations, and the most frequently haplotype observed was H1. AMOVA analysis revealed that the genetic variation rates were 10.91% (FST = 0.22290) and 77.71% (FSC = 0.12306) among and within populations, respectively, with high genetic diversity at the species level (Hd = 0.692). The genetic distance among populations ranged from 0 to 0.004. The results of Permut analysis showed that there was no significant correlation between genetic distance and geographic distance (NST > GST). The NJ tree was divided into two Clades (Clade A and Clade B), Clade B has obvious geographical specificity, and haplotypes of this clade are all specific to the GX-ZY population. Four types were found according to ITS sequences of A. eriantha, haplotypes H1 and H5 were ancient haplotypes. Conclusion: Our findings indicated that genetic diversity within populations was higher than observed among populations. This study is significant for further research endeavors focused on the efficient collection and preservation of wild resources of A. eriantha.

Strategies to enhance the response of liver cancer to pharmacological treatments.

In contrast to other types of cancers, there is no available efficient pharmacological treatment to improve the outcomes of patients suffering from major primary liver cancers, i.e., hepatocellular carcinoma and cholangiocarcinoma. This dismal situation is partly due to the existence in these tumors of many different and synergistic mechanisms of resistance, accounting for the lack of response of these patients, not only to classical chemotherapy but also to more modern pharmacological agents based on the inhibition of tyrosine kinase receptors (TKIs) and the stimulation of the immune response against the tumor using immune checkpoint inhibitors (ICIs). This review summarizes the effort to develop strategies to overcome this severe limitation, including searching for novel drugs derived from synthetic, semisynthetic, or natural products with vectorial properties against therapeutic targets to increase drug uptake or reduce drug export from cancer cells. Besides, immunotherapy is a promising line of research that is already starting to be implemented in clinical practice. Although less successful than in other cancers, the foreseen future for this strategy in treating liver cancers is considerable. Similarly, the pharmacological inhibition of epigenetic targets is highly promising. Many novel "epidrugs", able to act on "writer", "reader" and "eraser" epigenetic players, are currently being evaluated in preclinical and clinical studies. Finally, gene therapy is a broad field of research in the fight against liver cancer chemoresistance, based on the impressive advances recently achieved in gene manipulation. In sum, although the present is still dismal, there is reason for hope in the non-too-distant future.

Sercocephalous latifolius fruit attenuates aluminum chloride-induced oxidative stress and neurotoxicity in Drosophila melanogaster via Drn1 regulation of the IMD signaling pathway

IntroductionAlzheimer disease (AD) is a form of dementia that is a heterogeneous dysfunction of various pathophysiological features. Its morphological characteristics consist of tau aggregates and amyloid plaques. The need for novel therapy in the treatment of AD is required. Hence use of antioxidant, natural products are widely employed for the management and treatment of AD and other neurodegenerative diseases. However, there are still a lot of limitations. Sercocephalous latifolius fruit (SLF) is also known as the African peach and has numerous well-being-endorsing advantages. The Chinese name of SLF is Feizhou hong tao, while the Nigeria (Yoruba) name is Eso Gberesi. It can be grown all over the world. SLF has anti-neurodegenerative properties, however, there is a lack of evidence on their probable molecular mechanism for novel therapeutic properties. Investigations have been conducted on the SFL which shows its medicinal capability, but its ability to attenuate neurodegenerative diseases such as AD is yet to be fully elucidated, and the molecular signally pathways whichmay serve as a therapeutic target. MethodsThe modulatory effect of SLF on aluminum chloride-induced neurotoxicity and oxidative stress in Drosophila melanogaster via Defense repressor-1 (Drn1) regulation of immune deficiency (Imd) signaling pathway which may be a useful therapeutic target. D. melanogaster was divided into nine groups. Group 1 served as the basal control as they were fed with a normal basal diet, group 2 served as the negative control as they were fed with Basal Diet and 0.5 ml of aluminum/100 ml distilled water, group 3 served as the positive control as they were fed with basal diet 0.5 ml aluminum chloride/100 ml distilled water and Garlic acid, group 4 and 5 were fed with basal diet and 0.1 and 1 % SLF respectively, group 6 and 7 were fed with basal diet, aluminum chloride and 0.1 and 1.0 % respectively, group 8 and 9 were fed with basal diet, garlic acid, aluminum chloride and 0.1 and 1.0 % SLF respectively. All the groups were left for seven days. The experiment was conducted for 3 months, and the fruit flies were changed every 5 days. ResultsSuperoxide dismutase, catalase, malondialdehyde, and nitric oxide enzymatic enzymes were assayed. However, the relative expression of Defense repressor-1 was also determined both in vitro and on aluminum-induced neurodegenerative D. melanogaster tissue. A significant increase was observed in the catalase when 0.1 % and 1 % were compared, it could be inferred that the extract proved effective at low concentrations, since its highest antioxidant potential was observed at low concentrations. The results revealed decrease in the activity of malondialdehyde, superoxide dismutase, and nitric oxide biological enzymes in the test groups. There was upregulation of Defense repressor -1 in groups 3, 4, 5, and 6, when compared with the positive and negative control, respectively. DiscussionThe result provides evidence that SLF has the potential of upregulating defense repressor genes and modulating biological antioxidant enzymes, which could be further exploited to fully understand the underlying molecular mechanisms responsible for the attenuation of neurotoxicity, oxidative stress, and neurodegenerative diseases such as AD. The results suggest that SLF may be useful as a therapeutic target in AD and other neurodegenerative diseases

Natural Compounds for Bone Remodeling: A Computational and Experimental Approach Targeting Bone Metabolism-Related Proteins.

Osteoporosis, characterized by reduced bone density and increased fracture risk, affects over 200 million people worldwide, predominantly older adults and postmenopausal women. The disruption of the balance between bone-forming osteoblasts and bone-resorbing osteoclasts underlies osteoporosis pathophysiology. Standard treatment includes lifestyle modifications, calcium and vitamin D supplementation and specific drugs that either inhibit osteoclasts or stimulate osteoblasts. However, these treatments have limitations, including side effects and compliance issues. Natural products have emerged as potential osteoporosis therapeutics, but their mechanisms of action remain poorly understood. In this study, we investigate the efficacy of natural compounds in modulating molecular targets relevant to osteoporosis, focusing on the Mitogen-Activated Protein Kinase (MAPK) pathway and the gut microbiome's influence on bone homeostasis. Using an in silico and in vitro methodology, we have identified quercetin as a promising candidate in modulating MAPK activity, offering a potential therapeutic perspective for osteoporosis treatment.

Enamel remineralisation prospect of Moringa Oleifera hydrogel, eggshell hydrogel versus sodium fluoride varnish on artificially demineralised primary teeth: in vitro study.

The purpose of the present in vitro study is to investigate and compare the remineralising potential of Moringa Oleifera extract, eggshell, and sodium fluoride varnish on microhardness of artificially demineralised enamel of primary teeth with biomimetic minimally invasive approach following the world paradigm shift towards natural products in paediatric dentistry. Sample size included 44 primary molars. The mineral content and surface microhardness of all specimens were initially assessed using energy dispersive x-ray examination (EDX) and Vickers microhardness. The specimens were artificially demineralised for 96 h at a temperature of 37°C and then reassessed directly after demineralisation. The demineralised enamel specimens were randomly divided into four groups according to the remineralisation regimen utilised. Group 1: Artificial saliva (control); Group 2: Sodium fluoride varnish; Group 3: Eggshell hydrogel; and Group 4: Moringa Oleifera hydrogel. The specimens were stored for 8 days and then subsequently evaluated using EDX and microhardness assessment by Vickers microhardness test and scanning electron microscope (SEM). Results: Regarding the microhardness test, there was a significant difference between the Moringa Oleifera group and Eggshell group compared to fluoride varnish (p < 0.05). Regarding EDX analysis, there was a statistically significant difference (p < 0.05) between Moringa Oleifera group and Eggshell group compared to fluoride varnish as the highest values were for Moringa Oleifera and Eggshell. On the other hand, there was no statistically significant difference (p > 0.05) between Moringa Oleifera and Eggshell in both the measurements. Moringa Oleifera and Eggshell might be considered as a biomimetic natural material capable of guiding enamel tissue remineralisation in early carious lesion of primary teeth. This research demonstrated the capability for early enamel caries to be remineralised using novel materials with a naturally counterpart implicated in biomineralisation as proved to be more effective than traditionally used fluoride varnish in primary teeth.

Enantioselective synthesis of chiral α,α-dialkyl indoles and related azoles by cobalt-catalyzed hydroalkylation and regioselectivity switch

General, catalytic and enantioselective construction of chiral α,α-dialkyl indoles represents an important yet challenging objective to be developed. Herein we describe a cobalt catalyzed enantioselective anti-Markovnikov alkene hydroalkylation via the remote stereocontrol for the synthesis of α,α-dialkyl indoles and other N-heterocycles. This asymmetric C(sp3)−C(sp3) coupling features high flexibility in introducing a diverse set of alkyl groups at the α-position of chiral N-heterocycles. The utility of this methodology has been demonstrated by late-stage functionalization of drug molecules, asymmetric synthesis of bioactive molecules, natural products and functional materials, and identification of a class of molecules exhibiting anti-apoptosis activities in UVB-irradiated HaCaT cells. Ligands play a vital role in controlling the reaction regioselectivity. Changing the ligand from bi-dentate L6 to tridentate L12 enables CoH-catalyzed Markovnikov hydroalkylation. Mechanistic studies disclose that the anti-Markovnikov hydroalkylation involves a migratory insertion process while the Markovnikov hydroalkylation involves a MHAT process.

The beneficial health effects of puerarin in the treatment of cardiovascular diseases: from mechanisms to therapeutics.

Cardiovascular diseases (CVDs) are the leading causes of death globally that seriously threaten human health. Although novel western medicines have continued to be discovered over the past few decades to inhibit the progression of CVDs, new drug research and development for treating CVDs with less side effects and adverse reactions are continuously being desired. Puerarin is a natural product found in a variety of medicinal plants belonging to the flavonoid family with potent biological and pharmacological activities. Abundant research findings in the literature have suggested that puerarin possesses a promising prospect in treating CVDs. In recent years, numerous new molecular mechanisms of puerarin have been explored in experimental and clinical studies, providing new evidence for this plant metabolite to protect against CVDs. This article systematically introduces the history of use, bioavailability, and various dosage forms of puerarin and further summarizes recently published data on the major research advances and their underlying therapeutic mechanisms in treating CVDs. It may provide references for researchers in the fields of pharmacology, natural products, and internal medicine.

Development of bioactive films loaded with extract and polysaccharide of Pinus brutia bark.

Society's interest in natural and clean products in many areas, such as food and cosmetics, has increased considerably. It has led to the development of new techniques in the packaging of products so that the wastes from the preferred products can be recycled. In this context, Pinus brutia bark was preferred within the scope of the study to transform natural wastes into functional components and use them as packaging material. P. brutia bark (PBB) samples were collected from Bursa, Turkey. PBB samples were ultrasonically extracted using various solvents (acetone, butanol, ethanol, ethyl acetate, hexane, methanol, petroleum ether, and water) and a solvent-acidic hydrolysis system. The phenolic content profile of PBB samples was determined using high-performance liquid chromatography with diode-array detection, and total flavonoid content, antioxidant capacity, and total phenolic content were determined. Chitosan-polyvinyl alcohol (CS-PVA) films loaded with polysaccharides and containing methanolic extract were developed. The physical, chemical, and mechanical properties of the films were characterized. It is known that the thickness of the films determines the mechanical properties required to maintain the integrity of the packaging during storage and transport. From the results of the study, it was concluded that the elongation at break value was higher in CS-PVA-PBB-M films (111.08%±10.46%), Young's modulus (31.74±21.37N/mm2), and tensile strength (3.01±0.50N/mm2) values were higher in CS-PVA films. In this case, it was concluded that adding proanthocyanidin to edible films gives flexibility to the films.

A Fluorinated Chaperone Gives X‐ray Crystal Structures of Acyclic Natural Product Derivatives up to 338 Molecular Weight

A Fluorinated Chaperone Gives X‐ray Crystal Structures of Acyclic Natural Product Derivatives up to 338 Molecular Weight

Accessing SuFExable Cyclobutane‐Fused Indolines via Photocatalytic Intermolecular [2+2] Cycloaddition of Indoles

Indoline‐fused polycycles are commonly found as a key structural component in numerous natural products and biologically active compounds. In recent times, the incorporation of sulfonyl fluoride groups has drawn significant attention in research due to their potential to enhance or confer new biological activities to molecules. In this study, we report the development of a novel and modular approach for synthesizing FSO&lt;sub&gt;2&lt;/sub&gt;‐functionalized cyclobutane‐fused indolines by employing an intermolecular [2+2] cycloaddition reaction between indoles and SuFExable ethenesulfonyl fluoride under triplet energy‐transfer catalysis. This method features mild reaction conditions, metal‐free photocatalysts, and excellent tolerance to various functional groups. Moreover, we demonstrate the feasibility of further modifying the FSO&lt;sub&gt;2&lt;/sub&gt;‐functionalized indoline products via SuFEx click reactions, enabling their conjugation with other molecules.