Constituents of the Root Wood of Zanthoxylum wutaiense with Antitubercular Activity

ISHII H., ISHIKAWA T., LU S., CHEN I.

ISHII H., CHEN I., AKAIKE M., ISHIKAWA T., LU S.

ISHIKAWA T., SEKI(nee IMAI) M., NISHIGAYA K., MIURA Y., SEKI H., CHEN I., ISHII H.

The chemical constituents of the wood of Xanthoxylum nitidum (ROXB.) D. C.(Fagara nitida ROXB.) were examined. Two phenylpropanoids, methyl nitinoate (2) and dihydrocuspidiol (3), and a benzodioxane type lignan, nitidanin (4), were newly isolated. The structures of the phenylpropanoids were chemically determined. In addition, the application of a selective insensitive nuclei enhanced by polarization transfer selective (INEPT) technique in the NMR spectrum to the new lignan allowed us to deduce the structure.

ITO C., FURUKAWA H.

ITO C., MIZUNO T., MATSUOKA M., KIMURA Y., SATO K., KAJIURA I., OMURA M., JU-ICHI M., FURUKAWA H.

A new flavonoid, citflavanone (1), and prenylated phenol derivatives, etrogol (7) and valencic acid (8), were isolated from roots and root barks of Citrus natsudaidai (natsudaidai), C. medica (etrog citron), C. sinensis (valencia orange), and several hybrid seedlings resulting from hyuga-natsu × hirakishu, and characterized. In order to determine the structure of citflavanone (1), prenylation of naringenin (3) was attempted to give 6- and 8-prenylnaringenin (4 and 5, respectively) as well as 6, 8-diprenylnaringenin (6). The location of the prenyl moiety in 4 and 5 was established by means of the long-range selective proton decoupling technique in nuclear magnetic resonance spectrometry.

ABE F., YAHARA S., KUBO K., NONAKA G., OKABE H., NISHIOKA I.

The stem bark of Xanthoxylum piperitum DC. was phytochemically examined and five new lignans, viz., xanthoxylol (3), piperitol (5), their γ, γ-dimethylallyl ethers (6, 7) and sanshodiol (8) were isolated besides l-asarinin (1) and l-sesamin (2) and their structures were determined. Phytosterol, γ-fagarine, skimmianine, syringaldehyde, piperonylic acid, menisperine, laurifoline and magnoflorine were also isolated from the same source.

HAYASHI K., KOMURA S., ISAJI N., OHISHI N., YAGI K.

One new and 11 previously known antioxidative compounds were isolated from Brazilian propolis. The new compound was determined as 3,4-dihydroxy-5-prenylcinnamic acid (3-[3,4-dihydroxy-5-(3-methyl-2-butenyl)phenyl]-2-(E)-propenoic acid) by various physical analyses (MS, IR, 1 H-NMR, 13 C-NMR, and 2D-NMR). The inhibitory activity of each compound against peroxidation of linoleic acid in a micelle solution was measured. We found that the novel compound possessed the highest potency (IC50, 0.17 m M) among them and was more effective than butylated hydroxytoluene (BHT; IC50, 0.36 m M) under the experimental conditions employed. Among the isolated antioxidative compounds, 3,5-diprenyl-4-hydroxycinnamic acid (artepillin C; IC50, 0.44 m M) was found to be most abundant in Brazilian propolis.

Ross S.A., Krishnaveni K.S., Burandt C.L.

Two new benzofuran derivatives (1 and 2) have been isolated from the roots of Zanthoxylum flavum Vahi. The structures of the new compounds 1 and 2 were characterised as 6-methoxybenzofuran-5-propionylmethylester (1) and 6,7-dimethoxybenzofuran-5-propionyl-methylester (2) based on one- and two-dimensional NMR spectroscopy and high-resolution mass spectrometry.

Su Y., Ren X., She X., Pan X.

An enantioselective synthesis of Virologins 1-(S and R), 2-trans-(S and R) and 3-cis-(S and R) were achieved by Mitsunobu reaction to construct a chiral center and Ando reagent to form cis-olefin.

Lee C., Lu C., Kuo Y., Chen J., Sun G.

Two new prenylated flavanones, ficubee A and ficubee B, respectively, as 7,8-(2,2-dimethylpyrano)-6-prenyl-5,3',4'-trihydroxyflavone and 6,7-(2,2-dimethylpyrano)-8-prenyl-5,3',4'-trihydroxyflavone were isolated from the roots of Ficus beecheyana together with twelve known compounds: β-sitosterol, 5-stigmasten-3β,7α-diol, 5-stigmasten-3β,7β-diol, 3β-hydroxystigmast-5-en-7-one, 4-hydroxybenzaldehyde, 4-hydroxy-3-methoxybenzaldehyde, 1-(4-hydroxyphenyl)-ethanone, 4-hydroxy-3-methoxybenzoic acid, 4-hydroxy-cinnamic acid, seseline, xanthyletin, and psoralene. The structures of these secondary metabolites were determined by spectroscopic means and in comparison with published data.

Mhaske S.B., Argade N.P.

Starting from glutaric anhydride ( 5 ) we have demonstrated an elegant six-step practical synthesis of bioactive natural product rutaecarpine ( 1a ) via o -amidoglutaranilic acid formation, esterification, chemoselective ester reduction, intramolecular dehydrative cyclizations, hydrazone formation and zeolite induced Fischer-indole synthesis with 53% overall yield. The conditions employed in the present synthesis are mild, efficient and general.

Wattanapiromsakul C., Forster P.I., Waterman P.G.

Five alkaloids, four beta-indoloquinazoline and one furoquinoline, and four terpenoids, three limonoids and one modified sesquiterpene, have been obtained from the aerial parts of Bouchardatia neurococca (Rutaceae). Two of the alkaloids, 1,2-dihydroxyrutaecarpine and 2-(2-[3-formylindolyl])-(3H)-quinazolin-4-one (bouchardatine), and two of the limonoids, 23-oxo-21xi-hydroxy-21,23-dihydroveprisone (veprisonic acid) and 21-oxo-23xi-hydroxy-21,23-dihydroveprisone (isoveprisonic acid) are new. The pattern of secondary metabolites isolated is rather unusual in the Rutaceae and is reminiscent of Tetradium, a genus with which Bouchardatia has not previously been associated.

Wu T., Shi L., Wang J., Iou S., Chang H., Chen Y., Kuo Y., Chang Y., Tenge C.

Nineteen compounds have been isolated from the methanol extract of the root and aerial parts of Ruta graveolens. The structural elucidation of these isolated compounds were determined by the spectroscopic methods and/or comparison of the physical data with literature values. Their antiplatelet aggregation and cytotoxic activities were examined to find potent antiplatelet aggregation and cytotoxic compounds from natural resources. Among them, dictamine (5), skimmianine (7), psoralen (8), chalepensin (12), clausindin (13), and graveolinine (16) showed significant inhibition of platelet aggregation, induced by arachidonic acid and collagen. Arborinine (2), dictamine (5), isopimpinellin (11), clausindin (13), and graveoline (17) exhibited cytotoxic activity against KB, Hela, DLD, NCI and Hepa tumor cell lines.

Girard C., Colombain M., Muyard F., Bévalota F., Tillequin F., Waterman P.G.

Phebarudol, a novel prenylated p-coumarate, was isolated from the twigs of Phebalium rude Bartl. subsp. amblycarpum (F. Muell.) P. G. Wilson (Rutaceae) together with the two already known related compounds, werneria chromene and methyl demethoxywutaiensate. The structure of phebarudol was established by spectroscopic methods.

Ito J., Chang F., Wang H., Park Y.K., Ikegaki M., Kilgore N., Lee K.

A new triterpenoid named melliferone (1), three known triterpenoids, moronic acid (2), anwuweizonic acid (3), and betulonic acid (4), and four known aromatic compounds (5−8) were isolated from Brazilian propolis and tested for anti-HIV activity in H9 lymphocytes. Moronic acid (2) showed significant anti-HIV activity (EC50 186) and was modified to develop more potent anti-AIDS agents.

Yang S.Y., Phong N.V.

Zanthoxylum piperitum, commonly known as Japanese pepper, is a versatile plant from the Rutaceae family that has attracted significant scientific research interest due to its culinary and medical applications. Herein, we present a phytochemical investigation of Z. piperitum stems, leading to the isolation and characterization of a new compound, zanthopiperitol (1), along with four known phenolic compounds (2–5). Among them, ailanthoidiol (2) demonstrated potent β-glucuronidase inhibition with an IC50 of 68.39 ± 2.29 µM. The results of an enzyme kinetics analysis suggest that it acts as a competitive inhibitor of β-glucuronidase while molecular docking simulation outcomes reveal that it can bind effectively to key amino acid residues in the main catalytic binding site of β-glucuronidase. Moreover, the strong stability of compound 2 bound to the enzyme binding site is indicated via a 100-ns molecular dynamics simulation study. This study highlights the potential of exploiting naturally occurring β-glucuronidase inhibitors such as ailanthoidiol for treating various gastrointestinal health issues.

Antonova Alexandra S., Zubkov Fedor I.

Catalytic olefin metathesis using Hoveyda-Grubbs type ruthenium complexes is a powerful tool for creating complex molecules possessing a variety of practically useful properties. This method is also applied for obtaining modern polymer materials from low-demand petroleum products. Among all ruthenium complexes containing five- or six-membered chelate rings, the commercially available HG-II catalyst is the most common. In addition, other Hoveyda-Grubbs type complexes, which include a Het→Ru donor–acceptor bond in the chelate ring, often exhibit metathesis activity equal to or superior to that of HG-II. This review considers second-generation N-heterocyclic ruthenium carbene Hoveyda-Grubbs type complexes with donor–acceptor bonds such as O→Ru, S→Ru, Se→Ru, N→Ru, P→Ru and Hal→Ru in the chelate ring. Methods of preparation, analysis of stability and catalytic activity of such complexes are compared, and examples of the application of these organometallic ruthenium derivatives in the synthesis of practically relevant products are provided. The literature from 2010 to 2023 is summarized, making this review useful for a broad audience of chemists working in heterocyclic and organometallic chemistry, as well as practitioners involved in the production of catalysts and polymers.The bibliography includes 174 references.

Zuo X., Lin H., Song Z., Yu B., Zhao C.

Colorectal cancer (CRC) is an aggressive cancer type globally. Surgery and chemotherapy are often ineffective at curing CRC. Dictamnine is a natural product derived from Dictamnus dasycarpus Turcz. root bark and possesses multi-pharmacological properties, including anticancer effects. Nevertheless, the biological roles and the possible mechanism of dictamnine in CRC are still unclear. Here, we demonstrated that dictamnine blocked cell viability and proliferation in DLD-1 human colorectal adenocarcinoma cells and LoVo human colon cancer cells. Dictamnine triggered CRC cell ferroptosis, as evidenced by enhanced levels of reactive oxygen species, malondialdehyde, and Fe2+ levels, alongside downregulation of glutathione peroxidase 4 protein expression. In addition, CD163 (HPA ID: HPA046404) was highly expressed and CD68 (HPA ID: CAB000051) was lowly expressed in CRC tissues and CRC cell culture medium-cultured THP-1 monocytes-derived macrophages. The patients with CD163 low-expression lived much longer than those with CD163 high-expression, indicating that M2 polarization of macrophages was related to poor prognosis of CRC. Dictamnine markedly inhibited CD163 protein expression, transforming growth factor-β and arginase 1 mRNA expressions and IL-10 production in macrophages with CRC cell co-culture, suggesting that dictamnine impeded M2 polarization of macrophages. Mechanistically, dictamnine repressed ERK phosphorylation in CRC cells. The treatment with the ERK activator tBHQ counteracted the effects of dictamnine on CRC cell proliferation and ferroptosis, as well as its inhibitory effect on M2 polarization of macrophages. Results of a xenograft model showed that dictamnine effectively hindered CRC tumor growth in vivo. Collectively, these data provide evidence for the clinical trials of dictamnine as a novel drug for CRC therapy.

Wu T., Wang W.

Abstract: 2,3-Dihydrobenzofuran and coumaranone are readily available in numerous naturally occurring compounds. They mostly exist in plenty of food plants and medicinal plants. Such compounds constitute a series of flavor components and bioactive molecules. Their preparation has been an attractive field of research. In the past few decades, great efforts have been made in the preparation of the 2,3-dihydrobenzofuran structure through both metal-catalyzed and organocatalyzed ways. Visible light-promoted reactions sprang up in the early 21st century and represent a green manner of transformations. Under the irradiation of visible light, radicals could be generated under milder conditions. Thus, visible light-promoted reactions spread widely in the field of chemical synthesis. In recent years, visible light-promoted preparation of 2,3-dihydrobenzofuran and coumaranone has been developed by different groups, including both intramolecular and intermolecular reactions. The benign reaction conditions allow better functional group-tolerance and lead to diverse structures. Several reviews on the synthesis of 2,3-dihydrobenzofuran have been reported. However, visible light-promoted approaches to such structures have not been well reviewed. Our review will cover the literature that has been reported on the discovery of 2,3-dihydrobenzofuran in food and visible light-promoted preparation of 2,3- dihydrobenzofuran, attempting to summarize the existing methods and provide guidance to the chemists on the present challenges.

Yang J., Li W., Wang Q., Zhang J., Li M., Wang H., Gao R., Li Y., Ma S.

Shi J., Deng L., Li J., Wang M., Fan Y., Pan W., Hao X., Mu S.

AbstractThree new compounds, including two new sesquiterpenes (1–2), named Annuumine E−F, and one new natural product, 3‐hydroxy‐2,6‐dimethylbenzenemethanol (3), together with seventeen known compounds (4–20) were isolated from the ethanol extract of the roots of Capsicum annuum L. Among them, five compounds (4, 5, 9, 10 and 20) were isolated from this plant for the first time. The structures of new compounds (1–3) were determined via detailed analysis of the IR, HR‐ESI‐MS and 1D and 2D NMR spectra. The anti‐inflammatory activities of the isolated compounds were evaluated by their ability to reduce NO release by LPS‐induced RAW 264.7 cells. Notably, compound 11 exhibited moderate anti‐inflammatory activity (IC50=21.11 μM). Moreover, the antibacterial activities of the isolated compounds were also evaluated.

Mutinda E.S., Kimutai F., Mkala E.M., Waswa E.N., Odago W.O., Nanjala C., Ndungu C.N., Gichua M.K., Njire M.M., Gituru R.W., Hu G.

Plants have been used in various parts of the world to treat various diseases. The genus Zanthoxylum L. (Rutaceae) is the second largest genus of this family and comprises approximately 225-549 species distributed in the tropical and temperate regions of the world. Plants of this genus are trees and shrubs with various applications in folklore medicine for food, medicine, construction, and other uses.The goal of this review is to give an updated data on the ethnobotanical applications, phytochemistry, and pharmacology of the Zanthoxylum species to investigate their medicinal potential and identify research gaps for future research studies.Data was obtained through a systematic search of published literature and online databases such as Google Scholar, Web of Science, PubMed, Science Direct, and Sci-Finder. The botanical names were confirmed using the World Flora Online and chemical structures were drawn using the ChemBio Draw Ultra Version 14.0 Software.The Zanthoxylum species have a wide use in different parts of the continents as a remedy for various diseases such as digestive diseases, gastrointestinal disorders, venereal diseases, respiratory diseases, rheumatism, bacterial diseases, viral, and other diseases. Various parts of the plant comprising fruits, seeds, twigs, leaves, oils, and stems are administered singly or in the form of decoction, infusion, powder, paste, poultice, juice, or mixed with other medicinal plants to cure the disease. More than 400 secondary metabolites have been isolated and characterized in this genus with various biological activities, which comprise alkaloids, flavonoids, coumarins, lignans, alcohols, fatty acids, amides, sesquiterpenes, monoterpenes, and hydrocarbons. The crude extracts, fractions, and chemical compounds isolated from the genus have demonstrated a wide range of biological activities both in vivo and in vitro, including; anti-cancer, antimicrobial, anti-sickling, hepatoprotective, antipyretic, antitumor, and other pharmacological activities.This genus has demonstrated an array of phytoconstituents with therapeutic potential. The ethnobotanical uses of this genus have been confirmed in modern pharmacological research. This genus is a potential source for modern drug discovery and health care products. Further and extensive research is therefore required on the safety approval and therapeutic application of the species of this genus as well as clinical trials and pharmacokinetic studies.

Sulaiman M., Jannat K., Nissapatorn V., Rahmatullah M., Paul A.K., de Lourdes Pereira M., Rajagopal M., Suleiman M., Butler M.S., Break M.K., Weber J., Wilairatana P., Wiart C.

The emergence of multidrug-resistant bacteria and fungi requires the development of antibiotics and antifungal agents. This review identified natural products isolated from Asian angiosperms with antibacterial and/or antifungal activities and analyzed their distribution, molecular weights, solubility, and modes of action. All data in this review were compiled from Google Scholar, PubMed, Science Direct, Web of Science, ChemSpider, PubChem, and a library search from 1979 to 2022. One hundred and forty-one antibacterial and/or antifungal alkaloids were identified during this period, mainly from basal angiosperms. The most active alkaloids are mainly planar, amphiphilic, with a molecular mass between 200 and 400 g/mol, and a polar surface area of about 50 Å2, and target DNA and/or topoisomerase as well as the cytoplasmic membrane. 8-Acetylnorchelerythrine, cryptolepine, 8-hydroxydihydrochelerythrine, 6-methoxydihydrosanguinarine, 2′-nortiliacorinine, pendulamine A and B, rhetsisine, sampangine, tiliacorine, tryptanthrin, tylophorinine, vallesamine, and viroallosecurinine yielded MIC ≤ 1 µg/mL and are candidates for the development of lead molecules.

Hong K., Yang X., Zhang Z., Xie X., Lv X., Xu X., Hu W.

A Rh2(OAc)4 catalyzed intermolecular aldol-type interception of phenolic oxonium ylides with isatins has been developed, which provides an effective access to 2,2-disubstituted dihydrobenzofuran derivatives containing 3-hydroxyoxindole in high yields and with high diastereoselectivities under mild reaction conditions. The antiproliferation activity of these synthesized dihydrobenzofuran and 3-hydroxyoxindole hybrid products has been tested via the CCK8 assay in different cancer cell lines; compounds 3s and 3t exhibit good anticancer potency against human colon cancer cells (HCT116 cells, 3s: IC50 = 15.99 μM; 3t: IC50 = 14.48 μM) compared to other tested compounds.

Das S.

AbstractQuinoline derivatives are frequently found in natural products and biologically active compounds; however, construction of quinoline fused polyheterocycles is a challenging goal in synthetic organic chemistry. In this regard, quinolinium salts meet the demand to a great level, as they can be synthesized readily and employed effectively for rapid construction of the condensed heterocyclic core. The present review focuses on recent (2015–2021) applications of different quinolinium salts, which react with suitable partners to access diverse annulated products. Most of the reactions discussed here involve easily available starting materials, are operationally simple, offer high atom-efficiency, and are environmentally benign. Mechanistic aspects of representative transformations have also been highlighted to better understand the reaction pathways.1 Introduction2 Annulation Involving N-Alkyl Quinolinium Salts2.1 Reaction with Alkenes2.2 Reaction with Alkynes/Arynes2.3 Reaction with Phenolic Compounds2.4 Reaction with Cyclic/Acyclic Diketones2.5 Reaction with Amines/Cyclic Amines2.6 Reaction with Enamines2.7 Reaction with Isocyanoacetates2.8 Reaction with Cyclopropanes2.9 Ring Expansion Reactions3 Annulation Involving Quinolinium Zwitterionic Tosylates3.1 Reaction with Alkynes/Arynes3.2 Reaction with Allenes/Ketenes3.3 Reaction with Aldehyde-Amino Acid (Azomethine Ylide)3.4 Reaction with Sulfonium Salts3.5 Reaction with Diazoacetate4 Annulation Involving Quinolinium Zwitterionic Thiolates4.1 Reaction with Sulfonium Salts4.2 Reaction with Sulfenes4.3 Reaction with Arynes5 Annulation Involving Quinoline N-Oxides5.1 Reaction with Diynes and Ynones5.2 Lactonization Involving Acrylate6 Annulation Involving N-Iminoquinolinium Salts6.1 Reaction with Allenoates6.2 Reaction with Hydroxymethylallyl Carbonate7 Miscellaneous Cyclizations8 Conclusions

Shen Q., Zheng X., Li L., Zhong T., Yin C., Yu C.

A visible-light-induced photocatalyst-free three-component radical cascade bicyclization has been achieved to obtain diverse difluoroamidosulfonylated dihydrobenzofurans in moderate to good yields. This protocol avoids potential toxicity and the tedious removal procedure for photocatalysts and also features mild reaction conditions and a good functional group tolerance. Moreover, mechanistic investigations reveal the formation of a charge-transfer complex and the involvement of an intramolecular 1,5-hydrogen atom transfer process in this transformation.

Kotha S., Solanke B.U.

Benzofurans, 2H-chromenes and benzoxepines are key structural elements present in several natural products and pharmaceuticals. Here, we describe an easy-to-execute strategy for the synthesis of benzofurans, 2H-chromenes and benzoxepines, by employing Claisen rearrangement and ring-closing metathesis as key steps. A variety of phenols were converted into useful oxacycles in good to excellent yields. The ring-closing metathesis approach has been used to produce phenylpropanoid natural products. Examples described here include, the naturally occurring benzofurans such as 7-methoxywutaifuranal, 7-methoxywutaifuranol, 7-methoxywutaifuranate and the O-prenylated natural products like boropinic acid, boropinols A and C.

Swain S.S., Pati S., Hussain T.

Today, tuberculosis (TB) caused by the acid-fast bacilli, Mycobacterium tuberculosis (Mtb) is the most infectious killer disease globally with high morbidity and mortality rates. The rapid development of multi-drug-resistant (MDR) strains via intrinsic (efflux pumps) and acquired (biological mutations) mechanisms reduce the efficacy of applied anti-TB regimens. Nevertheless, only bedaquiline (BDQ) and pretomanid (PMD) were added to anti-TB therapy in the last decade. The existing anti-TB drugs also exhibited cytotoxicity and hepatotoxicity from long-term treatment. Thus, exploring or developing potential and less toxic anti-TB candidates, preferably natural-based candidates, is the call of the day. At present, 'quinoline' could be considered one of the versatile scaffolds presented in most mainstream medicines from comprehensive drug reports. Notably, BDQ with two clinically evaluating anti-TB candidates, TBJA-587 and DC-159a was motivated for utilizing quinoline heterocycles. Accordingly, we have selected 65 natural quinoline heterocycles bearing potential anti-TB agents (40 plant-derived and 25 marine-derived) within MIC value ≤ 50 μg/mL from an extensive literature search. Briefly, source, drug chemistry, structural activity relationship, prior pharmacokinetics profiles with drug-ability, toxicity, and hierarchical clustering analysis using various computational tools to identify the most 'drug-able lead' candidate is the uniqueness of the review. From extensive drug analysis, tetrandrine, 2'-nortiliacorinine, tiliacorine, globospiramine, evocarpine, allocuspareine from plant sources, and ecteinascidin 770, 6-hydroxymanzamine E, (-)-8-hydroxymanzamine A, ecteinascidin 786, manzamine F from marine sources are the most potential-cum-drug-able anti-TB candidates. We hope the systematic and critical drug analyses on quinoline-bearing natural anti-TB candidates are helpful to design potential-cum-less toxic anti-TB drugs in the future.

Lood K., Tikk T., Krüger M., Schmidt B.

Four combinations of type-I olefins isoeugenol and 4-hydroxy-3-methoxystyrene with type-II olefins acrolein and crotonaldehyde were investigated in cross-metathesis (CM) reactions. While both type-I olefins are suitable CM partners for this transformation, we observed synthetically useful conversions only with type-II olefin crotonaldehyde. For economic reasons, isoeugenol, a cheap xylochemical available from renewable lignocellulose or from clove oil, is the preferred type-I CM partner. Nearly quantitative conversions to coniferyl aldehyde by the CM reaction of isoeugenol and crotonaldehyde can be obtained at ambient temperature without a solvent or at high substrate concentrations of 2 mol·L-1 with the second-generation Hoveyda-Grubbs catalyst. Under these conditions, the ratio of reactants can be reduced to 1:1.5 and catalyst loadings as low as 0.25 mol % are possible. The high reactivity of the isoeugenol/crotonaldehyde combination in olefin metathesis reactions was demonstrated by a short synthesis of the natural product 7-methoxywutaifuranal, which was obtained from isoeugenol in a 44% yield over five steps. We suggest that the superior performance of crotonaldehyde in the CM reactions investigated can be rationalized by "methylene capping", i.e., the steric stabilization of the propagating Ru-alkylidene species.

Yang W., Liu P., Chen Y., Lv Q., Wang Z., Huang W., Jiang H., Zheng Y., Jiang Y., Sun L.

Uropathogenic Escherichia coli (UPEC) is the most common pathogenic bacteria associated with urinary tract infection (UTI). UPEC can cause UTI by adhering to and invading uroepithelial cells. Fimbriae is the most important virulence factor of UPEC, and a potentially promising target in developing novel antibacterial treatments. In this study, the antibacterial properties and effects of the compound dictamnine, extracted from the traditional Chinese medicine Cortex Dictamni, on the bacterial morphology, cell adhesion, and invasion of UPEC were studied. Dictamnine exhibited no obvious antibacterial activity against UPEC, but significantly impeded the ability of UPEC to adhere to and invade uroepithelial cells. RT-qPCR analysis showed that treatment downregulated the expression of type 1 fimbriae, P fimbriae, and curli fimbriae adhesion genes, and also downregulated adhesion-related receptor genes of uroepithelial cells. Transmission electron microscopy showed that dictamnine destroyed the structure of the fimbriae and the surface of the bacteria became smooth. These results suggest that dictamnine may help to prevent UTI by simultaneously targeting UPEC fimbriae and urothelial adhesin receptors, and may have a potential use as a new anti-UPEC drug.