Fallopia convolvulus (L.) Á. Löve: Review of traditional use, phytochemistry and pharmacology

Fallopia convolvulus (L.) Á. Löve: Review of traditional use, phytochemistry and pharmacology Zhanbota Akmuratkyzy1, Aknur Turgumbayeva1, Marzhan Kulbayeva2, Amirkan Azembayev3,4 , Zhanar Nurgaliyeva5, Roza Seisebayeva6, Gulshat Kulniyazova1, Kulyash Jaxalykova7, Bekturgan Karin7, Zhanar Aubakirova8, Bibigul Doskenova9, Marina Zhanaliyeva10 , Ruslan Zharikassimov11 , Zhanar Bukeyeva12 1 Higher School of Medicine, Al-Farabi Kazakh National University, Almaty 050040, Kazakhstan 2 Faculty of Biology and Biotechnology, Department of Biophysics, Biomedicine and Neuroscience, Al-Farabi Kazakh National University, Almaty 050040, Kazakhstan 3 JSC “Scientific Center for Anti-Infectious Drugs”, Almaty 050000, Kazakhstan 4 Department of organization, management and economics of pharmacy and clinical pharmacy, JSC “S.D. Asfendiyarov Kazakh National Medical University”, Almaty 050000, Kazakhstan 5 School of Pediatrics, Department of Outpatient Pediatrics, JSC “S.D. Asfendiyarov Kazakh National Medical University”, Almaty 050000, Kazakhstan 6 JSC “S.D. Asfendiyarov Kazakh National Medical University”, Almaty 050000, Kazakhstan 7 Department of Neonatology, NJSC “Astana Medical University”, Astana 010000, Kazakhstan 8 Department of Medical sciences, NJSC “Astana Medical University”, Astana 010000, Kazakhstan 9 Department of Pediatric diseases with courses in pulmonology and nephrology, NJSC “Astana Medical University”, Astana 010000, Kazakhstan 10 Department of Human Anatomy Republic of Kazakhstan, NJSC “Astana Medical University”, Astana 010000, Kazakhstan 11 Department of Surgical Diseases with a course of cardio-thoracic surgery and maxillofacial surgery, NJSC “Astana Medical University”, Astana 010000, Kazakhstan 12 Research Institute of Preventive Medicine named after Academician E.D.Dalenov, NJSC “Astana Medical University”, Astana 010000, Kazakhstan Corresponding authors: Zhanbota Akmuratkyzy (akmuratkyzyzha[email protected]); Aknur Turgumbayeva ([email protected]); Marzhan Kulbayeva (https://orcid.org/0000-0002-5622-8421) Received 14 May 2025♦ Accepted 14 September 2025♦ Published 27 October 2025 Citation: Akmuratkyzy Z, Turgumbayeva A, Kulbayeva M, Azembayev A, Nurgaliyeva Z, Seisebayeva R, Kulniyazova G, Jaxalykova K, Karin B, Aubakirova Z, Doskenova B, Zhanaliyeva M, Zharikassimov R, Bukeyeva Z (2025) Fallopia convolvulus (L.) Á. Löve: Review of traditional use, phytochemistry and pharmacology. Pharmacia 72: 1–12. https://doi.org/10.3897/pharmacia.72.e158944 Abstract Fallopia convolvulus (L.) Á. Löve, a widely distributed species of the Polygonaceae family, has long been valued in traditional medicine for its diverse therapeutic applications. This review investigates its phytochemical composition, traditional uses, and pharmacological potential, placing the plant in the broader context of natural product research. Bioactive compounds such as flavonoids, anthraquinones, steroids, and phenolic acids, which exhibit antioxidant, anti-inflammatory, antimicrobial, and anticancer activities, are compiled and analyzed. Modern techniques have identified novel compounds like falloconvolin A and B, as well as compounds with estrogenic and neuroprotective properties. To support this analysis, information was sourced from ethnobotanical, phytochemical, pharmacological, and clinical studies, utilizing databases like PubMed, Science Direct, and ResearchGate. This comprehensive analysis underscores the importance of further research to elucidate the mechanisms of action of its bioactive constituents and to explore its potential for pharmaceutical innovation. Fallopia convolvulus represents a promising, sustainable resource for developing novel therapeutic agents, bridging traditional medicine with modern science. Copyright Akmuratkyzy Z et al. This is an open access article distributed under the terms of the Creative Commons Attribution License (CC-BY 4.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. Pharmacia 72: 1–12 DOI 10.3897/pharmacia.72.e158944 Review Article Akmuratkyzy Z et al.: Fallopia convolvulus: traditional use, phytochemistry, and pharmacology2 Keywords Fallopia convolvulus, Polygonaceae, phytochemicals, flavonoids, pharmacological activities, traditional medicine Introduction Plants are natural sources that efficiently produce a wide variety of phytoconstituents with high selectivity. Since the mid-19th century, numerous bioactive phytoconstituents have been isolated and identified. Many of these compounds are now used as active ingredients in modern medicines or serve as lead compounds for the development of new drugs (Uddin et al. 2011). These compounds are produced through the primary or secondary metabolism of living organisms. Secondary metabolites are chemically and taxonomically diverse compounds whose functions are not fully understood. They are extensively utilized in human medicine, veterinary care, agriculture, scientific research, and many other fields (Vasu et al. 2009). Plant products have been used in phytomedicines for centuries, sourced from barks, leaves, flowers, roots, fruits, and seeds. Understanding the chemical constituents of plants is important, as this knowledge can aid in the synthesis of complex chemical compounds (Wadankar et al. 2022). Given their importance in the context mentioned above, it is crucial to screen the chemical and pharmacological properties of plants to discover and develop new therapeutic agents with enhanced efficacy (Yadav et al. 2014). Fallopia convolvulus (L.) Á. Löve, commonly referred to as black bindweed, is a species within the Polygonaceae family, which encompasses approximately twenty species. Most species of this genus are predominantly distributed in the northern temperate zone (Nimanthika 2014; Meng et al. 2021). F. convolvulus is a prevalent ruderal species in agroecosystems, including cultivated fields, gardens, and orchards. It can also be found in disturbed habitats such as wastelands, thickets, and along roadsides. Occasionally, it occurs along riverbanks and in pastures (Hume et al. 1983). F. convolvulus is indigenous to Eurasia and is widespread across Canada and the United States (Royer and Dickinson 1999). F. convolvulus has also been introduced to Africa, South America, Australia, New Zealand, and Oceania. It has been recorded in all three ecogeographic regions of Alaska (Klein 2011). F. convolvulus is an annual, climbing herb with slender, deep roots. The stems are delicate and can reach up to 91 cm in length, with long internodes. They exhibit free branching from the base and may sometimes display a reddish hue. The stems either trail along the ground or twine around neighboring plants. The leaves are alternate, ranging from 2.5 to 4 cm in length, and are elongate-ovate or sagittate in shape, with long petioles and basal lobes pointing backward. The leaves emerge from papery sheaths that encase the stems. The flowers are small, inconspicuous, measuring up to 6 mm in length, and are arranged in short axillary clusters of two to six. The fruits are triangular achenes, characterized by obtuse bases and pointed apices (Flora of North America Editorial Committee 1993; Royer and Dickinson 1999). Species of Fallopia are native to Asia, but they are now widespread across various regions globally. In Europe, these taxa were introduced in the 19th century for ornamental purposes (Kallenberger et al. 2016). Species within the Polygonaceae family have been recognized as medicinal plants in Asia since ancient times. For instance, members of the genus Calligonum L. have been utilized for treating infections, invasions, and immune system disorders. The primary region of origin and distribution for many Calligonum species is the Iran-Turan area. Out of the 80 species in the genus, 30 are found in Kazakhstan. The roots of the species from Acanthophyllum Mey (Caryophyllaceae) have been traditionally used in Central Asian medicine for wound healing and as expectorants. The plant’s constituents exhibit sedative, antisclerotic, and antimicrobial properties. This genus is native to southwestern Asia, particularly in areas bordering Iran and Afghanistan. Of the 50 species identified in Western Asia and the Iran-Turan region, 10 occur in Kazakhstan. Rheum wittrockii Lunstr was historically used by Kazakhs to treat gastroenteric and dermatological conditions, while Rheum altaicum Losinsk was employed as an anti-inflammatory and for treating skin diseases (Ryabushkina et al. 2008). Chemotaxonomic studies of the Fallopia genus have shown that all species possess flavonoids with a largely uniform profile, with quercetin glycosides being the primary components (Kim et al. 2000a; Kim et al. 2000b). The flavonoid composition of F. convolvulus includes glycosides of quercetin, kaempferol, myricetin, apigenin, luteolin, rhamnetin, and isorhamnetin (Kim et al. 2000a; Smolarz 2002). Additionally, three distinctive flavonoid structures have been identified in this species: falloconvolin A and B, and quercetin-3-O-(2-E-esinapoxyl)-glucopyranoside (Zhang et al. 2011). Among the primary phytochemicals, tannins, phenolic acids, flavonoids, stilbenes (e.g., resveratrol), and anthraquinones (e.g., emodin) stand out for their diverse physiological and therapeutic effects. Numerous species within this genus are utilized as herbal remedies in traditional Chinese medicine, such as Fallopia multiflora (Thunb.) Harald. and Fallopia denticulata (Huang) A. J. Li, for treating conditions like inflammation, insomnia, infection, arthritis, and diarrhea (Meng et al. 2021). Knotweed has historically been employed in Asia for the treatment of skin burns, gallstones, hepatitis, inflammation, and osteomyelitis (Shen et al. 2011). In traditional Chinese and Japanese medicine, the rhizomes of certain species are used to treat hepatitis, hypertension, skin injuries, and bleeding. Recent studies have investigated the antibacterial, antifungal, antioxidant, anti-inflammatory, and neuroprotective properties of these plants. Pharmacia 72: 1–12 3 Preliminary pharmacological data also suggest potential benefits in managing high cholesterol and certain types of cancer. Some species exhibit metal-binding properties and allelopathic effects, while others are being explored for agricultural applications, such as fodder production. The potential use of Fallopia species as energy plants is supported by their high calorific value. These findings underscore the need for further ecological, phytochemical, and pharmacological research to explore the broad potential applications of these plants (Kallenberger et al. 2016). Materials and methods Data from ethnobotanical, phytochemical, pharmacological, and clinical sources were gathered from various online journals, books, and magazines published between 1970 and 2024. Electronic databases such as Google Scholar, PubMed, Science Direct, ResearchGate, and other digital repositories were utilized for this research. Keywords such as Fallopia convolvulus, Polygonaceae, Fallopia convolvulus pharmacological activities, phytochemistry and related species were employed in these databases to explore their pharmacological and ethnomedicinal applications, which are discussed in this manuscript. Taxonomic classification of F. convolvulus within the Polygonaceae family The Polygonaceae is a family of angiosperms commonly known in the United States as the knotweed or smartweed-buckwheat family. The designation is derived from the genus Polygonum and was first introduced by Antoine Laurent de Jussieu in 1789 in his work Genera Plantarum. The name is attributed to the numerous swollen nodes found on the stems of certain species. It originates from Greek, where «poly» means «many» and «goni» refers to «knee» or «joint» (Jussieu 1789). The Polygonaceae family comprises around 50 genera and approximately 1200 species (David 2008). These species can be annual herbs, perennial herbs, shrubs, trees, or lianas. The leaves, which arise from often swollen nodes, are typically alternate, though they can sometimes be opposite or whorled, simple, and petiolate or sessile, with generally entire margins. The stipules are almost always well-developed, fused within a tubular sheath that can be persistent or deciduous, hyaline to membranous, bilobed, or fringed at the apex, referred to as the ocrea. The ocrea is a unique feature of the Polygonaceae family, though it may be reduced or absent in the subfamily Eriogonoideae. Extrafloral nectary pits are located at the base of the petioles and in the nodal areas of genera such as Fallopia (including Reynoutria) and Muehlenbeckia. The inflorescences are axillary or terminal, consisting of simple or branched thyrsi, panicle-like, racemose, or spike-like structures that form dichasia or helicoid cymes. Each partial inflorescence is subtended by bracts, and each flower or cluster of flowers is accompanied by a persistent membranous ocreola, which corresponds to the fusion of the bracteoles. The flowers are small, trimerous, and hermaphroditic or unisexual (with dioecy being common). The tepals number 2–6, are often persistent, and may enlarge in fruit, fused at the base within a somewhat developed hypanthium, forming two whorls of three elements or one whorl of five elements. In the latter case, the tepal arises from the fusion of one segment of the outer whorl with one from the inner whorl, resulting in characteristic quincuncial aestivation. The stamens are typically equal in number to, or double or triple the number of tepals, ranging from 2 to 9, rarely more, and may be free or basally connate, alternating with the tepals. Pollen is typically tricolporate or pantoporate. Nectaries are often present, located between the bases of the filaments or fused into an annular disc at the base of the ovary. The ovary is superior, generally 2-4-carpellate (most often 3-carpellate), unilocular; styles are 1-3, free or proximally connate, with filiform, peltate, or capitate stigmas, which may be entire or fringed. The ovules are unique. The fruit is an achene, often trigonous or lenticular, typically subtended by an enlarging perianth, and more specifically classified as a diclesium (Spjut 1994). Some species such as Fagopyrum (buckwheat) and Coccoloba (sea grape) produce edible fruit; the petioles of Rheum (rhubarb) are edible, as are the leaves of certain Rumex species (sorrel). The rhizomes of Rheum are also valued for their medicinal properties. Additionally, some genera contain ornamental species and common weeds. The Polygonaceae family is notably diverse in temperate regions of North America, Europe, and Southeast Asia, while having fewer representatives in South America, the Caribbean, Africa, and Australasia. Tropical species within the family are often woody shrubs, trees, or lianas. Several members of the Polygonaceae are recognized as problematic weeds, including Japanese knotweed (Reynoutria japonica), spiny three-corner jack (Emex spinosa L.), dock (Rumex L.), mile-a-minute (Persicaria perfoliata L.), and corallita (Antigonon leptopus). There are also crop species of minor economic significance, such as rhubarb (Rheum rhabarbarum L.) and buckwheat (Fagopyrum esculentum) (Ortiz 1994). The largest genera include Eriogonum (240 species), Rumex (200 species), Coccoloba (120 species), Persicaria (100 species), and Calligonum (80 species) (Freeman and Reveal 2005; Sanchez and Kron 2008). The classification of the Polygonaceae has primarily relied on macromorphological features, such as the presence or absence of an ocrea, woodiness, and the arrangement of tepals. However, the classification system has been widely debated, leading to numerous proposed taxonomic schemes (Decraene and Akeroyd 1988). Numerous studies utilizing molecular data have confirmed that the Polygonaceae family is monophyletic. However, only recently have molecular studies begun to explore the large-scale phylogenetic relationships within the family (Lledό et al. 1998; Cuénoud et al. 2002; Chase et al. 2002). The Polygonaceae Akmuratkyzy Z et al.: Fallopia convolvulus: traditional use, phytochemistry, and pharmacology4 is currently divided into three subfamilies: Eriogonoideae Arn., Polygonoideae Eaton, and Symmerioideae Meisn. (Haraldson 1978; Brandbyge 1993). The subfamilies Eriogonoideae and Polygonoideae do not align with many of the traditional classifications and were newly defined by Sanchez and Kron in 2008. Some surprising results emerged in the circumscription of these subfamilies when compared to traditional treatments based on morphological data. For example, genera within Coccolobeae, such as Fallopia, Harpagocarpus, Muehlenbeckia, and Reynoutria, were found to belong to Polygoneae (Sanchez and Kron 2008; Sanchez and Kron 2009). The phylogenetic relationship between Fallopia and Reynoutria has been a subject of ongoing debate, with some researchers suggesting that these two genera are so closely related that they should be considered synonymous. Authors such as Ronse De Craene and Akeroyd (1988), Bailey and Stace (1992), and Yonekura and Ohashi (1997) included Reynoutria within Fallopia. In contrast, other scholars, including Nakai (1926), Holub (1970), Haraldson (1978), Tzvelev (1987, 1989), and Brandbyge (1993), argued that the genera should remain distinct (Schuster et al. 2011). Muehlenbeckia has long been considered closely related to Fallopia and Reynoutria, yet its status as a separate genus was never questioned. Molecular studies have revealed that Fallopia is more closely related to Muehlenbeckia than to Reynoutria, suggesting that the latter should be treated as a distinct genus (Sanchez and Kron 2009; Schuster et al. 2011; Sanchez et al. 2011). Fallopia Adans. is a relatively small but highly variable genus with approximately 16 species (Kim et al. 2000a). The knotweed complex includes Black bindweed (Fallopia convolvulus (L.) Á. Löve), Japanese knotweed (Fallopia japonica (Houtt.)), a dwarf variant of Japanese knotweed (Fallopia japonica var. compacta (Hook.f.)), giant knotweed (Fallopia sachalinensis (F. Schmidt) Ronse Decr.), and their hybrid, Bohemian knotweed (Fallopia × bohemica (Chrtek and Chrtková)), among others (Drazan et al. 2021). In Fig. 1 provided a taxonomic classification of Fallopia species. A taxonomic investigation aims to classify, identify, and determine the systematic placement of plant species. It involves the examination of morphological, molecular, and genetic traits to elucidate their phylogenetic relationships within the family. This analysis enhances the understanding of the specie’s evolutionary lineage and its ecological adaptations. The integration of various data sources, including macroand micromorphological features, pollen morphology, and molecular markers, allows for the construction of a detailed phenotypic profile for multiple species within the Polygonaceae family. Evaluating these characteristics offers essential insights into the phylogenetic and phenetic connections among family members, elucidating the extent of their relatedness. Such comprehensive data are vital for precise species identification and resolving ambiguities due to phenotypic or ecotypic variation (Kosal 2023). Traditional use The genus Fallopia is renowned in traditional medicine, with extracts commonly used to treat conditions such as hepatitis, hepatic damage, inflammation, and post-menopausal disorders (Zhang et al. 2006a; Zhang et al. 2007; Chen et al. 2011; Liao et al. 2011) (Table 1). Bioactive compounds isolated from the rhizomes of Fallopia species have shown vasorelaxant, antioxidant, antibacterial, anti-inflammatory, and anti-tumor activities, contributing to the widespread use of Fallopia in traditional Chinese medicine. Several polyphenolic compounds with phytoestrogenic activity have been identified in the roots and rhizomes of various Fallopia species, including F. multiflorum and F. japonica (Frémont 2000; Matsuda et al. 2001; Zhang et al. 2005; Li-Shuang et al. 2006; Zhang et al. 2006b; Avula et al. 2007; Noda et al. 2009; Shen et al. 2011; Liao et al. 2011). Many of these phytoestrogens preferentially activate estrogen receptor beta (ERβ) over estrogen receptor alpha (ERα), and diets rich in phytoestrogens have been associated with a reduced incidence of hormone-related cancers, such as breast and prostate cancers (Adlercreutz 2002; Harris et al. 2005). ERβ activation has been shown to exert an antiproliferative effect in breast cells, providing a protective balance against ERα activation, which is linked to cellular proliferation (Sotoca Covaleda et al. 2008; Sotoca et al. 2008; Williams et al. 2008). Recent research further supports F. convolvulus’s medicinal value, uncovering a broader range of pharmacological activities, including anti-fungal and neuroprotective effects. Phytochemicals are isolated from F. convolvulus Phytochemicals are bioactive compounds derived from plants that offer health and therapeutic benefits, including the prevention and treatment of various diseases. Naturally occurring in foods, these substances work synergistically, enhancing their potential to combat infections (Khaliq et al. 2023). Scientists globally have investigated F. convolvulus, isolated numerous phytochemicals and conducted biological assays to evaluate their effects. A summary of the compounds isolated from F. convolvulus to date is presented in Table 2. Although F. convolvulus has a long history of medicinal use, its chemical constituents began to be studied relatively recently. However, research into the isolation of bioactive molecules continues, with new compounds being discovered each year. For instance, in China, researchers isolated twenty compounds from an 85% ethanol extract of F. convolvulus roots. These included three sterols, three phenols, four anthraquinones, one chromone, two stilbenes, three amides, three flavonoids, and one organic acid. Modern phytochemical isolation techniques were employed, and the structures of these compounds were determined using Pharmacia 72: 1–12 5 Figure 1. The phylogenetic tree of Fallopia species from the Polygonaceae family derived from a literature review. spectroscopic methods and compared with existing data in the literature (Li et al. 2019). Additionally, a team of scientists isolated twenty-one flavonoid compounds from the leaves of F. convolvulus, identifying them as glycosylated derivatives of the flavonols kaempferol, quercetin, and myricetin, and the flavones apigenin and luteolin. Among these, quercetin 3-O-galactoside and quercetin 3-O-glucoside were found to be the major flavonoid constituents (Kim et al. 2000a). Flavonoids are known for their anti-inflammatory, antiviral, antitumor, and antibacterial activities (Agrawal 2011). Furthermore, twelve compounds were isolated from the herbs of F. convolvulus using Sephadex LH20 column chromatography. These compounds, identified through physicochemical properties and spectroscopic evidence, included quercetin, luteolin, chrysoeriol, apigenin, kaempferol-3-O-beta-D-glucoside, quercetin-3-O-rhamnoside, N-trans-coumaroyl tyramine, loliolide, ethylparaben, beta-sitosterol, daucosterol, and n-hexadecanoic acid. Akmuratkyzy Z et al.: Fallopia convolvulus: traditional use, phytochemistry, and pharmacology6 Notably, quercetin-3-O-rhamnoside, N-trans-coumaroyl tyramine, loliolide, and ethylparaben were isolated from the Fallopia genus for the first time (Chen et al. 2010). The structures of biologically active compounds isolated from F. convolvulus are presented in Fig. 2. The researchers identified three novel flavonoids: falloconvolin A, falloconvolin B, and quercetin-3-O-(2-E-sinapoxyl)-glucopyranoside, together with 17 known phenolic compounds, which were isolated from the active ethyl acetate (EtOAC) extract. Their structures were determined using spectroscopic methods and based on literature data (Zhang et al. 2011). There is limited information available in databases regarding their structures and pharmacological properties. Phenolic compounds are a diverse group of chemicals characterized by the presence of a phenol ring. These compounds exhibit a range of biological activities, although the precise mechanisms underlying their disease-preventive effects remain unclear. Their primary pharmacological property is antioxidant activity, although numerous studies have also reported their anti-inflammatory, anti-aging, antiproliferative, and antioxidant effects. Antioxidant enzymes play a key role in mitigating oxidative damage (Rahman et al. 2021). In addition, the research team isolated emodin and a novel flavan-3-ol, (-)-epiafzelechin-3-O-p-coumarate (rhodoeosein), from the roots of F. convolvulus. The absolute stereochemistry of rhodoeosein was determined using 1D and 2D Nuclear Magnetic Resonance (NMR), optical rotation, and circular dichroism. Emodin was identified through High-performance liquid chromatography with diode array detection (HPLC/DAD), Liquid chromatography with tandem mass spectrometry (LC/MS/MS), and Fourier transform ion cyclotron resonance mass spectrometry (FT/ICR-MS) (Brennan et al. 2013). Phytochemical analysis of F. convolvulus identified the presence of steroids, anthraquinones, flavonoids, chromones, and amides. As a result, the plant’s composition showcases a wide range of pharmacological properties, emphasizing its considerable potential in natural medicine. These compounds, commonly linked to antioxidant, Table 1. Medicinal properties of F. convolvulus. Plant Medicinal properties Activity mechanism References F. convolvulus anti-tumor Inhibition of cell growth, inhibition of protein kinase activities, induction of apoptosis, inhibition of metalloproteinases secretion, inhibition of tumor cell invasion, inhibition of adhesion/spreading of cells Kanadaswami et al. 2005 anti-inflammatory suppression of proinflammatory gene expression, inhibition of proinflammatory cytokine production and chemotactic agents Alshalmani 2011 antibacterial disruption of cell membranes, inhibition of nucleic acid synthesis, suppression of key bacterial enzymes, efflux pump inhibition, prevention of biofilm formation Rodríguez et al. 2023 antioxidant neutralization of free radicals via redox reactions, direct scavenging of free radicals, metal ion chelation, inhibition of oxidases, activation of antioxidant enzymes Sanjay and Shukla 2021 vasorelaxant stimulation of O₂⁻ production in endothelial cells and scavenging of O₂⁻ in interstitial fluid, reduction of cytosolic Ca²⁺ in smooth muscle cells Alshalmani 2011 Table 2. Biologically active compounds are found in F. convolvulus. Chemical class Chemical compounds Part of the plant Country References Flavonoids (flavonol aglycones) kaempferol leaf South Korea Kim et al. 2000a quercetin myricetin Flavonoids (flavone aglycones) apigenin leaf South Korea Kim et al. 2000a luteolin chrysoeriol herbs China Chen et al. 2010 Flavonoids (flavonol glycosides) quercetin 3-O-galactoside leaf South Korea Kim et al. 2000a quercetin 3-O-glucoside quercetin 3-O-rhamnoside herbs China Chen et al. 2010 kaempferol 3-O-beta-D-glucoside herbs China Chen et al. 2010 Flavonoids (flavan-3-ol) 2,3-cis-(2R, 3R)-(−)-epiafzelechin-3-O-pcoumarate (rhodoeosein) seed USA Brennan et al. 2013 Alkaloid (amide) N-trans-coumaroyl tyramine herbs China Chen et al. 2010 Lactones (monoterpene lactones) loliolide herbs China Chen et al. 2010 Parabens ethylparaben herbs China Chen et al. 2010 Steroids beta-sitosterol herbs China Chen et al. 2010 daucosterol Fatty acids n-hexadecanoic acid herbs China Chen et al. 2010 Polyphenols (anthraquinones) emodin seed USA Brennan et al. 2013 Pharmacia 72: 1–12 7 Figure 2. The structures of biologically active compounds isolated from F. convolvulus: 1. Kaempferol; 2. Quercetin; 3. Myricetin; 4. Apigenin; 5. Luteolin; 6. Quercetin 3-O-galactoside; 7. Quercetin 3-O-glucoside; 8. Chrysoeriol; 9. Kaempferol-3-O-beta-D-glucoside; 10. Quercetin-3-O-rhamnoside; 11. Loliolide; 12. Ethylparaben; 13. Beta-sitosterol; 14. Daucosterol; 15. 2,3-cis-(2R,3R)-(−)- epiafzelechin-3-O-p-coumarate (rhodoeosein); 16. n-hexadecanoic acid; 17. Emodin. Akmuratkyzy Z et al.: Fallopia convolvulus: traditional use, phytochemistry, and pharmacology8 anti-inflammatory, and anticancer effects, offer promising opportunities for pharmaceutical research and the creation of new therapeutic agents. The ongoing discovery of novel compounds further broadens the therapeutic applications of Fallopia, underscoring its potential integration into contemporary pharmaceutical practices. Pharmacology activities of F. convolvulus The exploration of numerous plant species for their phytochemical content and pharmacological properties remains limited, presenting a crucial gap in current research. Future studies on the bioactive compounds in F. convolvulus are necessary to gain a deeper understanding of their molecular actions both in vivo and in vitro and to ensure their safety for human consumption. Consequently, the accumulation of data regarding the pharmacological properties of F. convolvulus is expanding continuously. For instance, recent studies have elucidated two novel pharmacological activities of F. convolvulus. Table 3 summarizes several pharmacological properties associated with the bioactive compounds identified in this plant. Anticancer activity Cancer is a term used to describe a diverse group of diseases characterized by the uncontrolled and abnormal proliferation of cells, which can invade and damage normal body tissues. These cells often possess the ability to metastasize, spreading throughout the body. Cancer is the second leading cause of death globally, highlighting the urgent need for effective therapeutic interventions. F. convolvulus and F. dumetorum comprised stems, leaves, flowers, and fruits, whereas F. aubertii included flowers (AF), as well as stems and leaves (AH). These plant components were subjected to extraction using three solvents: ethanol (EtOH), 50% ethanol (EtOH 50%), and water (H2O) under reflux conditions. The resulting extracts were concentrated using a rotary evaporator (RVO 004; Ingos, Prague, Czech Republic) and lyophilized at -55 °C (CoolSafe ScanVac 55; LaboGene, Lynge, Denmark). For cell culture experiments, the extracts (AFha, AFe, AFw, and AHha) were reconstituted in dimethyl sulfoxide (DMSO) at a final concentration of 100 mg/ml and stored at -20 °C. Serial dilutions were made to achieve concentrations of 3, 30, 100, and 300 µg/ml. The highest cytotoxicity to cancer cells was observed in extracts derived from F. convolvulus, indicating its potential for further therapeutic investigation (Olaru et al. 2015). Antifungal activity The fungus Xylaria sp. Z184, isolated for the first time from the leaves of F. convolvulus, led to the discovery of several novel compounds. These include three new pyranone derivatives, named fallopiaxylaresters A–C, a new bisabolane-type sesquiterpenoid called fallopiaxylarol A, and the Table 3. Pharmacological activities of bioactive compounds identified in F. convolvulus. № Chemical compounds Pharmacological activities References 1 kaempferol anti-carcinogenic, antibacterial, antifungal, antiprotozoal Periferakis et al. 2022 2 quercetin antioxidant, anti-inflammatory, anti-tumor Haghi et al. 2017 3 myricetin hepatoprotective, antitumour, antiinflammatory, analgesic, and antidiabetic Imran et al. 2021 4 apigenin anti-inflammatory, anti-tumor, anti-oxidation, neuroprotection, antibacterial Li et al. 2023 5luteolin antioxidant, antidiabetic Kozlovskaya et al. 2022 6 quercetin 3-O-galactoside antioxidant, hepatoproective, antimicrobial, anti-ostoporotic Karadeniz et al. 2023 7 quercetin 3-O-glucoside antihistamine, anti-inflammatory, anticarcinogenic Razavi et al. 2009 8 chrysoeriol anticancer, anti-hyperlipidemic, antioxidant Aboulaghras et al. 2022 9 kaempferol-3-O-beta-D-glucoside antioxidant, anticancer, anticoagulant Demydiak et al. 2023 10 quercetin-3-O-rhamnoside antioxidant, anti-inflammatory Cui et al. 2022 11 N-trans-coumaroyl tyramine anti-diabetic Qais et al. 2018 12 loliolide anti-viral, anti-inflammatory Park et al. 2018 13 ethylparaben estrogenic, antiandrogenic Gao et al. 2020 14 beta-sitosterol antimicrobial, anticancer, antioxidant Ambavade et al. 2014 15 daucosterol anticancer, anti-hyperlipidemic, antioxidant El Omari et al. 2022 16 n-hexadecanoic acid antioxidant, antibacterial Purushothaman et al. 2024 17 falloconvolin A – – 18 falloconvolin B – – 19 quercetin-3-O-(2-E-sinapoxyl)- glucopyranoside – – 20 2,3-cis-(2R,3R)-(−)-epiafzelechin-3-Op-coumarate (rhodoeosein) estrogen activity Brennan et al. 2013 21 emodin antiviral, anti-ulcerogenic, anticancer Hsu and Chung 2012 Pharmacia 72: 1–12 9 first complete set of spectroscopic data for the previously identified pestalotiopyrone M. Additionally, a range of known compounds were isolated, consisting of six pyranone derivatives, three sesquiterpenoids, three isocoumarin derivatives, and one aromatic allenic ether. The biological activities of these compounds were investigated, with a focus on their anti-inflammatory, antimicrobial, and α-glucosidase-inhibitory effects. In vitro bioassays revealed that compounds 5, 7, and 8 exhibited weak growth inhibition against Staphylococcus aureus ssp. aureus, while the crude fungal extract demonstrated a potent ability to inhibit nitric oxide (NO) production in LPS-stimulated RAW 264.7 mouse macrophages, with an inhibition rate of 77.28 ± 0.82% at 50 μg/mL. However, none of the isolated compounds displayed similar inhibitory effects on no production, suggesting that other structural types of compounds in the extract may be responsible for the observed anti-inflammatory activity. This study not only identifies four novel compounds but also expands the understanding of the structural diversity within the Xylaria metabolomes (Zhang et al. 2024). Estrogenic activity The estrogenic properties of seeds from Fallopia species have not been previously investigated, precluding direct comparisons with seeds of other Fallopia species. However, extracts of seeds from F. convolvulus and F. dumetorum were analyzed for estrogenic activity using the human ovarian carcinoma cell line BG1Luc4E2. Following the initial screening, the F. convolvulus seed extract was subjected to crude fractionation by normal-phase chromatography, and the resulting fractions (equivalent to 8 mg of seeds per mL) were evaluated for estrogenic activity in the BG1Luc4E2 cell line. The estrogenic compounds within the seeds were hypothesized to exhibit both polar and nonpolar characteristics, as active fractions were eluted with solvents ranging from 20% ethyl acetate in n-hexane to 5% ethanol in ethyl acetate. Estrogenic potency of the crude fractions was quantified relative to an E2-dependent luciferase induction standard curve (data not shown), following the protocol described by Natarajan et al. (Natarajan et al. 2002). Crude fractions 3, 4, and 6 of F. convolvulus exhibited estrogenic potencies of 0.21, 2.4, and 0.76 nM E2 equivalents per gram of seed, corresponding to 4 ± 0.6%, 39 ± 1%, and 16 ± 1% of maximal E2 activity, respectively. The estrogenic activity of rhodoeosein was assessed in two human cell lines, where its cell-type-specific effects were demonstrated. To the best of our knowledge, rhodoeosein is the first reported flavan-3-ol to exhibit estrogenic properties in vitro. In addition to rhodoeosein, F. convolvulus seeds were found to contain emodin, a wellknown and potent estrogenic compound. Both rhodoeosein and emodin were also detected in the closely related species F. dumetorum. Analysis of the relative estrogenic potencies (REP) of emodin and rhodoeosein in SKBR3 cells transfected with either ERα or ERβ revealed that both phytoestrogens exhibit greater potency in ERβ-transfected cells compared to ERα-transfected cells. Furthermore, emodin displayed higher potency than rhodoeosein across both estrogen receptor subtypes. The in vivo effects of these compounds have not yet been investigated; however, the complex polyphenolic composition of F. convolvulus seeds suggests potential therapeutic applications (Brennan et al. 2013). Conclusions Fallopia convolvulus (L.) Á. Löve, from the Polygonaceae family, shows strong pharmacological potential due to its rich content of flavonoids, anthraquinones, steroids, and phenolic compounds. Modern studies confirm its traditional use for treating inflammation, infections, and liver disorders, and reveal additional antioxidant, anti-inflammatory, anticancer, estrogenic, antimicrobial, and neuroprotective effects. Notable compounds like falloconvolin A and B, along with quercetin and kaempferol, enhance its value, particularly for cardiovascular and metabolic diseases. Its ecological adaptability makes it a sustainable resource for drug development. However, further research is needed to fully understand its bioactive mechanisms and integrate it into modern medicine. Additional information Conflict of interest The authors have declared that no competing interests exist. Ethical statements The authors declared that no clinical trials were used in the present study. The authors declared that no experiments on humans or human tissues were performed for the present study. The authors declared that no informed consent was obtained from the humans, donors or donors’ representatives participating in the study. The authors declared that no experiments on animals were performed for the present study. The authors declared that no commercially available immortalised human and animal cell lines were used in the present study. Use of AI No use of AI was reported. Funding No funding was reported. Author contributions Conceptualization, Z.A. (Zhanbota Akmuratkyzy), A.A. and M.K.; writing-original draft preparation, Z.A. (Zhanbota Akmuratkyzy); writing-review and editing, Z.A. (Zhanbota Akmuratkyzy); visualization, A.A., Z.N., R.S., G.K. and K.J.; supervision, A.T.; project administration, B.K., Z.A. (Zhanar Aubakirova) and B.D.; funding acquisition, M.Z., R.Z. and Z.B. All authors have read and agreed to the published version of the manuscript.