This review provides a comprehensive overview of the chemical classification, pharmacological mechanisms, and clinical translation of major metabolites derived from T. wilfordii that highlight their application in autoimmune diseases, cancer, fibrosis, and metabolic disorders, while addressing current challenges in safety, solubility, and bioavailability.
Abstract
Tripterygium wilfordii, a traditional Chinese botanical drug, has emerged as a rich source of bioactive metabolites with promising therapeutic potential. Among its metabolites, diterpenoids and triterpenoids—such as triptolide, triptonide, and celastrol—exhibit potent immunosuppressive, anti-inflammatory, and anti-tumor properties through modulation of key molecular pathways including NF-κB, JAK/STAT, and TGF-β/Smad. This review provides a comprehensive overview of the chemical classification, pharmacological mechanisms, and clinical translation of major metabolites derived from T. wilfordii. It highlights their application in autoimmune diseases, cancer, fibrosis, and metabolic disorders, while addressing current challenges in safety, solubility, and bioavailability. Advancements in drug delivery systems, structural modification, and precision medicine approaches are also discussed. Together, these insights aim to guide future research and translational development of T. wilfordii-based compoundic therapeutics.
Natural products play a crucial role in the discovery of new medications and sustainable health innovations. Daphnoretin (DAP) is a naturally occurring biscoumarin found in different plant families. It has emerged as a potent phytochemical with diverse bioactivities, including anticancer, antiviral, antidiabetic, antigout, antimicrobial, nematocidal, anti-inflammatory, and kinase-modulating activities. The current review provides an in-depth overview of DAP, including its botanical sources, isolation and separation techniques, identification, structural characterization, and analytical and pharmacokinetic studies. This review discusses the reported pharmacological activities of these compounds, focusing on the underlying molecular mechanisms and the signaling pathways involved. It also summarizes the current knowledge of its bioactivities, with a special focus on its anticancer potential and the underlying mechanisms. Collectively, the available evidence not only underscores DAP's potential as a promising lead compound in drug discovery for cancer, viral infections, and metabolic and neurological disorders but also supports multiple Sustainable Development Goals (SDGs), particularly SDG 3 (Good Health and Well-being), SDG 9 (Industry, Innovation, and Infrastructure), and SDG 15 (Life on Land). This work also highlights future directions and main research gaps that could facilitate the translation of DAP into clinically relevant applications.
S. Ibrahim, H. M. Mohamed, A. Ibrahim et al.· Fitoterapia· 0 citations
Traditional medicinal plants continue to serve as important sources of therapeutic agents due to their diverse bioactive compounds and generally favorable safety profiles. This review aims to comprehensively summarize the ethnomedicinal uses, phytochemical constituents, and therapeutic activities of Lycopodium cernuum, highlighting its potential for drug development. A systematic search of major scientific databases and authoritative references was conducted with no a priori restriction on publication year or language, yielding 50 eligible articles published between 1948 and 2024. L. cernuum has been widely utilized in traditional medicine systems across Asia, Latin America, and other regions to manage conditions related to inflammation, metabolic disorders, infections, and cancer-associated symptoms. Phytochemical investigations have identified diverse secondary metabolites, particularly alkaloids, flavonoids, phenolics, and terpenoids, which are proposed to underlie its pharmacological effects. Preclinical evaluations indicate that L. cernuum exerts multi-target activities on inflammatory, oxidative, metabolic, infectious, and immune pathways, including anti-inflammatory, antioxidant, antimicrobial, anticancer, antiviral, antidiabetic, antiplatelet, and immunomodulatory effects, thereby providing mechanistic support for several of its traditional uses. Preliminary toxicological studies suggest a relatively wide safety margin at commonly tested doses. Nevertheless, the current evidence base is limited by a predominance of in vitro and animal studies, heterogeneous experimental designs, and a lack of standardized extracts and dose–response evaluations, while clinical data in humans are virtually absent. Collectively, these findings underscore the promising pharmacological potential of L. cernuum and highlight the need for rigorously designed studies, particularly well-controlled clinical trials and mechanistic investigations, to validate its efficacy and safety and to inform its rational development as a therapeutic agent.
Rollando Rollando, Dodi Iskandar, V. D. Kharisma et al.· Majalah Obat Tradisional· 0 citations
Ganoderma lucidum , a classical top-grade herbal medicine with over 2000 years of application history, is officially listed as a food-medicine homologous material. Its core bioactive substances include polysaccharides and triterpenoids (including ganoderic acids), alongside sterols, nucleosides and amino acids, which endow multi-target pharmacological properties. This review systematically summarizes extraction, structural characteristics and quality control bottlenecks of its key components, and elaborates comprehensive preclinical pharmacological effects covering immunoregulation, neuroprotection, cardiovascular and renal protection, gastrointestinal homeostasis, anti-tumor, anti-aging, radioprotection and antiviral activities, with underlying signaling pathways such as NF-κ B, MAPK, Nrf2 and TGF-β/Smad clarified. Current clinical trials suggest its auxiliary therapeutic value in tumors, metabolic syndromes and urinary tract disorders, yet high-quality multi-center clinical evidence remains insufficient. Critical challenges include unclear structure-activity relationships, low bioavailability of lipophilic triterpenoids, severe raw material batch variation and incomplete component synergism mechanisms. Future research directions involve precise component characterization, multi-omic mechanistic dissection, novel delivery system development and standardized large-scale clinical verification to facilitate translational application of G. lucidum in modern biomedicine.
Yukun Zhang, Yang Yao, Zhu-Jun Liu et al.· Traditional Medicine Researc...· 0 citations
Saraca indica is a well-known medicinal plant widely used in traditional systems of medicine for the treatment of various ailments, particularly gynecological disorders, inflammation, microbial infections, and metabolic diseases. Owing to its rich phytochemical composition, including flavonoids, phenolic compounds, tannins, terpenoids, glycosides, and saponins, the plant has attracted considerable attention as a potential source of novel therapeutic agents. This review summarizes the current scientific evidence on the phytochemical profile, pharmacological activities, molecular mechanisms, and drug development potential of S. indica. An extensive literature survey was conducted using major scientific databases to collect relevant studies on its botanical characteristics, bioactive constituents, biological activities, and pharmaceutical applications. Experimental investigations have demonstrated that S. indica exhibits significant antioxidant, anti-inflammatory, antimicrobial, antidiabetic, anticancer, hepatoprotective, cardioprotective, neuroprotective, and wound-healing properties through the modulation of multiple signaling pathways. Despite promising preclinical findings, challenges related to phytochemical standardization, bioavailability, safety evaluation, and clinical validation remain. Future research integrating advanced analytical techniques, nanotechnology, and well-designed clinical studies is essential to facilitate the development of S. indica-based phytopharmaceuticals. Overall, Saraca indica represents a promising natural source of bioactive compounds with significant potential for future drug discovery and therapeutic development.
Pooja Balkrishna Kale, S. Jayakumari· Genetics and Molecular Resea...· 0 citations
Ipomoea aquatica Forsk
. a semi‐aquatic vegetable common in Asian diets, has recently gained scientific attention for its diverse phytochemical profile and therapeutic versatility. The species is a rich source of flavonoids, phenolic acids, alkaloids, carotenoids, and essential micronutrients that contribute synergistically to its bio‐functional activity. These metabolites demonstrate wide‐ranging effects, including antioxidant, anti‐inflammatory, antimicrobial, hepatoprotective, antidiabetic, neuroprotective, and anticancer actions. Such outcomes are largely attributed to the regulation of oxidative balance, inflammatory mediators, and key metabolic enzymes. Owing to its nutrient composition,
I. aquatica
represents a potential functional food for combating oxidative and metabolic disorders. Nevertheless, clinical translation remains limited due to inadequate pharmacokinetic characterization, extract standardization, and optimal dose determination. Innovative biotechnological strategies—such as nanoformulation‐based delivery and metabolic pathway optimization—offer promising routes to enhance its stability and efficacy. This review summarizes recent advances in the chemistry, structure–activity relationships, and biological mechanisms of
I. aquatica
, emphasizing its potential as a renewable phytochemical resource for nutraceutical and therapeutic applications.
Ashish Majumdar, S. Saraf· ChemistrySelect· 0 citations