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The new natural products reported in 2024 in peer-reviewed article s in journals with good reputations were reviewed and analyzed. The advances made by Asian research groups in the field of natural products chemistry in 2024 were summarized. Compounds with unique structural features and/or promising bioactivities originating from Asian natural sources were discussed based on their structural classification.
Natural products (NPs) provide a chemically precise strategy to overcome gut dysbiosis-driven resistance in cancer immunotherapy. This review deconstructs how distinct structural determinants of polysaccharides, terpenoids, polyphenols, and alkaloids dictate specific microbial remodeling and immunomodulatory outcomes. These structure-activity relationship (SAR)-driven mechanisms selectively enrich beneficial microbes, modulate metabolites, and reprogram host immune pathways, thereby potentiating diverse immunotherapies and converting "cold" tumors into "hot" ones. Future integration of SAR with AI-driven multi-omics and synthetic biology will enable rational design of next-generation NPs and personalized interventions, offering a promising avenue for more effective and less toxic cancer immunotherapies.
In this research, HS-CoFe2O4/Cu(ΙΙ) has been synthesized as a novel, natural based and recoverable magnetic composite with high catalytic activity. The structure of this magnetic natural based catalyst was investigated and approved using various analytical tools such as FT-IR, EDX-map, X-ray diffraction (XRD), VSM and FE-SEM. Among the advantages of the developed catalyst, one can point to compatibility with the environment, easy preparation and separation, reusability and low production cost. According to the principles of green chemistry, this study seeks to highlight the possibility of applying renewable and cheap materials and preparing catalysts with waste materials. The synthesized HS-CoFe2O4/Cu(ΙΙ) has shown high catalytic activity for the preparation of bis(indolyl)methane and dihydropyrano[2,3-c]pyrazole derivatives.
Determining the chemical structures and stereochemistry of natural compounds present in trace amounts via derivatization or hydrolysis is a considerable challenge. Nonetheless, when employing conventional deuterated reagents, consistent patterns in the subtle variations in chemical shifts and coupling constants observed in the 1H or 13C NMR spectra may provide a straightforward and reliable approach for the structural elucidation in specific cases. Importantly, the 1D NMR-based empirical method presented herein is simple to perform and does not require additional support from other techniques. This mini-review is the first to thoroughly compile these empirical rules by combining our research with existing studies.
Per- and polyfluoroalkyl substances (PFAS) are persistent and harmful environmental pollutants of international concerns. Despite widespread use of PFAS in industrial and consumer products, research exploring their effects on kidney function among Asian populations remains limited. Therefore, this study analyzed the Korean National Environmental Health Survey cycle 4 (2018-2020) data to determine the relationship between renal function and serum concentrations of perfluorooctanoic acid (PFOA), perfluorooctanesulfonic acid (PFOS), perfluorohexanesulfonic acid (PFHxS), perfluorononanoic acid (PFNA), and perfluorodecanoic acid (PFDeA) using the estimated glomerular filtration rate (eGFR). Subjects with eGFR values less than 60 mL/min/1.73 m2 were classified as having chronic kidney disease (CKD). Multiple linear and logistic regression models were used to assess the associations between PFAS concentrations and eGFR, and Bayesian kernel machine regression was used to evaluate the combined effects of PFAS on renal function. Among the general Korean adult population (n = 2985) significant negative associations were observed between all PFAS and the eGFR (p < 0.001). Natural log transformed level of PFOA, PFOS, PFHxS, PFNA, and PFDeA were associated with odds ratios of 1.801 (95 % confidence interval [CI]: 1.010-3.213), 1.961 (95 % CI: 1.407-2.732), 1.545 (95 % CI: 1.178-2.026), 2.334 (95 % CI: 1.424-3.825), and 1.782 (95 % CI: 0.976-3.254), respectively. Additionally, eGFR was significantly reduced as all PFAS concentrations simultaneously increased, and this association was mainly driven by PFNA and PFDeA. These associations remained consistent after stratification by sex and age. These findings suggest that PFAS exposure is associated with CKD and may have adverse effects on kidney function.
The aim of this study was to optimize, formulate, and evaluate a hydrogel composed of chitosan and β-glycerophosphate (β-GP) for the delivery of lycopene in the treatment of breast cancer. Box-Behnken design (BBD) was employed to optimize the formulation, where chitosan concentration (A), β-GP concentration (B) as critical material attributes (CMAs), and stirring speed (C) as critical process parameter (CPP) were selected. The hydrogel was optimized based on gelation time and swelling ratio. The optimized formulation exhibited a gelation time of 145 ± 1.2s, and a swelling ratio of 130.57 ± 2.4%. In Vitro drug release studies demonstrated lycopene release over 24 h. Cytotoxicity studies against breast cancer cell lines demonstrated IC50 values of 95.45 μg/mL for MCF-7 and 91.16 μg/mL for MDA-MB-231 cells under in vitro conditions. These results suggested that the optimized hydrogel may serve as a feasible platform for localized drug delivery against breast cancer.
Triple-negative breast cancer (TNBC) is a type of breast cancer that has a high rate of growth and metastasis. In this study, the liquid fermentation product (EX-9) of Penicillium griseofulvum, an endophytic fungus derived from the medicinal plant Delphinium grandiflorum L., has exhibited significant anti-cancer activity against TNBC. We investigated the therapeutic effects and potential mechanisms of EX-9 on TNBC both in vivo and in vitro. Our findings demonstrated that EX-9 exhibited remarkable efficacy against TNBC both in vivo and in vitro, while showing negligible toxicity. The potential mechanism for its anti-TNBC effect involved the inhibition of the PI3K/Akt signaling pathway. Additionally, we employed liquid chromatography-mass spectrometry (LC-MS) technology and network pharmacology methods to uncover the potential pharmacological substance basis of EX-9 in combating TNBC.
This study investigates the therapeutic effects and mechanisms of the Yiqi Huoxue Recipe (YHR) on renal injury in Diabetic nephropathy (DN). Through mass spectrometry analysis, animal experiments, and network pharmacology approaches, it was found that YHR can ameliorate renal function indicators and pathological changes in DN rats, and reduce cell apoptosis. Mechanistic studies indicate that YHR alleviates hyperglycemia-induced renal inflammation and damage by inhibiting the HIF-1 signaling pathway, thereby improving DN.
10-Methoxycamptothecin (MCPT), a natural camptothecin derivative, shows notable anticancer activity. Using UPLC-QTOF-MS, this study characterized MCPT metabolite profiles in rats, detecting 14 metabolites in urine, 5 in bile, 7 in feces, and 2 in plasma. The findings indicated that phase I metabolites of MCPT were primarily formed via demethylation, demethoxylation, and hydroxylation, while phase II metabolites mainly included glucuronide and sulfate of MCPT and its phase I metabolites. MCPT, hydroxycamptothecin, and the subsequent glucuronide conjugates were the predominant forms of MCPT in rats. This study provided a comprehensive overview of the metabolite profile of MCPT in rats.
A new isoflavone-quinone, placovinone E (1), and a new natural isoflavone, placovinone F (2), together with four known isoflavones (3-6), were isolated from the leaves of P. vietnamense. The chemical structures of all isolated compounds were elucidated using spectroscopic techniques (NMR and HRESIMS) and confirmed by comparison with literature data. All isolated compounds were evaluated for their α-glucosidase and xanthine oxidase inhibitory activities. Among them, compound 1 exhibited the strongest α-glucosidase inhibition (IC50 21.6 ± 1.04 µM), which was markedly more potent than the positive control, acarbose (IC50 156.2 ± 5.43 µM). In addition, compound 1 showed the highest xanthine oxidase inhibitory activity (IC50 32.8 ± 0.08 µM), although it remained considerably less potent than the positive control, allopurinol (IC50 2.45 ± 0.01 µM).
This study evaluated the potential of methyl jasmonate (MeJA) to modulate oxidative stress damage and hyperglycemia in rats with STZ-induced diabetes. MeJA treatment (5 and 10 mg/kg) improved the destructive effects of STZ-induced oxidative damage, as proved by the decline in ROS formation and lipid peroxidation. In addition, MeJA displayed a substantial upsurge in the level of tissue GSH and activity of CAT and SOD enzymes. Histological analysis confirmed MeJA alleviated liver damage. Given the crucial part oxidative stress plays in the etiology of diabetes, this study offers a novel viewpoint on MeJA's potential as a treatment.
Genome mining has become a powerful method for linking biosynthetic gene clusters to chemical structures of their encoded natural products, driven by advances in genomic sequencing and the accumulated knowledge of natural product biosynthesis. Guided by this strategy, Actinoalloteichus hymeniacidonis DSM 45092 was identified as a potential producer of pentangular polyketides. Subsequently, five pentangular polyphenols were isolated from this strain, including two new compounds 19-hydroxy-KS-619-1 (1) and 19,20-dehydro-KS-619-1 (2), and three known analogues 3-5. Their structures were elucidated through comprehensive spectroscopic analysis and electronic circular dichroism calculations, and all compounds were evaluated for antibacterial and cytotoxic activities.
Broussonetia papyrifera leaves are a medicinal plant rich in bioactive substances. This study utilized microbial fermentation of B. papyrifera leaf extract (BLE) to screen out Lactobacillus rhamnosus and Bifidobacterium papyrifera as the most suitable fermentation strains. The total phenols, total flavonoids, total tannins and total triterpenoids content increased after fermentation. The fermentation broth of L. rhamnosus and BLE (BLFs) could inhibit the tyrosinase, melanin production and related protein expression of mouse melanoma cell B16-F10. The fermentation broth of B. bifidum and BLE (BBFs) exhibited significant antioxidant effects. It indicates that the fermented BLE has great application potential in the fields of medicine, cosmetics and related areas.
Four new limonoids (1-4), reticulactone A (1), 21,23-dihydro-23-ethoxy-21-oxolimonin (2), tetrahydro-20,22-dihydroxy-21,23-diethoxy-nomilin (3), and dasycarinone B (4), as well as 11 known limonoids and one known carbolic acid, were isolated from the EtOH extract of the seeds of Citrus reticulata Blanco. The inhibitory effects of 15 limonoids (1-15) on the proliferation of HepG2 liver cancer cells were evaluated using the CCK-8 assay. Based on their structural characteristics, the results revealed that the typical limonoid compounds 2, 5, 10, and 12 exhibited stronger cytotoxicity compared to other limonoid compounds. Notably, the novel compound 2 demonstrated the strongest cytotoxic activity (IC50 = 18.24 ± 2.78 μM).
Two new (1-2) and five known (3-7) dihydro-β-agarofuran derivatives were isolated from the roots of Tripterygium wilfordii. The structures of new compounds were elucidated by spectroscopic techniques, such as UV, IR, HRESIMS and NMR. And the structure of compound 1 was confirmed by X-ray crystallographic. Cytotoxic activity assays against four human tumor cell lines (SK-MEL-2, HCC1806, HUH-7, PANC-1) were assessed for compounds 1-7. Compound 2 exhibited pronounced cytotoxicity against SK-MEL-2 cells with an IC50 value of 9.18 μM. Additionally, compound 5 showed significant cytotoxic effects on SK-MEL-2 and HCC1806 cells with IC50 values of 4.59 μM and 8.14 μM, respectively.
Targeting Survivin with small molecules is a validated oncological strategy. Fourteen novel asiatic acid (AA) derivatives incorporating phosphate ester pharmacophores were designed and synthesized guided by the principles of fragment-based drug discovery and informed by the essential pharmacophoric features of known potent Survivin inhibitors. In vitro evaluation revealed that these compounds, particularly compound II6, effectively inhibited the proliferation of MCF-7, A549 and HeLa cells. Molecular docking indicated that the designed compounds interact with key residues of Survivin through covalent and non-covalent interactions. The selected compound may suppress tumor proliferation via Survivin inhibition, constituting a potential lead for cancer therapy.
The study investigates Panax ginseng nanoemulsion role in counteracting male infertility in rats. Nanoemulsion was prepared by oil in water method, then it was characterized by transmission electron microscope (TEM), Zeta sizer, Fourier transform infrared spectroscopy (FTIR), and thermogravimetric analysis (TGA). The serum total testosterone, free testosterone, Luteinizing Hormone (LH), and Follicle-Stimulating Hormone (FSH) were measured. Phosphatidylinositol 3-kinase (PI3K), Protein kinase B (AKT), mammalian target of rapamycin (mTOR), E-cadherin (E-cad), and connexin 43 (Cx43) expression were analyzed. A histological examination of testes was also carried out. Nanoemulsion exhibited a spherical morphology, with diameter from 5.98 to 51.80 nm. Additionally, Zeta sizer determined size distribution by number from 97.74 to 147.4 nm. Zeta potential revealed negatively charged surface. FTIR showed common active groups. Nanoemulsions demonstrated thermal stability up to 207 °C. Biological experiments indicated that adverse effects of bisphenol A (BPA) were counteracted by Panax ginseng in either nanoemulsion or free form and vitamin E (Vit.E). Panax ginseng nanoemulsion recovers male infertility in rats. These outcomes may have a significant impact on developing a new therapeutic entity to treat male infertile patients.
Two new metabolites, 29-demethyl-3-ene-cycloastragenol (2) and 1α,12α-dihydroxy-cycloastragenone (3), along with six known compounds (4-9) were obtained from the microbial transformation of cycloastragenol (1) by Penicillium spinulosum AS3.149. The structures of these metabolites were determined by extensive spectroscopic (IR, UV, HRESIMS, 1D and 2D NMR) data analyses. Compound 2 features a 29-nor-triterpenic skeleton, possibly formed through sequential oxidation, decarboxylation, and dehydration reactions. Biological assays revealed that compound 6 exhibited significant cytotoxic activity against the K562 cell line with an IC50 value of 1.0 μM.
This evidence-based review highlights the cardioprotective potential of punicalagin, a major polyphenolic ellagitannin from Punica granatum L., focusing on its pharmacological mechanisms in cardiovascular disease (CVD) pathogenesis. Preclinical studies demonstrate that punicalagin reduces oxidative stress via Nrf2/HO-1 and AMPK pathways, suppresses inflammatory cytokines (TNF-α, IL-1β, IL-6) through NF-κB and MAPK inhibition, improves endothelial function by upregulating eNOS, and modulates lipid metabolism through ApoB100 binding and cholesterol efflux. Clinical trials further support these effects, showing improvements in lipid profile, blood pressure, and carotid intima-media thickness. Punicalagin's multitarget actions support its translational potential in the management of CVD.
Glutinol (GT), a major triterpenoid component of Orostachys japonica, suppresses TGF-β-induced epithelial-mesenchymal transition (EMT) in human cancer cells. GT treatment restored epithelial characteristics by upregulating E-cadherin and downregulating Snail, thereby reducing cancer cell migration and invasion in A549 and MCF-7 cells. In vivo, GT significantly inhibited lung metastasis of TGF-β-treated A549-luc cells in mice. These findings demonstrate that GT exerts potent anti-metastatic effects through modulation of the TGF-β/Snail/E-cadherin signaling axis, highlighting its potential as a natural therapeutic agent against cancer metastasis.