Natural Product Research最新文献

Extract preparation is critical for recovering bioactive from plants. Impacted by many different variables and even slight variations may alter the extraction. Therefore, it is crucial for precisely examining the parameters. Quality by design, can obtain high recovery of bioactive. In this study, a process was developed to enrich Bergenia ciliata (Haw.) Sternb. rhizome extract with bergenin. One Factor at a Time succeeded by Response Surface Methodology were followed to achieve the objectives using developed quantitative method for bergenin on high-pressure liquid chromatography. Three variables- time, ethanol %, and solvent volume, were optimised by Central Composite Design to generate novel protocol. The generated data recommends 50 mL/g, 70% ethanol for 60 min reflux (x 2 cycles) for the best extraction. Future manufacturing processes and standardisation may benefit from the developed approach. Additionally, the effect of altitude on bergenin was evaluated, and the findings showed high-altitude samples contained higher bioactive component.

Momordica cymbalaria Fenzl ex Naudin, distributed across South and Central India, is traditionally used for diabetes and hyperlipidaemia and shows notable antibacterial activity. Its hairy roots are rich in steroidal and triterpenoid saponins. In this study, 24-nor-olean-3-one-28-oic acid (NOA), a nor-oleanane triterpenoid, was isolated for the first time from the petroleum ether extract of M. cymbalaria roots and structurally confirmed through spectroscopic analyses. The antitumor potential of NOA was assessed in Ehrlich ascites carcinoma (EAC)-bearing mice. NOA significantly and dose-dependently reduced tumour volume, packed cell volume, viable cell count, and tumour-associated weight gain (p < 0.001). Survival increased markedly, reaching 44.5 ± 0.32 days at 2.5 mg/kg and 49.0 ± 0.42 days at 5 mg/kg, exceeding the effect of 5-fluorouracil. NOA also normalised EAC-induced hematological disturbances and improved antioxidant status by lowering hepatic MDA and restoring GSH, SOD, and CAT levels, indicating strong anticancer potential.

A new β-alkyl pyridine alkaloid, leucascine (1), was isolated from the Okinawan marine sponge Leucascus protogenes. Its planar structure was elucidated using a combination of 1D and 2D NMR spectroscopy, mass spectrometry, and comparison with reference compounds. The configuration at the stereogenic centre C-2 was determined through Mosher's method using MPA derivatives (compounds 2 and 3), supported by the analysis of ¹H NMR chemical shifts. To validate this assignment, model compounds 7 and 8 were synthesised and subjected to density functional theory (DFT) calculations. Conformational analysis revealed that both enantiomers favour the anticlinal-E (ac-E) conformation, and the computed chemical shifts closely matched the experimental data, further confirming the possibility of the 2S configuration of leucascine (1). Notably, compound 1 demonstrated significant cytotoxicity, exhibiting an IC₅₀ value of 9.2 µM against NBT-T2 tumour cells.

Atherosclerosis (AS) is a prevalent typical chronic inflammation disease characterised by lipid deposition, immune cell infiltration and inflammatory response in the arterial intima. The long-term treatments of the existing drugs suffered safety concerns. Stevia rebaudiana Bertoni, a perennial shrub of the Asteraceae family, is known as a sweetener for its leaves, which are mainly composed of steviol glycosides, steviosides, and rebaudiosides. Stevia rebaudiana Bertoni roots polysaccharide (SRRP), an inulin-type fructan, possess the potential roles for hypoglycaemic property, the reduction of hepatic lipid deposition and abdominal lipid accumulation, anti-inflammatory, antioxidant. These properties suggest that SRRP might ameliorate atherosclerosis. This study aims to focus on the ameliorating AS effect of SRRP on lipid metabolism and the inflammatory response though high-fat-diet-induced atherosclerosis in ApoE-knockout (ApoE^-/-)mice. The results indicated SRRP ameliorated high-fat-diet-induced atherosclerosis in ApoE^-/- mice by reducing the serum lipid concentrations, inflammatory responses and oxidative stress.

Phytochemical investigation of Butea monosperma (Lam.) Kuntze flowers resulted in the isolation of seven compounds: medicarpin (1), sulfuretin (2), liquiritigenin (3), kaempferol (4), butein (5), iso-butrin (6), and butrin (7). Structures were identified by 1D and 2D NMR and confirmed with literature data. Antioxidant assays (DPPH^•, ABTS^•+, FRAP) revealed butein (5) as the most active, followed by sulfuretin (2) and iso-butrin (6). Liquiritigenin (3) exhibited the strongest tyrosinase inhibition (IC₅₀ = 13.07 ± 2.58 µM) via competitive inhibition and effectively suppressed melanin production in MNT-1 cells, reducing pigmentation by 22-41%, outperforming α-arbutin without cytotoxicity. Compounds 4 and 5 showed potent anti-inflammatory activity, with NO inhibitory IC₅₀ values of 51.60 and 66.93 µM, respectively, while 2, 3, 5, and 6 exhibited moderate cytotoxicity against HeLa (IC₅₀ = 34-38 µM) and HCT116 cells (IC₅₀ = 21-28 µM). Overall, B. monosperma flowers provide multifunctional natural products with promising cosmetic and pharmaceutical potential.

This study evaluated the anticancer potential of essential oils from Cedrus libani cones. Gas chromatography-mass spectrometry identified 23 compounds, mainly α-pinene (51.29%), β-pinene (31.12%), and β-phellandrene (4.12%). The cone essential oil (CEO) showed strong cytotoxicity against human melanoma (A375) cells, with an IC₅₀ value of 7.64 μg/mL in MTT assays. Annexin V-FITC/PI staining revealed a twofold increase in apoptosis, and qRT-PCR analysis confirmed an elevated Bax/Bcl-2 ratio. CEO also suppressed proliferation and migration: colony formation decreased by nearly 40%, and wound closure was 37.8% in treated cells versus 4% in controls. These findings suggest that C. libani cone oil exerts potent cytotoxic, pro-apoptotic, anti-proliferative, and anti-migratory effects, supporting its potential as a natural anticancer agent.

Sorbariakirine A (1), a cucurbitane-type triterpene, along with nine known compounds (2-10), were isolated from the aerial parts (stems and leaves) of Sorbaria kirilowii (Regel) Maxim. The structure of compound 1 was determined through comprehensive spectroscopic analysis (IR, MS, 1D/2D NMR, and CD). Compound 4 showed potent phosphodiesterase 1 inhibitory effect (IC₅₀ = 12.90 ± 0.12 µg/mL). Enzyme kinetics demonstrated that compound 4 irreversibly inhibits PDE1. Molecular docking studies reveal that 4 adopts a binding mode that forms a 'covalent-anchored synergistic non-covalent interaction network' with the PDE1 protein, thereby enhancing its inhibitory activity. Additionally, In Silico drug-likeness predictions using the pkCSM platform were performed to evaluate the drug-likeness of these compounds.

This study investigates sulphated exopolysaccharide (EPS) produced by Halomonas titanicae PCRB123b, isolated from the polyextreme Antarctic Ocean. The EPS has molecular weight ∼1.48 × 10⁴ Da. Surface topography revealed smooth, non-porous "weaving flasks" configuration. The CHNS data confirmed high carbon (21.41%) and sulphur (8.99%) content in EPS. Monosaccharide analysis bares a heteropolysaccharide configuration with mannose (82.9%), glucose (8.85%), and xylose (2.25%) etc. NMR and FTIR spectroscopy confirmed →4)-β-D-Manp-(1→ and →4)-β-D-Glcp-(1→ glycosidic linkages of mannose with glucose monomers, and xylose linked with mannose by →3)-β-D-xylp-(1→ glycosidic linkage. EPS was stable up-to >300 °C and exhibited a strong antioxidant activity against several free radicals. It has excellent emulsification properties for different food oils and strong flocculation bioactivity rate of 98.23% at 15 mg/L concentration, also 342.5% water and 185% of oil holding capacity. These findings suggest that PCRB123b EPS could be a beneficial addition to the food processing industry, potentially replacing synthetic polymers.

Lavandula L. is the single genus of the tribe Lavanduleae (Endl.) Boiss, member of the Lamiaceae (Labiatae), distributed in Macaronesia to Mediterranean area. and India. Lavandula subnuda Benth., growing in Oman and Gulf State, and Lavandula macra Baker, present in Oman, Somalia and Yemen, are two taxa belonging to the almost unexplored Section Subnudae Chaytor. The compositions of the essential oils (EOs) of L. subnuda (LS) and L. macra (LM), the last one never been previously investigated, collected in Oman, were evaluated by GC-MS. The EOs of both species were characterised by a remarkable amount of esters and acids (40.25% and 33.49%, respectively for LS and LM) and sesquiterpenes (31.63% and 31.5.5%, respectively for LS and LM). Main constituents of LS were ethyl linoleate (15.93%), hexadecanoic acid (13.97%) and δ-cadinene (6.22%), whereas the principal metabolites of LM were hexadecanoic acid (21.38%), germacrene D (9.70%) and methyleugenol (6.71%).