Search

Rationale: Nerium oleander L. (Apocynaceae) is a medium-sized evergreen flowering tree and is distributed widely in China. Various parts of N. oleander have been used medicinally and are reported to possess a wide range of biological activities, including cardiotonic, cytotoxic, and central nervous system depressant activities. However, there is a lack of in-depth understanding of the chemical constituents in various parts of N. oleander., Methods: An ultrahigh-performance liquid chromatography coupled to quadrupole Orbitrap high-resolution mass spectrometry (UHPLC-Q-Orbitrap HRMS) method was developed for the qualitative analysis of the chemical constituents in the leaves and twigs of N. oleander., Results: As a result, 50 compounds, including phenolic derivatives, flavonoids, cardenolides, and triterpenoids, were identified in N. oleander. Among them, 50 compounds were identified in the leaves of N. oleander, whereas 25 compounds were identified in the twigs of N. oleander. It is noteworthy that 16 phenolic derivatives and 4 flavonoids were first detected in this plant and 10 cardenolides were deduced as potential new compounds., Conclusions: This study provided an effective method for comprehensively analyzing the complex system of medicinal plants and enriched the chemical compositions in N. oleander., (© 2024 John Wiley & Sons Ltd.)

The present study focused on extracting the anthocyanin dyes in ethanol, acidic ethanol, methanol, and acidic methanol solvents from Nerium oleander flowers by a simple maceration extraction process. FTIR spectroscopy and vibrational studies have confirmed the existence of polyphenolic groups in 2-phenyl chromenylium (anthocyanin) dyes. The optoelectronic results show the least direct bandgap (2.89 eV), indirect bandgap (1.98 eV), Urbach energy (0.120 eV), high refractive index (1.654), dielectric constant (3.294) and high optical conductivity (1.813 10 3  S/m) for the anthocyanin dye extracted found in acidic ethanol solvent. The photoluminescence properties such as Stokes' shift, quantum yield, and lifetime results show that anthocyanin dyes are promising candidates for red-LEDs and optical materials. The excellent correspondence between the absorption and emission spectra reinforces that the anthocyanins are efficient (89%) FRET probes. Further, the donor and acceptor undergo redshift in excitation and emission spectra in all studied solvents. The photometric properties such as CIE, CRI, CCT and color purity results of anthocyanins in all studied solvents revealed that this material exhibits pink to red shades (x = 0.40 → 0.50 and y = 0.46 → 0.39) and is well suitable for have great potential in the manufacturing of Organic-LEDs and other optoelectronic device applications., (© 2024 John Wiley & Sons Ltd.)

Objective: To perform testing for cytokines involved in dermal inflammatory reactions and to document and compare the effects of an oleander extract (OE), oleandrin, and oclacitinib on biomarkers relevant to allergic reactions. The effects of these compounds under inflamed culture conditions are of direct importance to the treatment of canine atopic dermatitis., Methods: Testing involved primary canine dermal fibroblasts and the canine DH82 macrophage cell line; both cell types are important for initiating, regulating, and resolving dermal allergic reactions via cytokine communication., Results: Under inflamed conditions, OE and oleandrin downregulated key cytokines secreted by canine dermal fibroblasts and the DH82 macrophage cell line; all of which are treatment targets in dermatitis. In the DH82 macrophage cultures, the most noteworthy reductions involved IL-6, IL-12/IL-23p40, interferon-γ, tumor necrosis factor-α, VEGF, and nerve growth factor-β. Oclacitinib triggered reductions of some cytokines involved in allergic reactions, including TGF-β1, IL-12/IL-23p40, and tumor necrosis factor-α; however, these reductions were less robust than the reductions triggered by OE and oleandrin and accompanied by increases in other cytokines involved in dermal inflammation, including IL-6, interferon-γ, and nerve growth factor-β. In cultures of primary dermal fibroblasts, OE and oleandrin reduced the levels of IL-8 and monocyte chemoattractant protein-1, whereas oclacitinib had little or no effect., Conclusions: Oleander extract and oleandrin directly modulate immune responses under inflamed conditions. Moreover, OE and oleandrin appear to provide a more beneficial overall cytokine regulation than oclacitinib under inflamed culture conditions., Clinical Relevance: These results suggest that OE and oleandrin are efficacious agents to treat canine atopic dermatitis. Future studies should evaluate the efficacy of these compounds in dogs affected by atopic dermatitis.

Mosquitoes, one of the deadliest animals on the planet, cause millions of fatalities each year by transmitting several human illnesses. Synthetic pesticides were previously used to prevent the spread of diseases by mosquitoes, which was effective in protecting humans but caused serious human health problems, environmental damage, and developed mosquito pesticide resistance. This research focuses on exploring new, more effective, safer, and environmentally friendly compounds to improve mosquito vector management. Phytochemicals are possible biological agents for controlling pests and many are target-specific, rapidly biodegradable, and eco-friendly. The potential of extracts of Lantana camara, Melia azedarach, Nerium oleander, Ricinus communis, and Withania somnifera against 3rd instar Culex pipiens (Common house mosquito) larvae was evaluated. Methanol extracts had more toxic effects against Cx. pipiens larvae (95-100%, 24 h post-treatment) than aqueous extracts (63-91%, 24 h post-treatment). The methanol extracts of Nerium oleander (LC 50  = 158.92 ppm) and Ricinus communis (LC 50  = 175.04 ppm) were very effective at killing mosquito larvae, 24 h after treatment. N. oleander (LC 50  = 373.29 ppm) showed high efficacy in aqueous plant extracts. Among the different extracts of the five plants screened, the methanol extract of R. communis recorded the highest ovicidal activity of 5% at 800 ppm concentration. Total developmental duration and growth index were highly affected by R. communis and M. azedarach methanol extracts. In field tests it was clear that plant extracts decreased mosquito larval density, especially when mixed with mosquito Bti briquette, with stability up to seven days for N. oleander. GC-MS results showed that the methanol extract had a higher number of chemical compounds, particularly with more terpene compounds. A high-performance liquid chromatography (HPLC) technique was used to detect the existence of non-volatile polyphenols and flavonoids. All five methanol extracts showed high concentrations of active ingredients such as gallic acid, chlorogenic acid (more than 100 μg/ml) and the rosmarinic acid was also found in all the five extracts in addition to 17 active polyphenols and flavonoids presented at moderate to low concentrations. Molecular modeling of 18 active ingredients detected by the HPLC were performed to the vicinity of one of the fatty acid binding proteins of lm-FABP (PDB code: 2FLJ). Rutin, Caffeic acid, coumaric acid and rosmarinic acid which presented densely in R. communis and N. oleander showed multiple and stable intermolecular hydrogen bonding and π-π stacking interactions. The inhibition ability of the fatty acid binding protein, FABP4, was evaluated with remarkable receptor inhibition evident, especially with R. communis and N. oleander having inhibitory concentrations of IC 50  = 0.425 and 0.599 µg/mL, respectively. The active phytochemical compounds in the plants suggest promising larvicidal and ovicidal activity, and have potential as a safe and effective alternative to synthetic insecticides., (© 2024. The Author(s).)

Men with diabetes frequently experience spermatogenic dysfunction, which is the most significant sign that diabetes has harmed their ability to reproduce. The effect of various doses of the hydro-alcoholic extract of Nerium oleander leaves on the pituitary-gonadal axis, sperm motility and number, antioxidant system, changes in testicular tissue structure, and spermatogenesis in healthy and diabetic rats has been examined in the current study. Eighty male rats that had been streptozotocin-induced diabetic and healthy were divided into eight groups: (1) control, (2) Nerium (50 mg/kg), (3) Nerium (100 mg/kg), (4) Nerium (200 mg/kg), (5) DM (6) DM+ Nerium (50 mg/kg), (7) DM+ Nerium (100 mg/kg) and (8) DM+ Nerium (200 mg/kg) and were administered orally for 48 days consecutive. Following the studies, analysis of the testicular tissues' antioxidant capacity as well as sperm parameters, Johnsen's scoring and morphometric evaluation, histology, biochemical and stereology studies were performed.The outcomes showed that Nerium 50 and 100 mg/kg considerably enhanced the testicular morphology, sperm parameters, and reproductive organs to varying degrees in diabetic rats. After Nerium 50 mg/kg administration, glutathione peroxidase (GPX) and catalase (CAT) levels in the testicular tissue were increased whereas malondialdehyde (MDA) levels were markedly decreased. Nerium may help protect against diabetic-induced spermatogenic dysfunction in male rats by enhancing the activities of antioxidant enzymes in lower dosages.

Cancer drug resistance remains a major obstacle in clinical oncology. As most anticancer drugs are of natural origin, we investigated the anticancer potential of a standardized cold-water leaf extract from Nerium oleander L., termed Breastin. The phytochemical characterization by nuclear magnetic resonance spectroscopy (NMR) and low- and high-resolution mass spectrometry revealed several monoglycosidic cardenolides as major constituents (adynerin, neritaloside, odoroside A, odoroside H, oleandrin, and vanderoside). Breastin inhibited the growth of 14 cell lines from hematopoietic tumors and 5 of 6 carcinomas. Remarkably, the cellular responsiveness of odoroside H and neritaloside was not correlated with all other classical drug resistance mechanisms, i.e., ATP-binding cassette transporters (ABCB1, ABCB5, ABCC1, ABCG2), oncogenes (EGFR, RAS), tumor suppressors (TP53, WT1), and others (GSTP1, HSP90, proliferation rate), in 59 tumor cell lines of the National Cancer Institute (NCI, USA), indicating that Breastin may indeed bypass drug resistance. COMPARE analyses with 153 anticancer agents in 74 tumor cell lines of the Oncotest panel revealed frequent correlations of Breastin with mitosis-inhibiting drugs. Using tubulin-GFP-transfected U2OS cells and confocal microscopy, it was found that the microtubule-disturbing effect of Breastin was comparable to that of the tubulin-depolymerizing drug paclitaxel. This result was verified by a tubulin polymerization assay in vitro and molecular docking in silico. Proteome profiling of 3171 proteins in the NCI panel revealed protein subsets whose expression significantly correlated with cellular responsiveness to odoroside H and neritaloside, indicating that protein expression profiles can be identified to predict the sensitivity or resistance of tumor cells to Breastin constituents. Breastin moderately inhibited breast cancer xenograft tumors in vivo. Remarkably, in contrast to what was observed with paclitaxel monotherapy, the combination of paclitaxel and Breastin prevented tumor relapse, indicating Breastin's potential for drug combination regimens.

Since 1987, several cytochalasins were isolated from Phoma exigua var. heteromorpha , the causal agent of foliar blight disease of oleander ( Nerium oleander L.), and chemically and biologically characterised. During the purification process of a large-scale production of cytochalasins A and B, necessary to continue the study on their anticancer activity, a metabolite having a different carbon skeleton compared to that of cytochalasans, was isolated. It was identified as terpestacin, a well-known toxic fungal stestertepenoid, isolated for the first time from P. exigua var. heteromorpha , by spectroscopic investigation (essentially 1D and 2D 1 H and 13 C-NMR and ESI MS) and optical methods in comparison with the literature data. Terpestacin and some its derivatives (including a natural one, fusaproliferin) were prepared and tested for their biological activity. Terpestacin and fusaproliferin had some inhibitory effects on seed germination of Phelipanche ramosa , whereas none of the compounds caused phytotoxic effects on weed leaves.[Formula: see text].

Oleandrigenin-3-O-β-D-diginoside (a derivative of odoroside A), isolated and purified by our group, has seldom been explored for its pharmacological activity. This study aimed at clarifying the mechanisms towards the leukaemia-suppressive role of odoroside A (compound #1) and its derivative, oleandrigenin-3-O-β-D-diginoside (compound #2) isolated from Nerium oleander. Viability and nuclear morphology change were assessed by CCK-8 assay and fluorescence microscope, respectively. Then, the cell apoptosis and autophagy induced by the compounds were detected by flow cytometry and Western blot. Xenograft model of nude mice was also applied to measure the leukaemia-suppressive effects of compound #2 in vivo. The result displayed that compound #1 and compound #2 inhibited the proliferation of HL60 and K562 cells and stronger effects were found in HL60 than K562 cells. Both of the compounds induced a dose-dependent apoptosis and autophagy in HL60 cells, where compound #2 was more potent than compound #1. Compound #2 also demonstrated a time-dependent apoptosis and autophagy in HL60 cells. Furthermore, ROS generation and JNK phosphorylation occurred in a dose-dependent manner in the cells treated with compound #2. Mitochondria also played critical role, proved by the decrease of Bcl-2, the release of cyto c to cytosol and the activation of caspase-3 and caspase-9. Moreover, the antitumour effects of compound #2 were validated in the nude mouse xenograft model in vivo. Odoroside A and its derivative inhibited the growth of leukaemia by inducing apoptosis and autophagy through the activation of ROS/JNK pathway. These results suggest that the compounds can serve as potential antitumour agents against leukaemia, especially acute myeloid leukaemia (AML)., (© 2021 Nordic Association for the Publication of BCPT (former Nordic Pharmacological Society). Published by John Wiley & Sons Ltd.)

Background: Colon cancers are among the top three causes of cancer-related deaths. This study is a continuation of previous research aiming to identify effective treatments., Objective: This study investigated the effects of Tarantula cubensis alcoholic extract (TCAE) and Nerium oleander (NO) distillate on the levels of midkine, transforming growth factor (TGF)-β, vascular endothelial growth factor (VEGF), alpha-fetoprotein (AFP), cyclooxygenase (COX)-2, insulin-like growth factor (IGF) and caspase-3 in the liver and colon tissues of rats with experimentally induced colon cancer., Methods: The liver and colon tissues of rats were homogeneously divided into control, colon cancer (azoxymethane, AZM), AZM + TCAE, and AZM + NO distillate groups. The levels of midkine, TGF-β, VEGF, AFP, COX-2, IGF, and caspase-3 in the colon and liver tissues were measured by ELISA., Results: The levels of all parameters in colon and liver tissues in the AZM group were higher (p<0.05) than those in the control group. TCAE and NO distillate prevented (p < 0.05) increases in midkine, TGF-β, VEGF, AFP, COX-2, IGF, and caspase-3 levels in the colon. NO distillate prevented the increase in all parameters except IGF, whereas TCAE prevented the increase in all values apart from COX-2 and IGF levels in the liver (p<0.05)., Conclusion: NO distillate and TCAE may prevent the studied markers from reaching specified levels observed in the colon in AZM-induced colon cancer. The increases in the levels of the parameters in the liver were not as severe as those in the colon; however, an 18-week study period may not be sufficient for liver metastasis formation. Future molecular studies should investigate the mechanisms and pathways of these treatments in greater detail., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)