Resveratrol is a polyphenol with diverse pharmacological activities, but its clinical efficacy is limited due to low solubility/permeability, light-induced isomerization, auto-oxidation, and rapid metabolism. Nanodelivery systems, such as liposomes, polymeric nanoparticles, lipid nanocarriers, micelles, nanocrystals, inorganic nanoparticles, nanoemulsions, protein-based nanoparticles, exosomes, macrophages, and red blood cells (RBCs) have shown great potential for improving the solubility, biocompatibility, and therapeutic efficacy of resveratrol. This review comprehensively summarizes the recent advances in resveratrol nanoencapsulation and describes potential strategies to improve the pharmacokinetics of existing nanoformulations, enhance targeting, reduce toxicity, and increase drug release and encapsulation efficiency. The article also suggests that in order to avoid potential safety issues, resveratrol nanoformulations must be tested in vivo in a wide range of diseases.

Purpose: Triple-negative breast cancer (TNBC) is the most lethal subtype of breast cancer. However, the effect of current treatment strategies by inducing tumor cell apoptosis alone is not satisfactory. The growth, metastasis and treatment sensitivity of tumors can be strongly influenced by cancer-associated fibroblasts (CAFs) in the microenvironment. Effective cancer therapies may need to target not only the tumor cells directly but also the CAFs that protect them. Methods: Celastrol and small-sized micelles containing betulinic acid were co-encapsulated into liposomes using the thin-film hydration method (CL@BM). Folic acid was further introduced to modify liposomes as the targeting moiety (F/CL@BM). We established a novel NIH3T3+4T1 co-culture model to mimic the tumor microenvironment and assessed the nanocarrier’s inhibitory effects on CAFs-induced drug resistance and migration in the co-culture model. The in vivo biological distribution, fluorescence imaging, biological safety evaluation, and combined therapeutic effect evaluation of the nanocarrier were carried out based on a triple-negative breast cancer model. Results: In the present study, a novel multifunctional nano-formulation was designed by combining the advantages of sequential release, co-loading of tretinoin and betulinic acid, and folic acid-mediated active targeting. As expected, the nano-formulation exhibited enhanced cytotoxicity in different cellular models and effectively increased drug accumulation at the tumor site by disrupting the cellular barrier composed of CAFs by tretinoin. Notably, the co-loaded nano-formulations proved to be more potent in inhibiting tumor growth in mice and also showed better anti-metastatic effects in lung metastasis models compared to the formulations with either drug alone. This novel drug delivery system has the potential to be used to develop more effective cancer therapies. Conclusion: Targeting CAFs with celastrol sensitizes tumor cells to chemotherapy, increasing the efficacy of betulinic acid. The combination of drugs targeting tumor cells and CAFs may lead to more effective therapies against various cancers.

Dendrobium nobile (Lindl.) have long been used as herbal tea and a traditional herbal medicine to treat Alzheimer’s disease (AD). In the current study, nineteen compounds (1–19), including two new vitamin E homologues (1–2), one new sesquiterpene (6), and two new dendrobines (7, 8), were isolated and identified from stems of Dendrobium nobile. Their structures were elucidated on the basis of NMR, ¹³C NMR calculation, and DP4⁺ probability analyses. The absolute configurations of new compounds were determined by electronic circular dichroism (ECD) data analysis. Antioxidant, anti-inflammatory, and cytotoxic activities of isolated compounds were evaluated. Among them, compound 2 demonstrated significant antioxidant activity compared with ascorbic acid (VC), while compounds 2 and 4 also exhibited an equal effect to positive control cisplatin. This study on the biological activity of the new vitamin E homologues from Dendrobium nobile may indicate its potential application in the pharmaceutical and food industries.

Four new compounds, including two new polyketides, heterocornols M and N (1, 2), and a pair of epimers, heterocornols O and P (3, 4), were isolated from the fermentation broth of the marine sponge-derived fungus Pestalotiopsis heterocornis XWS03F09, together with three known compounds (5–7). The new chemical structures were established on the basis of a spectroscopic analysis, optical rotation, experimental and calculated electronic circular dichroism (ECD). All of the compounds (1–7) were evaluated for their cytotoxic activities, and heterocornols M-P (1–4) exhibited cytotoxicities against four human cancer cell lines with IC₅₀ values of 20.4–94.2 μM.

One strain-many compounds (OSMAC) manipulation of the sponge-derived fungus Pestalotiopsis heterocornis XWS03F09 resulted in the production of new secondary metabolites. The chemical study of the fermentation, cultivated on 3% artificial sea salt in the rice media, led to the isolation of twelve compounds, including eight new polyketide derivatives, heterocornols Q–X (1–8), one new ceramide (9), and three known analogues (10–12). The structures and absolute configurations of the new compounds were elucidated by spectroscopic data and calculated ECD analysis. Heterocornols Q (1) and R (2) are novel 6/5/7/5 tetracyclic polyketide derivatives featuring dihydroisobenzofuran and benzo-fused dioxabicyclo [4.2.1] nonane system, which might be derived from the acetyl-CoA by epoxidation, polyene cyclization, and rearrangement to form the core skeleton. Compound 12 showed moderate or weak antimicrobial activities against with MIC values ranging from 25 to 100 μg/mL. Heterocornols T and X (7 and 8) could inhibit the production of LPS-induced NO significantly, comparable to dexamethasone. Further Western blotting analysis showed 7 and 8 markedly suppressed the iNOS protein expression in LPS-induced RAW 264.7 cells in a dose-dependent manner. The result showed that 7 and 8 might serve as potential leads for development of anti-inflammatory activity.