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ADVANCED FUNCTIONAL MATERIALS · 2025 · IF 19

Charge-Guided Cartilage-Penetrating Micro/Nanocarriers That Inhibit Piezo1 and Protect Cartilage to Alleviate Osteoarthritis

Fan Chen,Wenzhe Wang,Zian Zhang,Nanyu Pang,Chang Liu,Zhenchao Huang,Haoshen Wu,Haining Zhang

Osteoarthritis (OA), characterized by progressive cartilage degeneration and chronic joint pain, represents a major global health challenge. While intra-articular drug delivery is a common therapeutic approach, its efficacy is limited by poor drug penetration through the dense cartilage matrix, particularly for hydrophobic compounds. Here, a novel charge-guided micro/nanocarrier system designed to overcome these delivery challenges is presented. By modifying amylose with glycidyl trimethyl ammonium chloride (GTAC), it is developed positively charged carriers that demonstrate enhanced penetration into the negatively charged cartilage matrix. The hydrophobic Piezo1 inhibitor, Margaric acid (MA), is efficiently encapsulated within the helical cavity of modified amylose through DMSO-ultrasound treatment, creating Cationic Amylose Micro/Nanocarriers@MA (CAMNC@MA). This system effectively delivers MA to chondrocytes, where Piezo1, a crucial mechanosensor implicated in OA development, can be precisely modulated. These results demonstrate that CAMNC@MA successfully inhibits abnormal mechanical force-induced Piezo1 activation in chondrocytes, enhances cell survival, reduces matrix degradation, and effectively alleviates OA progression. This innovative drug delivery platform offers a promising strategy for clinical OA treatment by combining enhanced matrix penetration with efficient matrix penetration of hydrophobic therapeutic agents.

研究领域: 医学 · 药理学 · 生物材料学
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Foods · 2025 ·Vol. 14 ·期 7 ·1206 · IF 5.1

Phytosterol–γ-Oryzanol–Glycerol Monostearate Composite Gelators for Palm Stearin/Linseed Oil Oleogel-Based Margarine: Nutrient Enrichment, Textural Modulation, and Commercial Product Mimicry

Jingwen Li,Yujuan Hu,Qing Ma,Dongkun Zhao,Xinjing Dou,Baocheng Xu,Lili Liu

This study prepared palm stearin/linseed oil-based margarines (PST/LO-BMs) and palm stearin/linseed oil oleogel-based margarines (PST/LO-OBM) by incorporating varying proportions (20–60% oil phase) of linseed oil (LO) and LO-based oleogel, respectively. By comparing PST/LO-OBMs and PST/LO-BMs, it was found that the introduction of phytosterol–γ-oryzanol (PO) complexes and glycerol monostearate (GMS) to PST/LO-OBM induced three distinct crystalline morphologies: needle-like crystals, spherical crystals, and cluster-type crystals. These crystal assemblies synergistically constructed a robust three-dimensional network, effectively entrapping both aqueous droplets and liquid oil fractions while substantially reinforcing the structural integrity of PST/LO-OBM. Notably, the incorporated gelators modified the crystallization behavior, where GMS likely served as a nucleating site promoting triglyceride crystallization. This structural modulation yielded favorable β’-form crystal polymorphism, which is critically associated with enhanced textural properties. Comparative analysis with commercial margarine revealed that the PST45/LO40-OBM formulation exhibited comparable rheological performance, crystalline type, and thermal properties, while demonstrating superior nutritional characteristics, containing elevated levels of α-linolenic acid (23.54%), phytosterol (1410 mg/100 g), and γ-oryzanol (2110 mg/100 g). These findings provide fundamental insights for margarine alternatives with nutritional attributes.

CAS / MDL: 8002-43-5
研究领域: 食品科学 · 营养学 · 油脂化学
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FOOD RESEARCH INTERNATIONAL · 2015 · IF 2.818

Discovering anti-osteoporosis constituents of maca (Lepidium meyenii) by combined virtual screening and activity verification

Hao Liu,Wenwen Jin,Chunhua Fu,Penfei Dai,Yuantao Yu,Qin Huo,Longjiang Yu

Maca ( Lepidium meyenii Walp.) is a traditional medicine and nutritional supplement from South America with many pharmacological effects, such as enhancing female and male fertility, improving sexual dysfunction, preventing osteoporosis and relieving menopausal syndrome. Until now, the active principles behind most of these effects have not been clarified, severely hindering the exploitation and application of maca products. In this study, the effective anti-osteoporotic components of maca are uncovered. Through virtual screening against estrogen receptor and verification of pharmacological activity on osteoblasts, we found that N-benzyl-palmitamide is an active constituent of maca in preventing osteoporosis. As well, N-benzyl-palmitamide promotes osteoblast proliferation, differentiation and mineralization, plus it benefits bone formation through enhanced expression of osteogenesis-related genes, such as bone morphogenetic protein-2, core binding factor alpha 1, type 1 collagen and alkaline phosphatase. The effects of N-benzyl-palmitamide on enhanced bone formation are very likely through the estrogen receptor pathway, as N-benzyl-palmitamide also increases the expression of ERα and ERβ genes. Clarifying single-component biological activity will greatly enable exploitation and application of maca as a medication and health supplement to prevent osteoporosis.

CAS / MDL: 123-03-5
研究领域: 药理学 · 分子生物学 · 传统医学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2021 · IF 6.953

Micelle nanovehicles for co-delivery of Lepidium meyenii Walp. (maca) polysaccharide and chloroquine to tumor-associated macrophages for synergistic cancer immunotherapy

Ye Yang,Tingting Guo,Junwei Xu,Yin Xiong,Xiuming Cui,Yang Ke,Chengxiao Wang

Here, we fabricated amphiphilic polysaccharide micelles for synergistic cancer immunotherapy targeting tumor-associated macrophages (TAMs). Lepidium meyenii Walp. (maca) polysaccharide (MP), a naturally derived macromolecule with a strong TAM-remodeling effect, was grafted on a hydrophobic poly(lactic- co -glycolic acid) (PLGA) segment, with a disulfide bond for redox-sensitive linkage. The amphiphilic polysaccharide derivatives could self-assemble into core (PLGA)–shell (MP)-structured micelles and encapsulate chloroquine (CQ) into the hydrophobic core. By using a 4T1-M2 macrophage co-culture model and a 4T1 tumor xenograft mouse model, we showed that the prepared micelles could co-deliver MP and CQ to the tumor sites and selectively accumulate at TAMs because of the specific properties of MP. Furthermore, the nanoparticles exerted synergistic tumor immunotherapeutic and antimetastatic effects, which might be attributable to the enhanced cell internalization of the micelles and the multiple regulatory mechanisms of MP and CQ. Thus, immunomodulatory MP may be a promising biomaterial for cancer immunotherapy.

研究领域: 纳米技术 · 药学 · 免疫学 · 癌症研究
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Frontiers in Microbiology · 2025 · IF 4.5

Chewable tablets containing rape bee pollen and maca attenuate testosterone propionate–induced benign prostatic hyperplasia in Sprague–Dawley rats by regulating the gut microbiota and modulating the IL-6/JAK2/STAT3 signaling pathway

Xiaoqiang Huang,Guohua Ru,Hengyun Tian,Pengbo Zhang,Hongchang Zhao,Shouren Zhang,Sijie Wang,An Jia,Wanli Zhao

Background Benign prostatic hyperplasia (BPH) significantly compromises patients' quality of life, has detrimental effects on both physical and mental well-being, and poses a substantial economic burden. Current pharmacological interventions primarily focus on symptom relief; nevertheless, their associated adverse effects are evident. Rape bee pollen and maca are both homologous food products, which are not only rich in nutrition, but also have many biological activities. There is no report on the combination of rape bee pollen and maca in benign prostatic hyperplasia therapy, and no report on the molecular mechanism. This study aims to systematically investigate the therapeutic efficacy and underlying molecular mechanisms of a chewable tablet formulation containing rape bee pollen and maca in the management of BPH. Methods First, the chewable tablets were prepared from rape bee pollen and maca, and the High Performance Liquid Chromatography (HPLC) fingerprint was established. During a 4-week period, rats were subjected to subcutaneous injections of testosterone propionate solution to establish a BPH model, while simultaneously receiving orally administered chewable tablets for BPH treatment via gavage. We assessed the body weight, prostate tissue index, serum levels of dihydrotestosterone (DHT), testosterone (T), estradiol (E2), interleukin-6 (IL-6), tumor necrosis factor-alpha (TNF-α), interleukin-1beta (IL-1β), superoxide dismutase (SOD), malondialdehyde (MDA) and glutathione (GSH) levels in rats. Prostate tissues were collected for histopathological analysis. The protein expression levels of IL-6, phosphorylated Janus kinase 2 ( p -JAK2), and phosphorylated signal transducer and activator of transcription 3 ( p -STAT3) were determined by Western blotting. Rat feces were collected aseptically for 16S rDNA gene sequencing to assess gut microbiota levels. Additionally, our research findings demonstrate that the combined application of rape pollen and maca exhibits superior therapeutic efficacy compared to the individual use of either rape pollen or maca alone. Results We prepared the rape bee pollen and maca chewable tablets, established the HPLC fingerprint map, and quantitatively analyzed four of these main components. We found that the rape bee pollen and maca chewable tablets significantly inhibited DHT, T, E2, E2/T ratio, IL-6, TNF-α, and IL-1β and reduced MDA levels and increased SOD, GSH levels. 16S rDNA gene sequencing revealed that the chewable tablet increased the abundance of the beneficial bacteria Faecalibacterium, Collinsella, Phascolarctobacterium, Kineothrix , and Lactobacillus , and decreased that of the pro-inflammatory bacterium Prevotella . Western blot indicated that the chewable tablet could significantly inhibit the IL-6, p -JAK2, and p -STAT3 protein expression levels. Conclusion We found that rape bee pollen and maca chewable tablets had a protective effect on rats with BPH, and also found that the combination of rape bee pollen and maca was better than separate application. The mechanism may be related to the gut microbiota and IL-6/JAK2/STAT3 signaling pathway.

✓ 已验证 DOI PubMed 高影响因子
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2018 · IF 3.909

Maca polysaccharides: Extraction optimization, structural features and anti-fatigue activities

Yujuan Li,Yizhou Xin,Fangxue Xu,Mengmeng Zheng,Xiaozhi Xi,Xiaowei Cui,Hui Cao,Hong Guo,Chunchao Han

The maca polysaccharides optimal extraction conditions were obtained by using response surface methodology (RSM) method and the anti-fatigue activity of maca polysaccharides (MCP) was explored. The maca polysaccharides extract yield of RSM could reach 9.97 mg/g by using the model predicts, and the total sugar and protein purity were 61.00% and 4.46% with the further isolation process, respectively. And the monosaccharide compositions obtained by gas chromatograph (GC) were composed of rhamnose (rha), glucose (glc), galactose (gal) with the ratio of 2.34:10.21:1.00. Furthermore, the anti-fatigue activity was evaluated by the swimming parameter, biochemistry parameters (liver glycogen (LG), blood urea nitrogen (BUN), and lactic acid (LD)), the result indicated that the low-dose maca polysaccharides group had the significant anti-fatigue activity.

CAS / MDL: 76-05-1
研究领域: 药学 · 食品科学 · 生物化学
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