Mishra Abhay P, Yalo Masande, Nambooze Jennifer, Pohl Carolina H, Kemp Gabré, Setsiba Lekgoana K, Matsabisa Motlalepula G
Department of Pharmacology, University of Free State, Bloemfontein - South Africa.
Cosmetics and Natural Products Research Centre (CosNat), Department of Pharmaceutical Technology, Naresuan University, Tha Pho, Phitsanulok - Thailand.
Drug Target Insights. 2025 Jan 13;19:1-10. doi: 10.33393/dti.2025.3171. eCollection 2025 Jan-Dec.
biofilm formation is a significant contributor to antifungal resistance, necessitating new treatment strategies. Lin., a traditional herbal remedy, has shown promise in combating microbial infections. The purpose of this study was to assess the antibiofilm activity of the methanol extract of leaves alone or with the addition of fluconazole against .
Phytochemicals from the methanol extract were analyzed by LC-MS, the XTT assay was used for metabolic activity, and morphological characteristics were examined using scanning electron microscopy (SEM). Molecular docking screening of identified compounds in methanol leaves extract against a Sap3 receptor (PDB: 2H6T) was also performed.
The LC-MS analysis detected 17 possible phytochemicals. The methanol extract showed a dose-dependent inhibition of biofilm formation, with maximum inhibition of ~60% observed at 240 μg/ml, and inhibition by fluconazole increased from 32% to 76% as the concentration increased from 15 to 240 μg/ml. The combination of and fluconazole increased the inhibition significantly, from 74% to 78% at 15 μg/ml to 240 μg/mL, respectively. SEM of control and treated biofilms showed an altered morphology and loss of cell integrity by the combination, corroborating the findings. Plant phytochemicals also possess high binding affinity (-9.7 to 8.0 kcal/mol, respectively) for the Sap3 enzyme and may therefore have therapeutic potential against .
Consequently, the findings indicate that compounds in the methanol extract may function in concert with fluconazole at sub-inhibitory concentrations to suppress biofilm formation. This finding paves the way for the formulation and development of antifungal treatment regimens that may limit the development of fluconazole resistance employing this plant part.
生物膜形成是导致抗真菌耐药性的一个重要因素，因此需要新的治疗策略。传统草药林已显示出对抗微生物感染的潜力。本研究的目的是评估叶甲醇提取物单独或添加氟康唑对的抗生物膜活性。
通过液相色谱-质谱联用（LC-MS）分析甲醇提取物中的植物化学物质，采用XTT法检测代谢活性，并使用扫描电子显微镜（SEM）检查形态特征。还对甲醇叶提取物中鉴定出的化合物针对Sap3受体（蛋白质数据银行：2H6T）进行了分子对接筛选。
LC-MS分析检测到17种可能的植物化学物质。甲醇提取物对生物膜形成表现出剂量依赖性抑制，在240μg/ml时观察到最大抑制率约为60%，随着氟康唑浓度从15μg/ml增加到240μg/ml，其抑制率从32%增加到76%。林和氟康唑的组合显著提高了抑制率，分别从15μg/ml时的74%增加到240μg/ml时的78%。对照和处理后的生物膜的扫描电镜观察显示，组合处理使形态改变且细胞完整性丧失，证实了上述结果。植物植物化学物质对Sap3酶也具有高结合亲和力（分别为-9.7至8.0千卡/摩尔），因此可能具有抗的治疗潜力。
因此，研究结果表明林甲醇提取物中的化合物可能在亚抑制浓度下与氟康唑协同作用，以抑制生物膜形成。这一发现为制定和开发抗真菌治疗方案铺平了道路，该方案可能利用该植物部位限制氟康唑耐药性的发展。
