Chen Chieh-Yin, Wu Pei-Chen, Tsao Nai-Wen, Tseng Yen-Hsueh, Chu Fang-Hua, Wang Sheng-Yang
Experimental Forest, College of Bio-Resources and Agriculture, National Taiwan University, Nantou County 55750, Taiwan.
Department of Forestry, National Chung Hsing University, Taichung 40227, Taiwan.
Plants (Basel). 2022 Nov 26;11(23):3252. doi: 10.3390/plants11233252.
is an endemic species of Taiwan. Although most Cinnamomum plants have significant biological activity, the bioactivity investment of is rare. Since inflammation plays an important role in many diseases, anti-inflammatory compounds can be developed into healthcare products. Therefore, we first conducted a study on the anti-inflammatory activity of leaves. First, we examined the antiinflammation activity of essential oil from leaves, and it revealed potent anti-inflammatory activity. A total of 23 volatile compounds were identified in leaves' essential oil by using GC/MS analysis. Among them were 1,8-cineole (35.94%), α-eudesmol (6.17%), pinene (7.55%), sabinene (5.06%), and isobornyl acetate (4.81%). According to previous studies, 1,8-cineole might be an anti-inflammation principal compound of leaves. Next, the ethanolic extracts of leaves also exhibited good anti-inflammatory activity. Two bioactive compounds, isoburmanol () and burmanol (), were isolated from the ethyl acetate soluble fraction by using the bioactivity-guided separation protocol and spectroscopic analysis. was obtained from for the first time, and was isolated for the first time from natural resources. Both and could inhibit the production of nitric oxide (NO), and the IC values were 14.0 μM and 43.8 μM, RAW 264.7 cells after induction of lipopolysaccharide. Furthermore, and also revealed significant inhabitation effects on iNOS and COX-2 protein expression. The anti-inflammation activity of and was different from the common pathway of inhibiting NF-κB. Both of them could inhibit the production of NO and PGE by directly inhibiting the AP-1 (c-Jun) protein and then inhibiting the downstream iNOS and COX-2. Although both and possessed significant anti-inflammatory activity, the activity of was better than . Through molecular docking simulation analysis, the results show that and interact with AP-1, inhibit the binding of AP-1 to DNA, and cause AP-1 to fail to transcribe the related factors of inflammation. The binding ability of AP-1 and was stronger than , and that is the reason why exhibited better activities in both downstream proteins and inflammatory cytokines. Based on the results obtained in this study, the essential oil and and isolated from leaves have good anti-inflammatory activities, and it is expected to be used as a reference for the development of medical care products in the future.
是台湾的特有物种。虽然大多数樟属植物具有显著的生物活性，但[该物种名称]的生物活性研究较少。由于炎症在许多疾病中起重要作用，抗炎化合物可开发成保健品。因此，我们首先对[该物种名称]叶的抗炎活性进行了研究。首先，我们检测了[该物种名称]叶精油的抗炎活性，结果显示其具有较强的抗炎活性。通过气相色谱/质谱联用（GC/MS）分析，在[该物种名称]叶精油中鉴定出23种挥发性化合物。其中包括1,8-桉叶素（35.94%）、α-桉叶醇（6.17%）、蒎烯（7.55%）、桧烯（5.06%）和乙酸异冰片酯（4.81%）。根据以往研究，1,8-桉叶素可能是[该物种名称]叶的抗炎主要化合物。接下来，[该物种名称]叶的乙醇提取物也表现出良好的抗炎活性。采用生物活性导向分离法和光谱分析，从乙酸乙酯可溶部分分离出两种生物活性化合物，异布尔马醇（[化合物名称1]）和布尔马醇（[化合物名称2]）。[化合物名称1]首次从[该物种名称]中获得，[化合物名称2]首次从自然资源中分离得到。[化合物名称1]和[化合物名称2]均可抑制一氧化氮（NO）的产生，在脂多糖诱导的RAW 264.7细胞中，其半数抑制浓度（IC）值分别为14.0 μM和43.8 μM。此外，[化合物名称1]和[化合物名称2]对诱导型一氧化氮合酶（iNOS）和环氧化酶-2（COX-2）蛋白表达也有显著的抑制作用。[化合物名称1]和[化合物名称2]的抗炎活性不同于抑制核因子κB（NF-κB）的常见途径。它们均可通过直接抑制激活蛋白-1（AP-1，c-Jun）蛋白，进而抑制下游的iNOS和COX-2，从而抑制NO和前列腺素E（PGE）的产生。虽然[化合物名称1]和[化合物名称2]均具有显著的抗炎活性，但[化合物名称1]的活性优于[化合物名称2]。通过分子对接模拟分析，结果表明[化合物名称1]和[化合物名称2]与AP-1相互作用，抑制AP-1与DNA的结合，导致AP-1无法转录炎症相关因子。AP-1与[化合物名称1]的结合能力强于[化合物名称2]，这就是[化合物名称1]在下游蛋白和炎性细胞因子方面表现出更好活性的原因。基于本研究所得结果，从[该物种名称]叶中分离得到的精油以及[化合物名称1]和[化合物名称2]具有良好的抗炎活性，有望为未来医疗保健产品的开发提供参考。
