Gouthamchandra Kuluvar, Sudeep Heggar Venkataramana, Chandrappa Siddappa, Raj Amrith, Naveen Puttaswamy, Shyamaprasad Kodimule
Department of Biomedicinal Research, R&D Centre for Excellence, Vidya Herbs Pvt. Ltd, Bangalore, Karnataka, 560105, India.
Department of Phytochemistry, R&D Centre for Excellence, Vidya Herbs Pvt. Ltd, Bangalore, Karnataka, 560105, India.
J Inflamm Res. 2021 Mar 12;14:859-868. doi: 10.2147/JIR.S291293. eCollection 2021.
It is well known that regular turmeric extract with 95% curcuminoid is comprised of curcumin (70.07%), desmethoxycurcumin (20.28%), and bisdemethoxycurcumin (BDMC) (3.63%). In the current study for the first time, we have enriched about 3% of bisdemethoxycurcumin (BDMC) to 70% as well as named it as REVERC3 and compared anti-inflammatory activity with regular turmeric extract using in vitro and in vivo models of inflammation.
To reveal the potential anti-inflammatory mechanism of action, we investigated nitric oxide (NO) scavenging, xanthine oxidase, and lipoxygenase inhibitory activity, further determined the level of pro-inflammatory cytokines, such as interleukin 6 (IL-6), tumor necrosis factor (TNF-α) and major inflammatory mediators like cyclooxygenase (COX-2) and inducible nitric oxide synthase (iNOS), inhibition in lipopolysaccharide (LPS) induced inflammation in RAW macrophage cells. In the other hand, a carrageenan-stimulated inflammatory rat model was carried out.
Our study findings exhibited a significant anti-inflammatory activity of REVERC3 together with nitric oxide (NO), xanthine oxidase, and lipoxygenase inhibition. Further, we attenuated the levels of cyclooxygenase (COX-2), inducible nitric oxide synthase (iNOS), interleukin (IL-6) and tumor necrosis factor (TNF-α) expressions in the LPS-elicited RAW macrophage cells. REVERC3 showed a potential anti-inflammatory activity by inhibiting carrageenan induced paw edema after 4 hr at the dose of 100mg/kg body weight.
Thus, our findings collectively indicated that the REVERC3 could efficiently inhibit inflammation compared to regular turmeric extract. Since bisdemethoxycurcumin is a stable molecule it could be effectively used in the applications of health care and the nutraceutical industry, indeed which deserves further investigations.
众所周知，含95%姜黄素类化合物的常规姜黄提取物由姜黄素（70.07%）、去甲氧基姜黄素（20.28%）和双去甲氧基姜黄素（BDMC）（3.63%）组成。在本研究中，我们首次将约3%的双去甲氧基姜黄素（BDMC）富集至70%，并将其命名为REVERC3，同时使用体外和体内炎症模型，将其抗炎活性与常规姜黄提取物进行比较。
为揭示潜在的抗炎作用机制，我们研究了一氧化氮（NO）清除、黄嘌呤氧化酶和脂氧合酶抑制活性，进一步测定了促炎细胞因子水平，如白细胞介素6（IL-6）、肿瘤坏死因子（TNF-α）以及主要炎症介质如环氧合酶（COX-2）和诱导型一氧化氮合酶（iNOS），观察其对脂多糖（LPS）诱导的RAW巨噬细胞炎症的抑制作用。另一方面，建立了角叉菜胶刺激的炎症大鼠模型。
我们的研究结果显示，REVERC3具有显著的抗炎活性，同时伴有一氧化氮（NO）、黄嘌呤氧化酶和脂氧合酶抑制作用。此外，我们降低了脂多糖诱导的RAW巨噬细胞中环氧合酶（COX-2）、诱导型一氧化氮合酶（iNOS）、白细胞介素（IL-6）和肿瘤坏死因子（TNF-α）的表达水平。在100mg/kg体重剂量下，REVERC3在4小时后通过抑制角叉菜胶诱导的爪肿胀显示出潜在的抗炎活性。
因此，我们的研究结果共同表明，与常规姜黄提取物相比，REVERC3能有效抑制炎症。由于双去甲氧基姜黄素是一种稳定的分子，它可有效地用于医疗保健和营养保健品行业的应用，确实值得进一步研究。
