炎症与心血管疾病有关,生育三烯酚是有效的低胆固醇血症药物,可降低β-羟基-β-甲基-戊二酰辅酶A还原酶的活性,通过泛素-蛋白酶体途径降解。各种生育三烯酚(α-,γ-,或δ-生育三烯酚)治疗抑制RAW264.7细胞和BALB/c小鼠中20S兔肌肉蛋白酶体(>50%)的胰凝乳蛋白酶样活性。此外,各种生育三烯酚(α-,γ-,或δ-生育三烯酚),α-生育酚,槲皮素,核黄素,(-)科里内酯,阿米洛利,补充地塞米松的饮食饲喂鸡(4周)导致总胆固醇降低,LDL-胆固醇,和甘油三酯。在来自RAW264.7细胞的巨噬细胞中也观察到这种趋势,在LPS诱导的巯基乙酸引起的来自C57BL/6,BALB/c,LMP7/MECL-1-/-,和PPAR-α-/-敲除小鼠来自年轻(4周龄)和衰老(42周龄)小鼠,导致显著抑制TNF-α和一氧化氮水平(30%至70%),阻断P-IκB蛋白的降解,和减少NF-κB的激活,随后TNF-αmRNA水平的基因抑制,IL-1β,IL-6和iNOS。在人类研究中,正常或高胆固醇血症受试者服用两次胶囊/天NS-7或NS-6(4周)显示血清CRP降低,NO,γ-GT,总胆固醇,LDL-胆固醇,与高胆固醇血症受试者相比,正常的甘油三酯水平(12%至39%)。在第二项研究中,高胆固醇血症的受试者被给予增加剂量的δ-生育三烯酚(125毫克,250毫克,500毫克,和750毫克/天)加AHA第一步饮食(4周)。最有效剂量的生育三烯酚(250毫克/天)可用于降低血清NO(40%),CRP(40%),MDA(34%),γ-GT(22%),和炎症细胞因子IL-1α,IL-12,IFN-γ下降15%至17%,并将TAS水平提高22%。
Inflammation has been implicated in cardiovascular disease and tocotrienols are potent hypocholesterolemic agents that reduce β-hydroxy-β-methyl-glutaryl coenzyme A reductase activity, which is degraded via the ubiquitin-proteasome pathway. Impact of various tocotrienols (α-, γ-, or δ-tocotrienol) treatments inhibit the chymotrypsin-like activity of 20S rabbit muscle proteasome (>50%) in RAW 264.7 cells and BALB/c mice. Moreover, the effect of various tocotrienols (α-, γ-, or δ-tocotrienol), α-tocopherol, quercetin, riboflavin, (-) Corey lactone, amiloride, dexamethasone supplemented diets fed to chickens (4-weeks) resulted in reduction of total cholesterol, LDL-cholesterol, and triglycerides. This trend was also observed in macrophages from RAW 264.7 cells, in LPS-induced thioglycolate-elicited peritoneal macrophages derived from C57BL/6, BALB/c, LMP7/MECL-1-/-, and PPAR-α-/- knockout mice from young (4-week-old) and senescent (42-week-old) mice, resulting in significant inhibition of TNF-α and nitric oxide levels (30% to 70%), blocked degradation of P-IκB protein, and decreased activation of NF-κB, followed gene suppression of mRNA levels of TNF-α, IL-1β, IL-6, and iNOS. In human study, normal or hypercholesterolemic subjects administered two capsules/d of NS-7 or NS-6 (4-weeks) showed decrease in serum CRP, NO, γ-GT, total cholesterol, LDL-cholesterol, and triglycerides levels in normal as compared to hypercholesterolemic subjects (12% to 39%). In second study, hypercholesterolemic subjects were given increasing doses of δ-tocotrienol (125 mg, 250 mg, 500 mg, and 750 mg/day) plus AHA Step-1 diet (4-weeks). The most effective dose of tocotrienols (250 mg/day) may be used to lower serum NO (40%), CRP (40%), MDA (34%), γ-GT (22 %), and inflammatory cytokines IL-1α, IL-12, IFN-γ by 15% to 17%, and increase TAS levels by 22%.