Nakano Daisuke, Ogura Kyoichi, Miyakoshi Masazumi, Ishii Fumie, Kawanishi Hideaki, Kurumazuka Daisuke, Kwak Chol-Jun, Ikemura Kenji, Takaoka Masanori, Moriguchi Shigeo, Iino Taeko, Kusumoto Aki, Asami Sumio, Shibata Hiroshi, Kiso Yoshinobu, Matsumura Yasuo
Department of Pharmacology, Osaka University of Pharmaceutical Sciences, Japan.
Biosci Biotechnol Biochem. 2006 May;70(5):1118-26. doi: 10.1271/bbb.70.1118.
Sesame peptide powder (SPP) exhibited angiotensin I-converting enzyme (ACE) inhibitory activity, and significantly and temporarily decreased the systolic blood pressure (SBP) in spontaneously hypertensive rats (SHRs) by a single administration (1 and 10 mg/kg). Six peptide ACE inhibitors were isolated and identified from SPP. The representative peptides, Leu-Val-Tyr, Leu-Gln-Pro and Leu-Lys-Tyr, could competitively inhibit ACE activity at respective Ki values of 0.92 microM, 0.50 microM, and 0.48 microM. A reconstituted sesame peptide mixture of Leu-Ser-Ala, Leu-Gln-Pro, Leu-Lys-Tyr, Ile-Val-Tyr, Val-Ile-Tyr, Leu-Val-Tyr, and Met-Leu-Pro-Ala-Tyr according to their content ratio in SPP showed a strong antihypertensive effect on SHR at doses of 3.63 and 36.3 microg/kg, which accounted for more than 70% of the corresponding dosage for the SPP-induced hypotensive effect. Repeated oral administration of SPP also lowered both SBP and the aortic ACE activity in SHR. These results demonstrate that SPP would be a beneficial ingredient for preventing and providing therapy against hypertension and its related diseases.
芝麻肽粉（SPP）具有血管紧张素I转换酶（ACE）抑制活性，单次给药（1和10 mg/kg）可显著且暂时降低自发性高血压大鼠（SHR）的收缩压（SBP）。从SPP中分离并鉴定出六种肽类ACE抑制剂。代表性肽段Leu-Val-Tyr、Leu-Gln-Pro和Leu-Lys-Tyr可分别以0.92 microM、0.50 microM和0.48 microM的Ki值竞争性抑制ACE活性。根据其在SPP中的含量比例重新配制的Leu-Ser-Ala、Leu-Gln-Pro、Leu-Lys-Tyr、Ile-Val-Tyr、Val-Ile-Tyr、Leu-Val-Tyr和Met-Leu-Pro-Ala-Tyr芝麻肽混合物，在3.63和36.3 microg/kg剂量下对SHR显示出强烈的降压作用，这占SPP诱导的降压作用相应剂量的70%以上。重复口服SPP也可降低SHR的SBP和主动脉ACE活性。这些结果表明，SPP将是预防和治疗高血压及其相关疾病的有益成分。
