Taiwe Germain Sotoing, Kouamou Arielle Larissa Ndieudieu, Ambassa Armelle Rosalie Mbang, Menanga Joseph Renaud, Tchoya Thierry Bang, Dzeufiet Paul Desire Djomeni
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J Basic Clin Physiol Pharmacol. 2017 Sep 26;28(5):425-435. doi: 10.1515/jbcpp-2017-0048.
The root bark of Anthocleista djalonensis A. Chev. (Loganiaceae) is widely used in traditional medicine in Northern Cameroon to treat epilepsy and related conditions, such as migraine, insomnia, dementia, anxiety, and mood disorders.
To investigate the anticonvulsant effects and the possible mechanisms of this plant, an aqueous extract of Anthocleista djalonensis (AEAD) was evaluated by using animal models of bicuculline-, picrotoxin-, pilocarpine-, and pentylenetetrazole-induced convulsions. Their effects on brain γ-aminobutyric acid (GABA) concentration and GABA-T activity were also determined.
This extract significantly protected mice against bicuculline-induced motor seizures. It provided 80% protection against picrotoxin-induced tonic-clonic seizures, and strongly antagonized convulsions induced by pilocarpine. AEAD also protected 100% of mice against pentylenetetrazole-induced seizures. Flumazenil, a central benzodiazepine receptor antagonist and FG7142, a partial inverse agonist in the benzodiazepine site of the GABAA receptor complex, were found to have an inhibitory effect on the anticonvulsant action of AEAD in pentylenetetrazole test. Finally, the brain GABA concentration was significantly increased and GABA-T activity was inhibited by AEAD.
The effects of Anthocleista djalonensis suggested the presence of anticonvulsant properties that might involve an action on benzodiazepine and/or GABA sites in the GABAA receptor complex or by modulating GABA concentration in the central nervous system (CNS).
喀麦隆北部传统医学中广泛使用 Djallon 非洲山橙（夹竹桃科）的根皮来治疗癫痫及相关病症，如偏头痛、失眠、痴呆、焦虑和情绪障碍。
为研究该植物的抗惊厥作用及其可能机制，采用荷包牡丹碱、印防己毒素、毛果芸香碱和戊四氮诱导惊厥的动物模型对 Djallon 非洲山橙水提取物（AEAD）进行评估。还测定了其对脑γ-氨基丁酸（GABA）浓度和 GABA 转氨酶（GABA-T）活性的影响。
该提取物能显著保护小鼠免受荷包牡丹碱诱导的运动性癫痫发作。对印防己毒素诱导的强直阵挛性癫痫发作提供 80%的保护，并强烈拮抗毛果芸香碱诱导的惊厥。AEAD 还能 100%保护小鼠免受戊四氮诱导的癫痫发作。在戊四氮试验中，发现中枢苯二氮䓬受体拮抗剂氟马西尼和 GABAA 受体复合物苯二氮䓬位点的部分反向激动剂 FG7142 对 AEAD 的抗惊厥作用有抑制作用。最后，AEAD 可显著提高脑 GABA 浓度并抑制 GABA-T 活性。
Djallon 非洲山橙的作用表明其具有抗惊厥特性，可能通过作用于 GABAA 受体复合物中的苯二氮䓬和/或 GABA 位点，或通过调节中枢神经系统（CNS）中的 GABA 浓度来实现。
