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Herbs with Antidepressant Effects
Published in Scott Mendelson, Herbal Treatment of Major Depression, 2019
Tetramethylpyrazine from Ligusticum chuanxiong has significant antioxidant and neuroprotective effects. It scavenges free radicals generated by the neurotoxin kainic acid and thus can attenuate kainate-induced excitotoxicity in cultured rat hippocampal neurons.3 Tetramethylpyrazine also protects the hippocampus from kainate-induced toxicity in intact rats. It partially alleviates kainate‑induced status epilepticus in rats and prevents neuronal loss in the CA3 region. It acts, at least in part, by quenching ROS, blocking lipid peroxidation, and protecting activity of the antioxidant enzymes glutathione peroxidase and glutathione reductase.4
Essential Oils as Carrier Oils
Published in K. Hüsnü Can Başer, Gerhard Buchbauer, Handbook of Essential Oils, 2020
Romana Aichinger, Gerhard Buchbauer
Eucalyptus oil, isolated from Eucalyptus globulus, a member of the Myrtaceae family, consists of more than 80% cineole and represents a promising penetration enhancer that acts on the skin barrier as it disrupts the SC bilayers, thus improving the partitioning and permeation of small polar molecules. 2,3,5,6-Tetramethylpyrazine (TMP), a lipophilic calcium-channel antagonist isolated from Ligusticum wallichii—a member from the Apiaceae family—and used for treating cardiovascular disorders, exhibits some problems when administered orally. The first-pass metabolism causes low bioavailability besides a short half-life that leads to a high, frequent dosing. To avoid the side effects that come with oral administration, a reservoir-type transdermal delivery system (TDS) that incorporates the drug and the penetration enhancer is produced; namely, a transdermal delivery system patch. For creating such a reservoir-type TDS for TMP, the following compounds are required: Carbopol gel for gelling, an EVA membrane for rate control and silicone adhesive for pressure sensitivity. With these components, an effective TDS can be formed to reach an appropriate clinical concentration. Further, the TMP patch with a clinical surface area of 20 cm2 consists of 5% eucalyptus oil, which turned out to be the best concentration for promoting drug permeation. The penetration enhancer causes a 17-fold higher permeation rate compared to an application without enhancer, as well as a lower Cmax needed for a prolonged steady-state concentration, Tmax, and mean residence time. The reservoir-type transdermal delivery system presents a promising alternative route to oral administration as it improves the permeation and, thus, the compliance (Shen et al., 2013).
Borneol and Α-asarone as adjuvant agents for improving blood–brain barrier permeability of puerarin and tetramethylpyrazine by activating adenosine receptors
Published in Drug Delivery, 2018
Jun-Yong Wu, Yong-Jiang Li, Le Yang, Yi-Yun Hu, Xiong-Bin Hu, Tian-Tian Tang, Jie-Min Wang, Xin-Yi Liu, Da-Xiong Xiang
Puerarin (PUE) is the primary bioactive ingredient from the root of Pueraria lobata (willd.) ohwi. PUE has therapeutical effects on cerebral infraction for its various pharmacological activities on cerebrovascular system, such as anti-inflammation (Wei et al., 2014; Zhang et al., 2014), anti-oxidation (Wang et al., 2014a; Zhong et al., 2014), antiplatelet aggregation (Liu et al., 2006), anti-apoptosis (Li et al., 2018), vasodilation (Wang et al., 2014c) and improving cerebral microcirculation (Wu et al., 2014; Yuan et al., 2014). Tetramethylpyrazine (TMP) is the major pharmacological ingredient of traditional Chinese medicine Chuanxiong Hort (Rhizoma Chuanxiong), TMP has been used as one of the most effective treatment for ischemic stroke (Sun et al., 2008). TMP also protects the brain from cerebral injury by anti-platelet (Sheu et al., 2000). However, the clinical application of PUE and TMP are limited by their poor brain bioavailability due to low BBB permeability.
Preparation, preliminary pharmacokinetics and brain tissue distribution of Tanshinone IIA and Tetramethylpyrazine composite nanoemulsions
Published in Pharmaceutical Development and Technology, 2019
Beilei Wang, Lufeng Hong, Yuanxu Liu, Sean K. Bedingfield, Caiyun Zhang, Can Peng, Jiajia Qian, Liqiong Zha
Ligusticum chuanxiong Hort, also known as Ligusticum wallichii Franchat (Chuan Xiong), belongs to the family of Umbelliferae and its rhizome segment has been traditionally applied for treating a range of nervous and cardiovascular system diseases in traditional Chinese medicine. Tetramethylpyrazine (TMP), an alkaloid, is one of the most important bioactive ingredients from Chuan Xiong (Qing et al. 2019), and is used clinically to treat ischemic brain injury (Shao et al. 2018) and also used to reduce migration of circulatory leukocytes (Gao et al. 2008), as a free radical scavenger (Zhou et al. 2019) and downregulating proinflammatory cytokine production. In fact, TMP has been extensively demonstrated to explicitly provide neuroprotective effects (Li et al. 2017).
Intraocular administration of tetramethylpyrazine hydrochloride to rats: a direct delivery pathway for brain targeting?
Published in Drug Delivery, 2019
Dan Mao, Fang Li, Qun Ma, Manman Dai, Huimin Zhang, Luyu Bai, Ning He
Ligustrazine, also known as tetramethylpyrazine (TMP), is the main active component in the Chinese herbal medicine Ligusticum wallichii. Tetramethylpyrazine hydrochloride (TMPH) is a fully synthetic version of this compound. Pharmacological studies have shown that TMPH is a calcium antagonist, which has many functions such as anti-platelet aggregation, stimulating the medullary respiratory center and the vasomotor center, dilating vascular and bronchial smooth muscle, and improving microcirculation (Wang et al., 2011). At present, it is widely used in the treatment of acute occlusive cardio-cerebrovascular and ischemic cardio-cerebrovascular diseases such as coronary heart disease, cerebral thrombosis, and cerebral artery embolism. The pharmacological effect is specific and the side effects are small (Ding, 2007). The commonly used dosage forms are injection and tablet. As the half-life of TMPH is short achieving sustained effects is inconvenient (Yan et al., 2015). When administered orally, the bioavailability of TMPH is decreased because of the first-pass effect of the liver (Feng et al., 2009). As a mucosal administration route, io administration is convenient, facilitates patient compliance, and can avoid gastrointestinal degradation and the first-pass effect. Therefore, I consider that tetramethylpyrazine’s target organs (brain and heart) and the ocular administration herein proposed can be advantageous in relation to classic routes. In the current study, the in vivo pharmacokinetics, including plasma pharmacokinetic and tissue distribution, of TMPH after io administration were studied to investigate the potential of the drug to exert therapeutic effects.