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Prophylactic Effects of Asiaticoside-Based Standardized Extract of Centella Asiatica (L.) Urban Leaves on Experimental Migraine: Involvement of 5HT1A/1B Receptors

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Prophylactic Effects of Asiaticoside-Based Standardized Extract of Centella Asiatica (L.) Urban Leaves on Experimental Migraine: Involvement of 5HT1A/1B Receptors Chinese Journal of Natural Chinese Journal of Natural Medicines 2015, 13(4): 0274−0282 Medicines doi: 10.3724/SP.J.1009.2015.00274 Prophylactic effects of asiaticoside-based standardized extract of Centella asiatica (L.) Urban leaves on experimental migraine: Involvement of 5HT1A/1B receptors Vijeta Bobade1, Subhash L. Bodhankar1*, Urmila Aswar2, Vishwaraman Mohan3, Prasad Thakurdesai3 1Department of Pharmacology, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Erandwane, Pune-411038, India; 2Department of Pharmacology, Sinhgad Institute of Pharmacy, Narhe, Pune 411041, India; 3Indus Biotech Private Limited, 1, Rahul residency, Kondhwa, Pune-411026, India Available online 20 Apr. 2015 [ABSTRACT] The present study aimed at evaluation of prophylactic efficacy and possible mechanisms of asiaticoside (AS) based standardized extract of Centella asiatica (L.) Urban leaves (INDCA) in animal models of migraine. The effects of oral and intranasal (i.n.) pretreatment of INDCA (acute and 7-days subacute) were evaluated against nitroglycerine (NTG, 10 mg·kg−1, i.p.) and bra- dykinin (BK, 10 µg, intra-arterial) induced hyperalgesia in rats. Tail flick latencies (from 0 to 240 min) post-NTG treatment and the number of vocalizations post-BK treatment were recorded as a measure of hyperalgesia. Separate groups of rats for negative (Normal) and positive (sumatriptan, 42 mg·kg−1, s.c.) controls were included. The interaction of INDCA with selective 5-HT1A, 5-HT1B, and 5-HT1D receptor antagonists (NAN-190, Isamoltane hemifumarate, and BRL-15572 respectively) against NTG-induced hyperalgesia was also evaluated. Acute and sub-acute pre-treatment of INDCA [10 and 30 mg·kg−1 (oral) and 100 µg/rat (i.n.) showed significant anti-nociception activity, and reversal of the NTG-induced hyperalgesia and brain 5-HT concentration decline. Oral pre-treatment with INDCA (30 mg·kg−1, 7 d) showed significant reduction in the number of vocalization. The anti-nociceptive effects of INDCA were blocked by 5-HT1A and 5-HT1B but not 5-HT1D receptor antagonists. In conclusion, INDCA demonstrated promising anti-nociceptive effects in animal models of migraine, probably through 5-HT1A/1B medicated action. [KEY WORDS] Centella asiatica (L.) Urban; Experimental migraine; Anti-nociception; Serotonin, 5HT1A and 5HT1B receptors [CLC Number] R965 [Document code] A [Article ID] 2095-6975(2015)02-0274-09 cluding nausea, vomiting, and increased sensitivity to light Introduction and sounds. Migraine attacks can be unilateral throbbing headache, worsened by movements and routine daily activi- Migraine is a disabling headache characterized by inter- ties, and lasting from 4 to 72 h. The underlying mechanisms mittent attacks with a number of physiological and emotional of migraine interspersed with acute symptoms of attack ap- stressors associated with pain, tiredness, nausea, vomiting, pear to be increasingly complex. An important aspect of mi- photophobia, or phonophobia [1]. Migraine is multi-mechanistic graine heterogeneity is comorbidity with other neurological, disease and associated with a wide array of symptoms in- cardiovascular, and psychiatric diseases [2]. Migraine associ- ated aura is associated with peripheral sensitization is an acute, chemical-induced form of functional plasticity, which con- [Received on] 28-May-2014 verts high-threshold nociceptors into low-threshold sensory [Research funding] This work was supported by Indus Biotech Pri- vate Limited, Pune. neurons. This form of sensitization occurs in migraine attacks [*Corresponding author] Tel: +91-20-24537237 (Ext. 29), Fax: where the nerve terminals (meningeal nociceptors) of the +91-20-25439386, E-mail: [email protected] neurons of the trigeminal ganglion are soaked with the "in- All the authors have no conflict of interest to declare. flammatory" soup (prostaglandin E2, bradykinin, serotonin, – 274 – Vijeta Bobade, et al. / Chin J Nat Med, 2015, 13(4): 274−282 and cytokines) along with the vasculature of the cerebral dura major pentacyclic triterpenoid saponin component of CAE mater [3]. and has been shown to be bioactive component of CAE and Pharmacological treatment for migraine falls into two TTCA. Amongst the most promising pharmacological activi- main categories: symptomatic (acute) and prophylactic [4]. ties of AS are antidepressant [18] and anxiolytic [19-20] activities. Despite the pharmacological advances for the treatment of These effects are believed to be mediated through the hypo- migraine, patients are forced to endure symptoms until the thalamic-pituitary-adrenocortical (HPA) axis, relieving stress medications take effect and so experience a poor quality of and increasing the contents of monoaminergic neurotransmit- life despite an aggressive regimen of pharmacotherapy [5]. ters [21]. Recently, we have reported promising antidepressant Current acute symptomatic therapy for migraine includes activity of AS-based standardized extract of Centella asiatica NSAIDS, and migraine specific therapies such as triptans and L. leaves (INDCA) against mood related parameters in ergot derivatives play an important role in aborting the mi- chronic stress-medicated depression, in olfactory bulbectomy graine attacks [6]. Such symptomatic treatments can be quick (OBX) rats [22] and suicidal behaviour related traits [23]. As the and effective for pain relief and disappearance of associated management of stress, anxiety and depression is an important symptoms (nausea, photophobia, and phonophobia). However, component in the migraine prophylaxis, INDCA can be ex- inability to provide complete full pain relief and contraindica- plored and developed as a promising agent. However, such tions such as cardiovascular diseases [7] limit the use of studies have not been attempted. Therefore, the present study symptomatic treatments. Therefore, prophylactic (preventive) was undertaken with an objective to evaluate prophylactic treatment of migraine is recommended for patients with fre- efficacy INDCA in nitroglycerine (NTG) and bradykinin quent and/or disabling attacks. Most of the drugs recently (BK)-induced hyperalgesia in rats. Both models are used in migraine prophylaxis have been identified by seren- well-validated and produce acute hyperalgesia condition dipity and they have been originally approved for other indi- similar to migraine. Considering the important role of sero- cations [8]. Most notable amongst them are antidepressants [9], tonergic (5-HT) receptor system in migraine prophylaxis, we beta-adrenergic blockers, calcium channel blockers, and an- also attempted to explore role of 5-HT1 serotonergic receptor tiepileptic drugs [8]. However, the use of these agents is lim- subtypes (5-HT1A, 5-HT1B and 5-HT1D) in the mechanism ited by inconclusive evidences on targets of migraine prophy- of INDCA. laxis (reduction in frequency and intensity of attacks and to Material and Methods decrease disability related to chronic headache) and dose limiting side-effects. Animals Stress is reported to impact the migraine sufferer at many Wistar rats (weighing 200–250 g) of either sex were pur- levels [10]. The stress related psychological factors such as chased from National Toxicology Centre (NTC), Pune, India. mood and anxiety are known causes of poor response to mi- The animals were housed at a temperature of 25 ± 1 °C and graine prophylaxis therapies [11]. These stress related disorders relative humidity of 45%–55% under 12 : 12 light: dark cycle. are often highlighted as trigger factors of migraine attacks, The animals had free access to feed pellets (Chakan oil mills but may also appear as a psychological reaction to recurrent Ltd., Sangli, Maharashtra, India) and tap water ad libitum. and severe migraine attacks [2, 12]. The experimental protocol (No: CPCSEA/51/2010) was ap- Serotonin (5-HT), a neurotransmitter, has been impli- proved by the Institutional Animal Ethics Committee (IAEC) cated in the pathophysiology of the migraine syndrome. Me- of Poona College of Pharmacy, Pune, India. All observations thysergide (nonspecific antagonist of 5-HT receptors) is re- were recorded between 8: 00 and 15: 00 and each rat was ported to be effective for migraine prophylaxis [13]. Among a used only once. To avoid subjective bias, the observer was not variety of identified serotonin receptors, 5-HT1A attracts aware of the administrated treatment. Each experimental particular attention due to its central role in the regulation of group consisted of 6 rats unless otherwise stated. The rats 5-HT-ergic neurotransmission and the data on its involvement were transported from the animal house to the testing area in in the mechanisms of stress response, aggressive behavior, their own cages and were allowed to adapt to the new en- anxiety, and depression [14-15]. vironment before testing. One of the promising natural products having evidence of Drugs and chemicals anxiolytic and mood elevating activity in clinic is the extract NTG (New Medicon Lab Pvt Ltd., Bangalore, India), of leaves of Centella asiatica (Linn.) Urban (CAE) [16]. Cen- sumatriptan succinate (ST) (Sun Pharmaceuticals Ltd, Mum- tella asiatica (Linn) Urban has a long history of traditional bai, India) and pentazocine (Ranbaxy Laboratories Ltd., use as a medicinal herb in traditional Chinese medicine Ahmadabad, India) ampules were purchased from local sup- (TCM), Ayurveda, and African medicine systems. Total pliers. Bradykinin (BK) and NAN-190 (selective 5-HT1A triterpenes of Centella asiatica L. leaves (TTCA) are shown receptor antagonist) were purchased
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