Appraising the Neurobehavioural Toxicity Potential of Aqueous Methanol Leaf Extract of Tapinanthus globiferus Growing on Azadirachta indica

The high prevalence and disease burden of anxiety disorders against the paucity and liabilities of existing anxiolytics indicates a need for the discovery of additional/new anti-anxiety agents. However, it is necessary to further screen these new/putative anxiolytic compounds/extracts to rule out the unwanted neurobehavioural toxicities inherent in the existing anti-anxiety drugs. Aqueous methanol leaf extract of Tapinanthus globiferusgrowing on Azadirachta indicahost tree has previouslydemonstrated significant (p<0.05) anxiolytic effects in mice. This study, therefore, set out to counter-screen this extract for locomotion-suppressant, acute amnesic, sedative (myorelaxant) and hypnotic effects using standard mouse behavioural and biochemical paradigms. The leaf extract (150, 500 and 1500 mg/kg) did not cause significant (p>0.05) alterations in spontaneous locomotor activity, motor coordination/balance, sleep onset or duration,but dose-dependent and significant (p<0.05) increases (63.28±5.63, 65.63±4.12 and 69.18±3.69) in novel object recognition indices of extract-treated compared to 51.54±4.03 and 61.06±2.91 scores in diazepam-and aqua-treated mice, respectively.These findings indicate the aqueous methanol leaf extract is mostly devoid of the evaluated neurobehavioural toxicities and may possess short-term memory enhancement property in mice. These findings may justifythe traditional use of Tapinanthus globiferusextracts for memory enhancement

Masking Efficiency and Regularity of Bitterness Suppressants to Berberine Hydrochloride Based on Tongue Taste and Electronic Tongue Taste / 中国药学杂志

OBJECTIVE: To explore the masking efficiency and regularity of bitterness suppressants (BS) to a representative bitterness substance berberine hydrochloride (BBR). METHODS: Some quantitative evaluation methods of BS efficiency were established based on relevant literature and our previous research. Efficiency of respectively added into eight kinds of BS such as acesulfame, on bitter degree 3 BBR solution (0.05 mg•mL-1) were evaluated using the established methods. Bitterness masking regularity of BS on BBR solution were explained by respectively establishing the relationships between tongue tasted bitter decreased value (ΔI), electronic tongue tasted bitter decreased value (ΔIe) with BS concentration (ρ). RESULTS: ①Five tongue taste bitter masking efficiency (calibrated masking rate, bitterness revised standard half effect index and so on), two electronic tongue bitter masking efficiency(first taste reduce and aftertaste reduce) were established. ②Seven kinds of bitterness suppressants efficacy indicators can be used to compare the bitterness suppressants efficacy of BS to BBR solution, and the maximum bitterness reduction of 8 kinds of BS to BBR solution is above 1.8. ③ΔI-ρ Weibull regularity models of eight BS and nine ΔIe-ρ models of six BS were brlilt.HP-β-CD, glycine and crystalline fructose had good response to two sensor, stevioside, soluble soybean polysaccharide and acesulfame had a good response to one sensor and xanthan gum and aspartame had no response to any sensor. CONCLUSION: Seven evaluation indexes and methods are built based on human tongue and electronic tongue taste method. Max standard capability index of BS is suitable for the development of bitterness suppressants in taste method and two indicators of electronic tongue are also can be used as indicative indicators. Masking regularity of BS to BBR solution is exposed which could provide reference for the development and application of more BS.

Neuropharmacological Targets for Drug Action in Vestibular Sensory Pathways

The use of pharmacological agents is often the preferred approach to the management of vestibular dysfunction. In the vestibular sensory pathways, the sensory neuroepithelia are thought to be influenced by a diverse number of neuroactive substances that may act to enhance or inhibit the effect of the primary neurotransmitters [i.e., glutamate (Glu) and acetylcholine (ACh)] or alter their patterns of release. This review summarizes various efforts to identify drug targets including neurotransmitter and neuromodulator receptors in the vestibular sensory pathways. Identifying these receptor targets provides a strategic basis to use specific pharmacological tools to modify receptor function in the treatment and management of debilitating balance disorders. A review of the literature reveals that most investigations of the neuropharmacology of peripheral vestibular function have been performed using in vitro or ex vivo animal preparations rather than studying drug action on the normal intact vestibular system in situ. Such noninvasive approaches could aid the development of more accurate and effective intervention strategies for the treatment of dizziness and vertigo. The current review explores the major neuropharmacological targets for drug action in the vestibular system.

Neuropharmacological Targets for Drug Action in Vestibular Sensory Pathways

The use of pharmacological agents is often the preferred approach to the management of vestibular dysfunction. In the vestibular sensory pathways, the sensory neuroepithelia are thought to be influenced by a diverse number of neuroactive substances that may act to enhance or inhibit the effect of the primary neurotransmitters [i.e., glutamate (Glu) and acetylcholine (ACh)] or alter their patterns of release. This review summarizes various efforts to identify drug targets including neurotransmitter and neuromodulator receptors in the vestibular sensory pathways. Identifying these receptor targets provides a strategic basis to use specific pharmacological tools to modify receptor function in the treatment and management of debilitating balance disorders. A review of the literature reveals that most investigations of the neuropharmacology of peripheral vestibular function have been performed using in vitro or ex vivo animal preparations rather than studying drug action on the normal intact vestibular system in situ. Such noninvasive approaches could aid the development of more accurate and effective intervention strategies for the treatment of dizziness and vertigo. The current review explores the major neuropharmacological targets for drug action in the vestibular system.

Intracerebral Hemorrhage related to Phentermine as an Appetite Suppressant

We present a case report indicating that the administration of phentermine, an appetite suppressant with sympathomimetic activity, can provoke an intracerebral hemorrhage. A 48-year-old woman with no previously established cerebrovascular risk fa ctors and who had taken phentermine for 30 days developed sudden-onset left hemiparesis. Brain magnetic resonance imaging revealed an acute intracerebral hemorrhage involving the right thalamus. This case indicates that physicians should be aware of the relevant cause of medication history including appetite suppressants in young patients with an acute intracerebral hemorrhage.

Evaluating Muco-suppressant, Anti-tussive and Safety Profile of Polyscias fruticosa (L.) Harms (Araliaceae) in Asthma Management.

Background: Polyscias fruticosa is been used in Ghanaian folkloric medicine for the management of asthma and its related complications. Aim: This study evaluated the muco-suppressant, anti-tussive, and safety profile of an ethanolic leaf extract of Polyscias fruticosa in its use as an anti-asthmatic. Place and Duration of Study: Department of Pharmacology, Faculty of Pharmacy and Pharmaceutical Sciences, KNUST, Kumasi, Ghana and the School of Physical Sciences, University of Cape-Coast, Cape-Coast, Ghana; between December, 2013 and May, 2014. Methodology: Preliminary phytochemical screening was carried out on the extract. Ammonium chloride-induced tracheal mucus phenol red secretion in ICR mice and the suppression of citric acid-induced cough in Dunkin-Hartley guinea pigs were determined after treatment of experimental animals with 100 mg/kg sodium cromoglycate, or 20 mg/kg dihydrocodeine respectively, as well as with 100, 250, or 500 mg/kg of the extract. A 100, 250, and 500 mg/kg dose of the extract was administered daily for 28 days to groups of guinea pigs to establish a safety profile in a sub-chronic toxicity study. Results: Phytochemical screening revealed the presence of saponins and cyanogenetic glycosides, alkaloids, and sterols. The extract significantly inhibited (P ≤ .01 - 0.001) tracheal mucus phenol red secretion, and suppression of citric acid-induced cough. There were no significant changes in body weight, haematological profile, as well as liver and kidney functions in the sub-chronic toxicity study. Conclusion: The findings indicate that the ethanolic leaf extract of Polyscias fruticosa has muco-suppressant and anti-tussive properties, and is safe to use; hence a suitable adjunct/remedy for the management of asthma.

Recent Progress in Clinical Application of Ranibizumab / 中国药师

Ranibizumab is a recombinant rat monoclonal antibody fragment of the second generation humanized VEGF. Ranibi-zumab can bind all of active VEGF-A to inhibit the bond between VEGF-A and VEGFR1 or VEGFR2. As the results, the vascular en-dothelial proliferation and vascular permeability can be reduced, and the new vessels angiogenesis can be prevented. The article sys-tematically searched and summarized the relative literatures to offer high-quality evidences for the recent clinical application of ranibi-zumab in ophthalmology.

Anti-tussive, muco-suppressant and expectorant properties, and the safety profile of a hydro-ethanolic extract of Scoparia dulcis.

Background: Scoparia dulcis is used in Ghanaian folkloric medicine for the management of asthma and its related complications. This study was therefore aimed at evaluating the anti-tussive, muco-suppressant and expectorant properties of hydroethanolic extract of S. dulcis (SDE), and to ascertain its safety for use in asthma and obstructive pulmonary disease management. Methods: The number of coughs induced in guinea pigs using citric acid and the concentration of phenol red secreted in tracheae of mice were measured. Preliminary phytochemical analysis was conducted on the extract using standard procedures. Safety for use of the extract was assessed by conducting an acute and delayed toxicity test. Results: The extract showed a dose-independent inhibition (p ≤ 0.001) of cough elicited by 7.5% citric acid, and a dose-dependent increase (p ≤ 0.05) in the amount of phenol red output in mice tracheae similar to that of ammonium chloride. For the muco-suppressant activity, SDE dose-dependently reduced (p ≤ 0.001) the concentration of ammonium chloride-induced phenol red secretions from mice tracheae. Phytochemical screening showed the presence of tannins, alkaloids, glycosides, saponins, steroids, and phenolic compounds. No acute and/or delayed toxic symptoms were observed after an oral administration of up to 5 g/kg of S. dulcis extract. Conclusion: The results showed that S. dulcis extract has anti-tussive, muco-suppressant and, expectorant and/or mucolytic properties; making it a possible remedy for asthma, and obstructive pulmonary disease.

A Case of Ischemic Stroke Associated with Phendimetrazine as an Appetite Suppressant

The published case series have suggested that appetite suppressants had some association with the development of stroke. Phendimetrazine is an appetite suppressant with sympathomimetic activity and it has a similar chemical structure with amphetamines. We report that a 22-year-old woman who had taken phendimetrazine for one month developed sudden right homonymous hemianopsia. MRI showed acute infarction in the territory of left posterior cerebral artery (PCA). Phendimetrazine should be considered as a cause of ischemic stroke.