Neuropharmacological Assessment of the Hydroethanolic Leaf Extract of Calotropis procera (Ait). R. Br. (Apocynaceae) in Mice

Background. Calotropis procera has been widely used traditionally for its analgesic and anti-inflammatory effects. It is also reportedly used in ethnomedicine for mental health disorders including epilepsy even in the absence of supporting scientific data. Thus, the potential of the plant to affect neurological functions was evaluated. Methods. Irwin’s test was performed to determine the effect of the oral administration of the extract (30–3000 mg kg−1) on gross behaviour and physiological function. The activity meter, rotarod, pentylenetetrazol- (PTZ-) induced convulsion, pentobarbitone-induced sleep test, and the tail immersion tests were used to evaluate the spontaneous activity, neuromuscular function, convulsive threshold, sedation, and analgesic effects of the Calotropis procera extract (30–1000 mg/kg), respectively, in mice. Results. Calotropis procera extract (CPE) exhibited significant ( p < 0.0001 ) anticonvulsant and analgesic effects. There was a significant increase in withdrawal latency of the CPE-treated animals in the tail immersion test for analgesia ( p < 0.0001 ), while latency and duration of PTZ-induced convulsions were positively modulated. Calotropis procera extract showed significant ( p < 0.0001 ) central nervous system depressant effects in pentobarbitone-induced hypnosis at 100–1000 mg/kg and spontaneous activity test (30–1000 mg/kg). The extract also depicted impaired motor coordination at 100–1000 mg/kg dose levels. LD50 was estimated to be above 1000 mg kg−1. Conclusions. Calotropis procera extract has significant central nervous system depressant and analgesic effects in mice.

PHYTOPHARMACOLOGY OF HOLMSKIOLDIA SANGUINEA RETZ.: A REVIEW

Holmskioldia sanguinea Retz. is a Sub-Himalayan plant that has been cultivated in the Americas, Europe, Indo-china, Asia-Pacific, and Southern Africa. It has been used traditionally to treat rheumatism and rheumatoid arthritis, dysentery, headaches, hypertension, boils, blain, ulcers, and gynaecological problems, as well as a blood purifying concoction. The botanical description of the plant, its phytochemical constituents, and its pharmacological activities are discussed, with an emphasis on antibacterial, antihepatotoxic, antifungal, anti-inflammatory, antioxidant, antimicrobial, analgesic, central nervous system depressant, diuretic, oestrogenic, anti-implantation, and anticancer properties. Most pharmacological effects are a result of plant constituents such as alkaloids, terpenoids, tannins, flavonoids, glycosides and phenols, to name a few. Conventional wisdom should be confirmed through in vitro and in vivo studies, as well as clinical trials. Herb's anti-tumor and anti-cancer properties have generated significant interest.

Behavioural activities and chemical composition of fresh leaf essential oil of Plectranthus aegyptiacus from Southwest Nigeria in mice

Objectives: This study determined the chemical composition of essential oil obtained from fresh leaf of Plectranthus aegyptiacus, and evaluated it for novelty-induced behavioural (NIB) and determine its mechanism(s) of action in mice. Methods: The oil was hydro-distillated, and analyzed using gas chromatography-mass spectrometry. The effects of the oil (50, 100 and 150 mg/kg; i.p., n=6) on novelty-induced behavioural was assessed using open field test and head dipping on hole board. Probable mechanism(s) were evaluated using antagonists: flumazenil, naloxone and cyproheptadine at 2 mg/kg each, atropine and yohimbine at 5 mg/kg and 1 mg/kg respectively. Key Findings: The LD50 values obtained were 2154 and 490 mg/kg for oral and intraperitoneal routes respectively. The oil (50, 100 and150 mg/kg) significantly (p<0.05, 0.01 and 0.01) inhibited all NIB and head dips. Flumazenil significantly (p<0.05) reversed the effect of the oil on NIB; atropine, naloxone and cyproheptadine significantly (p<0.01, 0.01 and 0.001) potentiated inhibitory effect on NIB respectively, while yohimbine showed no significantly effect. The analyzed oil showed 61 compounds, and the major compounds were carvacrol, germacrene-D, p-cymene and [1,1'-Bicyclopentyl]-2,2'-diol. Conclusions: The study concluded that the oil possessed central nervous system depressant activity, which could be mediated mainly through augmentation of GABAergic neurotransmission, while cholinergic-(muscarinic), adrenergic and serotonergic pathways may be involved.

Importance of Herba Passiflorae in Medicinal Applications: Review on Experimental and Clinical Pharmacology

The dried aerial parts of Passiflora incarnate L. plant are called Herba Passiflorae. This plant belongs to the Passifloraceae family. This review aims to focus on the importance of Herba Passiflorae in medicinal applications with special reference to its experimental and clinical pharmacology. Herba Passiflorae possesses flavonoids and alkaloids ingredients. The major constituents of Herba Passiflorae are flavonoids such as vicenin-2, orientin, isoorientin, vitexin, and isovitexin. Herba Passiflorae is applied for the cure of dysmenorrhoea, neuralgia, and nervous tachycardia. It is a slight sedative for nervous restlessness, insomnia, and anxiety. The fruit of Herba Passiflorae is used for jams, jellies, and desserts. The juice is a favorite flavoring in drinks. The pharmacology effect of Herba Passiflorae includes experimental and clinical pharmacology. Experimental pharmacology includes analgesic, antipyretic, anti-inflammatory, antimicrobial, cardiovascular, central nervous system depressant, and uterine stimulant effects. Clinical pharmacology includes anxiolytic, analgesic, and sedative effects, as well as its effect on nausea, menopause, dysmenorrhea, and diabetes. Herba Passiflorae stimulates uterine contractions, so it is used during pregnancy. The water extract of Herba Passiflorae is not genotoxic. The passion fruit is more appropriate for children's use due to the incorporation of Lactobacillus casei in passion fruit. The daily oral intake of passion fruit at public doses is non-toxic and safe. The daily dose in adults as a sedative is 0.5-2 g of aerial parts 3-4 times. In conclusion, Herba Passiflorae has analgesic, antipyretic, anti-inflammatory, antimicrobial, cardiovascular, central nervous system depressant, uterine stimulant, anxiolytic, analgesic, and sedative effects, as well as, its effect on nausea, menopause, dysmenorrhea, and diabetes.

Buprenorphine Prevalence in DUID Cases in Southwestern Virginia: Case Studies and Observations

Buprenorphine, a semisynthetic mixed agonist/antagonist opioid used primarily for the treatment of opioid use disorder, was reported in 194 driving under the influence of drugs (DUID) cases in Southwestern Virginia during the period from 2017 through 2019. Identifying and confirming buprenorphine in DUID cases is common in this region. Interpretation is complex due to the large range of concentrations of buprenorphine found in blood and frequent combinations with other therapeutic and abused drugs. Buprenorphine was identified by immunoassay and quantified by liquid chromatography–tandem mass spectrometry. A sensitive method was necessary as one-third of concentrations of buprenorphine and/or norbuprenorphine were &lt;1.0 µg/L. Concentrations of buprenorphine ranged from &lt;0.5 to 11 µg/L (mean 2.5 µg/L, median 1.8 µg/L) and concentrations of norbuprenorphine ranged from &lt;0.5 to &gt;20 µg/L (mean 3.3 µg/L, median 2.2 µg/L). Buprenorphine polysubstance use was common. Only 10% of the cases examined did not contain other drugs confirmed in routine DUID screening tests. The most common drug groups confirmed were benzodiazepines, amphetamines and cannabinoids. The DUID case histories presented represent examples of buprenorphine abuse, buprenorphine with no other drug groups, buprenorphine combined with other drug groups, cases consistent with impairment and cases with minimal impairment. Central nervous system depressant and narcotic analgesic symptoms were commonly observed; however, some cases contained stimulant symptoms. Buprenorphine-to-norbuprenorphine (B/NB) ratios had a mean and median ratio of 1.1 and 0.8, respectively. B/NB ratios &gt;3.0 were found in 4.7% of the cases. The finding of a higher B/NB ratio may indicate a more recent buprenorphine administration and a greater potential for impairment. No relationship between the concentration of buprenorphine and/or norbuprenorphine in blood and the performance on drug recognition expert evaluation or standardized field sobriety tests could be determined.