Identification of a Novel GABAA Receptor Channel Ligand Derived from Melissa officinalis and Lavandula angustifolia Essential Oils

Abstract

Aims: Melissa officinalis (Mo) and Lavandula angustifolia (La) essential oils and their major constituents ((E) -caryophyllene, caryophyllene oxide, geranyl acetate, linalool, nerol, Oct-1-en-3-ol, 3-Octanone, myrcene, allo-ocimene, p-cymene and α-terpineol) assessed by GC-MS) which are shared by these two essential oils were probed in an attempt to identify the GABA A R ligand(s). [810][811][812][813][814][815][816][817][818] 2014 811 IC 50 of 40 M. Concentrations (0.001 mg/ml) of whole (Mo) were shown to display modest beneficial effects upon neuronal viability while at a higher concentration (0.1 mg/ml) of (Mo) and (La) oils induced a neurotoxicity effect. Conclusion: These data provide the first evidence that allo-ocimene is an neuroactive GABA A R inhibitory component found in both (Mo) and (La), and represents a novel GABA A receptor channel chemotype derived from a natural product.

GABA‐modulating phytomedicines for anxiety: A systematic review of preclinical and clinical evidence

“…A neurotropic tissue study (Yoo et al, ) reported decreased GABA‐T levels in the dentate gyrus of C57BL/6 J mice, along with an increase in total GABA levels, following extract 50/200 mg/kg daily for 3 weeks. Finally, in radio‐ligand/electrophysiological studies using male Wistar rat cortical cultures in vitro, M. officinalis extract and selected constituents have shown trans‐ocimene inhibited [35S] (TBPS) binding (set radio ligand) at GABA‐A receptor level, in a dose‐dependent fashion (Mahita et al, ), building upon previous similar findings in preclinical investigations (Abuhamdah et al, ; Huang et al, ).…”

“…Awad et al (); Awad et al (); Abuhamdah et al (); Huang et al (); Mahita et al (); Raines et al (); Salah and Jager (); Yoo et al ()…”

A Comparative Study of Melissa officinalis Leaves and Stems Ethanolic Extracts in terms of Antioxidant, Cytotoxic, and Antiproliferative Potential

“…M. officinalis has an average height of 30–125 cm and displays ovate, dark-green leaves and white flowers which bloom in the summer [ 9 , 10 ]. M. officinalis has a large use in traditional medicine, food industry, and aromatherapy, due to its fresh smell and its medicinal properties including hypoglycemic, hepatoprotective, antimicrobial, antidepressant, hypnotic, and sedative [ 1 , 11 – 14 ]. In addition, there are studies that pointed out the cytotoxic effect of lemon balm extract on breast cancer [ 13 ] and colon carcinoma [ 15 ].…”

Correction: Wissam Zam et al. An Updated Review on The Properties of Melissa officinalis L.: Not Exclusively Anti-anxiety. Frontiers in Bioscience-Scholar. 2022; 14: 16

“…M. officinalis decoctions also showed hepatotoxicity activity with GI 50 greater than 400 µg/mL on fresh porcine liver cells, PLP2 [106]. M. officinalis volatile oil was non-toxic to HEp-2 cells, a human cervical carcinoma cell line at 100 µg/mL [46] but induced a neurotoxicity effect on mixed cortical cell cultures from 16-to 18-day-old rat embryos (Sprague-Dawley strain) at the same concentration via volt aggregated sodium channels [106].…”

“…M. officinalis decoctions and hot extract showed an antiproliferative effect on human tumor cell lines, with GI 50 ranging from 51 to 258 µg/mL for breast (MCF-7), non-small lung (NCI-H460), cervical (HeLa), and hepatocellular carcinoma (HepG2) [104] and at a concentration of 500-1000 µg/mL for human colon cancer cell lines DLD-1 HCT116, SW620, HT-29, and inhibited HT-29 cells [105]. M. officinalis decoctions also showed hepatotoxicity activity with GI 50 greater than 400 µg/mL on fresh porcine liver cells, PLP2 [106]. M. officinalis volatile oil was non-toxic to HEp-2 cells, a human cervical carcinoma cell line at 100 µg/mL [46] but induced a neurotoxicity effect on mixed cortical cell cultures from 16-to 18-day-old rat embryos (Sprague-Dawley strain) at the same concentration via volt aggregated sodium channels [106].…”