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Adverse Effects and Intoxication with Essential Oils
Published in K. Hüsnü Can Başer, Gerhard Buchbauer, Handbook of Essential Oils, 2020
In several studies, application of bergamot oil directly to the skin was shown to have a concentration-dependent phototoxic effect after exposure to UV light, presumably due to bergapten and also bergamottin (Kaddu et al., 2001; Kejlova et al., 2007). Cutaneous lesions developed gradually within 48–72 h when aromatherapy with bergamot oil was applied 2–3 days prior to ultraviolet (UV) exposure (Kaddu et al., 2001). Thus, for applications on areas of skin exposed to sunshine, excluding bath preparations, soaps, and other products which are washed off the skin, bergamot oil should not be used such that the level in the consumer products exceeds 0.4% (International Fragrance Association, IFRA). Cases have become much more rare since the introduction of psoralen-free bergamot oil.
Mammalian CYP2D Members A Comparison of Structure, Function, and Regulation
Published in Shufeng Zhou, Cytochrome P450 2D6, 2018
Grapefruit juice significantly increases the plasma concentrations of drugs that are substrates for CYP3A4 such as felodipine, triazolam, midazolam, diazepam, terfenadine, cyclosporine, and nifedipine (Bailey and Dresser 2004; Bailey et al. 2000, 2003). The principal components of grapefruit juice have been identified as the furanocoumarin bergamottin and its metabolite 6′,7′-dihydroxybergamottin, as well as the flavonoids naringenin, naringin, quercetin, and kaempferol. Bergamottin is a potent inhibitor of human CYP3A4. In humans, grapefruit juice exposure decreases concentrations of intestinal CYP3A4 but does not affect CYP3A5, 1A1, 2D6 protein, or 3A4 mRNA (Lown et al. 1997). In contrast to the results described above, long-term grapefruit juice treatment in rats has been shown to increase nifedipine clearance (Mohri et al. 2000). In mice, a single dose of grapefruit juice inhibits hepatic oxidative enzyme activity, whereas multiple dosing increases activity (Dakovic-Svajcer et al. 1999). The results of these rodent studies imply that grapefruit juice is both an inhibitor and an inducer. However, this compound is both an inhibitor and an inducer of P450 enzymes in dogs. Bergamottin predosing increases the plasma levels of diazepam in beagle dogs (Sahi et al. 2002). In dog hepatic microsomes, bergamottin treatment for 10 days reduces the activity of CYP3A12 by 50% and 1A1/2 by 75%. Tolbutamide hydrox-ylase activity does not change, and CYP2B11 activity is moderately induced. In jejunal microsomes, CYP3A12 activity doubles with bergamottin treatment. CYP2B11 and 1A1/2 activity and tolbutamide hydroxylation are not detected.
Pharmacokinetics and pharmacodynamic interaction of bergamottin with atorvastatin in rats
Published in Xenobiotica, 2022
Xinjuan Zhang, Jinyao Guo, Jin Li, Chen Chen, Guijun Su
Herbals or phytomedicines derived from plants have become increasingly complementary and alternative medicine in recent times. In many cases, isolated natural bioactive compounds outperform synthesised drugs (Cheuka et al. 2016). As a result, the number of herb–drug interactions rises, potentially resulting in negative clinical outcomes. It highlighted the importance of potential interaction risk when herbal medicines or herbal active ingredients were used in combination with other drugs (Parvez and Rishi 2019). Therefore, basic research related to herb–drug interactions will provide scientific evidence for the efficacy and safety of herbal products. The inhibition of drug-metabolizing enzymes (such as cytochrome P450) is usually responsible for toxicological effects of drugs or herbs. The inhibitory effects of bergamottin on both CYP3A and CYP1A1/2 have been reported in human and monkey hepatocytes (Wen et al. 2002). And bergamottin is abundant in the diet and herbs are consumed frequently, such as bergamot and grapefruit (Le Goff-Klein et al. 2004; Akiyoshi et al. 2022). Given the fact that atorvastatin is metabolised by CYP3A, the present study explored the effect of bergamottin on pharmacokinetic profiles and antihyperlipidemic properties of atorvastatin in hyperlipidaemia rats.
Bergamot oil as an integral component of nanostructured lipid carriers and a photosensitizer for photodynamic treatment of vitiligo: Characterization and clinical experimentation
Published in Expert Opinion on Drug Delivery, 2021
Mai Shaaban, Maha Nasr, Abeer A. Tawfik, Maha Fadel, Omaima Sammour
The use of plants rich in psoralens (natural photosensitizers) was employed many centuries ago in ancient India and Egypt for the treatment of leukoderma and vitiligo [23]. One of the most important plant products that have been frequently used is bergamot oil (BO), which is the oil of citrus bergamia belonging to family Rutaceae [24], and is mainly composed of volatile ingredients as limonene, linalool, linalyl acetate, and nonvolatile compounds as bergamottin, bergapten, and citropten. BO was reported to induce phototoxic reactions with persistent pigmentation following application to the skin, and subsequent irradiation using ultraviolet light either UVA or UVB light [25–27]. This can be particularly advantageous for the treatment of dermatological diseases such as vitiligo, which is an acquired idiopathic skin pigmentation disease resulting from the loss of melanocytes from the basal layer of the epidermis [28]. Among the phototherapy protocols used for the management of vitiligo is the narrowband ultraviolet B (NB-UVB) light (with a peak at 311 nm) [29]. However, the NB-UVB light was reported to be more effective when combined with psoralens (P-NBUVB) owing to the direct melanin-inducing effect of 311 nm radiation, in addition to the psoralen-induced photochemical effects [29–31].
Patent landscape of novel technologies for combating category-A Arenavirus infections
Published in Expert Opinion on Therapeutic Patents, 2020
Harshal Sudhakar, Jignesh Bhate, Asish Kumar Patra
Bergamottin is naturally occurring furanocoumarin, found in grapefruit and pomelo. It is known as an antioxidant in Chinese medicine. CN109864988A [21] describes the use of Bergamottin as an antiviral inhibitor, with an IC50 of 3.3 µM, inhibiting Junin virus in-vitro. Bergamottin acts by interfering with the entry of viral particles by binding to the glycoprotein on the viral surface. 9879003 USDB2 [22] discloses compounds that exert therapeutic action by covalently modifying cysteine residues of the host target proteins, particularly cysteine residues at the active site of enzyme molecules. The advantage of this approach is that such compounds have broad spectrum antiviral activity. QL-XII-47 a tricyclic quinoline derivative compound, was tested against Junin virus for antiviral activity, and was seen to inhibit the cytopathic effects during infection. 20150297677 USDA1 [23] discloses antibodies against human T-cell Immunoglobulin and Mucin(TIM)-domain containing proteins including its four subtypes for inhibiting virus entry into the host cell. The antibodies bind to TIM preventing interaction of host cells with the virus envelope. Mouse monoclonal antibody against TIM1 inhibited Junin virus entry into Huh7 cells by 70% at a concentration of 50 nM.