Mitchell777
Member
- Joined
- Oct 25, 2019
- Messages
- 41
After researching emodin, I have learnt that the oral bioavailability seems to be very low. This seems to be due to extensive metabolism into its glucuronide form.
The study below which I will quote, suggests using piperine alongside emodin as a method to increase bioavailability, due to piperines property of inhibiting glucuronidation.
Obviously, I am not entirely sure if inhibiting glucuronidation is a side effect free process long term of if piperine is considered beneficial and relatively safe, as the process of glucuronidation is there for a reason, and using piperine to inhibit it, for the benefit of increasing emodin absorption, may be outweighed by the consequence of inhibiting glucuronidation in the first place.
I just wondered if anyone could chime in and pit their thoughts across? I know piperine is used almost always alongside turmeric to again increase absorption by the same mechanism I assume.
www.ncbi.nlm.nih.gov
“In pharmacokinetic experiments, emodin was predominantly found in the liver and the brain after oral intake of P. cuspidatum (Lin et al., 2012). After intragastric administration at doses of 20 and 40 mg/kg, emodin rapidly underwent phase II metabolism to form its glucuronide, and the parent form of emodin was almost undetectable in vivo. Even when administered at higher dose (82.4 mg/kg), the in vivo emodin levels detected remained very low (Shia et al., 2010).”
“Moreover, Ma et al. was the first to demonstrate that 2,3,5,4'‐tetrahydroxystilbene‐2‐O‐β‐D‐glucoside (TSG) could inhibit the phase II metabolism of emodin in vivo through down‐regulation of the expression of UGT1A8 (Ma et al., 2013). A similar study showed that piperine significantly increased the Cmax and area under concentration‐time curve (AUC) of emodin and decreased the AUC and Cmax of emodin glucuronide.”
“Traditional oral administration would not be the best method of application of emodin because of poor intestinal absorption, fast elimination and low bioavailability in vivo. The pharmacokinetics of emodin could be improved by inhibiting its glucuronidation metabolism.”
@haidut
I wonder if you had any thoughts about emodin and its oral bioavailability when you formulated Lapodin? It would be interesting to know if you have specifically avoided piperine and also why and what your thoughts are regarding piperine as a compound in general, as it seems to be employed especially with turmeric.
Thank you!
The study below which I will quote, suggests using piperine alongside emodin as a method to increase bioavailability, due to piperines property of inhibiting glucuronidation.
Obviously, I am not entirely sure if inhibiting glucuronidation is a side effect free process long term of if piperine is considered beneficial and relatively safe, as the process of glucuronidation is there for a reason, and using piperine to inhibit it, for the benefit of increasing emodin absorption, may be outweighed by the consequence of inhibiting glucuronidation in the first place.
I just wondered if anyone could chime in and pit their thoughts across? I know piperine is used almost always alongside turmeric to again increase absorption by the same mechanism I assume.
Emodin: A Review of its Pharmacology, Toxicity and Pharmacokinetics
Emodin is a natural anthraquinone derivative that occurs in many widely used Chinese medicinal herbs, such as Rheum palmatum, Polygonum cuspidatum and Polygonum multiflorum. Emodin has been used as a traditional Chinese medicine for over 2000 years ...
www.ncbi.nlm.nih.gov
“In pharmacokinetic experiments, emodin was predominantly found in the liver and the brain after oral intake of P. cuspidatum (Lin et al., 2012). After intragastric administration at doses of 20 and 40 mg/kg, emodin rapidly underwent phase II metabolism to form its glucuronide, and the parent form of emodin was almost undetectable in vivo. Even when administered at higher dose (82.4 mg/kg), the in vivo emodin levels detected remained very low (Shia et al., 2010).”
“Moreover, Ma et al. was the first to demonstrate that 2,3,5,4'‐tetrahydroxystilbene‐2‐O‐β‐D‐glucoside (TSG) could inhibit the phase II metabolism of emodin in vivo through down‐regulation of the expression of UGT1A8 (Ma et al., 2013). A similar study showed that piperine significantly increased the Cmax and area under concentration‐time curve (AUC) of emodin and decreased the AUC and Cmax of emodin glucuronide.”
“Traditional oral administration would not be the best method of application of emodin because of poor intestinal absorption, fast elimination and low bioavailability in vivo. The pharmacokinetics of emodin could be improved by inhibiting its glucuronidation metabolism.”
@haidut
I wonder if you had any thoughts about emodin and its oral bioavailability when you formulated Lapodin? It would be interesting to know if you have specifically avoided piperine and also why and what your thoughts are regarding piperine as a compound in general, as it seems to be employed especially with turmeric.
Thank you!
