Boerhaavia diffusa extract exhibits anti-estrogenic effect

What is Boerhaavia diffusa?

Boerhaavia diffusa is a plant of tropical region used in Ayurvedic as well as some other traditional herbal medicines taken for pain relief, anti-inflammation, and treating indigestion. It is also used for its anti-diabetic and diuretic properties. However, animal studies are promising there were no human studies conducted using Boerhaavia diffusa.

Boerhaavia diffusa Anti-diabetic Activity Properties

Daily oral administration of aqueous solution with 200mg/kg of the leaf Boerhaavia diffusa extract was able to significantly reduce blood glucose (50.5%) and significant increase in plasma insulin levels (52.6%) in alloxan-induced diabetic rats [1].

Another study came to comparable anti-diabetic effect using same dose [2]. Orally administered Boerhaavia at a dose of 500mg/kg body weight for a period of 30 days to alloxan-induced diabetic rats exhibited normalized blood glucose and serum insulin levels with a similar potency as a standard hypoglycaemic drug Metformin [3]. There was no effect in non-diabetic rats [3]. Observed anti-diabetic effect is believed to be mediated by increased release of insulin from the existing beta cells of pancreas [2,7] or through extra pancreatic action [7].

Interaction with Liver Enzymes

200 mg/kg of Boerhaavia diffusa leaf extract somewhat improved activities of the hepatic enzymes in experimentally induced diabetic rats (increased hexokinase, decreased glucose-6-phosphatase [G6P], fructose-1,6-bisphosphatase [F1,6P]) [1]. Effect was comparable to 600 microg/kg Glibenclamide [1].

Boerhaavia Diffusa Extract and Anti-Estrogenic Effect

One in vitro study demonstrated potent anti-estrogenic properties of methanol extract of Boerhaavia diffusa in MCF-7 breast cancer cell lines [4]. At 100mcg/mL, Boerhaavia methanolic extract exhibited similarly effectiveness as ICI 182-780 (strong estrogen receptor antagonist) on the expression of a selected estrogen responsive gene pS2, however estrogen receptor binding with IC₅₀ at 320+/-25ug/mL is fairly weak [4].

Diuretic Action

Boerhaavia diffusa appears to posses diuretic effect [5] as it was able to further increase diuresis (urination) associated with kidney stone formation in a dose-dependent manner [8]. Leaves and roots seem to have diuretic effect with minimal effects noted when using stem [6].

Other Possible Benefits of Boerhaavia Diffusa Root

One in vitro study showed that Boerhaavia posseses the ability to reduce kidney stones formation (anti-urolithiasis) and may even reduce the stone size [9]. This was confirmed in animal study in ethylene glycol-induced hyperoxaluric rats [8]. Boerhaavia diffusa (at the dose of 100 and 200 mg/kg body weight orally for 28 days) not only ameliorated hyperoxaluric oxidative stress and renal cell injury in urolithiasis but also prevented kidney stone formation in a dose-dependent manner [8].

One study even reported cortisol lowering activities in male mice [10]. Aqueous extract of B. diffusa roots also exhibits significant free radicals scavenging activity [8]. In alloxan-induced diabetic, 200 mg/kg of B. diffusa leaf extract was able to significantly increase reduced glutathione, superoxide dismutase, catalase, glutathione peroxidase and glutathione S-transferases (GSTs) in liver and kidneys [2]. In thioacetamide intoxicated rats, Boerhaavia (2 ml/kg root) exhibited hepatoprotective activity as visible by protection of a majority of serum parameters, i.e. GOT, GPT, ACP and ALP, but not GLDH and bilirubin [11].

Side Effects and Toxicity

The extract does not show any signs of toxicity up to an oral dose of 2 g/kg in mice [9].

(Other common names: Punarnava, Nyctinaceae, BME, BDE, BLEt, Boerhaavia diffusa Linn., Nyctaginaceae, B. diffusa)

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References

1. Pari, L., and M. Amarnath Satheesh. “Antidiabetic activity of Boerhaavia diffusa L.: effect on hepatic key enzymes in experimental diabetes.” Journal of ethnopharmacology 91.1 (2004): 109-113.
2. Satheesh, M. Amarnath, and L. Pari. “Antioxidant effect of Boerhavia diffusa L. in tissues of alloxan induced diabetic rats.” Indian J Exp Biol 42.10 (2004): 989-92.
3. Singh, Prem Kumar, Darshee Baxi, and Ankita Doshi. “Antihyperglycaemic And Renoprotective Effect of Boerhaavia diffusa L. in Experimental Diabetic Rats.” Journal of Complementary and Integrative Medicine 8.1 (2011).
4.  Sreeja, Sreekumar, and Sreeharshan Sreeja. “An in vitro study on antiproliferative and antiestrogenic effects of Boerhaavia diffusa L. extracts.” Journal of ethnopharmacology 126.2 (2009): 221-225.
5. Singh, S. K. P., B. L. Pandey, and R. G. Singh. “Recent approach in clinical and experimental evaluation of diuretic action of Punarnava.” (1992).
6. Mudgal V. “Studies on medicinal properties of Convolvulus pluricaulis and Boerhaavia diffusa.” Planta Med. (1975)
7. Nalamolu, Rao K., Krishna M. Boini, and Srinivas Nammi. “Effect of chronic administration of Boerhaavia diffusa Linn. leaf extract on experimental diabetes in rats.” Tropical Journal of Pharmaceutical Research 3.1 (2007): 305-309.
8. Pareta, Surendra K., et al. “Aqueous extract of Boerhaavia diffusa root ameliorates ethylene glycol-induced hyperoxaluric oxidative stress and renal injury in rat kidney.” Pharmaceutical biology 49.12 (2011): 1224-1233.
9. Yasir, Fauzia, and Muhammad A. Waqar. “Effect of indigenous plant extracts on calcium oxalate crystallization having a role in urolithiasis.” Urological research 39.5 (2011): 345-350.
10. Gholap, S., and A. Kar. “Hypoglycaemic effects of some plant extracts are possibly mediated through inhibition in corticosteroid concentration.” Die Pharmazie-An International Journal of Pharmaceutical Sciences 59.11 (2004): 876-878.
11. Rawat, A. K. S., et al. “Hepatoprotective activity of Boerhaavia diffusa L. roots—a popular Indian ethnomedicine.” Journal of ethnopharmacology 56.1 (1997): 61-66.