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Sweet Broomweed

Scientific Name(s): Scoparia dulcis L.
Common Name(s): Escobilla, Sweet broomweed, Typycha kuratu, Vassourinha

Clinical Overview

Use

Sweet broomweed has been investigated for its antimalarial, antiulcer, antipyretic, and aphrodisiac activity as well as for its cytotoxic activity against cancer cells.

Dosing

None suggested because of the lack of clinical data. S. dulcis is available commercially in combination with other herbs. It is available in tablet, capsule, and powder doseforms.

Contraindications

Contraindications have not been identified.

Pregnancy/Lactation

Avoid use because of the lack of clinical data regarding safety and efficacy in pregnancy and lactation.

Interactions

None well documented.

Adverse Reactions

The plant species is associated with sympathomimetic effects.

Toxicology

None reported.

Botany

S. dulcis is a perennial medicinal herb distributed throughout tropical and subtropical regions. The plant has serrated leaves, white flowers, and grows up to 0.7 m in height.1, 2, 3

History

Scoparia has been used as a remedy for treating diabetes mellitus in India and hypertension in Taiwan. Traditionally, the fresh or dried plant has been used as a remedy for treating stomach ailments, hypertension, diabetes, inflammation, bronchitis, hemorrhoids, and hepatosis, and as an analgesic and antipyretic agent.4, 5

A hot water infusion and/or decoction of the leaves or whole plant is used medicinally by indigenous tribes of Nicaragua to treat malaria, stomach disorders, menstrual disorders, insect bites, fevers, heart problems, liver disorders, and venereal disease. It has been used for blood cleansing, as an aid to child-birth, and as a general tonic.3

The herb is used in Brazilian folk medicine to treat bronchitis, gastric disorders, hemorrhoids, insect bites, and skin wounds. The herb is used in Asian medicine to treat hypertension.6

The ethnoveterinary use of the plant dates back to 1889 in Trinidad as a topical lotion to treat impetigenous and herpetic eruptions. Many of the indications for the plant's use parallel those practiced in veterinary folk medicine. Mucilage is released when the whole plant is soaked in water, thus helping to protect and regenerate normal cells; it may also act as an immunostimulator. The plant has been used to treat skin rashes in Martinique and Trinidad, for irritated skin in Brazil, and as a multi-ingredient preparation for treating burns in eastern Nicaragua. In Paraguay, the plant is used to kill lice and fleas, and used against vermin. The plant is also valued for its analgesic, anti-inflammatory, anticancer, and antiviral activity.2, 7

Chemistry

The scientific literature reveals numerous chemical studies on the herb; isolated chemical constituents include coumarins, phenols, saponins, tannins, amino acids, flavonoids, terpenoids, and catecholamines.4

High-performance liquid chromatographic analysis of an aqueous fraction of S. dulcis revealed the presence of noradrenaline and adrenaline, which have sympathomimetic effects.6

The herb's terpenoids are responsible for numerous medicinal effects. Scoparic acid A, scoparic acid B, scopadulcic acid A and B, scopadulciol, and scopadulin are all biologically active. These chemical compounds have various biological activities, including inhibition of the replication of herpes simplex virus, inhibition of proton pumps, potassium adenosine triphosphate (ATP)ase activator, and antitumor promoting activity. Additional identified terpenoids of broomweed include alpha-amyrin, betulinic acid, dulcioic acid, friedelin, glutinol, and ifflaionic acid.3, 5, 8, 9, 10, 11

The acetylated flavone glycosides from broomweed have nerve growth factor (NGF)-potentiating activity or neurotrophic activity that may be useful in treating neurological disorders. The flavone glycosides, including isovitexin, also inhibit β-glucuronidase.12, 13

The dried roots and aerial parts of S. dulcis contain economically important hydroxamic acids, which provide insect, fungal, and bacterial resistance.14

Uses and Pharmacology

A variety of applications have been suggested for S. dulcis extracts including antimalarial, antiulcer, antipyretic, and aphrodisiac activities, as well as cytotoxicity activity against cancer cells, and reviews of the topic have been published.2, 15

Analgesic and anti-inflammatory activity

Animal data

The diterpene scoparinol demonstrated significant analgesic (P < 0.001) and anti-inflammatory activity (P < 0.01) in animals.16

Pretreatment of ethanolic extracts of S. dulcis (0.5 g/kg) reduced acetic acid-induced writhing in mice 47%. The extract (0.5 and 1 g/kg) also inhibited paw edema in rats induced by carrageenan 46% and 58%, respectively, after 2 hours. The triterpene glutinol (30 mg/kg) reduced writhing in mice induced by acetic acid 40% and paw edema in rats induced by carrageenan 73%, indicating that the analgesic activity of S. dulcis is most likely related to the anti-inflammatory activity of glutinol.17

Clinical data

Research reveals no clinical data regarding the use of S. dulcis as an analgesic or anti-inflammatory agent.

Neurotrophic activity

In vitro data

The acetylated flavone glycosides from S. dulcis have NGF-potentiating activity, which may be useful in treating neurological disorders.

In control experiments, following incubation, the percentages of neurite-bearing cells in PC12D cells were 27% with 2 ng/mL NGF and 71% with 30 ng/mL NGF after 48 hours. After incubation with the glycosides from S. dulcis, neurite outgrowth in PC12D cells was increased by an additional 16% and 15%, respectively.12, 18

Antiviral activity

In vitro

The diterpenoid scopadulcic acid B inhibited viral replication of herpes simplex virus type 1 in a hamster test model. The mechanism of action is unknown but does not involve a direct virucidal effect or inhibition of virus attachment. Topical application or intraperitoneal injections at 100 and 200 mg/kg/day prolonged the development of herpetic lesions and survival time when treatment was initiated immediately after virus inoculation.19, 20

Antimalarial activity

In vitro

The diterpenoid scopadulcic acid A has activity against various Plasmodium falciparum isolates with an IC50 of 27 mcM against the D6 clone (African Sierra isolate) and an IC50 of 19 mcM against the W2 clone (Indochina isolate). The IC50 against the multidrug-resistant TM91C235 (Thailand) isolate was 23 mcM. For comparison, IC50 values for chloroquine were 9.3, 266, and 24 nM against D6, W2, and TM91C235. The IC50 values for mefloquine were 36, 4.8, and 59 nM against D6, W2, and TM91C235.5

GI activity

The mechanism of action of the diterpenoid scopadulcic acid B and its debenzoyl derivative, diacetyl scopadol (DAS) involves inhibition of K+-dependent dephosphorylation of proton pumping for gastric acid secretion.20

In vitro

Scopadulcic acid B and its debenzoyl derivative, DAS, dose-dependently and specifically inhibited the ATP hydrolysis by gastric H+K-ATPase (proton pump for gastric acid secretion) but not Na+K+-ATPase activity. With respect to activating the cation K+, scopadulcic acid B is considered a mixed inhibitor, while DAS is considered an uncompetitive inhibitor. This action differs from the irreversible inhibitor omeprazole. Detailed mechanisms and specific inhibition effects in the catalytic reaction of scopadulcic acid B and DAS are provided in the study.21, 22

Anticancer activity

In vitro and in vivo

Scopadulcic acid B inhibited the effects of the tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA). Scopadulcic acid B also inhibited TPA-enhanced phospholipid synthesis in cultured cells and inhibited the effect of TPA on skin tumor formation in mice initiated with 7,12-dimethylbenz[a]anthracene.23

Four new labdane-derived diterpenes, isolated from the aerial parts of S. dulcis, were cytotoxic against the following 6 human stomach cancer cell lines: SCL, SCL-6, SCL-37′6, SCL-9, Kato-3, and NUGC-4. Vinblastine sulfate and mitomycin C were used as positive controls.24

Scopadulcic acid C, another diterpene, enhanced the antitumor efficacy of acyclovir and ganciclovir in a HSV-TK gene therapy system. The synergistic activity was caused by the activation of viral thymidine kinase.25, 26

Diabetes

Animal data

Treatment with aqueous S. dulcis extracts and glibenclamide significantly improved specific insulin binding in streptozotocin-induced male Wistar rats. The number of insulin receptors and affinity binding (P < 0.001) was reduced to normal nondiabetic levels. Overall, the results suggest an increase in total endoplasmic reticulum (ER) membrane insulin binding sites with a concomitant increase in plasma insulin in rats treated with aqueous S. dulcis extract or glibenclamide. The mean specific binding of insulin to ER was lower in diabetic control rats (55 +/- 2.8%) than in aqueous S. dulcis–treated (70 +/- 3.5%) and glibenclamide-treated (65 +/- 3.3%) diabetic rats, resulting in a decrease in plasma insulin.27

An aqueous extract of S. dulcis plant was administered orally for 6 weeks to streptozotocin diabetic rats. The level of plasma insulin was decreased, and the levels of blood glucose and plasma glycoproteins were increased in diabetic control rats. The diabetic control rats also had a decrease in the level of sialic acid and elevated levels of hexose, hexosamine, and fucose in the liver and kidney. After oral administration of S. dulcis plant extracts, the controls had decreased levels of blood glucose and plasma glycoproteins. Plasma insulin and tissue sialic acid levels were increased, and hexose, hexosamine, and fucose tissue levels were near normal in controls.28

Similar animal experiments using aqueous S. dulcis extracts of 200 mg/kg/day resulted in antihyperglycemic effects, including increased hemoglobin levels, decreases in hemoglobin A 1c levels, increased sorbitol dehydrogenase, lipid peroxidation, and antioxidant activity in the liver of diabetic rats.29

Several animal studies documented the antioxidant activity of the plant, particularly against lipidperoxidation-induced membrane damage. A typical dosage regimen of an aqueous S. dulcis extract of 200 mg/kg/day resulted in an increase in the activities of pancreatic superoxide dismutase, catalase, glutathione peroxidase, and glutathione-S-transferase, and reduced glutathione.30, 31, 32

Clinical data

A small (n = 35) randomized crossover clinical trial with type 2 diabetic patients evaluated the effect of porridge made with S. dulcis leaf extract, and reported decreased fasting blood glucose and HbA1c at the 3 month evaluation point. No effect on cholesterol indices was found.33

Other uses

In an animal study, an aqueous fraction of S. dulcis revealed the presence of 2 catecholamines, noradrenaline and adrenaline, that may account for the hypertensive and inotropic effects after parenteral administration.6

A significant effect on onset and duration of sleep (P < 0.05) was caused by scoparinol on pentobarbital-induced sedation in animals. In another animal study, sleeping time induced by sodium pentobarbital 50 mg/kg was prolonged 2-fold in mice pretreated with 0.5 g/kg of an ethanolic extract of S. dulcis. Scoparinol has a diuretic action in animals as demonstrated by the measurement of urine volume after administration.16, 17

The flavone glycosides, including isovitexin, inhibit activity against β-glucuronidase.13, 34

Dosing

Clinical trials are lacking upon which to provide guidance. Commercially, S. dulcis is often sold in combination with other herbs. It is available in tablet, capsule, and powder doseforms.

Pregnancy / Lactation

Avoid use because of the lack of clinical data regarding safety and efficacy in pregnancy and lactation. An aqueous fraction of S. dulcis contained catecholamines, noradrenaline and adrenaline, that may account for the sympathomimetic effects of the plant.6

Interactions

Scopadulcic acid C, a diterpene from S. dulcis, enhanced the antitumor efficacy of acyclovir and ganciclovir in a HSV-TK gene therapy system. Patients diagnosed with cardiovascular disease should avoid use because the aqueous fraction of S. dulcis revealed the presence of 2 catecholamines that may account for its hypertensive and inotropic effects. Avoid use or monitor therapy if using proton pump inhibitors (omeprazole [Prilosec]) or antacids because of the potential drug-drug interaction if also consuming any of the commercially available products containing S. dulcis. Avoid use or monitor therapy if diagnosed with diabetes and/or using insulin products.6, 25, 26

Adverse Reactions

The plant species is associated with sympathomimetic effects.

Toxicology

None suggested because of the lack of clinical data.

References

1. Scoparia dulcis. USDA, NRCS. 2017. The PLANTS Database (http://plants.usda.gov, March 2017). National Plant Data Team, Greensboro, NC 27401-4901 USA. Accessed March 2017.
2. Pamunuwa G, Karunaratne DN, Waisundara VY. Antidiabetic Properties, Bioactive Constituents, and Other Therapeutic Effects of Scoparia dulcis. Evidence-based Complement Altern Med:eCAM. 2016;2016:8243215.27594892
3. Latha M, Pari L, Sitasawad S, Bhonde R. Insulin-secretagogue activity and cytoprotective role of the traditional antidiabetic plant Scoparia dulcis (Sweet Broomweed). Life Sci. 2004;75:2003-2014.
4. Ratnasooriya WD, Jayakody JR, Premakumara GA, Ediriweera ER. Antioxidant activity of water extract of Scoparia dulcis. Fitoterapia. 2005;76:220-222.15752634
5. Riel MA, Kyle DE, Milhous WK. Efficacy of scopadulcic acid A against Plasmodium falciparum in vitro. J Nat Prod. 2002;65:614-615.11975516
6. Freire SM, Torres LM, Souccar C, Lapa AJ. Sympathomimetic effects of Scoparia dulcis L. and catecholamines isolated from plant extracts. J Pharm Pharmacol. 1996;48:624-628.8832498
7. Lans C, Harper T, Georges K, Bridgewater E. Medicinal plants used for dogs in Trinidad and Tobago. Prev Vet Med. 2000;45:201-220.10821961
8. Mahato S, Das M, Sahu N. Triterpenoids of Scoparia dulcis. Phytochemistry. 1981;20:171-173.
9. Hayashi T, Gotoh K, Kasahara K. Production of scopadulciol by cultured tissues of Scoparia dulcis. Phytochemistry. 1996;41:193-196.
10. Hayashi T, Kasahara K, Sankawa U. Efficient production of biologically active diterpenoids by leaf organ culture of Scoparia dulcis. Phytochemistry. 1997;46:517-520.
11. Hayashi T, Asai T, Sankawa U. Mevalonate-independent biosynthesis of bicyclic and tetracyclic diterpenes of Scoparia dulcis L. Tetrahedron Lett. 1999;40:8239-8243.
12. Li Y, Chen X, Satake M, Oshima Y, Ohizumi Y. Acetylated flavonoid glycosides potentiating NGF action from Scoparia dulcis. J Nat Prod. 2004;67:725-727.
13. Kawasaki M, Hayashi T, Arisawa M, Morita N, Berganza L. 8-Hydroxytricetin 7-glucuronide, a beta-glucuronidase inhibitor from Scoparia dulcis. Phytochemistry. 1988;27:3709-3711.
14. Pratt K, Kumar P, Chilton WS. Cyclic hydroxamic acids in dicotyledonous plants. Biochem Syst Eco. 1995;23:781-785.
15. Hayashi T. Investigation on traditional medicines of Guarany Indio and studies on diterpenes from Scoparia dulcis. Yakugaku Zasshi. 2011;131(9):1259-1269.21881299
16. Ahmed M, Shikha HA, Sadhu SK, Rahman MT, Datta BK. Analgesic, diuretic, and anti-inflammatory principle from Scoparia dulcis. Pharmazie. 2001;56:657-660.11534346
17. Freire SM, Torres LM, Roque NF, Souccar C, Lapa AJ. Analgesic activity of a triterpene isolated from Scoparia dulcis L. (Vassourinha). Mem Inst Oswaldo Cruz. 1991;86 (suppl 2):149-151.1841990
18. Li Y, Ohizumi Y. Search for constituents with neurotrophic factor-potentiating activity from the medicinal plants of paraguay and Thailand. Yakugaku Zasshi. 2004;124:417-424.
19. Hayashi K, Niwayama S, Hayashi T, Nago R, Ochiai H, Morita N. In vitro and in vivo antiviral activity of scopadulcic acid B from Scoparia dulcis, Scrophulariaceae, against herpes simplex virus type 1. Antiviral Res. 1988;9:345-354.2852487
20. Hayashi T, Kawasaki M, Miwa Y, Taga T, Morita N. Antiviral agents of plant origin. III. Scopadulin, a novel tetracyclic diterpene from Scoparia dulcis L. Chem Pharm Bull (Tokyo). 1990;38:945-947.2379289
21. Asano S, Mizutani M, Hayashi T, Morita N, Takeguchi N. Reversible inhibitions of gastric H+,K(+)-ATPase by scopadulcic acid B and diacetyl scopadol. New biochemical tools of H+,K(+)-ATPase. J Biol Chem. 1990;265:22167-22173.2176205
22. Hayashi T, Asano S, Mizutani M, et al. Scopadulciol, an inhibitor of gastric H+, K(+)-ATPase from Scoparia dulcis, and its structure-activity relationships. J Nat Prod. 1991;54:802-809.1659612
23. Nishino H, Hayashi T, Arisawa M, Satomi Y, Iwashima A. Antitumor-promoting activity of scopadulcic acid B, isolated from the medicinal plant Scoparia dulcis L. Oncology. 1993;50:100-103.
24. Ahsan M, Islam SK, Gray AI, Stimson WH. Cytotoxic diterpenes from Scoparia dulcis. J Nat Prod. 2003;66:958-961.12880314
255. Nkembo KM, Lee JB, Hayashi T. Selective enhancement of scopadulcic acid B production in the cultured tissues of Scoparia dulcis by methyl jasmonate. Chem Pharm Bull (Tokyo). 2005;53:780-782.15997134
26. Nakagiri T, Lee J, Hayashi T. cDNA cloning, functional expression and characterization of ent-copalyl diphosphate synthase from Scoparia dulcis L. Plant Sci. 2005;169:760-767.
27. Pari L, Latha M, Rao CA. Effect of Scoparia dulcis extract on insulin receptors in streptozotocin induced diabetic rats: studies on insulin binding to erythrocytes. J Basic Clin Physiol Pharmacol. 2004;15:223-240.15803960
28. Latha M, Pari L. Effect of an aqueous extract of Scoparia dulcis on plasma and tissue glycoproteins in streptozotocin induced diabetic rats. Pharmazie. 2005;60:151-154.15739907
29. Latha M, Pari L. Effect of an aqueous extract of Scoparia dulcis on blood glucose, plasma insulin and some polyol pathway enzymes in experimental rat diabetes. Braz J Med Biol Res. 2004;37:577-586.15064821
30. Pari L, Latha M. Protective role of Scoparia dulcis plant extract on brain antioxidant status and lipidperoxidation in STZ diabetic male Wistar rats. BMC Complement Altern Med. 2004;4:16.
31. Pari L, Latha M. Antidiabetic effect of Scoparia dulcis: effect on lipid peroxidation in streptozotocin diabetes. Gen Physiol Biophys. 2005;24:13-26.15900084
32. Latha M, Pari L, Sitasawad S, Bhonde R. Scoparia dulcis, a traditional antidiabetic plant, protects against streptozotocin induced oxidative stress and apoptosis in vitro and in vivo. J Biochem Mol Toxicol. 2004;18:261-272.15549711
33. Senadheera SP, Ekanayake S, Wanigatunge C. Anti-hyperglycaemic effects of herbal porridge made of Scoparia dulcis leaf extract in diabetics - a randomized crossover clinical trial. BMC Complement Altern Med. 2015;15:410.26582144
34. Hayashi T, Kawasaki M, Okamura K, et al. Scoparic acid A, a beta-glucuronidase inhibitor from Scoparia dulcis. J Nat Prod. 1992;55:1748-1755.1294695

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