Gen info
- Spilanthes acmella belongs to the family Asteraceae, a genus of about 60 species that are widely distributed in tropical and subtropical regions viz., Africa, America, Asia.
- The plant has been reported as a highly endangered species (Sharma & Shazad 2013). Conventional propagation methods are not enough for mass propagation. The major constraint for large multiplication are its poor vegetative propagation and low rate of seed germination (Rios-Chavez et al. 2003).
(44)
Botany
Biri is an erect, branched, annual herb which reaches a height of 15 to 60 centimeters. Leaves are opposite, smooth or nearly so, ovate or ovate-lanceolate, and 1.5 to 3 centimeters long, with pointed tip and wedge-shaped base, and with toothed or wavy margins. Conical heads occur singly at the ends of long stalks, and are about 1 centimeter in length. Flowers are yellow. Achenes are flattened, oblong, dark-brown and enclosed separately in scales.
 Distribution
- In open waste places, old clearings, etc., at low and medium altitudes.
- In Benguet Subprovince, Cagayan, Nueva Viscaya, Rizal, and Laguna Provinces in Luzon, and in Mindoro and Balabac.
- Pantropic in distribution.
- In Brazil, cultivated year-round as an ornamental and medicinal plant.
Constituents
- Study has isolated an active principle, spilanthol (C14H25NO), an isobutylamide, a known insecticidal.
- Leaves yield alkaloids, carotenoids, essential oils, sesquiterpenes, amino acids.
- Phytochemical analysis of leaves yielded alkamides (spilanthol), isobutylamide derivatives, a- and ß-amyrin esters, stigmasterol, triterpenoidal saponins, amino acids, and alkaloids.
- Study isolated bioactive compounds: phenolics (vanillic acid, trans-ferulic acid, and trans-isoferulic acid), coumarin (scopoletin), and triterpenoids like 3-acetylaleuritolic acid (1), β-sitostenone (3), stigmasterol and stigmasteryl-3-O-β-D-glucopyranosides. (17)
- Studies on secondary metabolites yielded spilanthol, undeca-2E,7Z,9E-trienoic acid isobutylamide, undeca-2E-en-8,10-diyonic acid isobutylamide, 2E-N-(2-Methylbutyl)-2-undecene-8,10-diynamide, 2E,7Z-N-Isobutyl-2,7-tridecadiene-10,12-diynamide, 7Z-N-Isobutyl-7-tridecene-10,12-diynamide, ß-sitosterol, stigmasterol, α-amyrin, ß-amyrin, limonene, ß-caryophyllene, (Z)-ß-ocimene, germacrene-D, myrecene,
3-acetylaleuritolic acid, vanillic acid, ß-sitosterone, scopoletin, trans-ferulic acid, trans-isoferulic acid. (32)
- Bioassay-guided isolation yielded bioactive compounds such as phenolics (vanillic acid, trans-ferulic acid, and trans-isoferulic acid), coumarin (scopoletin), and triterpenoids ( 3-acetylaleuritolic acid, β-sitostenone, stigmasterol and stigmasteryl-3-O-β-D-glucopyranosides), in addition to a mixture of stigmasteryl- and ß-sitosteryl-3-O-ß-D-glucopyranosides. (see study below) (33)
Properties
- Adaptogenic, antibacterial, anti-inflammatory, anti-scorbutic, digestive, diuretic, immunomodulatory, insecticidal,larvicidal, lithotriptic, sialogenic, tonic.
- Saliva-inducing and trigeminal effects attributed to spilanthol.
- Studies have shown anti-inflammatory, analgesic, diuretic, antioxidant, antibacterial, antihypertensive, antimalarial, immunomodulatory, vasorelaxant, mosquitocidal, larvicidal, insecticidal, anti-tumor, hepatoprotective properties.
Parts used
Roots, leaves, leaf juice.
Uses
Edibility / Culinary
- In some Asian countries, used as spice.
- Flower heads used by Japanese as spice for appetizers.
Folkloric
- Root decoction used as purgative - 4 to 8 grams to a cup of water.
- Infusion used for itches and psoriasis.
- Decoction of plant used as diuretic and as solvent for vesical calculi.
- Leaf juice and bruised leaves applied to wounds and atonic ulcers.
- Whole plant used in treatment of dysentery and rheumatism.
- Leaves, mixed with Blumea balsamifera and Tamarindus indica, used to prepare aromatic baths for convalescents, rheumatics and pregnant women.
- Tops and decoction of roots used as vulnerary.
- Decoction of roots used as purgative.
- Flower heads, the most pungent of parts, chewed by Hindus to relieve toothache, as it produces numbness, redness of the gums and salivation.
- Flower heads used as hemostatic and analgesic.
- Tincture of flower heads used for toothache in lieu of tincture of pyrethrum.
- Used for inflammation of the periosteum of the jaws.
- In Old Calabar, used for toothaches.
- In South Africa, powdered leaf placed in carious tooth; rubbed on lips and gums for sore mouth in children.
- In Sri Lanka, flowers used for its diuretic activity.
- In the Cameroons, flowering heads are rubbed on the forehead for headaches. Also, combined with other plants, chewed and swallowed for snake bites and as local treatment for wounds.
- In Assam, used after childbirth.
- In Ayurvedic medicine, flower heads and roots are used in the treatment of scabies, psoriasis, scurvy, toothache, gum and throat infections; also used for stammering in children.
Others
• Fish Poison: Among the Mundas of Chota Nagpur, crushed plants used a fish poison.
• Flavoring: Extract of flowers used as flavoring material for dentrifices and gum.
Studies
• Anti-Inflammatory / Analgesic: Study of aqueous extract of S. acmella in experimental animal models showed dose-dependent inhibition of paw edema and increased pain threshold indicating significant anti inflammatory and analgesic properties. (2)
• Diuretic: Study of cold-water extract showed a marked increase in urine output, marked increase in urinary Na and K levels and reduction of urine osmolarity suggesting loop diuretic activity. It may also inhibit ADH release and/or action. (3)
• Anti-Inflammatory / Spilanthol: Study has isolated spilanthol which has shown to have significant anti-inflammatory activity on lipopolysaccharide-activated murine macrophage model, partly from inactivation of NF-kappaB which negatively regulates production of proinflammatory mediators.
• Vasorelaxant / Antioxidant: Study showed SA extract exerts maximal vasorelaxation in a dose-dependent manner, although less than acetylcholine-induced NO vasorelaxation. Chloroform extract showed the highest vasorelaxation and antioxidant activity. (9)
• Immunomodulatory / Antioxidant: Total ethanolic extract of leaves showed significant activation of macrophages and enhanced their function as compared to control, suggesting the herb as a potential natural drug for immunostimulant effect. (4)
• Bioactive Compounds / Spilanthol: Study analyzing the active chemical compounds of S. acmella revealed the naturally occurring insecticide, spilanthol, in the mother plant, flower heads and in vitro plantlets. Antioxidants, butylated hydroxytoluene (BHT) and fatty acids (n-Hexadecanoic acid and tetradecanoic acid) were obtained from all the sample extracts. (8)
• Spilanthol / Larvicidal: Study showed spilanthol to be a major constituent of ethanolic extract of flower heads, with potent ovicidal, larvicidal and pupicidal activity. It exhibited 100% mortality of eggs, larvae, and pupae of Anopheles culex and Aedes mosquito. (10)
• Antioxidant: Study showed the methanolic extract of stem of SA to have the highest superoxide radical scavenging activity while leaves showed maximum DPPH scavenging activity.
• Bioactive Compounds / Spilanthol / Insecticidal: Study detected the naturally occurring insecticide, spilanthol, in the mother plant, flower heads, and in vitro plantlets. N-isobutyl-2E, 4Z, 8Z, 10E- dodecatetraenamide was also detected in in vitro plantlets of S. acmella. It is a potent mosquito larvicide with 100% mortality against third instar larvae of A. aegypti.
• Antimicrobial: Study of various extracts of leaves of Spilanthes acmella showed the ethyl acetate and methanol extracts with activity against bacterial strains of Klebsiella pneumoniae and the water and EAE with good activity against fungal strains of Rhizopus stolonifer and R. arrhigus. (11)
• Diuretic / Antihypertensive: Leaf extracts were evaluated for diuretic activity in animals. The alcohol extract showed significant and marked increase in urine output, with a pattern of diuresis similar to that induced by furosemide. Results suggest a potential traditional use of the plant as diuretic in the treatment of hypertension. (13)
• Analgesic / Fresh Flowers: Study evaluated the analgesic potential of fresh flowers as used by Sri Lankan traditional practitioners to treat toothache. Results showed a dose-dependent analgesic activity. The analgesic was rapid and of short duration, not blocked by naloxone. The activity was presumed mediated supra-spinally accompanied by sedation. (12)
• Local Anesthetic / Antipyretic: Study evaluated an aqueous extract for local anesthetic activity by intracutaneous wheal in guinea pigs and plexus anesthesia in frogs, with xylocaine as standard drug in both models. Antipyretic activity was tested using yeast-induced pyrexia in rats, with aspirin as standard drug. Results showed significant anesthetic and antipyretic activities. (14) Study evaluated the local anesthetic action of ethanol extract of S. acmella in guinea pigs and frogs' sciatic nerves. Results showed S. acmella possessed local anesthetic activity. (30)
• Bioactive Metabolites / Alkamides: Major isolates are lipophilic alkylamides or alkamides bearing different number of unsaturated hydrocarbons, such as spilanthol or affinin ((2E,6Z,8E)-N-isobutyl-2,6,8- decatrienamide) and amide derivatives. Alkamides are structurally related to animal endocannabinoids, highly active in the CNS. Anandamide (N-arachidonoyl-ethanolamine) is an endogenous cannabinoid cerebral neurotransmitter. (15)
• Insecticidal Toxicity / Spilanthol / Plutella xylostella: Study showed the potential of S. acmella seed extract for insecticidal toxicity for the management of P. xylostella and other insects of agricultural importance. (16)
• Antioxidant / Roots: Study of root extracts of Spilanthes acmella in in vitro DPPH assay showed radical scavenging activity with an IC50 of 16.3 µg/ml. (18)
• Sexual Stimulant / N-Alkylamide / Flowers: Study evaluated ethanolic extracts of flowers and its effect on general mating patter, penile erection and serum hormone levels of normal male Wistar albino rats, compared with sildenafil citrate. The orally administered extract had a dose-dependent effect on mounting frequency, intromission frequency and ejaculation frequency, with a dose-dependent effect on FSH, LH, and serum testosterone levels. The effect might be attributable to N-alkylamide. Study lends support to the traditional use of S. acmella as a sexual stimulating agent. (19)
• Modulation of Genotoxic Damage Induced by Cyproterone Acetate: Study showed an extract of S. acmella modulated the genotoxic damage induced by cyproterone acetate in cultured human peripheral blood lymphocytes. (20)
• Phytopesticidal / Leaves: Study evaluated the antifeedant and larvicidal activities of various extracts of S. acmella leaves against Earias vitella, Helicoverpa armigera and Spodoptera litura. The leaves extract exhibited larvicidal activity, with maximum mortality in the dichloromethane extract. Results suggest a potential for the development of an eco-friendly pest control agent. (21)
• Antibacterial / bla Genes: An alcoholic extract of plant and its callus showed good antibacterial activity against gram positive and gram negative bacterial and also effectively controlled the growth of most resistant bacteria harboring bla genes. (23)
• Laxative / bla Genes: Study evaluated a methanolic extract of Spilanthes acmella for its laxative effect in animal models. Crude extract showed laxative properties, increasing the total number of feces. (24)
• Insecticidal / Anti-Cockroach: Study evaluated the potential insecticidal activity of Spilanthes acmella. Extracts were shown to be toxic against American cockroach, Periplaneta americana. The active component isolated was identified as N-isobutyl-2,6,8-decatrienamide (spilanthol). Spilanthol was more toxic than carbaryl, bioresmethrin, and lindane. Electrophysiological studies showed immediate hyperexcitation followed by complete inhibition of cockroach cercal nerve activity. (25)
• Anti-Tumor / Cytotoxicity: Study evaluated the cytotoxicity of a hydroalcoholic extract of inflorescence of S. acmella and its effects on the cytoskeleton of tumour cells. Results showed high cytotoxicity—the actin cytoskeleton arrangement of HEp2 cells showed depolymerization of the filaments, causing loss of morphology and compromised cell adhesion. (26)
• Larvicidal and Pupicidal: Study evaluated the effect of two plant extracts (Spilanthes acmella and Andrographis paniculata) on different larval instar and pupae of mosquito vector Aedes aegypti. S. acmella flower extract showed more effect than A. paniculata. Results suggest plants as alternative insecticidal to synthetic pesticides for vector control. (27)
• Hepatoprotective / CCl4-Induced Liver Toxicity: Study evaluated various extracts of S. acmella for hepatoprotective activity in CCl4-induced liver toxicity in rats. Results showed concentration dependent protection in the reduction of enzymes. The methanol extract showed the best activity. (28)
• Bioactive N-isobutylamides / Flower Buds / Mosquitocidal and Larvicidal: A hexane extract of dried flower buds yielded three N-isobutyl amides: spilanthol, undeca-2E,7Z,9E- trienoic acid isobutylamide and undeca-2E-en-8,10-diynoic acid isobutylamide. All were active against Aedes aegypti and Helicoverpa zea. (29)
• Anti-Malarial / Alkylamides: Alkylamides, spilanthol and undeca-2E-ene-8,10-diynoic acid isobutylamide,
isolated from S. acmella showed IC50s of 16.5 µg/mL and 41.4 µg/mL on Plasmodium falciparum strain PFB and IC50 of 5.8 µg/mL and 16/3 µg/mL for chloroquine resistant P. falciparum K1 strain, respectively. Lower concentrations of spilanthol and water extract reduced parasitemia by 59% and 53% in mice infected with P. yoelii. Results provide evidence of active constituents and antimalarial activity. (31)
• Bioactive Metabolites / Antibacterial / Antioxidant: Study isolated bioactive metabolites from S. acmella. Results showed fractions from the chloroform and methanol extracts inhibited the growth of many test organisms, e.g., Corynebacterium diphtheriae NCTC 10356 with MIC of 64-256 µg/mL and Bacillus subtilis ATCC 6633 with MIC of 128-256 µg/mL. All tested fractions exhibited antioxidant properties in both DPPH and SOD assays. Potent radical scavenging activity was observed in the DPPH assay. (33)
• Antifungal / Flower Head: Study evaluated Spilanthes acmella flower head extract for antifungal activity. Study showed the flower head possesses remarkable fungi toxic activity against many human and agricultural pathogens. Among fungal species, high inhibition zones were observed in Fusarium oxysporim (2.3 cm) and Fusarium moniliformis (2.1 cm) followed by Aspergillus niger and Aspergillus parasiticus. (34)
• Antimicrobial / Topical Antifungal: Study evaluated the potential of novel vesicular carrier, ethosomes, containing the methanolic extract of S. acmella, for anti-inflammatory action via transdermal route and the potential of the extract as antimicrobial in oral mucoadhesive gel formulation. Results validated the use of Akkalkara in traditional medicine as local anti-inflammatory and antimicrobial and confirmed the suitability of the ethosomes for transdermal delivery of herbal constituents. (35)
• Anthelmintic / Antioxidant / Cell Cultures: Study verified the potential of Spilanthes as a reservoir of bioactive agents and substantiated the value of callus cultures as a new source of anthelmintic and antioxidant compounds. (36)
• Increased Testosterone Level and Osteoblast Cells: Study evaluated the effect of S. acmella and physical exercise in increasing testosterone and osteoblast cells of femoral's trabecular glucocorticoid-induced osteoporosis in male mice. Results showed a 70% ethanol extract of S. acmella has an additive effect to weight-bearing exercise in glucocorticoid-induced osteoporosis in male mice. (37)
• Antibacterial / Antifeedant / Leaves: Study evaluated the antibacterial and antifeedant activities of various extracts o Spilanthes acmella against selected bacterial strains and larvae of Leucinodes orbonalis Guen. A dichlormethane extract of leaves showed broad spectrum antibacterial activity against all tested bacteria with maximum inhibition against E. coli. Phytochemical screening of leaves yielded the presence of alkaloids, terpenoids, phytosterols, saponins, steroid, tannins and phenolic compounds. (38)
• Antimicrobial /
Leaves and Flowers: Study evaluated the antimicrobial activity and chemical composition of crude extracts of flowers and leaves of S. acmella. All crude extracts of leaves were more effective than flowers against fungal strains of Aspergillus niger. All extracts showed maximum inhibition against E. coli and B. subtilis. (39)
• Neuroprotective on Pesticide-Induced Neuronal Cells Death: Study evaluated the protective effects of S. acmella extracts against pestidcie-induced neuronal cells death and underlying mechanisms in dopaminergic (SH-SY5Y) cell lines. Pretreatment of SH-SY5Y cells with S. acmella extract significantly increased the dopaminergic neurons in pirimicarb-induced neurotoxicity. Pretreatment led to decreased calpain but increased calpastatin protein levels. The extract exerted a neuroprotective effect via an alteration of calcium homeostasis, against pirimicarb induced neurotoxicity. (40)
• Herb-Drug Interactions: (1) Cytochrome P4502E1 (CYP2E1) substrates: Spilathol significantly inhibits CYP2E1 and may increase adverse effects of substrate drugs, including those used in anesthesia such as isoflurane and sevoflurane. (2) Antiandrogen Drugs (bicalutamide, flutamide, abiraterone): S. acmella may increase testosterone levels and counter the effects of these drugs. (3) Diuretics: S. acmella has loop diuretic activity and may have additive effects with other diuretic drugs. (41)
• Anti-Inflammatory: Study evaluated the anti-inflammatory properties of methanol extracts of S. acmella (MSA) in murine macrophages. The MSA at ≤300 µg/ml inhibited NO production in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages through transcriptional inhibition of inducible NO synthase expression in a dose-dependent manner. The MSA inhibited excessive inflammatory responses in LPS-stimulated murine macrophages by inhibition of phosphorylation of MAPKs and NF-kB, suggesting potential for use in treatment of severe inflammatory states. (42)
• Zinc Nanoparticles / Leaves: Study reports on the green, ecofriendly, cost-effective biological synthesis of zinc nanowires using Spilanthes acmella leaves extracts as reducing agent. (43)
• Hepatocurative / Paracetamol Induced Toxicity / Gel: Study evaluated the hepatocurative effect of S. acmella extract based gel in paracetamol intoxicated rabbits. Treatment caused a significant reduction in elevated serum markers (SGOT, SGPT, ALP). (45)
Availability
- Wild-crafted.
- Supplements in the cybermarket.
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