The 16+ Benefits Of Spilanthes, Spilanthol, And Alkylamides

The 16+ Benefits Of Spilanthes, Spilanthol, And Alkylamides 

 
spilanthes.jpg
 

Spilanthes is a genus of plants that have major potential as an aphrodisiac and anti-aging tool.

In this post, we will discuss spilanthes, the benefits of its bioactive components, and where to get it.

Contents:

  1. Basics Of Spilanthes
  2. Benefits Of Spilanthes
  3. My Experience With Spilanthes
  4. Where To Buy Spilanthes
  5. Caveats Of Spilanthes
  6. Mechanism Of Action

Basics Of Spilanthes

Plants belonging to genus Acmella are called Spilanthes and there are over 30 species with the most common species used in Africa and India. R

Traditionally, spilanthes has been used for treatment of toothache, stomatitis, throat complaints, malaria, soreness, dysentery, and gum care. R

The major bioactive compounds, spilanthol (affinin) and alkylamides are found in: R

  • Spilanthes species (other names: Acmella Oleracea, Paracress, Jambu, Tshishengelaphofu, Sichuan buttons)
  • Heliopsis longipes (other names: Chilcuague, Chilcuán, Chilmecatl, Aztec root, Golden root)

Other bioactive activities of Spilanthes are attributed to multiple bioactive compounds, N-isobutylamides, phenolic compounds, coumarins, and triterpenoids. R

 
 

Benefits Of Spilanthes

1. Combats Skin Aging

In Spilanthes acmella, spilanthol is responsible for anti-aging effects while trans-ferulic acid possess antioxidant activity. R

In combination with Gotu Kola (Centella asiatica) and Ginger (Zingiber officinale), Spilanthes has an anti-aging effect on the skin. R

More specifically in this combination, Gotu Kola stimulates the synthesis of type I collagen in fibroblasts and decrease the degradation of collagen, Spilanthes accelerates the collagen synthesis, while Ginger exerts potent inhibitory activity against fibroblast elastases. R

Spilanothol can penetrate the skin. R R

Spilanothol has anti-inflammatory effects on the skin (by suppressing COX-2) by reducing expression of inflammatory cytokines (such as IL-6, IL-8, MCP-1, ICAM-1) and increasing Heme Oxygenase (HO‑1). R

2. Has Antimicrobial Properties

Spilanthes has antibacterial effects agaisnt:

  • Bacillus cereus R
  • Bacillus subtilis R
  • Eikenella corrodens R
  • Enterococcus faecalis R
  • Escherichia coli R R
  • Lactobacillus paracasei R
  • Lactobacillus rhamnosus R
  • MRSA R
  • Pectobacterium carotovorum R
  • Ralstonia solanacearum R
  • Saccharomyces cerevisiae (brewer's yeast) R
  • Staphylococcus aureus R R
  • Staphylococcus epidermidis R R
  • Streptococcus mutans R
  • Streptococcus oralis R
  • Streptococcus pyogens R
  • Streptococcus sanguis R
  • Streptococcus sobrinos R
  • Pseudomonas aeruginosa R

Spilanthes can act as an antifungal against:

  • Aspergillus fumigatus R
  • Aspergillus niger R
  • Candida albicans R
  • Candida krusei R
  • Candida parapsilosis R
  • Fusarium oxysporum R
  • Penicillium spp R
  • Piriformospora indica R
  • Trichophyton mentagrophytes R

Spilanthes can act as an antiparasitic against:

  • Plasmodium berghei R
  • Plasmodium falciparum (and may help prevent malaria) R R
  • Trypanosoma brucei rhodesiense R 

Spilanthes is able to reduce HIV/AIDS replication. R

Spilanthes has insecticidal/pesticidal properties against:

  • Anopheles gambiae R
  • Anopheles stephensi (and may help prevent malaria) R R
  • Culex quinquefasciatus R
  • Diamondback Moth/Cabbage Moth (Plutella xylostella) R
  • Ticks, such as Rhipicephalus microplus (Australian cattle tick, southern cattle tick, Cuban tick, Madagascar blue tick, and Porto Rican Texas fever tick) and Dermacentor nitens (American Levi tick) R R R R R R
  • Tomato leafminer R

Spilanthes may be toxic to some shellfish:

  • Crustacea ie Shrimp R
  • Mollusks R

3. Increases Urine Output and Water Intake

 
 

Spilanthes can act on the kidneys as a diuretic and can increase urine/salt excretion (increases urine Na+, K+ and a reduces osmolarity). R R

Spilanthes may also help increase water intake. R

Spilanthol can also significantly increase salivary output - for example, saliva flow increased 440% over baseline with use of a flavored toothpick and 628% over baseline with similarly flavored toothpicks infused with spilanthol. R

4. Enhances Oral Health

Spilanthes has bioactivity on oral health. R

For example, spilanthes (as well as Black GarlicBlack Seed Oil ((Nigella Sativa), and Propolis) can protect the microbiome in the mouth from dysbiosis caused by bad bacteria and fungi. R 

Spilanthes can also be used to reduce oral candida (thrush). R

Spilanthes can also be used in films for reducing oral pain. R

5. Protects The Brain

Spilanthes is neuroprotective against pesticide-induced neuronal death (by stabilizing calcium induced excitotoxicity and improving dopamine release). R

Spilanthes can provide neuroprotection from oxidative stress by upregulating Sirtuin-1 (SIRT1) and Forkhead Box O3a (FOXO3A) as well as Superoxide Dismutase 2 (SOD2), Catalase, and B-Cell Lymphoma 2 (Bcl-2) proteins. R

N-Alkylamides (NAAs) from Spilanthes can cross the gut barrier and are easily absorbed into the brain through the blood-brain barrier once it reaches the blood. R R R

Spilanthes also contains beta-caryophyllene which has major neuroprotective properties by acting on the endocannabinoid system.- R

Spilanthol (from heliopsis) may produce a stimulating effect similar to caffeine. R

6. Combats Ulcers In The Gut

Spilanthes may help protect against alcohol-induced ulcers. R

For example, in animals spilanthes can accelerate healing of ulcers by increasing of cellular proliferation and gastric mucus content, but reducing oxidative stress and inflammation. R

Spilanthes in animal models is also very effective at combating ulcerative colitis. R

7. Fights Pain

Extracts of spilanthes and heliopsis have been to create powerful anesthetics for combating pain. R R R

Spilanthol can counteract pain by acting on opiodergic, serotoninergic, and GABAergic systems, as well as the NO/cGMP/K channel pathway and TRPV1/TRPA1 receptors. R R R

For example, heliopsis can produce intense numbness and a tingling sensation in the lips, tongue and mouth. R

Spilanthes can also produce this numbing/tingling effect. R

N‑Alkylamides can work on the endocannabinoid system, bind to CB1 receptors, inhibit Fatty Acid Amide Hydrolase (FAAH), and inhibit of anandamide cellular uptake. R

Some of spilanthes' pain reducing effects can be attributed to it's antihistamine effects as well. R

8. Quenches Inflammation

Spilanthol has major anti-inflammatory effects. R R

For example, spilanthes can inhibit macrophage activation from Lipopolysaccharide (LPS)-induced inflammatory responses - reduces inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), NF-kb, IL-1beta, IL-6, and TNF-alpha. R

9. Promotes A Healthy Vascular System

 
 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5297847/

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5297847/

 

Spilanthes (as well as Spilanthol from Heliopsis) protects the vascular system as it increases antioxidant levels in the heart and can act as a vasorelaxant (acts as a vasodilator via NO/cGMP, CO/cGMP, H2S/KATP, and PGI2/cAMP). R R

Spilanthes may also help prevent thrombosis. R

10. Improves Lung Function

Spilanthes can combat fungi that contribute to Tuberculosis (TB), coughs, and sore throats. R R

Spilanthes can also reduce inflammation in the lungs by suppressing COX-2 and ICAM-1 expression. R

Spilanthes can also boost the antioxidant levels in the lungs by activating NRF2. R

11. Has Antioxidant Properties

Bioactive compound in spilanthes (such as their flavonoids) are potent free radical scavengers. R R

By reducing oxidative stress, spilanthes may help protect against carcinogen-induced DNA damage. R

12. Improves Wound Healing

 
wound finger.jpg
 

Spilanthol and α-Humulene can increase levels of collagen deposition in wounds. R

Spilanthes also has anesthetic properties (time ~83.6 (±28.5) min) making it useful for skin wounds, pressure sore, and infected surgical wounds treatment. R

13. Enhances Libido And Sex Behavior

Spilanthens is a popular female aphrodisiac and can influence the estrous cycle without altering folliculogenesis and fertility. R

For example in female animal models, splianthes can increase the frequency of the Proestrous (P) and Estrous (E) phase, while reducing the metaestrous (M) and diestrous (D) phases. R

In male animal models, N-alkylamides acted similarly to Sildeafinil (Viagra). R

In this study, N-alkylamides increased mounting frequency, intromission frequency and ejaculation frequency, as well as sex hormones Follicule Stimulating Hormone (FSH), Luteinizing Hormone (LH) and Testosterone (T). R

In Brazil, spilanthes has been used traditionally to induce labor. R

14. Improves Metabolic Disease

Spilanthes may help with parasite-induced metabolic disease. R

For example, in animal models, spilanthes can restore abnormal lipid levels caused by Plasmodium berghei infection - reduced plasma level Total Cholesterol (TC), Triacylglycerol and Low Density Lipoprotein Cholesterol (LDL-C) and increased High Density Lipoprotein Cholesterol (HDL-C). R

15. Combats Diabetes

Spilanthes may be useful as an antidiabetic as it can protect against high blood sugar levels (hyperglycemia) by normalizing blood sugar. R

Spilathenes can normalize other markers of diabetes, such as MDA, AST, ALT, and creatinine levels, while increasing glutathione and TAOS. R

16. Fights Cancer

Spilanthes may have anti-cancer effects on:

  • Breast Cancer R
  • Cervical Cancer R
  • Colon Cancer R
  • Skin Cancer R

Spilanthes can also reduce DNA damage and mutations from the consumption of Polycyclic Aromatic Hydrocarbons (PAHs).

My Experience With Spilanthes

Currently experimenting with spilanthes and heliopsis...

Where To Buy Spilanthes

 
 

Spilanthes can be bought here.

Heliopsis can be bought here.

Dosage And Use:

Spilanthes may be effective to use sublingually. R

Synergies:

Caveats Of Spilanthes

Spilanthes has shown to be generally safe in animal models (doses of 2,000 mg/kg or 5,000 mg/kg did not induce mortality, thus, the LD50 of the aqueous extract of S. africana has been estimated higher than 5,000 mg/kg). R

Although, high doses of spilanthes (100 to 150 mg/kg in rodents) have shown to cause seizures. R 

Heliopsis has also shown to be generally safe in animal models although doses with 1000 mg/kg dose has shown to induce Polioencephalomalacia (PEM). R

Although, heliopsis may also cause damage to sperm. R

Mechanism Of Action

Simple:

  • Increases BCL-2 R
  • Increases Calpastatin R
  • Increases Catalase R
  • Increases CB1 R
  • Increases Collagen R
  • Increases DA R
  • Increases eNOS R
  • Increases FOXO3A R
  • Increases FSH R
  • Increases GABA R R R
  • Increases GCMP R
  • Increases GSH R
  • Increases HDL-C R R
  • Increases HO-1 R
  • Increases LH R
  • Increases Neutrophils % R
  • Increases NRF2 R
  • Increases PDE1 (possibly) R
  • Increases PGI2 R
  • Increases SIRT1 R
  • Increases SOD2 R
  • Increases T R
  • Increases TAOS R
  • Increases TC R
  • Increases Triglycerides R
  • Increases TRPA1 (possibly via downstream of trvp1) R
  • Increases TRPV1 R
  • Reduces ALT R
  • Reduces AST R
  • Reduces AQP2 R
  • Reduces Calcium R
  • Reduces Calpain R
  • Reduces CAMP R
  • Reduces Claudin-1 R
  • Reduces Creatinine R
  • Reduces COX-2 R R R
  • Reduces CYP1A11 R
  • Reduces CYP1A12 R
  • Reduces CYP1A14 R
  • Reduces Desmopressin R
  • Reduces FAAH R
  • Reduces ICAM-1 R
  • Reduces IL-1b R R R
  • Reduces IL-6 R R R
  • Reduces IL-8 R
  • Reduces iNOS R
  • Reduces JNK R
  • Reduces LDL-C R R
  • Reduces MAPK R
  • Reduces MCP-1 R R
  • Reduces MDA R
  • Reduces NF-kb R R R
  • Reduces Occludin R
  • Reduces PGE2 R
  • Reduces ROS R
  • Reduces TGF-B1 R
  • Reduces TNF-a R R R

Advanced:

  • Spilanthol has log P of 3.4, PSA of 29.1, a molecular weight of 221 g/mol, two atoms of hydrogen acceptors, and one hydrogen donor atom, making it easy to cross the skin barrier like a hapten. R
  • In skin, spilanthol may exert its anti‑inflammatory activity by suppressing the TNF‑α‑induced expression of ICAM‑1, COX‑2 and pro‑inflammatory mediators by enhancing that of HO‑1, and inhibiting the activation of the phosphorylated JNK signaling pathway. R
  • Spilanthes has significant reduction in the mutagenicity of premutagens requiring CYP-450 metabolisms (estrogenic ones as well). R
  • Spilanthol is able to strongly inhibit NKCC2 phosphorylation/activation in both resting and activating conditions in freshly isolated kidney slices...inhibits vasopressin-induced AQP2...significantly increased intracellular Ca2+ levels in renal cells with a mechanism that involves both Ca2+ influx at the plasma membrane and Ca2+ release from the ER...spilantol-induced cytosolic Ca2+ increase significantly reduces cAMP levels in renal cells. R
  • The vasorelaxant activity of Spilanthes acmella is exerted by endothelial cells producing partial synthesis of NO and PGI2. R