The 28+ Benefits Of Embelin And Its Natural Sources

Embelin: Embelia Ribes And Other Natural Sources

 
 https://www.ncbi.nlm.nih.gov/pubmed/28289385

https://www.ncbi.nlm.nih.gov/pubmed/28289385

 

Embelin suppresses cancer, combats inflammation, ameliorates autoimmunity, and destroys many infectious agents.

It also has anti-diabetic, anti-obesity, neuroprotective, and cardioprotective effects.

In this post, we will discuss the MANY benefits of embelin, its natural sources, and some synergies of embelin.

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Basics Of Embelin

Embelin (also known as embelic acid or emberine) is the major active constituent of the fruits from Embelia ribes (embelin makes the fruit bright orange). R

Other names for Embelia ribes: R R

  • Baibidanga
  • False black pepper
  • Vidanga
  • Vaividang
  • Vai Vidang
  • Vavding
  • White-flowered Embelia

It is used in Indian, Folk, Homeopathy, Tibetian, Unani, and Siddha traditional medicinal systems for treating various ailments like chronic inflammatory disorders, heart and urinary conditions, snake and insect bites, and tumors. R

 
 

Benefits Of Embelin

1. Combats Cancer

 
 http://www.mdpi.com/1420-3049/23/3/621

http://www.mdpi.com/1420-3049/23/3/621

 

X-linked Inhibitor of Apoptosis (XIAP) is a viable molecular target for anticancer drugs that can overcome apoptosis-resistance of malignant cells. R

XIAP is an inhibitor of cell death and Embelin can inhibit XIAP's activity, thus promoting cell death (great for resistant cancer). R R

Embelin can induce apoptosis through the upregulation of Peroxisome Proliferator-Activated Receptor-gamma (PPARγ) transcription and suppressing Akt/mTOR (more in MOA section). R R

Embelin has activity on these cancers:

  • Adenocarcinoma R
  • Bile Duct R
  • Bladder R
  • Breast R R R
  • Colon R
  • Fibrosarcoma R
  • Gastric R
  • Glioma R R
  • Head and Neck Squamous Carcinoma R
  • Leukemia R R R R
  • Liver R
  • Lung R
  • Melanoma R
  • Multiple Myeloma R
  • Ovarian R
  • Pancreas R R R
  • Prostate R R
  • Sarcoma R 
  • Thyroid R R

Embelin may also help overcome radiation therapy resistant cancer and other selective resistances (see study -> R). R

2. Inhibits Inflammatory Response And Has Antioxidant Effects

Embelin is powerful at inhibiting the inflammatory response by its ability to inhibit Nuclear Factor Kappa Beta (NF-kb) and Signal Transducer and Activator of Transcription 3 (STAT3).R

For example, Embelin can protect against Lipopolysaccharide (LPS)-induced immune activation and neuroinflammation. R R

It can also suppress systemic inflammation in models of Sepsis. R

Embelin's free radical scavenging activity has been found to be better than that of Vitamin E (alpha-tocopherols). R

Technical - it can scavenge free radicals and has an antioxidant effect (it inhibits pro-inflammatory cytokines like NF-κB and p53, by modulating sodium channel, chloride conductance, and GABAA receptor, by inhibits STAT3 and XIAP pathways). R

3. Fights Alzheimer's Disease And Improves Cognition

Embelin has neuroprotective effects. R

In animal models, Streptozotocin (STZ) can be used to replicated symptoms of Alzheimer's Disease (AD) - such as increased ROS, decreased GSH, neurotransmitter alterations of AChE, DA, NA, 5-HT, GABA, and Glutamate, and elevation in neuroinflammatory cytokine (IL-1 β, IL-6, and TNF-α) levels. R

Embelin can improve the memory deficits caused by STZ and can also protect against/reverse other STZ-induced behavioral, biochemical, and neurochemical abnormalities (increases NE, DA, and 5-HT in hippocampus) in animal models. R

Familial Encephalopathy with Neuroserpin Inclusion Bodies (FENIB) is a disorder that causes progressive dysfunction of the brain which causes loss of intellectual functioning (dementia-like symptoms) and seizures. R

Embelin may help reduce the burden of Neuroserpins in FENIB by inhibiting neuroserpin polymerization. R

4. May Act As A Sunscreen Alternative

Embelin may be useful as a Sunscreen Alternative. R

For example, pre-treatment with embelin could protect against 30min of Ultraviolet B (UVB) radiation-induced oxidative damage and DNA damage. R

This may be because embelin is structurally similar to natural Coenzyme Q10 (CoQ10). R

    5. Relieves TBI, Hypoxia, And Stroke

    Embelin may protect against damage from a Traumatic Brain Injury (TBI). R

    For example, embelin can protect against delayed neuronal death after brain trauma (via inhibition of NFkB, p53 and XIAP). R

    Embelin protects against neuronal cells from Hypoxia-induced death. R

    Embelin may be beneficial for Stroke (both ischemic and Hemorrhagic). R R R

    For example, in mice given ischemia/reperfusion-induced brain injury, embelin could improve locomotor skills, reduce brain lipid oxidation, and improve brain antioxidant levels (GSH and thiol levels). R

    This beneficial effect in stroke may only be sex-specific - embelin administration made male mice better, but female mice worse. R

    Embelin can cross the Blood Brain Barrier (BBB). R 

    6. Improves Epilepsy And Seizures

    Embelin has Anticonvulsant promoting activities. R

    For example, in animal models, embelin administration showed a significant inhibition of the Seizures induced by electroshock and pentylenetetrazole in a dose dependent manner and the activity was comparable to Phenytoin and DiazepamR

    In the same model, at doses of 2.5, 5, and 10 mg/kg, it can protect (100%) against Electroconvulsive Death (possibly via GABA). R

    7. Relieves Depression

    In animal models, embelin shows significant Anti-Depressant effects (in Tail suspension test and Forced swimming test). R 

    This improvement may be mediated by embelin inhibiting Noradrenaline (NA) and Serotonin (5-HT) reuptake into neurons. R

    8. Improves Anxiety

    In animal models, embelin has significant anxiolytic effects in dose-dependent manner (improvements in elevated plus maze, light and dark model, and open field test). R

    This improvement may be mediated by embelin increasing GABA levels. R

    9. Fights Sickness Behavior

    Embelin has a protective effect against LPS-induced Sickness Behavior in mice. R

    In animal models, embelin can prevent Anhedonia and Anorexia, while improving social behavior. R

    In this model, embelin showed to ameliorate brain oxidative stress markers (such as IL-1β, IL-6 and TNF-α). R

    10. Combats Huntington's Disease

    In models of Huntington's Disease (HD), embelin can prevent loss of body weight. R

    It also decreases the oxidative stress and neurotoxicity of 3-NP (used to induce HD in animal models). R

    Embelin can also reverse memory loss and decreased locomotor counts induced by 3-NP. R

    Overall, it has shown to decrease of 69–76% brain lesions by 3-NP. R

    11. Improves Rheumatoid Arthritis

    Embelin may be beneficial for ArthritisR

    For example, embelin has shown to reduce inflammation and bone erosion in a mouse models of inflammatory arthritis (possibly through the induction of apoptosis and suppression of osteoclastogenesis). R R

    Shatpuspadya Churna (an Ayurvedic formula containing Vidanga, Misreya, Marica, and Sindhav) is commonly used for rheumatism and indigestion. R

    12. Fights Fevers

    Embelin may help reduce Fevers produced from Endotoxemia. R

    13. Improves Pain

    Embelin may help reduce Pain possibly by binding to mu- and kappa-Opioid receptors in the brain. R R R

    Its pain-reducing properties has been reported to be even stronger than the narcotic Pentazocine. R

    Its analgesic effects can be used when taken topically, orally, or injected. R

    14. Ameliorates Autoimmunity

    Embelin may be protective during autoimmune responses as it can reduce inflammatory TH1 and TH17 cytokines. R

    15. Improves Multiple Sclerosis

    Embelin may be  beneficial in Multiple Sclerosis (MS). R

    For example, it has shown to induce TGF-beta (a large body of evidence has show TGF-b may be protective against MS). R

    Embelin can also reduce CD14+ monocyte-derived dendritic cell differentiation and reduce Demyelination R

    16. Improves Diabetes

    Embelin may be helpful for Diabetes and Insulin ResistanceR R R

    Embelin improves insulin sensitivity without increasing weight gain, enhances glycemic control, protects pancreatic β-cells from damage. R R

    For example, in Type 2 Diabetic (T2D) rats, embelin reduced body weight gain, blood glucose and plasma insulin levels. R

    It also significantly increases PPARγ expression, inhibits adipogenic activity, and activates GLUT4 (via PI3K/p-Akt). R

    17. Has Antimicrobial Properties

    Embelin can help with Antibiotic ResistanceR

    New Delhi metallo-β-lactamase-1 (NDM-1) inactivates nearly every class of β-Lactam Antibiotics (carbapenems) making gram-negative bacteria resistant to antibiotics. R

    Embelin can inactivate NDM-1 and may be useful for fighting gram-negative bacteria. R

    Embelin has antibacterial effects against:

    • Acinetobacter baumannii R
    • Bacillus cereus (ATCC 10876) R
    • Bacillus Polymyxa R
    • Bacillus subtilis (ATCC 11774) R
    • Enterobacter aerogenesMay help with UTIs R
    • Enterococcus faecalis (ATCC 29212) R
    • Escherichia coli (incl ATCC 4157) R R
    • Micrococcus luteus (ATCC 4698) R
    • MRSA R
    • MSSA R
    • Klebsiella pneumoniae (incl ATCC 4352) R R
    • Proteus mirabilis (ATCC 7002) R
    • Proteus vulgaris R
    • Pseudomonas aeruginosa (incl ATCC 9027) R R
    • Salmonella typhi R
    • Shigella boydii R
    • Shigella flexneri (ATCC 9199) R
    • Shigella sonnei R
    • Staphylococcus aureus (incl ATCC 6538) R R R
    • Streptococcus mutans R
    • Streptococcus pyogenes R
    • TRSA R

    Embelin also has Biofilm Inhibiting properties against Streptococcus mutans. R

    Embelin has anti-fungal effects against:

    • Aspergillus flavus (871) R
    • Aspergillus fumigates (2550) R
    • Candida albican R
    • Candida albidus R
    • Candida parapsilosis (MTCC 1744) R
    • Candida laurintis (MTCC 2898) R
    • Candida parapsilosis R
    • Candida tropicalis R
    • Epidermophyton floccosum R
    • Microsporum canis R
    • Microsporum gypseum R
    • Trichophyton mentagrophytes R
    • Trichophyton rubrum R

    Embelin may also help with Chloroquine Resistance, which is a common problem with antimalarial drugs. R 

    Embelin has anti-parasitic effects against:

    • Cestodes (Hymenolepis diminuta and Hymenolepis microstoma) R
    • Haemonchus contortus R
    • Hymenolepis diminut R
    • Nematode (Heligmosomoides polygyrus) R
    • Hookwork (N. americanus) R
    • Leishmania amazonensis R
    • Leishmania braziliensis R
    • Phamphistomum cervi R
    • Plasmodium falciparum - helps with Malaria R
    • Pheretima posthuma R
    • Root-Knot Nematode (Meloidogyne incognitaR
    • Roundworm (Rhabditis pseudoelongata and Caenorhabditis elegans) R R
    • Tapeworms (H. nana when embelin is combined with castor oil and milk) R
    • Taenia canina R
    • Trematode (Echinostoma caproniR
    • Trypanosoma cruzi trypomastigotes R

    Embelin has antiviral activity against:

    • Hepatitis C virus R

    18. May Be Used As An Oral Contraceptive

    Embelin can act as a potent Oral Contraceptive (may be a caveat so see below for effects on hormones) for women and men. R

    Females (reversible, has ~85.7% efficacy in rodents): R

    • Embelin interferes with reproductive functions in female rats by suppressing ovarian production of sex steroid hormones. R
    • In rats, post-coitus, embelin taken orally can terminate pregnancy (ranging from doses of 10 to 120 mg/kg). R R
    • In rabbits, embelin has shown to have anti-ovulatory effects. R

    Males (reversible): 

    • In male rats, embelin can reduce sperm count and testes weight after 15 days of use. R
    • After 45 days of use it may have anti-androgenic activity. R

    19. Improves Psoriasis

    Topical application of embelin has anti-inflammatory activities in acute and chronic models of Psoriasis. R

    It does this by reducing proinflammatory cytokines (TNF-a, IL-1b) in keratinocytes. R

    20. Enhances Wound Healing

    Embelin can significantly accelerate the process of Wound HealingR

    When used topically, Embelin induces fast epithelialisation of incisions, wound contraction, increases tensile strength of the incision wounds, weight of granulation tissue, collagenation, more fibroblasts, blood vessels and an absence of monocytes. R

    When used orally, Embelin has shown to improve wound healing in cutaneous wounds in STZ-induced diabetic rats. R

    21. Relieves Inflammatory Bowel Disease

    Vidanga (commonly used in the drug Gasex) can be used as remedy for diarrhea, dysentery, abdominal pain, constipation, colic and flatulence. R

    Embelin taken orally can reduce symptoms of Inflammatory Bowel Disease (IBD) and may have a protective effect from Ulcerative Colitis (UC). R R

    Embelin-loaded enteric-coated have colon ulcer protective effect in rats. R

    Embelin may also help improve absorption of amino acids in diet. R

    22. Protects The Liver

    Embelin has liver-protective effects and has been compared to Milk Thistle (silymarin) in its hepato-protective effects. R

    Several Ayurvedic formulations containing Vidanga are available on the market for liver disorder treatments (e.g. Livomyn, Sanjivani vati, Kumariasava, Liv-52 and Livosin). R

    In animal models, Embelin can protect against liver toxicity from Tetrachloride (CCl4). R 

    It can also help with regeneration of liver cells and antioxidant production. R

    23. Improves The Vascular System

    Embelin can protect against high Cholesterol (hypercholesterolaemia) and high Triglyceride (hypertriglyceridaemia) levels. R

    In combination with Curcumin, embelin can reduce Low-Density Lipoproteins (LDL), Free Fatty Acids (FFA) and Very-Low-Density Lipoproteins (vLDL) levels. R

    Embelin may also help reduce high Blood Pressure. R

    By activating Endothelial Nitric Oxide Synthase (eNOS), embelin can increase vascular Nitric Oxide (NO) levels. R R

    Aqueous extract of Embelin Ribes can ameliorate Heart Injury by enhancing the antioxidant defense in animal models. R R R

    For example, in rats with heart attacks, embelin significantly decreased serum levels of cardiac enzymes (CK-MB, LDH, and AST). R

    Embelin also improves mitochondrial function of the heart. R

    24. Fights Obesity

    Embelin has a protective effect on Obesity and helps with Weight LossR R

    For example, in animal models of diet-induced obesity, oral embelin treatment reduces the gain in Body Weight, Blood Pressure, visceral fat pad weight, serum lipid levels, coronary artery risk and atherogenic indices, serum glucose (24.77%), Insulin (35.03%) and Leptin (43.39%) levels. R

    In addition, it significantly decreases the hepatic Thiobarbituric Acid-Reactive Substance (TBARS) levels, while increasing Superoxide Dismutase (SOD), Catalase (CAT) and Glutathione (GSH) levels in obese rats. R

    25. Improves Respiratory Disorders

    Embelin may be beneficial in treating Adult Respiratory Distress Syndrome (ARDS) and Chronic Obstructive Pulmonary Disease (COPD) as it may reduce LPS-induced airway inflammation. R

    Embelia ribes has Anti-Histamine effects and may be beneficial for Asthma. R R

    26. May Help Antipsychotic Treatment

    Embelin may be useful as an antipsychotic. R

    For example, embelin pre-treatment significantly inhibits apomorphine-induced climbing and psychotic behaviors in animals. R

    It also reverses elevated levels of Dopamine, Noradrenaline and Serotonin neurotransmitters in the brain of psychotic animals. R

    27. Protects The Kidneys

    E.ribes significantly and dose dependently protects against cisplatin-induced Nephrotoxicity by maintaining antioxidant levels and reducing serum Urea, Creatinine and Blood Urea Nitrogen (BUN) levels. R

    28. May Help As A Toothpaste Alternative

    E. ribes (in combination with Ajamoda satva, Vaikranta bhasma, Azadirachta indicaZanthoxylum alatum, Punica granatum, Acacia arabica, Vitex negundo, and Triphala) in a cream has been shown to be safe way to remove Dental Plaque. R 

    This combination may be a safer alternative and have similar antibacterial effects as Fluoride-based toothpastes. R 

    My Experience With Embelin

    In terms of neuroinflammation, embelin is comparable to nicotine (reducing LPS-anhedonia), but without the stimulatory effects. 

    I felt no change in libido, despite its probable effects on hormones.

    Natural Sources Of Embelin

     
     

    You can buy/find Embelin from a few sources:

    • Aegiceras Corniculatum R
    • Embelia Ribes (Myrsinaceae) - found in its fruits, pericarp, root bark, stem bark, seeds, and leaves (1.01-4.31% of weight) R R
    • Embelia Schimperi (Myrsinaceae) R
    • Embelia Tsjeriam-Cottam R
    • Erythrorhiza (Oxalidaceae) R
    • Lysimachia Punctata (Primulaceae) R

    If you do not get good effects from embelin, try taking it with fat, as embelin has poor water solubility (the designer versions have better water solubility), although this allows it to more easily pass the Blood-Brain Barrier (↑cell-membrane permeability). R R R

    Other Forms Of Embelin

    Designer Versions Of Embelin: R

    • PEG5K-embelin
    • PEG 3500-Embelin
    • CBDIV17+Embelin

    Embelin May Go Well With These:

    Polyherbal Vidanga Formulations In Market And Its Uses R

    Abhyarista

    • Ingredients - Harad, draksha, vidanga, maduka bhasma, guda, gokshurtrivrta, dhaniya, dhatki, indravaruni, chavya, danti, madhurika, shunthi, mocarasa, water
    • Use - Piles, urine retention and dyspepsia

    Eladi grita

    • Ingredients - Ela, ajmoda, harad, baheda, amla, saurastri, shunthi, kalimirch, pippali, arishtak, khadir, sala-sara, bijakasara, bhallataka-suddha, vidanga, ghrta, tavaksiri, sita, madhu, dalchini, ela, chitrak, tejpatra, water
    • Use - Tuberculosis, anal fistula, dyspepsia and eye diseases

    Krmimudgar rasa

    • Ingredients - Rasa-suddha, gandhaka-suddha, ajmoda, vidanga, visamustika-suddha, palaash
    • Use - Worm infestations and dyspepsia

    Kuberakshadi yoga

    • Ingredients - Putikaranja, vidanga, ajwain, jatiphala, lavangaha, jeeraka
    • Use - Antihelminthic

    Kumariasava

    • Ingredients - Kumari rasa, guda, makshika, parva loha, shunthi, kalimirch, paippali, laung, dalchini, ela, tejpatra, nagkeshar, chitrak, pippalamool, vidanga, chavya, gajpippali, hapusha, dhaniya, poog, katuka, mustak, harad, baheda, amla, rasna, devdaru, haldi, daruharidra, moorva, madhurasa, danti, dhatki, pushkarmool, bala, atibala, kapikachu, gokshur, shatpushpa, hingpatri, akaarkrabh, utingana, svetapunarnava, punarnava, lodhra, dhatumakshika
    • Use - Dyspepsia, duodenal ulcer, regurgitation, dysuria, stones, epistaxis, seminal disorders, dementia, debility, emaciation, weakness, anorexia and liver disorders

    Madhukasava

    • Ingredients - Madhuka, vidanga, chitrak, bhallatak, manjishtha, madhu, ela, mrnala, agaru, chandan, water
    • Use - Bile disorders, leprosy, leucoderma, blood disorders, dyspepsia and emaciation

    Madhusnuhi rasayana

    • Ingredients - Shunthi, kalimirch, pippali, harad, baheda, amla, dalchini, ela, tejpatra, jatiphal, agni, laung, dhaniya, saariva, krsna jirak, vidanga, chavya, kusth, trivtita, pippali, ashwagandha, bhangri, tejovati-bija, kesara, suddha gandha, mahisaksa guggul, ghrita, sita, madhu
    • Use - Diabetic carbuncle, tumour, goitre, anal fissure, gout, leprosy, piles and itching

    Pippalyadi yoga

    • Ingredients - Vidanga, pippali, borax
    • Use - Contraceptive

    Sunder vati

    • Ingredients - Vidanga, kutaj, amla, shunti
    • Use - Skin diseases

    Vidangadi lauh

    • Ingredients - Vidanga, clove, borax, jatiphala, lavangaka, shunthi, salt, nutmeg, long pepper, black pepper, lauha bhasma
    • Use - Vermifuge, dyspepsia, anorexia, piles, anaemia, swelling, fever, asthma and cough

    Vidangadi churna

    • Ingredients - Vidanga, yastimadhu, trikatu, dantamoola, trivrit, chitraka
    • Use - Antihelminthic, purgative, alternative, flatulence, dyspepsia and tapeworms

    Vidangadi yoga

    • Ingredients - Vidanga, japapushpa, hingu
    • Use - Anti-fertility

    Vidangarishta

    • Ingredients - Vidanga, pippali, rasna, kutaj, dalchini, kutaj phala, patha, elavalukamka, amla, ksadura, dhatki, dalchini, ela, tejpatra, priyangu, kanchnaar, lodhra, shunthi, kalimirch, pippali, water
    • Use - Goitre, anal fissure and cystitis

    Vidangasava

    • Ingredients - Vidanga, pippalimula, rasna, kutaja, indrayava, paripatha, amalaki, shunthi, pippali, tamalpatra, bruhatela, tvak taila
    • Use - Round worms, thread worms and hook worms

    Vidangsaravaleha

    • Ingredients - Vidanga, pippali, triphala
    • Use - Antihelminthic, fistula, sinus, urinary diseases, ulcers, leprosy and skin diseases

    More formulations (see table): 

     
     http://ijpsr.com/bft-article/importance-of-embelia-ribes-an-update/

    http://ijpsr.com/bft-article/importance-of-embelia-ribes-an-update/

     

    Caveats And Safety

    It is reported that embelin is safe up to 3 g/kg orally when tested in rodents after acute exposure. R

    Another report on subacute toxicity after repeated administration of embelin at 10 mg/kg dose found to be safe in rats. R

    In chronic toxicity study, the administration of embelin to Wistar rats at a dose of 50 mg/kg/day for 14 weeks did not cause any extreme drop in the blood counts but showed toxic effects on the hematopoietic cells. R

    The recommended doses in official Ayurvedic Pharmacopoeia and Indian Herbal Pharmacopoeia are 5 - 10 g of fruit powder which are considered practically safe without side effects. R R

    Embelin may lower Testosterone and Luteinising Hormone (LH) levels (in animals), but can increase Progesterone. R

    As an oral contraceptive, embelin has anti-fertility properties: R

    • Powdered berries of E. ribes (100 mg/day) orally administered to male bonnet monkeys for 3 months adversely affected the quantity and quality of semen, and testosterone levels were reduced. R
    • Ayurvedic formulations containing E. ribes, such as ROC-101 and Garbhanivarana aushadam were reported to impair the fertility of female mice and rats, inducing sterility in male mice. R
    • Pippalyadi yoga, AC-4 and Maswin tablets have been used in women for their contraceptive activities without side effects. R

    Mechanism Of Action

     
     https://www.ncbi.nlm.nih.gov/pubmed/24397264

    https://www.ncbi.nlm.nih.gov/pubmed/24397264

     

    Simple:

    • Increases Bax (in mitochondria) R
    • Increases β-catenin (reduces in cancer) R R R
    • Increases Caspase-3 R
    • Increases Caspase-8 R
    • Increases Caspase-9 (strong) R
    • Increases CAT R R R R
    • Increases DR4 R
    • Increases DR5 R
    • Increases E-cadherin R
    • Increases eNOS R
    • Increases ERK 1/2 R
    • Increases GABA R
    • Increases GLUT4 R
    • Increases GPR84 R
    • Increases GPx R
    • Increases GSH R R R R R
    • Increases GSK-3beta R
    • Increases GST R
    • Increases HDL R
    • Increases IL-4 (reduces it in lungs) R R
    • Increases NO R
    • Increases NRF2 R
    • Increases PARP R
    • Increases PI3K R
    • Increases Progesterone R
    • Increases PTEN R
    • Increases p38 R
    • Increases p53 R R R
    • Increases SOD R R R
    • Increases TCF-4 R
    • Increases TGF-β R
    • Reduces ACC1 R
    • Reduces AChE R
    • Reduces Akt (increases mRNA) R R R
    • Reduces ALP R
    • Reduces α-Glucosidase (leaves and stems) R R
    • Reduces ALT R
    • Reduces AST R
    • Reduces Bcl-2 R R
    • Reduces Bcl-x R R
    • Reduces Bilirubin R
    • Reduces CDK2 R
    • Reduces CDK6 R
    • Reduces C/EBPs R
    • Reduces COX-2 R R
    • Reduces CXCR4 R
    • Reduces cyclin D1 R R
    • Reduces c-myc R
    • Reduces c-Src R
    • Reduces DA (although increases in hippocampus) R R
    • Reduces Dkk1 R
    • Reduces EMT R
    • Reduces FABP4 R
    • Reduces Factor D R
    • Reduces FAS R
    • Reduces GGT R
    • Reduces Glucose R
    • Reduces GOT R
    • Reduces HER2/ERBB2 R R
    • Reduces hnRNP-K R
    • Reduces IAP-1 R
    • Reduces IAP-2 R
    • Reduces IFN-g R
    • Reduces IkBa R
    • Reduces IL-1b R R
    • Reduces IL-6 R R
    • Reduces IL-8 R
    • Reduces IL-12 R
    • Reduces IL-17A R
    • Reduces IL-23 R
    • Reduces Insulin R
    • Reduces JAK2 R
    • Reduces KAT2B R
    • Reduces LDH R
    • Reduces LDL R
    • Reduces Leptin R
    • Reduces LH R
    • Reduces LPO R R
    • Reduces Mcl-1 R
    • Reduces MDA R R
    • Reduces MMP-2 R R R
    • Reduces MMP-7 R
    • Reduces MMP-9 R R R
    • Reduces mTOR R
    • Reduces NA (also blocks reuptake and increases in hippocampus) R R
    • Reduces NF-kb R
    • Reduces NMD1 R
    • Reduces PAI-1 R R
    • Reduces PGE2 R
    • Reduces PPAR-g R R R
    • Reduces P65 R
    • Reduces ROS R
    • Reduces SCD1 R
    • Reduces Shh R
    • Reduces Slug R
    • Reduces Snail R
    • Reduces SREBPs R
    • Reduces STAT3 R
    • Reduces S6K1 R
    • Reduces Survivin R
    • Reduces TACE R
    • Reduces Testosterone R
    • Reduces TNF-α R R
    • Reduces TNFR1 R
    • Reduces TNFR2 R 
    • Reduces VEGF R
    • Reduces VEGFR R
    • Reduces vLDL R
    • Reduces XIAP R R
    • Reduces ZEB1 R
    • Reduces 5HT (also blocks reuptake and increases in hippocampus) R R
    • Reduces 5-LOX R

    Advanced:

    • Embelin's chemical name is chemically known as 2,5-dihydroxy-3-undecyl-1,4-benzoquinone.
    • Embelia ribes contains benzoquinone derivatives of Embelin and its dimeric form is named Vilangin as well as cyclitol quercitol, alkaloid christembine, tannins, as well as fatty ingredients including resinoid, fixed oil, and minute quantities of volatile oils. R
    • Embelin is also a phenolic lipid, and is photosensitive and in methanol, it shows a peak absorbance (k max) at 450 nm. R
    • Absorption was complete (bioavailability 97%) and fast with drug peak plasma at 0.28 h (9 µg/ml) and the disposition halflife was 9.5 h on i.v. and 11 h on oral administration...the kidney played a major role in drug excretion with 60.9% of the dose found in urine after 24 h. R
    • Most of the immune mechanisms of Embelin seem to be through agonism of GPR84. R
    • Possibly in autoimmunity (in cancer studies), embelin suppresses immune suppressive IL-17A+ cells, GM-CSF+ cells, MDSCs and Treg by inhibiting IL-6 secretion. R R
    • In MS, EB suppressed human CD14+ monocyte-derived dendritic cell (DC) differentiation, maturation, and endocytosis and further inhibited the stimulatory function of mature DCs on allogeneic T cell proliferation in vitro. R
    • Also in MS, EB blocked the DC-derived expression of the Th1 cell-polarizing cytokines interferon-γ and interleukin (IL)-12 and the Th17 cell-polarizing cytokines IL-6 and IL-23. R
    • In cancer, EB suppresses the constitutive activation of Akt/mTOR/S6K1 signaling cascade, which correlated with the induction of apoptosis as characterized by accumulation of cells in subG1 phase, positive Annexin V binding, down-regulation of anti-apoptotic (Bcl-2, Bcl-xL, survivin, IAP-1, and IAP-2) and proliferative (cyclin D1) proteins, activation of caspase-3, and cleavage of PARP. R
    • Also in cancer, EB promote the mitochondrial release of cytochrome c, thus activating the caspase proteins to cause apoptosis.R
    • In pancreatic cancer, embelin seems to work on the sonic hedgehog (shh) patways - Embelin inhibited pancreatic cancer growth in Kras(G12D) mice by modulating tumor immune microenvironment where CTL, NKT, γδT, NK, and IFNγ (Th1 type) cells were up-regulated, and Th17, PMN-MDSC, IL-6 and IL-8 (Th2 type) immune cells were inhibited. R
    • In diabetes, the PPARγ mRNA level in epididymal adipose tissue was significantly increased, while PPARγ mRNA expression in the liver and skeletal muscle of diabetic treated group increased slightly...the molecular docking of embelin into PPARg, PI3K, p-Akt and GLUT4 active sites promoting insulin sensitisation and glucose uptake. R
    • In pain, p-sulphonylamine phenylamino derivative of embelin showed better anti-inflammatory activity than the parent compound embelin with significant reduction in the paw oedema of 19.02% in 30 min in comparison to 14.74% after 120, 180 and 360 min, respectively. R
    • In wound healing, embelin is a novel dual 5-lipoxygenase/ microsomal prostaglandin E2 synthase inhibitor. R
    • In IBD, embelin ameliorated colitis by suppressing TNF-a, IL-1b and IL-6 mRNA expression levels. R
    • In HD, one mechanism it may do this is that embelin acts as a novel p300/CBP-associated factor (PCAF, KAT 2B)-specific non-competitive inhibitor which inhibits the lysine acetyltransferase (KAT) activity of PCAF which is useful in the muscle differentiation process...This PCAF KAT activity inhibition in turn inhibited the acetylation of MyoD, which blocks the differentiation of myoblasts into myotubes. R
    • Embelin elicits a rapid increase of intracellular free Ca(2+), leading to activation of endothelial nitric oxide synthase (eNOS) and NO-induced cGMP accumulation. R

    More Research

    • Embelin stimulates phospholipid scrambling of the erythrocyte cell membrane, an effect involving ceramide formation. R