Bitters (Terpenes) Flashcards

(6 cards)

1
Q

What are the bitter terpenes?

A
  • They are various phytochemical classes within terpenes
  • But they all increase appetite, secretion of saliva, gastric secretions and digestive function.
  • Helpful for the elderly as an aperitif.
  • Increase gallbladder motility, stimulate bile release and bile production by the liver, and promote secretion of pancreatic enzymes.
  • Useful in diabetes, help normalise blood sugar levels.

Gastric secretions - Gastric secretions are needed for nutrient absorption and healthy bowel flora. They are preventative against bacterial and parasitic enteric infection.

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2
Q

What are the iridoids, seco-iridoids bitters and what plants contain them?

A
  • They are monoterpene seco-iridoid glycosides with a very bitter taste (picro- and amari- denote bitterness).
  • Include Amarogentin, gentiopicrin, sweroside and swertiamarin
  • Amarogentin is found in gentian and chitretta, Swertia chirayita.
  • Gentiopicrin is found in gentian
  • Sweroside and swertiamarin is found in centaury and chitretta.

Amarogentin is Immunomodulatory in the skin interacting with mast cells and keratinocytes.
Inhibition of aldose reductase results in antidiabetic action. Stabilised glucose in an in vivo diabetic study.

Gentiopicroside - Analgesic and anti inflammatory, antispasmodic in smooth muscle. Cytoprotective and wound healing.
Antiviral, antihepatotoxic and choleretic.

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3
Q

What are the sesquiterpene
lactones bitters, and what herbs contain them?

A
  • Bitter principle, 15-carbon sesquiterpene backbone and a lactone ring
  • Milk-white latex-like sap (e.g. dandelion and wild lettuce)
  • Created in defence against fungi, bacteria, helminths, and insects.
  • Antimicrobial by disrupting the cell wall of fungi and invasive bacteria.
  • Anti-parasitic and anti-inflammatory with several mechanisms proposed.
  • Anticancer via NF-kB modulation, preventing metastasis, inducting apoptosis, and sensitising tumour cells to conventional drug treatments.
  • Antispasmodic, bitter digestive action increases production and release of bile from the liver.
  • Anti-proliferative on a range of human cancer cell types by releasing a high concentration of free radicals inside them.

Contained in
* Arnica
* Artichoke
* Burdock
* Chicory
* Dandelion
* Yarrow (achillicin and achillin).
* Feverfew and
* Sweet wormwood

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4
Q

What is the deepdive on Feverfew?

A

Traditional use - Long history of use by Ancient Greeks and early European herbalists. Used for migraine headaches, rheumatoid arthritis, stomach ache, toothache, insect bites, infertility, menstruation and labour during childbirth. Anticancer, anti-inflammatory, cardiotonic, an emmenagogue, and enema for worms. Fresh leaves inhibit smooth muscle spasm, possibly by blocking potassium channels in vitro.

Parthenolide Inhibits IκB kinase complex, an enzyme complex involved in propagating the cellular response to inflammation. Inhibited serotonin-mediated spasmogenic response.
Anticancer effects against several human cancer cell lines. Prophylactic for migraine headache, and arthritis, multi targeted (inhibition of prostaglandin synthesis and decrease of vascular smooth muscle spasm).

Feverfew extract
Inhibits histamine release from mast cells.
Antibacterial and antifungal activity in vitro.
Inhibits prostaglandin synthesis.

Sensitisation to sesquiterpene lactones in one plant can lead to cross-reactivity with other Compositae, e.g. chamomile.

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5
Q

What’s the deepdive on Sweet Wormwood?

A

Traditional use - Artemisia annua has a long tradition of treating intermittent fevers, malarial infections. Traditionally prepared Artemisia formulation is
claimed to be superior to the single purified drug.

Artemisinin - Was used to treat multiple drug resistant malaria (quinine); able to kill
immature plasmodia in the erythrocytes.
Contains an endoperoxide bridge, two oxygen atoms bonded to one another, and releases deadly free radicals into plasmodia. Multiple targets in plasmodia (including binding to haem, causing their death).

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6
Q

What are the monoterpene lactones, and which plants contain them?

A

Bitter principles occur as glycosides.
Monoterpene lactones = glycosides with lactone rings.

Aucubin - Pharmacokinetics: aucubin is hydrolysed to aucubigenin and glucose by bacterial beta-glucosidase, then metabolised to aucubinines.

Aucubigenin - Antibacterial, antifungal and antiviral against Micrococcus aureus, Escherichia coli, Bacillus subtilis, Mycobacterium phlei and hepatitis B.
Hepatoprotective in vivo inhibited cytochrome P450 in isolated hepatocytes in vitro.
Anti-inflammatory in vitro: aucubinigenin suppressed TNF-alpha. Beneficial activity for the pancreas in models of diabetes in vivo.
Neuroprotective affects against encephalopathy in vivo.

Plantain, Plantago major L. and Ribwort, P. lanceolata L. (with monoterpene lactone, catalpol). Ribwort, plantain and eyebright traditionally used for respiratory
conditions, including upper respiratory tract and plantain as a vulnerary.

Eyebright - Treatment of bacterial infections and might also help with liver toxicity, antiviral.
Nerve-regenerating activity due to the aucubin content. A trial evaluating the efficacy of eyebright eyedrops in patients with
inflammatory or catarrhal conjunctivitis gave positive results.

  • Vitex (with iridoids agnoside and aucubigenin)
  • Cleavers
  • Rehmannia
  • Devils claw, Harpagophytum procumbens. Grows in the Kalahari region of southern Africa
    Analgesic anti-inflammatory for arthritis, dyspepsia, fever, blood diseases, UTIs, sprains, sores, ulcers and boils. Iridoids of devil’s claw: harpagide, harpagoside and 8-O pcoumaroylharpagide transformed into aucubinine B by gut flora. Devil’s claw 50% ethanolic extract had anti-inflammatory effect
    in vivo for chronic arthritis. Effective for musculoskeletal pain and osteoarthritis of the
    spine, hip and knee.
  • Catnip - Cat nip, Nepeta cataria L. Nepetalactone is a mosquito repellent as effective as DEET, while ten times less
    toxic. Potential to be used in human and livestock protection.
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