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Arnica montana
Report by: Sham Mohammed Nihal jalal
University of Sulaymaniyah-
college of pharmacy
12/29/23
Practical Pharmacognosy I
Stage- 3
CONTENTS
Arnica montana l. ....................................................................................................................................2
Medicinal benefits...................................................................................................................................2
phytochemistry.......................................................................................................................................3
mechanism of action............................................................................................................................... 3
OTHER pharmacological activities..........................................................................................................4
toxicological effects................................................................................................................................5
discussion ...............................................................................................................................................5
References..............................................................................................................................................5
Arnica montana l.
Arnica montana (or mountain arnica & mountain tobacco) is a tall and
yellow perennial flowering plant that grows in high altitudes.
A. montana is in the family Asteraceae, one of the largest flowering plant
family containing more than 23 000 species, members of the family also
include daisies, sunflowers and lettuce.
It is indigenous to mountain slopes in Europe, northern Asia, Siberia and
America.
MEDICINAL BENEFITS
Arnica traditionally has been widely used as a therapeutic plant, the flowers of the plant have the
greatest medicinal value and are used in forms of dilute oral solutions or topical preparations, as they
pass through the skin easily, to treat various ailments and have been reported to possess anti-
inflammatory, antifungal, antibacterial, antitumor, antioxidant and immunomodulatory activity.
According to European pharmacopoeia (1809), A. montana tincture is produced from one part of the A.
montana flowers containing 0.04% active drugs in 10 parts of ethanol 70% (V/V). when the Tincture is
dried by evaporation, and the extract is used in numerous herbal medications.
The most common topical use for A. montana is the treatment of:
o Inflammation of skin
o Hematomas and bruises
o edema
o rheumatic muscle and joint pain
o post-surgery and post-laser treatment
This is usually found in the form of ointments, gels and creams containing (3-40%) of A. montana flower
extracts.
FIGURE 3
PHYTOCHEMISTRY
A. montana contains a wide variety of chemical
substances compounds including sesquiterpene
lactones and their short-chain carbonic acid esters,
flavonoids, carotenoids, essential oils, diterpenes,
pyrrolizidine alkaloids, etc., are found in different
parts of the plant.
The major secondary metabolites responsible for its anti-inflammatory activity are the
sesquiterpene lactones (Sls) which are: 10α-methyl pseudo-guaianolide like helenalin, 11α,13-
dihydrohelenalin and their ester derivatives. In figure 4.
In the flower head the dry weights of sesquiterpene lactones and flavonoids are (0,3-1% and 0.4-0.6%)
respectively, they vary according to maturity of the flower.
MECHANISM OF ACTION
Research shows that the sesquiterpene lactones (Sls) interferes with activation of nuclear factor kappa
B (NF-κB) and also inhibits nuclear factor of activated T-cells (NF-AT). [1] by precisely altering NF-
κB/IκB gene complex, inhibiting the release of IκB.[2]
Both transcription factors NF-κB and NF-AT are regulators of the immune response by regulating the
transcription of genes of cytokines IL-1, IL-2, IL-4, TNF-α, iNOS, cyclooxygenase II, etc. and play a
major role in the activation and differentiation of T-cells which enhances the inflammatory response.
Research shows that the anti-inflammatory activities correlate with the qualitative and quantitative
contents of sesquiterpene lactones in the plant, additionally the type of esterification in the
dihydrohelenalin influences its inhibitory activities.as we can see in figure 5 & 6[1]
FIGURE 4
FIGURE 5
In vitro analysis (on
human mononuclear
cells) showing percentage
of inhibition of IL-1β and
TNF- α release by two
arnica montana tinctures
from different regions. In
each experiment no
cytotoxic effects were
observed.[1]
The differences in IC50 results are due to SLs contents in the plant. Pure helenalin is 20x more active
than pure dihydrohelenalin. Since ‘Arbo’ arnica tincture contains more helenalin than Spanish arnica
tincture, its 2 folds more potent.
OTHER PHARMACOLOGICAL ACTIVITIES
o Immunostimulatory activity: Polysaccharides in A. montana flowers are reported to increase
phagocytosis by granulocytes (from cell cultures) by activating macrophages to release TNF and
fucogalactoxyloglucan which increases phagocytosis[2]
o Anti-platelet activity: In two reports it was found that hexuronic acids, phenolic glycoconjugates
and the sesquiterpene lactones present in A. montana are responsible for the anticoagulant activity
of the plant, both using human blood for tests, by inhibiting formation of thromboxane and
secretion of serotonin. [2]
o Anti-osteoarthritic activity: It is reported that topical montana gel containing sesquiterpene
lactones (Sls) It promotes functionality of hands, reduces morning stiffness, pain of joints. [2]
o Antimicrobial activity: Arnica extracts exhibit inhibitory activity against Streptococcus strains.
thymol derivatives present in the roots are also bactericidal and fungicidal. [2]
o Anti-osteoporotic activity: A. montana is a significant source of flavonol aglycone glycoside which
when combined with calcium assists calcium absorption. [2]
o Improves circulation: Arnica is reported to relieve symptoms of fibromyalgia, toxic neuropathy
and diabetic neuropathy. [2]
o Antioxidant activity: A. montana shows 71.52% and 63.68% total antioxidant activity (DPPH
scavenging and phosphomolybdate method) respectively. this is due to the presence of flavonoids
and phenolic compounds. Thymol present in the roots is also an antioxidant. [2]
FIGURE 6
In vivo analysis (mouse ear edema) showing percentage of ear edema inhibition by 1µmol/cm2
of two
different esterified dihydrohelenalins. Proving differences in potency from different acyl moieties.
Esters with unsaturated acyl moieties posses stronger activity than saturated ones.
o Increase respiration: Sesquiterpene lactones in A. montana, are also reported to increases
respiration frequency and volume in Rats and rabbits by I.V injection by 35 and 43%, respectively, at
a dose of 0.25 mg/kg. [2]
o Hyperpigmentation treatment: montana extract when used to treat cultured mouse melanoma
cells boosting hypo pigmenting gene expression, useful for hypo pigmenting cosmetics. [2]
o Wound healing: In literature A. montana is used to heal wounds. In mice at a dose of 100mg/kg and
in Rats in combination with another drug.[2]
o Anti-cough: Arnica 6CH pills showed significant decrease of esophageal reflux in hiatus hernia.[2]
o Anti-hemorrhagic: Stem tincture of A. montana possessed anti-hemorrhagic activity in women of
age group 20–35 years, reducing postpartum blood loss.[2]
TOXICOLOGICAL EFFECTS
Arnica is thought to have limited toxicity when applied to unbroken skin for short periods of time or
when taken by mouth in very dilute forms[6]. In a report it was determined that 0,000717 mg/kg/day is
an acceptable amount to take orally [5]
But if taken in moderate amounts orally it can cause adverse effects like vomiting, nervousness,
diarrhea, headaches and abortions. and in high doses can be lethal due to cardiac arrest. The oral LD50
of an extract was >5 g/kg in rats and 123 mg/kg in mice.[6]
Arnica is NOT safe to use if you are pregnant or breastfeeding. Drinking Arnica teas or tinctures can
result in miscarriage.[6] and it should not be taken in combination with blood thinner medications and
foods since it has anti-coagulant activities.
DISCUSSION
In conclusion CICABIO ARNICA + contains Arnica montana flower extract. Arnica montana has
significant therapeutic effects both topically and orally in dilute tinctures, and is widely and effectively
used for its topical anti-inflammatory activities, especially the flower heads since it contains more
sesquiterpene lactones (Sls) content which are the Active ingredient responsible for this activity.
REFERENCES
1. Sosa, Silvio. “Studies on the Anti-Inflammatory Activity of Phytopharmaceuticals Prepared from
Arnica Flowers1.” Planta Medica (2002): n. pag. Print.
2. Kriplani, P., Guarve, K., & Baghael, U. S. (2017). Arnica montana L. – a plant of healing: review. In
Journal of Pharmacy and Pharmacology (Vol. 69, Issue 8). https://doi.org/10.1111/jphp.12724
3. Cicabio arnica+ | cream for quick skin damage resorption treatment, bioderma.ae.
https://www.bioderma.ae/our-products/cicabio/arnica
4. “Arnica montana.” Wikipedia, Wikimedia Foundation, 3/Dec/2023,
https://en.wikipedia.org/wiki/Arnica_montana.
5. Aiello, E., Russo, R., Cristiano, C., & Calignano, A. (2018). The safety assessment of herbals
with a new and ethical approach. In Natural Product Research (Vol. 32, Issue 15).
https://doi.org/10.1080/14786419.2017.1402316
6. Liu, lindsy. (2019) Caution when using Arnica products. Poison control-National capital
poison center, https://www.poison.org/articles/caution-when-using-arnica-products-193.

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Arnica montana and its medicinal benefits

  • 1. Arnica montana Report by: Sham Mohammed Nihal jalal University of Sulaymaniyah- college of pharmacy 12/29/23 Practical Pharmacognosy I Stage- 3
  • 2. CONTENTS Arnica montana l. ....................................................................................................................................2 Medicinal benefits...................................................................................................................................2 phytochemistry.......................................................................................................................................3 mechanism of action............................................................................................................................... 3 OTHER pharmacological activities..........................................................................................................4 toxicological effects................................................................................................................................5 discussion ...............................................................................................................................................5 References..............................................................................................................................................5 Arnica montana l. Arnica montana (or mountain arnica & mountain tobacco) is a tall and yellow perennial flowering plant that grows in high altitudes. A. montana is in the family Asteraceae, one of the largest flowering plant family containing more than 23 000 species, members of the family also include daisies, sunflowers and lettuce. It is indigenous to mountain slopes in Europe, northern Asia, Siberia and America. MEDICINAL BENEFITS Arnica traditionally has been widely used as a therapeutic plant, the flowers of the plant have the greatest medicinal value and are used in forms of dilute oral solutions or topical preparations, as they pass through the skin easily, to treat various ailments and have been reported to possess anti- inflammatory, antifungal, antibacterial, antitumor, antioxidant and immunomodulatory activity. According to European pharmacopoeia (1809), A. montana tincture is produced from one part of the A. montana flowers containing 0.04% active drugs in 10 parts of ethanol 70% (V/V). when the Tincture is dried by evaporation, and the extract is used in numerous herbal medications. The most common topical use for A. montana is the treatment of: o Inflammation of skin o Hematomas and bruises o edema o rheumatic muscle and joint pain o post-surgery and post-laser treatment This is usually found in the form of ointments, gels and creams containing (3-40%) of A. montana flower extracts. FIGURE 3
  • 3. PHYTOCHEMISTRY A. montana contains a wide variety of chemical substances compounds including sesquiterpene lactones and their short-chain carbonic acid esters, flavonoids, carotenoids, essential oils, diterpenes, pyrrolizidine alkaloids, etc., are found in different parts of the plant. The major secondary metabolites responsible for its anti-inflammatory activity are the sesquiterpene lactones (Sls) which are: 10α-methyl pseudo-guaianolide like helenalin, 11α,13- dihydrohelenalin and their ester derivatives. In figure 4. In the flower head the dry weights of sesquiterpene lactones and flavonoids are (0,3-1% and 0.4-0.6%) respectively, they vary according to maturity of the flower. MECHANISM OF ACTION Research shows that the sesquiterpene lactones (Sls) interferes with activation of nuclear factor kappa B (NF-κB) and also inhibits nuclear factor of activated T-cells (NF-AT). [1] by precisely altering NF- κB/IκB gene complex, inhibiting the release of IκB.[2] Both transcription factors NF-κB and NF-AT are regulators of the immune response by regulating the transcription of genes of cytokines IL-1, IL-2, IL-4, TNF-α, iNOS, cyclooxygenase II, etc. and play a major role in the activation and differentiation of T-cells which enhances the inflammatory response. Research shows that the anti-inflammatory activities correlate with the qualitative and quantitative contents of sesquiterpene lactones in the plant, additionally the type of esterification in the dihydrohelenalin influences its inhibitory activities.as we can see in figure 5 & 6[1] FIGURE 4 FIGURE 5 In vitro analysis (on human mononuclear cells) showing percentage of inhibition of IL-1β and TNF- α release by two arnica montana tinctures from different regions. In each experiment no cytotoxic effects were observed.[1]
  • 4. The differences in IC50 results are due to SLs contents in the plant. Pure helenalin is 20x more active than pure dihydrohelenalin. Since ‘Arbo’ arnica tincture contains more helenalin than Spanish arnica tincture, its 2 folds more potent. OTHER PHARMACOLOGICAL ACTIVITIES o Immunostimulatory activity: Polysaccharides in A. montana flowers are reported to increase phagocytosis by granulocytes (from cell cultures) by activating macrophages to release TNF and fucogalactoxyloglucan which increases phagocytosis[2] o Anti-platelet activity: In two reports it was found that hexuronic acids, phenolic glycoconjugates and the sesquiterpene lactones present in A. montana are responsible for the anticoagulant activity of the plant, both using human blood for tests, by inhibiting formation of thromboxane and secretion of serotonin. [2] o Anti-osteoarthritic activity: It is reported that topical montana gel containing sesquiterpene lactones (Sls) It promotes functionality of hands, reduces morning stiffness, pain of joints. [2] o Antimicrobial activity: Arnica extracts exhibit inhibitory activity against Streptococcus strains. thymol derivatives present in the roots are also bactericidal and fungicidal. [2] o Anti-osteoporotic activity: A. montana is a significant source of flavonol aglycone glycoside which when combined with calcium assists calcium absorption. [2] o Improves circulation: Arnica is reported to relieve symptoms of fibromyalgia, toxic neuropathy and diabetic neuropathy. [2] o Antioxidant activity: A. montana shows 71.52% and 63.68% total antioxidant activity (DPPH scavenging and phosphomolybdate method) respectively. this is due to the presence of flavonoids and phenolic compounds. Thymol present in the roots is also an antioxidant. [2] FIGURE 6 In vivo analysis (mouse ear edema) showing percentage of ear edema inhibition by 1µmol/cm2 of two different esterified dihydrohelenalins. Proving differences in potency from different acyl moieties. Esters with unsaturated acyl moieties posses stronger activity than saturated ones.
  • 5. o Increase respiration: Sesquiterpene lactones in A. montana, are also reported to increases respiration frequency and volume in Rats and rabbits by I.V injection by 35 and 43%, respectively, at a dose of 0.25 mg/kg. [2] o Hyperpigmentation treatment: montana extract when used to treat cultured mouse melanoma cells boosting hypo pigmenting gene expression, useful for hypo pigmenting cosmetics. [2] o Wound healing: In literature A. montana is used to heal wounds. In mice at a dose of 100mg/kg and in Rats in combination with another drug.[2] o Anti-cough: Arnica 6CH pills showed significant decrease of esophageal reflux in hiatus hernia.[2] o Anti-hemorrhagic: Stem tincture of A. montana possessed anti-hemorrhagic activity in women of age group 20–35 years, reducing postpartum blood loss.[2] TOXICOLOGICAL EFFECTS Arnica is thought to have limited toxicity when applied to unbroken skin for short periods of time or when taken by mouth in very dilute forms[6]. In a report it was determined that 0,000717 mg/kg/day is an acceptable amount to take orally [5] But if taken in moderate amounts orally it can cause adverse effects like vomiting, nervousness, diarrhea, headaches and abortions. and in high doses can be lethal due to cardiac arrest. The oral LD50 of an extract was >5 g/kg in rats and 123 mg/kg in mice.[6] Arnica is NOT safe to use if you are pregnant or breastfeeding. Drinking Arnica teas or tinctures can result in miscarriage.[6] and it should not be taken in combination with blood thinner medications and foods since it has anti-coagulant activities. DISCUSSION In conclusion CICABIO ARNICA + contains Arnica montana flower extract. Arnica montana has significant therapeutic effects both topically and orally in dilute tinctures, and is widely and effectively used for its topical anti-inflammatory activities, especially the flower heads since it contains more sesquiterpene lactones (Sls) content which are the Active ingredient responsible for this activity. REFERENCES 1. Sosa, Silvio. “Studies on the Anti-Inflammatory Activity of Phytopharmaceuticals Prepared from Arnica Flowers1.” Planta Medica (2002): n. pag. Print. 2. Kriplani, P., Guarve, K., & Baghael, U. S. (2017). Arnica montana L. – a plant of healing: review. In Journal of Pharmacy and Pharmacology (Vol. 69, Issue 8). https://doi.org/10.1111/jphp.12724
  • 6. 3. Cicabio arnica+ | cream for quick skin damage resorption treatment, bioderma.ae. https://www.bioderma.ae/our-products/cicabio/arnica 4. “Arnica montana.” Wikipedia, Wikimedia Foundation, 3/Dec/2023, https://en.wikipedia.org/wiki/Arnica_montana. 5. Aiello, E., Russo, R., Cristiano, C., & Calignano, A. (2018). The safety assessment of herbals with a new and ethical approach. In Natural Product Research (Vol. 32, Issue 15). https://doi.org/10.1080/14786419.2017.1402316 6. Liu, lindsy. (2019) Caution when using Arnica products. Poison control-National capital poison center, https://www.poison.org/articles/caution-when-using-arnica-products-193.