PHARM.

D Chemical Pharmacognosy- I Lecture 25 May 4th, 2011

ANTHRAQUINONE GLYCOSIDESGLYCOSIDES-V
M. Ahsan Khalid, B.Pharm, Pharm. D B.Pharm,
M.Phil Scholar (RIPS/RIU) HIPSHIPS-HUKIC

10 Main Component Groups of Aloe

 

Vitamins
 

Lignins


Vitamin D, A, C, E and B12 Lipases, proteases, kinases Ca, Na, K, Mg, Mn, Cu, Zn, Mn, Cr, and Se Mono and poly saccharides, glucosaccharides, glucomannans Most important: Aloin, and Aloin, Emodin
   

Enzymes Minerals


Inert except when in topical treatments 3% of Aloe Vera gel Cholesterol, Campesterol, Sisosterol, Campesterol, Sisosterol, and Lupeol AspirinAspirin-like 20 amino acids

Saponins
 

Fatty Acids

Sugars


Salicyclic acid
 

Anthraquinones


Amino Acids

Aloe and Irritable Bowel Syndrome (IBS)



Normal: digestive tract absorbs nutrients into blood  bacteria helps breakdown food IBS: unabsorbed food coats the bowel preventing normal absorption Symptoms:Exhaustion, Symptoms:Exhaustion, constipation, diarrhea, and indigestion Colonic Irrigation: loosed and wash out residues

Aloe and Rheumatoid Arthritis



 

Two main types of arthritis  Osteoarthritis: wear and tear of life  Rheumatoid: autoimmune disease Symptoms: stiff, red, swollen joints Traditional treatment: antiantiinflammatory drugs with steroids Aloe helps repair damage  Mode of Action: stimulate the Cytokines  Varying results

Aloe and Cosmetics

 

Added because of known rejuvenating action Mode of Action:  Polysaccachrides act as moisturizers  Stimulates the fibroblasts to replicate faster  Smoothes skin because sticks epidermal cells together which normally flake  Interferes with melanin deposit production which lead to liver spots

Aloe and Diabetes



 

Characterized by hyperglycaemia and alterations of glucose and lipid metabolism  Lead to cell damage and elevation of reactive oxygen species Must control blood glucose and lipid levels Aloe shown to reduce blood glucose in diabetic rats

Aloe and Diabetes

Decrease in blood glucose due to stimulation of insulin secretion Decrease in cholesterol, triglycerides, phospholipids, and free fatty acids from increased clearance and decreased transporters

Anti-Microbial/Anti-Microbial/-Bacterial
    

50% gel leaf solution, complete inhibition of Staphylococcus aureus Due to phenolics Efficacy of gel or leaf? S. aureus inhibited by both Other bacteria inhibited by just leaf or gel

Aloe, Antimicrobials, and Wounds

When aloe is combined with other anti-microbials, antia wound heals faster than with the anti-microbial antialone. Possibly due to its moisturizing capability as well.

Alveolar Osteitis
Dry Socket (Wisdom teeth extraction) Acemannan Hydrogel (from clear inner gel of aloe vera) vera)  Normal treatment 7.6% develop AO  With Acemannan 1.1% develop AO


Normal

Dry socket, clot does not form properly

Burn Treatment
  

Shows increased healing effects on 2nd degree burns AntiAnti-inflammation and wound healing promotion Vessels return to normal size quicker than with untreated burns

Aloe and Cancer

  

AloeAloe-emodin induces apoptosis in T24 human bladder cancer cells Inhibits cell viability, induces G2/M arrest MechanismMechanism- p53, p21, caspase activation Treat Radiation Symptoms?

Investigated anticancer effect of AE (1,8-dihydroy-3-[hydroxymethyl]-anthraquione) in the T24 human bladder cancer cell line by studying apoptosis regulation. AE, is purified from aloe vera leaves, has been reported to have antitumor activity. Levels of cyclins, cyclin-dependent kinase 1 and other enzyme were examined Results: AE inhibited cell viability, and induced Growth2/Mitosis arrest and apoptosis in T24 cells. AE increased the levels of Wee1 and cdc25c AE may have led to inhibition of the levels of cyclin-dependent kinase 1 and cyclin 131, which cause G2/M arrest. AE induced p53 expression and was accompanied by the induction of p21 and caspase-3 activation, which was associated with apoptosis. Conclusions: AE induced apoptosis in T24 cells is mediated through the activation of p53, p2l, Fas/APO-1, Bax and caspase-3. No evidence that it can prevent radiation induced skin inflammation in Cancer patients.

Neuroectodermal Cancer
Inhibits neuroectodermal tumors in mice. Few toxic effects, does not inhibit normal fibroblasts. Induces apoptosis and is specific to a tumor energyenergydependent pathway of drug incorporation


 

Cancer U-373 Glioma Cells UAloe-emodin from Aloe vera leaves has been reported to have antitumor activity. How does aloe-emodin regulate the cell cycle, cell proliferation and protein kinase C (PKC) during glioma growth and development? Aloe-emodin delayed the number of cells entering and exiting DNA synthesis (S) phase in both SVG and U-373MG cells indicating that Aloe-emodin may inhibit S phase progression. The aloe-emodin-induced decreased proliferation was sustained at 48-96 h. Aloe-emodin suppressed PKC activity and reduced the protein content of most of the PKC isozymes. Cancer growth inhibition by aloe-emodin was due to apoptosis (i.e., programmed cell death).

Gastric and Colorectal Cancers

Anticancer effects of aloe on sarcoma 180 in ICR mouse or human cancer cells were determined.

Determine effect of aloe on life span prolongation, followed by oral administration of Aloe vera (10 mg/kg/day, 50 mg/kg/day) or Aloe arborescens (10 mg/kg/day, 100 mg/kg/day) once a day for 14 days. The administration of Aloe vera or Aloe arborescens did not suppress tumor growth. However the life span of ICR mouse was prolonged to 19% (P lt 0.05), 22% (P lt 0.05), and 32% (P lt 0.05) by administration of Aloe vera 10 mg/kg/day, Aloe vera 50 mg/kg/day, and Aloe arborescens 100 mg/kg/day, respectively.

Not necessarily an anti-cancer effect, but definitely an anti-growth effect.

Products
 

Gel and latex. GelGel- leaf pulp or mucilage obtained from the parenchymal tissue. LatexLatex- bitter, yellow substance obtained from pericyclic tubules just beneath the outer skin of the leaves. (otherwise called Aloe juice) Using a freshly cut leaf is thought to be the most effective treatment.

Summary
Dental Health and Hygiene 2. Provides Rapid Soothing 3. Aids in Healthy Digestion 4. Immune Support and Function Regulates Weight and Energy Levels 6. Collagen and Elastin Repair 7. Daily Dose of Minerals 8. Daily Dose of Vitamins 9. AntiAnti-inflammatory Properties 10. Essential Amino Acids
1.

5.

Aloe - Uses


Purgative Seldom prescribed alone activity is increased when administered with small quantities of soap or alkaline salts; Carminatives moderate griping tendency. Ingredient in Friars Balsam.

Aloe Additional Notes



Medicinal Uses:


Etymology


AntiAnti-bacterial, anti-fungal, antichologogue, chologogue, emmenogogue, emmenogogue, antiinflammatory (juice), antianti-inflammatory , demulcent, immuneimmunestimulating (gel).

Name derives from Arabic alu, alu, meaning shiny or bitter in reference to the gel.

Other uses


Radiation burns (internal and external use)



ContraContra-indications
Pregnancy & lactation (internal uses)

KhoiKhoi-San hunters rub gel on their bodies to reduce sweating and mask their scent. Used to break nail-biting nailhabit.

COCHINEAL

Cochineal


Definition: Cochineal is the dried female insect, Dactylopius coccus, coccus, containing eggs and larvae. Insects are indigenous to Central America, commercial supplies are derived from Peru.

Eggs are protected during the rainy season are sown on cacti on which it is intended to breed. Both male and females arise. After a time, fecundation occurs. Females attach themselves to the cacti and the males die out. Females swell to x2 their original size due to developing larvae & develop red colouring matter.

Cochineal

Cochineal


Larvae mature after 14days and escape from the now dead body of the parent. Only a small portion develop into males. For next 2 weeks, males fly and young females crawl on the plant. Life cycle = 6 weeks. 3-5 generations may be produced in 1 season.

Cochineal - Collection
  

  

Insects are brushed from plants with small brooms and killed (some left to provide for subsequent crops). First crop killed contains the most colouring matter. Insects are killed by plunging them in boiling water, stove heat or exposure to fumes by burning sulphur or charcoal. If heat is used insects change to purple black called black grain. Fume killed turn purple-grey called silver purplegrain. Small immature insects and larvae which can be separated by sieves are sold as granilla or siftings.

Cochineal Collection

Cochineal - Characteristics
Oval in shape Half cm in length Examined microscopically after removing the colouring matter (ammonia solution). Each insect contains 60 450 eggs and larvae.

Cochineal - Constituents
    

C-glycoside anthraquinone derivative purple, water-soluble colouring matter waterCarminic acid Fat Wax

bright

Adulteration: occurs by increasing the weight of the insects by dressing it with inorganic matter in a colour which blends in with that of the insect. Detected when insects are placed in water

Last Word on Anthraquinones



Anthraquinones take about 10hours to produce an effect (take overnight) Should not be used for more than 10 days. Should not be used by children, pregnant and lactating women. Cause griping pain. Are habit-forming. habitAnthraquinones = phenolic glycosides, used as an irritating laxative