Kolkilaksha

Last Updated: October 5 2021

Asteracantha longifolia (Kokilaaksha) is an ayurvedic aphrodisiac and liver protective agent. Currently, research on this plant is preliminary with limited information on both components of the plant and toxicology.

Kolkilaksha is most often used for


1.

Sources and Composition

1.1

Sources

Asteracantha longifolia (of the family Acanthaceae, synonymous the Hygrophila genera (auriculata and spinosa) as well as the Barleria genera (auriculata and spinosa)[1]) is a traditional Indian medicine[2] named either Kokilaaksha or Talimakhana (Ayurvedic and Unani medicine, respectively[1]) and some lesser known names of Ikshura, Ikshugandha,[3] and Ikkirie.[4]

Asteracantha longifolia belongs to the Ayurveda class of 'Vajikaran' for enhancement of sexual performance, and also has uses as a general tonic, sedative,[1] asthma, jaundice, liver ailments, and diuretic[5][6] as well as various 'diseases of the blood' and inflammatory diseases such as rheumatism and edema.[3][4] Traditional usage seems to recommend one ounce of the root (boiled in a pint of water until fourteen ounces remain) or two ounces of the dried leaves extracted with vinegar or water.[4]

The plant Asteracantha longifolia appears to be a traditionally recommended blood tonic and aphrodisiac from Indian medicine, and it is also known for its supposed liver benefits

1.2

Composition

The leaves of Asteracantha longifolia contain:

  • The aliphatic esters 25-oxo-hentriacontanyl acetate and methyl 8-n-hexyltetracosanoate[7]
  • Butelin[7]
  • Lupeol[7] at 0.051%[6]
  • Stigmasterol[7] and β-sitosterol (0.069%)[6]

The stems contain:

  • Lupeol (0.121%)[6]
  • β-sitosterol (0.029%)[6]

The seeds contain:

  • A seed oil containing linoleic acid (11%), palmitic acid (8%) and stearic acid (0.6%)[5]
  • Asterol I-IV[8]
  • Asteracanthine and asteracanthinine (alkaloids)[1][8]
  • Lupeol at 0.044%[6]
  • β-sitosterol (0.031%)[6]

The roots contain:

  • Lupeol (0.25% dry weight)[6]
  • β-sitosterol (0.06%)[6]

In a preliminary qualitative analysis of the compounds in Asteracantha longifolia leaves the classes of steroids, saponins (0.68+/-0.12%), tannins (4.92+/-0.18%), phenolics (0.16+/-0.10%), and cardiac glycosides were found while terpenoids, alkaloids, and flavonoids were absent.[2] Despite this, in the quantitative analysis there was a detectable alkaloid (1.14+/-0.14%) and flavonoid (0.24+/-0.19%) content.[2]

The composition of asteracantha longifolia is not very well known at this moment in time

2.

Neurology

2.1

Neurprotection

The terpenoid fraction of asteracantha longifolia (100-200mg/kg) orally for seven days in rats then subject to transient global cerebral ischemia, supplementation was associated with improvements in cognitive testing and reductions in brain lipid peroxidation with a potency comparable to 500mg/kg Vitamin E.[9]

May be slightly neuroprotective, which is thought to be associated with its antioxidative properties

2.2

Aphrodisia

An ethanolic extract of the seeds (100-200mg/kg) to rats over 28 days caused dose-dependent increaes in mounting frequency (380-472% of control) and similar reductions in mounting, intromission, and post-ejaculatory latencies; all doses were nonsignificantly more libido enhancing than the active control of 0.5mg/kg testosterone injections.[1]

Appears to have some aphrodisiac properties with prolonged ingestion, although it appears to be of comparable potency to other libido enhancing herbs in rats

3.

Cardiovascular Health

3.1

Blood

The chloroform extract of the leaves of asteracantha longifolia (250-500mg/kg intraperitoneal injections in mice) given for 22 days after cyclophosphamide-induced anemia was able to restore levels of blood cells (normalization after 15 days) indicative of haematopoietic potential.[10] The suppression in bone marrow cell count was also normalized by treatment with asteracantha longifolia[10] and elsewhere in haloperidol-induced anemic rats an ethanolic extract of the aerial parts (100-200mg/kg) given via intraperitoneal injections was able to almost normalize blood cell parameters (hematocrit, RBC count, hemoglobin) after 19 days.[11]

In rats that are not anemic and given 200mg/kg of the ethanolic extract (injections), administration of the supplement does not appear to stimulate erythropoesis and is met with a small (possibly clinically irrelevant) decline relative to untreated control.[11]

In instances of anemia where administered chemicals can reduce red blood cell count and functionality, it appears that asteracantha longifolia can stimulate erythropoesis and normalize the differences within a few weeks. This does not work in non-anemic animals, and no studies have used oral supplemental dosages yet

4.

Interactions with Glucose Metabolism

4.1

Absorption

Large oral doses of the water extract of the aerial parts of the plant (leaf and stem, dosed at 5g/kg bodyweight in rats) has failed to modify the absorption of glucose.[12]

Does not appear to inhibit glucose absorption

4.2

Glycogen

Oral ingestion of the water extract has failed to modify gluconeogenesis in the rat liver following an oral glucose tolerance test.[12]

In rats, administration of a water extract (at 5g/kg bodyweight) prior to glucose loading has resulted in increased glycogen storage in both the liver (108.5+/-9.5%) and skeletal muscle (57.8+/-4.2%) although an increase in triglyceride storage of adipose tissue (10.2+/-1.8%) was also noted.[12]

While the water extract of astercantha longifolia does not appear to promote nor hinder gluconeogensis, it appears that preloading this herb before carbohydrates augments the amount of glycogen that is stored in the liver and muscle tissue

4.3

Diabetes

100-250mg/kg of the ethanolic leaf extract for three weeks in diabetic rats is able to reduce fasting blood glucose associated with a normalization of antioxidant enzymes (glutathione peroxidase, catalase, and glutathione-S-transferase) and lipid peroxidation.[13]

Oral ingestion of 10mL/kg of a hot water leaf extract (where each mL is equivalent to 1g of plant material) in normal humans is able to reduce exposure to glucose following an oral glucose tolerance test by 25%; the drink was slightly more effective in diabetics since it reduced exposure by 36%.[14]

There appears to be a hypoglycemic effect when this herb is coingested with dietary carbohydrates, and this is thought to be related to the deposition of carbohydrates into muscle and the liver as glycogen

5.

Interactions with Oxidation

5.1

In vitro

As assessed by FTC method (used to assess peroxide formation at the initial stages), the water extract of the roots of asteracantha longifolia inhibited 55.29% of peroxide formation and appears to be nonsignificantly more potent than both Vitamin E and Vitamin C as reference compounds.[15] This potency carried over to the TBS assay where the water extract inhibited 60% of MDA formation, showing another effective anti-lipid peroxidation measurement.[15]

The water extract of the roots appears to have somewhat respectable antioxidative properties against lipid peroxidation, which nonsignificantly outperform the references of vitamins C and E

6.

Interactions with Organ Systems

6.1

Sexual Organs

An ethanolic extract of the seeds (100-200mg/kg) to rats over 28 days caused a dose-dependent increase in the weight of sexual organs (testicles, seminal vesicles, and epididymus) with a increase in prostatic weight that was not dose dependent.[1] This same dose caused increases in semen count associated with increased spermatogenesis.[1]

There may be a small increase in male sex organ weight that occurs alongside prolonged usage of the herb and its libidoo enhancing effects

6.2

Liver

In vitro, the isolated alkaloids of asteracantha longifolia appear to be protective against CCL4 in liver cells in the concentration range of 40-80µg/mL with the highest tested concentration having a potency comparable to 250µg/mL Silymarins.[16]

The alkaloids appear to be the main active component

A methanolic extract of the seeds of asteracantha longifolia appears to have hepatoprotective properties against both thioacetamide and paracetamol[17] as well as acetominophen in rats.[18] Protection against carbon tetrachloride (CCl4) has been noted in both mouse[19] and rat[20] models of hepatotoxicity.

A basic water extract of the roots (50-150mg/kg) alongside CCL4 in a rat model of hepatotoxicity was able to reduce the increase in liver enzymes (ALT, AST, ALP, and LDH) as well as bilirubin; the highest dose of the root extract (150mg/kg) was comparable to the reference drug of 50mg/kg Silymarins (from Milk thistle).[15] Elsewhere, the total alkaloid fraction of the leaves at 80mg/kg has been found to be comparable to 250mg/kg Silmyarins.[16]

Appears to have general liver protective properties in animal studies against hepatotoxins, and the potency of this plant is either comparable or lesser than that of other reference drugs such as Milk thistle although the isolated alkaloids may be more protective

7.

Interactions with Cancer Metabolism

7.1

Hepatocarcinoma

A methanolic extract of the seeds (200-400mg/kg) every other day for eight weeks in rats given hepatic tumors appears to be able to reduce subsequent foci development by up to 51% (relative to control) associated with an attenuation of the toxin-induced declinein glutathione peroxidase and catalase.[5]

8.

Safety and Toxicology

8.1

General

Both the alkaloidal[16] and terpenoid[9] fractions of the plant have been found to have no acute toxicity below 2000mg/kg oral ingestion in rats.

Preliminary and short term evidence in rats does not suggest any form of toxicity with single doses

References
1.^Chauhan NS, Sharma V, Dixit VKEffect of Asteracantha longifolia seeds on the sexual behaviour of male ratsNat Prod Res.(2011 Sep)
4.^Jayesingha WAOn Hygrophila Spinosa (Vel Asteracantha Longifolia)Br Med J.(1887 Jul 16)
5.^Ahmed S, Rahman A, Mathur M, Athar M, Sultana SAnti-tumor promoting activity of Asteracantha longifolia against experimental hepatocarcinogenesis in ratsFood Chem Toxicol.(2001 Jan)
7.^Misra TN, Singh RS, Pandey HS, Singh BK, Pandey RPConstituents of Asteracantha longifoliaFitoterapia.(2001 Feb)
8.^Thankamma ARheumatoid arthritis and astercantha longifoliaAnc Sci Life.(1999 Jan)
11.^Pawar RS, Jain AP, Lodhi S, Singhai AKErythropoietic activity of Asteracantha longifolia (Nees.) in ratsJ Ethnopharmacol.(2010 May 27)
13.^Vijayakumar M, Govindarajan R, Rao GM, Rao ChV, Shirwaikar A, Mehrotra S, Pushpangadan PAction of Hygrophila auriculata against streptozotocin-induced oxidative stressJ Ethnopharmacol.(2006 Apr 6)
14.^Fernando MR, Wickramasinghe N, Thabrew MI, Ariyananda PL, Karunanayake EHEffect of Artocarpus heterophyllus and Asteracanthus longifolia on glucose tolerance in normal human subjects and in maturity-onset diabetic patientsJ Ethnopharmacol.(1991 Mar)
16.^Raj VP, Chandrasekhar RH, P V, S A D, Rao MC, Rao VJ, Nitesh KIn vitro and in vivo hepatoprotective effects of the total alkaloid fraction of Hygrophila auriculata leavesIndian J Pharmacol.(2010 Apr)
19.^Hewawasam RP, Jayatilaka KA, Pathirana C, Mudduwa LKProtective effect of Asteracantha longifolia extract in mouse liver injury induced by carbon tetrachloride and paracetamolJ Pharm Pharmacol.(2003 Oct)
20.^Shailajan S, Chandra N, Sane RT, Menon SEffect of Asteracantha longifolia Nees. against CCl4 induced liver dysfunction in ratIndian J Exp Biol.(2005 Jan)