Aristolochia Indica Linn
Botanical Name: Aristolochia Indica Linn
Sanskrit Name: Isvari
Family Name: Aristolochiaceae
Vernacular names :
- Hindi – eswarmul
- Telugu –nallaisvari
- English –indian birthwort
- Tamil –perumarundu
Aristolochia Indica is a perennial creeper with greenish purple coloured flowers. It grows almost all over India. NakuliDvaya are quoted by BrihatTrayi. Thakurjiconsider thatNakuli means R. serpentina andGandhaNakuli means A. indica. Late Pt. HariprapannaSashtribelieved thatNakul and Gandhanakuli are Rasna varieties. A. indica and A. bracteata are considered as their botanical sources respectively.
Leaves simple, alternate, short petioled, the blade ovate or somewhat wedge shaped, very variable in shape and size (Plate 8). The young leaves are light purplish. The fruit is a capsule, roundish or oblong and hexagonal, 2.5-4 cm long and slightly less broad, with shallow grooves and six valves, containing many triangular seeds. The young roots are light brown and fairly smooth, whereas the older ones are comparatively rough due to the development of cork, lenticels and the presence of scars of rootlets. The cork layer somewhat friable. In a freshly cut transverse section of the root the entire bark appears as a narrow, cream-coloured strip, surrounding! a wide woody core. The wood has a light yellow colour and appears highly porous, with the pores being sufficiently large to be easily visible with the naked eye; the medullary rays are soft and creamy white in colour; there is no pith in the centre.
Throughout India , especially Kerala
Aristochine, aristolochene, ishwarone, aristolochic acid, ishwarane, cephaeradiones, artistolindiquinone
Rasa –tikta, katu, kasaya
Guna –laghu, ruksha
Virya – usna
Karma –kapha- vatahara, visaghna
Sarpa-Luta-Musika-Vrischika visa; Jvara, Vrana, Krimi
Part used –root , leaf
Powder 1-3 g, fresh juice (leaf) 5-10ml
(1) Vrddhi – Roots of isvari and Eranda are made as pastealong with the skin of rat and applied locally
(2) Sarpa visa – After blood letting, the roots of Carati and Nakuli are made into paste and applied (A.I-LUt.36).
Medicinal and pharmacological activities
- General antifertility activity
Aristolic acid, from Aristolochia indica, disrupted nidation in mice when administered on day 1 of pregnancy. The implantation-inhibiting effect of the compound was assessed with respect to tubal transport of ova into the uterus, hyperpermeability of endometrial capillaries, increase in uterine weight and total protein content, endometrial bed preparation and changes in uterine phosphatase enzymes during days 4-6 of pregnancy. The plant induces impairment of development, with a decrease in uterine weight and total protein content, in treated animals. Aristolic acid interfered with steroidal conditioning of the uterus, rendering it hostile to ovum implantation. An ethanol extract of A. indica root was found to decrease fertility in both rats and hamsters when administered postcoitally (on days 1-10 and 1-6 respectively). Methyl aristolate (60 mg/kg, orally) decreased the number of implantation sites when administered on the first two days of pregnancy in mice. When given at doses of 50 mg/kg (but not at 30 mg/kg) consecutively on days 1-4 of pregnancy, the number of implantation sites was also decreased, possibly by disturbing the hormone balance and thereby disrupting implantation. The aqueous alcoholic and petroleum ether extracts of Aristolochia indica at 1 :20 concentration affected the oestrus cycle adversely, terminating at the dioestrous stage. These extracts also showed a marked reduction in RNA, sialic acid, glycogen of the uterus and vagina, and ascorbic acid of the adrenal glands. An aqueous alcoholic extract (at 0.2 ml) was found to be more effective than the petroleum ether extract.
- Antioestrogenic activity
Aristolic acid exhibited antioestrogenic activity as shown by the prevention of oestrogen-induced weight increase and epithelial growth in the mouse uterus. It caused a decrease in alkaline phosphatase activity, glycogen content and mitotic counts in the oestrogen-treated uterus and prevented implantation in the early stages of pregnancy in mice.
- Abortifacient activity
In female mice, methyl aristolate produced 100% abortifacient activity at a single oral dose of 60 mg/kg when administered on the sixth or seventh day of pregnancy and 20-25% when given on days 10 or 12, respectively.
- Interceptive activity
Fractions isolated from the chloroform extract of Aristolochia indica at doses of 35-60 mg/kg demonstrated interceptive activity. Histological studies of the uterus and ovary at the minimum effective dose levels with each fraction revealed no overt changes apart from the presence of degenerated corpora lute a in the ovary of the animals treated, and no teratogenic effects were observed. A sesquiterpene isolated from the roots demonstrated 100% interceptive activity and 91.7% antiimplantation activity in mice at a single oral dose of 100 mg/kg, with no other toxic effects at the dose levels used. p- coumaric acid isolated from Aristolochia indica also showed 100% interceptive activity when administered at 50 mg/kg to mice, with a high margin of safety (> 1 000 mg/kg) and no teratogenic activity.
- Antitumour activity
Aristolochic acid was found to have activity against adenocarcinoma 755 in mice.
- Immunomodulatory activity
Aristolochic t acid has been shown to bind to surface f receptors of lymphocytes, altering immune t response.24 An immune-stimulating action was reported in a human study which measured ,increased phagocytic activity after 3 days of treatment at a dosage of 0.9 mg/day.
- Anti-inflammatory activity
Aristolochic acid also played a regulatory role in prostaglandin synthesis. It inhibited inflammation by both immunological and non-immunological agents. One mechanism of activity was thought to be as a direct inhibitor of phospholipase A2, decreasing the generation of eicosanoids and platelet-activating factors. Another anti-inflammatory mechanism may be the effect on arachidonic acid mobilisation in human neutrophils.
(I) The juice of A. indica was found to have a relaxant effect on the rhythmic contraction of uteri of rats and human beings. It had anon-specific antispasmodic effect on spasms induced by acetylcholine, barium chloride and pitocin al a cone. of 6 mg/ml (Tewari et al., 1966).
(2) Alcoholic extract of root was active against adenocarcinoma 755 in mice (J. Med.Phann.Chem.1962, .5, 657).
(3) Studies on interceptive properties of three fractions of chloroform extract in mice showed 40 to 60 mg/kg as MEO. Histological study of uterus and ovary revealed no change exceptfor presence of degenerated Corporalutea in case of one fraction (1.J.M.R. 1977, 66, 991).
(4) LD50, i.p., value of aristolochicacid in mice was 14.32mg/kg. It neither prolonged survival time of tumor-bearing mice nor enhanced immune function of the mouse RE system and did not: prevent the radiation and 2-dehydrodulcitol-induced damage to crythropoetic stem cells (Guangxi yixue 1981, 2).
(5)Oral administration or aristolochicacid showed dose dependent mutagenic activity in granuloma pouch assay (Mutat. Res. 1985, 143, 143).
(6) Aristolic acid, a potent antifertility agent, was 11011 mutagenic in Ames lest whereas aristolochic acid and its analogue were mutagenic; presence of nitro group in phenanthrenenucleus essential for mutagenic action (Ind. J. Pharrnacol. 1987, 19, 26).
Other Studies and Findings
Aristolochic acid is found to occur in varying amounts in different samples of drug, ranging in yield from 0.06 to 0. 7 per cent on dry wt basis. This variation in the yield may be due to the varying amounts of the stems in different drug samples (Krishnaswamy et al, loc. cit.; Kupchan&Merianos, loc. cit.).
Aristolochic acid acts as an anti-feedant and male sterilant for some insects. It is toxic to houseflies; at 0.18 per cent concentration, it caused 95 per cent mortality in eight days. A study ofchemosterilization effect against three insects, viz. DysdercuskoenigiiFabr., AedesaegyptiLino. and Triboliumcastaneum (Herbst.) (all fresh adults treated with aristolochic acid) suggests that the acid brings a mitotic death or behaves as a dominant lethal mutant possibly due to the presence of -COOH group with methylenedioxy phenyl ring and N02 group in the acid (Mathur& Sharma, Indian J Hort, 1978, 35, 406; Saxena et al, Indian J expBiol, 1979, 17, 354; ChemAbstr, 1972, 77, 147572).
Extracts or isolates of A. indica containing aristolochic acid possess anti-cancer activity. The compound is active against adenocarcinoma 755 and ascitichepatoma in rats. It is also active against Ehrlich ascites carcinoma in mice but is inactive against a wide spectrum of experimental neoplasms. It stimulates phagocytic activity in guineapigs administered chloramphenicol, cyclo-phosphamide and to a limited extent prednisone. Kidney damage has been observed in rats treated with aristolochic acid. The clinical assessment of the drug was terminated as a result of renal damage caused by the drug (ChemAbstr, 1962, 57, 2350; 1962, 56, 4060; 1966, 64, 18250; Kupchan&Doskotch, J medpharmChem, 1962, 5, 657; Angels et al, J Philipp med Assoc, 1970, 46, 505; Jewers et al in Ellis & West, IX, 26). Of the other important compounds isolated from the roots, aristolic acid (isolated from CHCi3 extract, yield, 0.007% of the root) (Table I) was found to be an effective anti-fertility agent in mature female albino rabbits. No adverse reaction in blood was observed. It has been found to possess anti-estrogenic activity and to prevent implantation in the early stage of pregnancy in mice. Methyl ester of aristo1ic acid (present in CHCl3 extract in small amounts), however, showed damage to liver and kidney and increase in uterine weight. A sesquiterpene (mp 150°) isolated from petroleum ether extract (see isomer of ledol, Table l) and p-coumaric acid (isolated from alcoholic extract; yield, 0.0025% of the root) showed I 00 per cent interceptive activity in mice (at !00 mg/kg and 50 mg/kg dose level, respectively) with high margin of safety, the former with 91.7 per cent anti-implantation activity, and the latter without any teratogenic effect (Pakrashi&Chakrabarty, Experientia, 1978, 34, 1377; Pakrashi&Shaha, ibid, 1978, 34, 1192; 1977, 33, 1498; Pakrashi&Chakrabarty, Indian J expBiol, 1978, 16, 1283; Pakrashi&Pakrasi, ibid, 1978, 16, 1285; Information from Dr S.C. Pakrashi, Indian Institute of Experimental Medicine, Calcutta).
In some regions, like some districts in Tamil Nadu, the roots yield alkaloids (0.05-0.07% dry wt) consisting mostly of 1-curine (Table 1), whereas root samples from other areas like Bangalore yield no alkaloids, or only traces. Alkaloid-bearing samples reveal that the higher the percentage of aristolochic acid, the lower is the percentage of alkaloid present in the roots (Krishna swamy et al, loc. cit.; Rao et al, loc. cit.; Pakrashi et al, Phytochemistry; 1977, 16, 1103; Kupchan&Merianos, loc. cit.; Govindachari&Viswanathan, loc. cit.),
The root is recommended in atonic types of dyspepsia, bowel troubles of children and in intermittent fevers. It is prescribed as a tincture. In Maharashtra it is administered as a powder. In large doses it acts as a local irritant provoking nausea and griping pains in the bowels and sometimes vomiting and tenesmus (J.P., 68; l.P.C., 22; Chopra et al, 1958, 284; Ghosh, R., 949; Datta&Mukerji, loc. cit.; Malhotra&Moorthy, Bull bot Suru India, 1973, 15, 13).
The chloroform extract of the roots has exhibited an anti-spermatogenic effect on mice, and the petroleum ether, chloroform and alcoholic extracts have exhibited 100 per cent interceptive activity in mice and hamsters at 50 mg/kg dose level. The roots are also active against Helminthosporiamsatiuum in vitro. The juice of fresh leaves is useful in treating cough of children by inducing vomiting without any depression. The seeds are tasteless and useful in treating inflammations, biliousness and dry cough [Sharma & Sharma, J Res Indian Med, Yoga, 1977,12(2), 18; Pakrashi&Pakrasi, Indian J expBiol, 1977, 15,256, 428; Pakrashi&Shaha, ibid, 1977, 15, 1197; Pakrashi&chakrabarty, Indian J med Res, 1977, 66, 991;Bhatnagar, ibid, 1961, 49, 799; Pakrashi et al, Experientia,1976, 32, 394].
Courtesy : The Wealth of India series , DravyaGuna by Dr. J.L.N. Sastry , InidanMateriaMedica by VaidyaBhagwan Dash , DravyaGuna by Dr. GnjanendraPandey