BIOACTIVE CHEMICAL CONSTITUENTS OF BLEPHARIS AND LEPIDAGATHIS (ACANTHACEAE) – A REVIEW

BIOACTIVE CHEMICAL CONSTITUENTS OF BLEPHARIS AND LEPIDAGATHIS (ACANTHACEAE) - A REVIEW

Rajeev Rattan

Government College, Haripur, Kangra, HPU - Shimla, India.

ABSTRACT: The herbal drugs derived from plant sources are used in traditional pharmacopeia and also act as precursor in lab to synthesize medicines at large scale. Acanthaceae is a large family comprising of various medicinally valuable species. In traditional use, the leaves of this family are commonly recognized to alleviate the poisonous bites of reptiles and insects and whole plants for the treatment of external wounds and ulcers. The pharmacological effects evaluated from various species of this family are antibacterial, antifungal, antipyretic, hepatoprotective, anti-inflammatory, cytotoxic, antioxidant, anti-platelet aggression and insecticidal activities. The phytochemicals reported from this family are mainly flavonoids, alkaloids, lignans, benzonoids, fatty acids, terpenoids, tannins and a few triterpenoid saponins. In the present study two genera namely Blepharis and Lepidagathis of the family Acanthaceae were selected with the focus on their traditional use, chemical constituents, and pharmacological activities. Various pharmacological experiments have verified their practice in traditional use and species of both the genera emerged as good source of herbal medicines. However, uncharacterized crude extract was employed in most of the studies with few exceptions. These species need to be explored for isolation of more compounds with their pre-clinical and clinical studies to establish as potential drugs. The review will help the researchers.

Keywords: Acanthaceae, Blepharis, Lepidagahtis, Flavonoids, Triterpenic Saponins

INTRODUCTION: Plants are potential source of phytonutrients and phytochemicals used as therapeutic aids across the globe. The herbal plants have been used as raw base in all the Unani, Chinese, Ayurveda, Siddha pharmacopeias ¹ and provided a valuable lead in establishing the life saving drug formulation to modern medicines. However, to the large available data of medicinal plants only 15% got phytochemical exploration ². In the developing world with increasing poverty and population, health care is the major concern and herbs have proven as inexpensive, reliable and accessible source of therapeutic significance ³.

Many drugs available in market are associated with serious side effects, toxicity, resistant to pathogenic microorganisms and even have restriction of use in some countries ⁴. Whereas the herbs have long history of their use in traditional medicines and latter as clinical candidate to treat serious diseases one might expect a little side effects ⁵. Acanthaceae species have been practiced as herbal medicines for centuries for the treatment of various diseases. The species have been investigated for extraction and isolation of chemical compounds responsible for various traditional uses.

In the present study two genera, namely Blepharis and Lepidagathis of the family Acanthaceae were selected with the focus on their traditional use, chemical constituents and pharmacological activities. The species of both the genera emerged as good source of traditional medicines. The objective of the study was to evaluate whether traditional claims of species have been validated in pre-clinical and clinical studies and whether any structure activity relationship studies have been carried out. The database was extracted from Google scholar, PubMed, Scopus-Elsevier, AGRICOLA and Shodhganga.

Family Acanthaceae: Acanthaceae comprises of 346 genera and 4300 species most of which have been herbs, shrubs and vines. The plants of this family are cosmopolitan and distributed in the old and new world. Mainly present in Africa, Central America, Malaysia, Indonesia, with few species extending to South Europe, Japan, Southern cost of New Holland and Southern to the Cape of Good Hopes ⁶.  In India, Acanthaceae genera are peculiar to the Southern parts, Indian Archipelago and Malayan Penisula but have spreaded from Sultej to Silhet and lower ranges of Himalayas ⁷.

Traditional uses of Family Acanthaceae: In traditional medicines the species Andrographis paniculata is used for the treatment of diarrhea, leprosy, malaria, flu, sinusitis, tuberculosis, rabies, respiratory infections, syphilis and HIV/ AIDS ⁸. The whole plants of mangrove (Avicennia) are used in treatment of tumor, ulcer, snakebites, rheumatism, asthma and diabetes ⁹. The parts of whole plant of Staurogyne merguensis are used in abstetrics, gynocoligical disorder and infertility ¹⁰. The most common species of Acanthus namely A. montanus, A. ilicifolius, and A. ebracteatus are mainly used for diseases of respiratory, nervous and reproductive system, gastrointestinal and urinary tract, and skin illness ¹¹.  Athatoda vasica a shrub is commonly used in traditional practice in Asia and Europe. The whole plant is prescribed for the treatment of respiratory tract infection, bronchodilator and antiallergic activities, antitussive activities. The leaves of this plant are the main gradient of commercially used Kada used in India, France, Sweden etc ¹².

Rhinacanthus nasutus has been used by local people for treatment of tinea versicolor, ringworm, eczema, herpes, influenza, and to relief from prickly heat, scruff and dedruff ¹³. Various parts of Phlogacanthus thyrsiflorus has been used as components in several folk medicines to treat fever, antidote to pox, skin diseases like sore, scabies, jaundice, liver and spleen diseases, indigestion, acidity, gastritis, pharyngitis, chronic leucorrhoea, cough and cold, chronic bronchitis, asthma and rheumatism ¹⁴. In upper Assam leaves of P. thyrsiflorus are used against helminthiasis, allergy, gout, rheumatism and fever ¹⁵. All parts of Justicia athatoda the official herb in Indian Pharmacopoeia is used in various ailments. The leaves are used for treatment of snakebites, expectorant, antispasmodic, malarial fever, nausea, and anthelmintic agent ¹⁶. Many species of Acanthaceae have been placed in different pharmacopeia for the treatment of various diseases like – Rungia linifolia-ulcers, Ruellia prostrata-fever, asthma, hair fall, cold, Barleria priontis- toothache, urinary irritation, antiseptic, gingival wounds, Diptera canthus prostate- hypoglycaemic, anticancer, ear- diseases, Rhinacanthus nasutus-leucoderma, hepatoprotective, antipyretic, snakebite, Thunbergia fragrans-snake bite, rheumatism and cough ¹⁷.

Infusion of two or three species is also used for various ailments. Ash leaves of Justicia betonica, Acathus pubescens and Justicia flava has been used for cough, ulcers and flu. The leaves of the species Acanthus eminens, Aystasias chimperi, Dyschoristethum bergiiflora, Thunbergiaalata, Dyschoris teradicans and Lepidagathis scariosa are infused to treat cough, skin diseases, wounds, eye infections, anti-diarrhea, edema, pneumonia ¹⁸ . Andrographis paniculata,  Hygrophila spinosa,  Barleria prionitis  and Adhatoda vasica are used  traditionally  as  antiviral,  antipyretic,  antiasthmatic  and  in respiratory diseases  ¹⁹.

Genus Blepharis: Blepharis genus has characteristic features adopted as diagnostic tools in taxonomical studies. The general floral patterns of Blepharis species are colorful petals, bracteoles, pistils of flowers, stamens and fruits are distinct ²⁰. Blepharis is recognized as Afro-Asian genus has wide ecological distribution extended to Southern parts of Middle East, Central Asia, Southern Africa, Southern China, and India including one species in Indonesia ²¹.

Traditional uses of Blepharis species: Blepharis is a large genus comprising of 126 species. For the purpose of traditional use, all parts of plant have been used while the use of leaves was predominant followed by seeds, whole plant, roots, young shoot and plant ash. The species are widely used to cure different ailments.   Blepharis ciliaris is distributed in Egypt, Oman, Pakistan, Jordan, Sudan and Iran. The leaves and whole plant are used for the treatment of Inflammation, wounds, sores, cough, cold, estringent, diuretic, and lungs diseases ²². The root charcoal ‘Kohl-el-agouz’ is used to improve vision ²³.  B. edulis – distributed from Soudi Arabia, Egypt, Iran, Pakistan, and India ²⁴. Popularly known as Shikhi in Ayurveda, whole plant is used for the treatment of asthma, cough, fever, inflammation of throat. Seeds possess diuretic, aphrodisiac, expectorant effects. Leaves “Utingana” have milk increasing effects in milching animals ²¹.  B. linariifolia is distributed in Mali, Somalia and Sudan ²⁵.

The whole plant is used to treat malaria, measles, infections, fever, kidney disorder, and dental problems ²⁶. B. maderaspatensis is distributed mainly in China and India ²⁷. Locally called as “Murivu porunthi” in Tamil is used by tribal people of India for the treatment of wounds, ulcers, throat inflammation, liver and spleen disorder. Decoction of whole plant is used to relieve abdominal gas problems and paste of leaves is used for bone fracture and heart pain ²⁸. B. scindica mainly present in India and Pakistan ²⁹. Seeds are used as tonic and to increase milk production of cattle, earache, eye disease, roots for urinary discharge and dysmenorrheal ³⁰.

Chemical Constituents Isolated from Blepharis species: Various extraction and isolation methods including GC-MS have been employed to obtain chemical compounds from Blepharis. The aerial parts of the plant were mainly employed for the purpose of extraction. The compounds identified from the genus Blepharis are 10 flavonoids from the species B. ciliaris, B. scindica and B. linarifolia. 9 phenolic acid derivatives from B. ciliaris, B. linarifolia and B. edulis. 5 alkaloids from B. edulis and B. scindica, 8 steroids, tritrpenoids and fatty acids from B. ciliaris, B. scindica. Major flavonoids were Apigenin, Naringenin, Genistein and their glycosides, Rutin, Blephariside A & B. Polyphenolic acid derivatives have been Vanillic acid, Verbaciside, Cis-Verbaciside, Isoverbaciside and leucoverbaciside. Steroids and Terpenoids- Stigmasterol, Sitosterol and their glycosides, oleanolic acid and fatty acids have been reported.

B. ciliaris ^{31, 21}- Apigenin, Apigenin 7-O-glucoside, Apigenin-7-O-(6ʹʹ-E-p-coumaroyl)- β-D-glucopyranoside, Apigenin7-(3"-acetyl-6"-E-p-coumaroyl)-glucopyranoside, Naringenin-7-O-(3ʹʹ-acetyl-6ʹʹ-E-p-coumaroyl) -β-_D-glucopyranoside, Naringenin-7-O-(6ʹʹ-E-p- coumaroyl)-β-D-Blephariside A, Blephariside B, Genistein-7-O-(6ʹʹ-O-E-caffeoyl)-β-D glucopyrano side, Protocatechuic acid, Methyl vanillate, Methyl veratrate, Verbascoside, β-Sitosterol-3-O-β-D-glucopyranose, Stigmasterol, Stigmaste rol-3-O-β-D-glucopyranose, Stigmasterol tetracosanoate.

B. edulis ^{32, 33}- Verbascoside, Cis-verbascoside, Isoverbascoside, Leucosceptoside A, Blepharin, Blepharigenin, 2-Benzoxazolone. The phytochemicals analysed through UHPLC/Q-TOF-MS-MS were Apigenin-7-O-glucoside, Diosmetin 7-O-rutinoside, Baicalein-7-O-guluronide, Diosmetin, Acacetin 7-O-neohespridoside, Biochanin A-7-O-glucoside, Isorhamnetin-3-O-rutinoside, Kaempferol-3- O –glucouronoid, Eriodictyol-7-O-glucoside, Kaempferol-3,7-O-bis-α-L-rahmnoside, Quercetin-4'- O –glucoside, Eriodictyol-7-O-neohespridoside, Pelargonidin-3,5- O- di-glucoside, Cyanidine-3- O –glucoside, Malvidin-3-O-glucoside, Cyanidine-3-O-rutinoside and Chalcone- Okanin-4'-O-glucoside, Naringenin chalcone.

 B. linariifolia ²⁶- Apigenin, Naringenin-7-O-(6ʹʹ-E-p-coumaroyl)-β-D-glucopyranoside, Vanillic acid, Verbascoside.

B. scindica ^{34, 35}- Apigenin, Apigenin-7-O-(6ʹʹ-E-p-coumaroyl)- β-D-glucopyranoside, Naringenin-7-O-(6ʹʹ-E-p- coumaroyl)-β-_D-glucopyranoside, Blepharin, Allantoin, Betaine hydrochloride, Oleanolic acid, β-Sitosterol, 9-Hydroxydodecanoic acid.

B. maderaspatensis ^{36, 37}- Rutin, Allantoin, Blepharin. Through GC-MS the chemical constituents identified are 9- Eicosyne, Sqalene, Phytol, 3,4-Dihhdro-3,5,8-trimethyl-3- (4,8,12trimethyltridecyl)-(2H)-benzopy- ran-6-acetate, 3,7,11,15 Trimethyl-2- hexadecen-1-ol and Cholestan-3-ol, 2 methylene,(3á,5à). The leaf extract showed Caffeic acid, Rutin, Quercetin, and Ferulic acid.

FIG. 1: STRUCTURES OF FLAVONOIDS FROM BLEPHARIS SPECIES

FIG. 2: STRUCTURES OF ALKALOIDS AND SAPONINS FROM BLEPHARIS AND LEPIDAGATHIS SPECIES.

Activities from Blepharis species: The traditional use and different phytochemicals isolated from Blepharis invited the attention to investigate these species for pharmacological activities responsible for their traditional claims. Several activities have been reported on various pharmacological methodologies. In vitro antioxidant activity was evaluated from B. edulis, B. maderas patensis, B. molluginifolia and B. linariifolia in DPPH assay Table 1. Different extracts exhibited strong antioxidant activity suggested to be attributed to the phenolic and flavonoids compounds as recorded in phytochemical screening tests of these species. Many species showed high antimicrobial potency with IC₅₀ value comparable to the standard. The species B. edulis, B. repens, B. maderaspatensis have expressed mortality against bacterial and fungal  strains such as Staphylococcus aureus, Enterococcus faecalis,  Staphylococcus epidermidis, Enterococcus faecium, Streptococcusagalactiae, Bacillus cereus, Bacillus subtilis, Streptococcus pyogenes, Staphylococcus saprophyticus, Klebsiella pneumoniae, Escherichia coli, Salmonella typhimurium, Shigella dysenteraie, Proteus vulgaris, Streptococcus sanjuis, Streptococcuss  alivarius,  Enterobacter aerogenes, Pseudomonas aeruginosa, and fungi Candida albicans, Aspergillusf lavus, Aspergillus niger, Aspergillus parasiticus. The cytotoxic activity from butanol extract of B. edulis was highest against MCF-7, HCT-116 and HepG2 cell lines using neutral red uptake assay Table 1. The cytotoxic concentration (CC50) ranged between 4.19 ± 0.51 μg/mL and 25.24 ± 2.3 μg/mL which is an acceptable level of plant extracts. The UHPLC/Q-TOF-MS-MS analysis revealed the presence of baicalein-7-O-glucuronide and malvidin-3-O-glucoside as major compounds 33. The anti-inflammatory activity was evaluated from B. ciliaris and B. maderaspatensis. The ethanol and chloroform extracts of both the species were compatible anti-inflammatory agents compared to their standard counterparts in carragean induced rat paw edema and tail clip pharmacological method. Enzyme inhibitory activity was recorded from B. linariifolia for isolated compounds namely Verbascoside, Vanillic acid, Apigenin, and 6”-O-p-Coumaroylprunin. Out of these apigenin and 6”-O-p-coumaroylprunin were more potent for all inhibitory activities. The apigenin was specifically more effective against α-Glucosidase and 6”-O-p-coumaroylprunin against lipase. The compounds were flavonoids and such activities have been recorded from other studies as well ²⁶.

TABLE 1: PHARMACOLOGICAL ACTIVITIES FROM BLEPHARIS SPECIES

Genus Lepidagathis: The genus Lepidagathis (Acanthaceae) is represented by more than 110 species distributed throughout the tropical and subtropical areas of Africa and Asia. Lepidagathis has nearly 30 species in India ⁴³. Lepidagathis has sinapomorphic feature of cytoliths on vegetative organs aclade within Acanthoideae subfamily and have Barlerieae lineage of quincuncial aestivation of the corolla ⁴⁴.

Traditional uses of Lepidagathis species: Though the Lepidagathis genus is less explored for scientific experimentations regarding biological activities still plants of this genus have been customarily used in traditional medicines to treat fever, headache, polyuria, dysentery, skin infections, jungle fever and calculi in the urinary tract ⁴⁵. L. keralensis is endemic to Kerala found on lateritic rocks near seashores. In tradition the plant is used by the paniya tribes for treating bronchial asthma in children ⁴⁶.

The spines of L. keralensis with rice are used to treat malabsorption, malnutrition, and digestive disorders. Decoction of the whole plant is recommended for kidney stone and albumin in urine. The plant is also used as a blood purifier and increases blood. Whole plant decoction with cumin seeds is given for chest pain ⁴⁷. L. cristata is spreaded in eastern and central parts of India including Karnatic, Deccan and Konkan. Dried plant material with honey is administered to treat asthma and powder mixed with coconut oil is used for skin infection. The plant of L.cristata mixed with honey is administered as regular dose for twenty days to treat asthma. The powder of plant mixed with coconut oil is used by local people for skin infections in Kurnool and Andhra Pradesh. The ash of entire plant is boiled with coconut oil and the infusion is applied externally on chronic wounds of pet animals twice a day up to 6-8 days ⁴⁸, dried shoot ash used for skin infections and paste of whole plant is used for itching infections.

The mixture of roots pastes of L. cristata, karanj oil and seed powder of Abrus precatorius is applied to treat leucoderma. The roots of L. cristata are also used as antidysenteric and to reduce heat in the stomach. The fumigation of herbs is inhaled to treat epilepsy. In Chhattisgarh, leaf extract is used for malarial fever and to clean the cattle in rainy season. The extract in boiled water is also used for skin itchy affection, burns and wounds. The leaf juice with copper sulphate is given during snake bite for gaining consciousness ⁴⁹.

L. hyline also known as “Curved Lepidagathis” is a wild herb from the Acanthaceaefamily that has various therapeutic potentials including antimicrobial and antidiabetic activities. This plant has been reported in various subtropical locations across the world, particularly in the Indian subcontinent. In Bangladesh, it is mostly found in hill tract regions which have a long history of use in the treatment of coughs and cardiovascular disorders ⁵⁰. L. cuspidata commonly known as spiny shrub (adulsa) is found in tropical Himalayas between the altitudes of 300-700m including Westerrn Ghats. In traditional herbal medicines of whole plant is used for the treatment of painful inflammation of fingers, boils and blisters, tonic in fever and itchy infections ⁵¹. The roots are used to procure abortion during the first three months of pregnancy.

Chemical Constituents Isolated from Lepidagathis species: L. cristata ⁵²- 6-hydroxyLuteolin, 6-hydroxyLuteolin-7-apioside a tryptophan derived alkaloid Cristatin A, Oleic acid, 3-(octadecyloxy) propyl ester, Heptadecane, 9-hexyl, Ethyliso-allocholate, Heptadecane, 9-hexylOctade cane, 3-ethyl-5-(2-ethylbutyl). L. hyaline Nees ⁵³- 3-β-O-[(-α-L-rhamnopyranosyl (1→4) - O-β-D-glucopyranosyl] 16 – α - hydro- xy-olean-12-en(13)-28-oic acid. L. scariosa ⁵⁴-1-Methyl-1-caprolactone,1-Tetra decanol, 1-Nonanol, Isopropylmyristate, Isopropyl, Tetradecanoate,5-(Hydroxy methyl )-2-(1-methyl-2-imidazolyl)-1H-benzimidaole, Hexadecanoic acid, Ethyl ester, 2-Hexadecen-1-ol, 3, 7, 11, 15-tetramethyl[R-[R*,R*-(E)]], Octa decanoic  acid,  Methy2-(4,8-Diacetoxy-3-bromo-6-methoxy-9,10-dioxo-9,  10-dihydro anthrax quinon-2-ylmethyl)-4-(2-methyl[1,3]dioxolane-2-yl)-3 - oxobutanoate, Lucenin, Quassin, Dimethoxyglycerol Docosyl Ether.

L. fasciculate ⁵⁵- δ-Cadinene, γ-Curcumene, Sandaracopimarinal, Germacrene D-4-ol, Cembrene, β-Calacorene, Arcurcumene, trans-4,10-epoxy-Amorphane, Abietatriene, and α Cubebene. The oil sesquiterpene hydrocarbons, oxygenated sesquiterpenes, diterpene hydrocarbons, oxygenated diterpenes. L. keralensis ⁵⁶- Cyclopentane, Decanoic acid methyl ester, Benzene, n-Hexadecanoic acid (palmitic acid) 10-Undecynoic acid, methyl ester, Benzene, (ethenyloxy)-, 2-Methoxy-4-Vinylphenol and n-Hexadecanoic acid, Cyclopentaneundecanoic acid, 1, 6-Octadiene, 3, 7-dimethyl, 10-Undecyn-1-ol, 3-Hydroxy-4-methoxybenzoic acid, 3-Hydroxy-4-methoxy benzoic acid, 2-Methoxy-4-vinylphenol, vanillic acid and 2-Piperidinone, N-[4-bromo-n-butyl], n-Hexadecanoic acid, Vanillic acid, (E)-4-(3-Hydroxyprop-1-en-1-yl)-2-methoxy phenol and 1,6-Octadiene,3,7-dimethyl. L. cuspidata ⁵⁷- 16,28-dihydroxy 22-acetyl-21-tigloylolean-12-ene-3-O-β-D-glucopyranosyl-(1→2)-β-D-glucopyrano syl-(1→3)-[β-D-glucopyranosyl - (1→2)] – β – D – glucopyranosi duronic acid  (Cuspidate A), 3-O-α-L-arabinopyranosyl-(1→3)-α-L-rhamnopyrano syl-(1→2)-α-L-arabinopyranoside hederagenin (Clemontanoside C).

TABLE 2: PHARMACOLOGICAL ACTIVITIES OF LEPIDAGATHIS SPECIES

Pharmacological activities of Lepidagathis Species: Antimicrobial, Immune suppressive, larvicidal, anti-inflammatory, analgesic and haemostatic agents ^{58, 62}. Phytochemicals present in plants such as flavonoids, phenolic, alkaloids and tannins possess antioxidant property. Various species of Lepidagathis are rich in such chemicals and are recorded as potential antioxidant ^58-61. The free radical scavenging action of the extract/ fraction is evaluated by ABTS and DPPH free radical decolorizing Assay. The DPPH is for lipophilic and ABTS for hydrophilic and lipophilic radicals. The ABTS free radical is generated by reaction of ABTS with Potassium persulfate to give blue-green ABTS⁺ chromophore. The ability of extract/ fraction to decolorize the chromophore has been measured as percentage scavenging potency. The scavenging effect of various extracts of L. prostrata was BuOH > Et OAc > MeOH > Pet. Ether > AQ (Table-). The IC₅₀ (µg/ ml) of BuOH-extract was 25.12± 0.52, 20.81± 1.13 and EtOAc-extract was 68.41± 6.15, 64.26± 2.02 for ABTS and DPPH respectively (Table-). The methanolic extracts of L. hyline and L. keralensis showed antioxidant potential with IC₅₀ value of 125.16, 122.46 µg/ ml using ascorbic acid as positive control in DPPH Assay. The ethanol extracts of L. cuspidata and L. pungens were also potential antioxidant in comparison to standard trolox, ascorbic acid and rutin in DPPH and NO Assay. The brine shrimp lethality and MTT assay are commonly used to evaluate cytotoxic potential of extract/ fraction. At low concentration of LC₅₀ 135.35 µg/ ml at with a quick response indicates that the plant extract of L. hyline is quite potent to give cytotoxic activity. The I_AC 28.95 for methanol extract of L. spinosa in different cancer cell lines indicates as potential cytotoxic effect. The antitumor and anticancer effects from ethanol extract of L. pungens with IC₅₀ 25.77± 0.36 and IC₅₀ 185 µg/ml respectively have been recorded.

The activity was tested for two doses 200 and 400 mg/kg. The activity was dose dependant for tumor and other haemological measures like RBC, WBC counts. The extract also exhibited potent anticancer activity recorded by short-term cytotoxicity trypan blue exclusion methods with IC₅₀ value 185 µg/ml. From L. cuspidata the isolated saponins cuspidate A, Clemontanoside C were potential antifungal compounds against the fungal strains-Aspergillus flavus, Rhizopus stolonifer, Penicillum nodatum and Aspergillus fumigates comparable to the synthetic counterpart Mancozeb ⁵⁷. Oleic acid isolated from L. cristata was also strong antifungal agent. The methanol extract of L. hyaline expressed various pharmacological effect such as anti-inflammatory, antidepressant, antiarithritis, thrombolytic and anxiolytic. The ethanol/methanol extracts of L. cristata possessed anti-diabetic, antiemetic, wound healing and anti-inflammatory activities ⁶².

CONCLUSION: All parts of plants of Acanthaceae have been reported for traditional use, but leaves part are used the most. Fresh leaves of the species Aystasias chimperi, Dyschoris teradicans, Acanthus eminens, Dyschoristethum bergiiflora, Lepidagathis scariosa and Thunbergia alata have been infused to treat cough, skin diseases, wounds, eye infections, anti-diarrhea, edema, pneumonia. The pharmacological activities investigated from the species of Acanthceae are antibacterial, antifungal, cytotoxic, anti-inflammatory, antipyretic, antiviral, antioxidant, hepatoprotective, insecticidal and anti- platelet aggregation activities. Various chemical compounds to the class of flavonoids, phenolic acids, alkaloids, saponins, oils, acids, esters, alcohols, aldehydes and their glycosides are characterized through different isolation and analysis methods. The two genera Blephris and Lepidagathis were selected to study the traditional use, chemical constituents and pharmacological effects. The survey revealed that compounds isolated from the genus Blepharis were Flavonoids - Apigenin, Naringenin, Genistein and their glycosides, Rutin, Blephariside A & B. Polyphenolic acid Deriveatives, Vanillic acid, Verbaciside, Cis-Verbaciside, Isoverbaciside and leucoverbaciside. Alkalois- Blepharin, Allantoin, Betain hydrochloride, Blepharigenin, Steroids and Terpenoids- Stigmasterol, Sitosterol and their glycosides. Whereas, from the genus Lepidagathis triterpenic saponins- Cuspidate A and Clemontanoside C, 3-β-O-[(-α-L-rhamnopyranosyl (1→4) – O – β – D - glucopyranosyl] 16 – α -hydroxy-olean-12-en(13)-28-oic acid, Alkaloids- a tryptophan derived oleic acid, 3-(octadecyloxy) propyl ester Cristatin A, oils, alcohols, esters, fatty acids have been isolated. The pharmacological activities reported from these genera were mainly antioxidant, cytotoxic, antimicrobial, anti-inflammatory, antidiabetic and insecticidal. The data revealed that the uncharacterized crude extract was used to evaluate these pharmacological effects with the exception of L. cuspidata where isolated pure compounds Cuspidate A and Clemontanoside C to evaluate antifungal potential ⁵⁷. The traditional use of the species of Acanthaceae pointed the strong evidence of pharmacological importance, but no systematic work has been carried out to validate their biological effects. The flavonoids and alkaloids are most potent compounds of these species responsible for these effects. The research remains possible for their bioactive principle. In lieu, of these observations it is suggested that research is needed to investigate more species for scientific validation. To isolate bioactive crude extract and to establish mode of action of Acanthceae species.

ACKNOWLEDGEMENT: Author is grateful to the Principal Governmet College Haripur Guler Kangra H. P.

CONFLICT OF INTERESTS: There is no conflict of interests of any type.

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    Rattan R: Bioactive chemical constituents of Blepharis and Lepidagathis (Acanthaceae) – a review. Int J Pharm Sci & Res 2024; 15(1): 54-65. doi: 10.13040/IJPSR.0975-8232.15(1).54-65.

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