CHAPTER – 1WORLD – WIDE TRADE IN MEDICINAL PLANTS & DERIVED PRODUCTS

DIOSGENIN

Diosgenin belongs to class of Sapogenin.
i.e. Aglycone found in Steroidal Saponin Glycoside Dioscin.
It is used for synthesis of Steroidal hormones.
B.S:
Diosgenin is commercially available from;

~ Dioscorea floribunda
~ Dioscorea compositae
~ Dioscorea deltoida

Generally it is collected from wild source, as for Cultivation correct Soil, proper Drainage, Freedom from Weed, Fungi is required.
Depending upon different species, it requires 3 – 5 years for development.

FAMILY: Dioscoreaceae

NO B.S SAPOGENIN %
SAPOGENIN HABITAT
D. deltoida Diosgenin 2 – 5% Growing well in Sub Himalayan region
D. floribunda Diosgenin 2 – 5% Central America
D. compositae Diosgenin 2 – 4% Mexico
D. prazeri Diosgenin 1 - 3% North Eastern India

SYNONYM:
Dioscorea Root, Rheumatism Root, Yam (Starchy Tubers)
Dioscorea Root is known as “Rheumatism Root”.
It is also called Yam (Starchy Tuber).

Dioscorea is cultivated by sowing Rhizome pieces with buds & is harvested after 18 – 24 months.
Plant contains about 4 – 6% of Diosgenin.
It is mainly present as Glycoside in plant.
Diosgenin occurs as the Rhamno – rhamno – glucoside, Dioscin, in the Rhizome of several species of Dioscorea.

CULTIVATION & COLLECTION:
 In view of the Pharmaceutical significance of the drug, it is tried & successfully grown in various parts of India.
 Commercially, it is grown in Tamil Nadu, West Bengal, Maharashtra, Karnataka & Jammu & Kashmir.
 The crop can be raised from seeds, but variability in progeny & comparatively longer time for harvesting are the disadvantage with this method.
 Therefore, Healthy Tubers of about 70 – 80 g in weight with crown are selected for cultivation.
 For checking the Tuber, they are treated with Fungicide & sown in Nursery beds.

 It takes about 30 – 40 days for their sprouting.
 After 2 – 3 months of growth, tubers are transplanted in the field, which is treated with Insecticide earlier.
 While planting, the Tubers are placed at a distance of 30360 cm.
 Initially, the Veins are weak & tender& they need support for their optimum growth.
 Trellis of 2.5 m in height are provided for this purpose.
 Since the Tubers are very Exhaustive, a high dose of farmyard manure to the extent of 5 – 10 tones per hectare is applied in the beginning.
 Organic fertilizers should be applied subsequently in equal doses at an interval of 1 month.
 Irrigation should be done every 10 days

 It is a Climber with Alternate Leaves.
 Rhizomes are;

~ Soft
~ Horizontally arranged
~ Very close to the Soil

 Drug is covered with scattered Roots.
 Weight è 20 – 50 gm
STRUCTURE OF DIOSGENIN:



DIOSGENIN
DIOSGENIN è D5 25 a Spirostan b - ol
DIOSGENIN is Steroidal Saponin
Subtype è Spirostanol, since here all rings are fused.
Sugar is attached at 3 – position.

ISOLATION & DEGRADATION OF DIOSGENIN

ISOLATION:
Dioscorea Rhizomes
Dioscin

(1) Hydrolyse Milled Root with Mineral acid.

(2) Filter, Neutralize & Dry the hydrolysed Root.

(3) Extract & Crystallize Diosgenin.



DEGRADATION:

(1) Cleave Spiroketal ring with Ac2O to form  20 – 22.

(2) Oxidize to generate 20 – keto group.

(3) Split side chain to yield C – 21 steroid.


16 Dehydro Pregnenolone acetate is used for the synthesis of various steroidal hormones.
All 4 types of Hormones like;


NO. HORMONES TYPES

1. Corticosteroids Cortisone, Hydrocortisone, Prednisolone
2. Progestrene / Pregnenes Progesterone, 17  OH progesterone
3. Androstins Testosterone, Methyl Testosterone
4. Contraceptives / 19 – Nor steroids Estnone, 17  ethynyl estradiol, Norethisterone acetate

 Such Hormones are produced from such natural sources only after 1980’s.
 Before that they were produced from Cholesterol or Stigmasterol.
 Such Hormones today cover 25% of market.


INDUSTRIES INVOLVED FOR SUCH HORMONE PRODUCTION IN INDIA

(1) REGIONAL RESEARCH LABORATORY (RRL)

Jammu
Working on Dioscorea compositae.

(2)WIADH LABORATORY

Bombay

(3)CIPLA LABORATORY

Bombay

(4)CHEMICAL, INDUSTRIAL & PHARMACEUTICAL LABORATORY LIMITED

Bangalore

Upto 1990, India was importing such hormones but, nowadays Diosgenin is not exported but different hormones prepared from it are exported widely.

Due to Development of Industrial companies like above in this field, Export gradually rises after 1998.

WORLD WIDE TRADE:
Much of the world’s production has come from MEXICO, where Tubers from D. compositae (Barbasco), D. mexicana, D. floribunda mainly harvested from wild plants, are utilized.
Other important sources of Dioscorea used commercially now include;

~ India (D. deltoida)
~ South Africa (D. sylvatica)
~ China (D. collettii, D. pathaicu, D. nipponica)

Demand for DIOSGENIN for Pharmaceutical is Huge, equivalent to 10,000 tones of Dioscorea Tuber per Annum.
DATA FOR 2005 – 2006

HORMONE AMOUNT (TONS) Rs. (CRORES)

Hydrocortisone 63 3.4
Prednisolone 2 0.5
Ethisterone & Derivative 2.2 7
Methyl Testosterone 17.5 1
Dexamethasone 7 1
Betamethasone 1.3 10

ALLIED SOURCES OF DIOSGENIN:

(!)COASTAL SPECIES TUBER

It gives 2 – 3 % Diosgenin.
Less Expensive
Since Dioscorea is Climber & needs support, while this is a shrub so no support is needed.

(!!)BALENITE ROXBURGHII  FRUIT

Xerophytic plant & can be cultivated in waste land also.
Good plant for Indian production.
Gives 1 – 2 % of Diosgenin.

(!!!)FENUGREEK  SEEDS
Not used commercially.

B.S: Seeds of Trigonella foenum – graecum
FAMILY: Leguminaceae
1 – 2 % Sapogenin
Because of ease of cultivation of Fenugreek & its rapid growth make the plant potentially viable crop for Steroid production in Temperate countries.